WO2016098881A1 - Tablet containing high amounts glucosamine and chondroitin sulfate, and method for producing same - Google Patents
Tablet containing high amounts glucosamine and chondroitin sulfate, and method for producing same Download PDFInfo
- Publication number
- WO2016098881A1 WO2016098881A1 PCT/JP2015/085488 JP2015085488W WO2016098881A1 WO 2016098881 A1 WO2016098881 A1 WO 2016098881A1 JP 2015085488 W JP2015085488 W JP 2015085488W WO 2016098881 A1 WO2016098881 A1 WO 2016098881A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- salt
- glucosamine
- chondroitin sulfate
- tablet
- solution
- Prior art date
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- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 title claims abstract description 137
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- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 title claims abstract description 106
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- 235000010987 pectin Nutrition 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 229960000292 pectin Drugs 0.000 description 1
- RFWLACFDYFIVMC-UHFFFAOYSA-D pentacalcium;[oxido(phosphonatooxy)phosphoryl] phosphate Chemical compound [Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O.[O-]P([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O RFWLACFDYFIVMC-UHFFFAOYSA-D 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Chemical class OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 235000008729 phenylalanine Nutrition 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000007065 protein hydrolysis Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- 235000005875 quercetin Nutrition 0.000 description 1
- 229960001285 quercetin Drugs 0.000 description 1
- OVSQVDMCBVZWGM-QSOFNFLRSA-N quercetin 3-O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O OVSQVDMCBVZWGM-QSOFNFLRSA-N 0.000 description 1
- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 description 1
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 238000005096 rolling process Methods 0.000 description 1
- 235000014102 seafood Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
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- 238000004513 sizing Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000009469 supplementation Effects 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 239000000892 thaumatin Substances 0.000 description 1
- 235000010436 thaumatin Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 235000013337 tricalcium citrate Nutrition 0.000 description 1
- 235000019156 vitamin B Nutrition 0.000 description 1
- 239000011720 vitamin B Substances 0.000 description 1
- 235000010374 vitamin B1 Nutrition 0.000 description 1
- 239000011691 vitamin B1 Substances 0.000 description 1
- 235000019164 vitamin B2 Nutrition 0.000 description 1
- 239000011716 vitamin B2 Substances 0.000 description 1
- 235000019160 vitamin B3 Nutrition 0.000 description 1
- 239000011708 vitamin B3 Substances 0.000 description 1
- 235000019158 vitamin B6 Nutrition 0.000 description 1
- 239000011726 vitamin B6 Substances 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 150000008494 α-glucosides Chemical class 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4415—Pyridoxine, i.e. Vitamin B6
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
- A61K31/51—Thiamines, e.g. vitamin B1
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/737—Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
Definitions
- the present invention relates to granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, as well as tablets containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, and their It relates to a manufacturing method.
- Glucosamine is a monomolecular amino sugar widely distributed as a component of mucopolysaccharide in cartilage and connective tissues in the animal body. Specifically, 2-amino acid in which the hydroxyl group at the 2-position of glucose is substituted with an amino group. Glucose. It is also abundant in crustacean chitin such as crabs and shrimps. Glucosamine is produced by chondrocytes and promotes the production of cartilage components. Therefore, glucosamine is effective for arthritis such as osteoarthritis and is commercially available as a supplement for nutritional supplementation.
- the crystal powder of glucosamine and its salts has poor fluidity, the uniform filling of the tablet machine into a die, and the occurrence of tableting troubles such as capping and lamination increases, and the tablet weight varies. There was a problem that occurred.
- a pulverized product of glucosamine or a salt thereof is used to obtain a pulverized product with high binding properties, and both the crystal with high binding properties and the crystal powder with low binding properties are used.
- the fluidity of the tablet composition can be improved and the occurrence frequency of tableting troubles can be kept low (Patent Document 1).
- the glucosamine crystal pulverized product-containing composition has insufficient practical fluidity.
- glucosamine has physical properties suitable for tableting.
- Granules are obtained (Patent Document 2).
- chondroitin sulfate is effective for arthritis and the like, and pharmaceuticals containing chondroitin sulfate are commercially available.
- a composition for treating connective tissues of humans and animals containing chondroitin sulfate and glucosamine has been reported (Patent Document 3). Synergistic effects on the treatment of connective tissue by administration of glucosamine and chondroitin sulfate are known.
- glucosamine supplements contain excipients to improve tableting properties of glucosamine, and therefore the contents of chondroitin sulfate and glucosamine must be lowered.
- spray-dried mixed slurry consisting of naproxen or naproxen sodium, a disintegrant, and a binder makes it spherical, porous, and excellent in fluidity Are reported to be uniform and highly compressible (Patent Document 4).
- An object of the present invention is to provide granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, and tablets containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof It is in providing the manufacturing method of them.
- the present invention relates to the following (1) to (19).
- Glucosamine or a salt thereof according to any one of (1) to (4), wherein the content of chondroitin sulfate or a salt thereof is 3 to 20% by weight with respect to granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof Granules containing a salt and chondroitin sulfate or a salt thereof.
- the granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (1) to (6) is selected from the group consisting of a lubricant, a fluidity improver and an additive.
- the tablet according to (8), wherein the content of glucosamine or a salt thereof in the tablet is 60 to 95% by weight.
- the total content of one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in the tablet is 0.1 to A tablet containing 10% by weight of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (8) to (10).
- a method for producing granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof comprising a step of spray-drying the solution 1 or 2.
- a step of spray-drying solution 1 or 2 and a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt obtained in the step are selected from the group consisting of a lubricant, a fluidity improver and an additive.
- a method for producing a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof comprising the step of adding one or more compounds.
- a method for producing tablets containing (18) A tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (16) or (17), wherein the content of glucosamine or a salt thereof in solution 1 or 2 is 15 to 27% by weight Production method. (19) The glucosamine or salt thereof and the chondroitin sulfate or salt thereof according to any one of (16) to (18), wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight. The manufacturing method of the tablet to contain.
- granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, and tablets containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof and A manufacturing method can be provided.
- the glucosamine used in the present invention can be obtained by, for example, a method for producing by fermentation, a method for extracting from shrimp or crab, and the like. Glucosamine can also be obtained by purchasing a commercial product from each company. Examples of the method for fermentative production of glucosamine include a method of producing glucosamine by microbial fermentation using a plant as a raw material, and a method described in Metabolic Engineering. 7 (3), 2005, 201-214 is preferable.
- Examples of the method for extracting glucosamine from shrimp and crab include a method of extracting chitin from shrimp and crab shells, hydrolyzing it, purifying it, and drying it. The methods described in Kaikai 2004-359908, US3683076 and the like can be mentioned.
- Examples of commercially available glucosamine include fermented glucosamine K (manufactured by Kyowa Hakko Bio) and glucosamine FM (manufactured by Kyowa Hakko Bio).
- Glucosamine or a salt thereof used in the present invention may be a commercially available glucosamine or a salt thereof, or glucosamine obtained by hydrolysis and purification of chitin, etc.
- a method of using the salt or pulverizing glucosamine or a salt thereof may be used.
- the pulverization method of glucosamine or a salt thereof may use any of the principles of compression, impact or shear by external force, and collision or friction by the inertial force of the particle itself, for example, ball mill, roller mill, high-speed rotary mill, jet mill. And the like.
- Examples of the ball mill include a rolling ball mill and a planetary mill.
- Examples of the roller mill include a solid roller mill, a roll crusher, and a high-pressure roll press.
- Examples of the high-speed rotation mill include a hammer mill. , Pin mill, cage mill and the like.
- the chondroitin sulfate or a salt thereof in the present invention can be obtained by, for example, a chemical synthesis method or an extraction method. Moreover, chondroitin sulfate can also be obtained by purchasing a commercial product of each company.
- Examples of the method for chemically synthesizing chondroitin sulfate include the method described in JP-A-2003-199583.
- Examples of the method for extracting chondroitin sulfate include the method described in JP-A-2014-009164.
- the chondroitin sulfate that can be obtained by the extraction method and the like may be derived from any organism, and examples include animals such as rays, sharks, cows, whales, rabbits, sheep, horseshoe crabs, pigs, squids, and the like. be able to.
- chondroitin sulfate Commercially available products of chondroitin sulfate include, for example, shark cartilage extract powder containing chondroitin sulfate extracted from raw materials such as shark cartilage and shark fin cartilage. ), SCP (NB) (manufactured by Maruha Nichiro), chondroitin HG-40 for shark cartilage food (manufactured by Nippon Pharmaceutical Co., Ltd.), and the like.
- the salt of glucosamine and the salt of chondroitin are the same or different and include acid addition salts, metal salts, ammonium salts, organic amine addition salts, amino acid addition salts, and the like.
- Examples of the acid addition salt include inorganic acid salts such as hydrochloride, sulfate, nitrate, and phosphate, acetate, maleate, fumarate, citrate, malate, lactate, ⁇ -ketoglutar And organic acid salts such as acid salts, gluconates and caprylates.
- Examples of the metal salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as magnesium salt and calcium salt, aluminum salt, zinc salt and the like.
- ammonium salt examples include salts such as ammonium and tetramethylammonium.
- organic amine addition salts include salts of morpholine, piperidine and the like.
- amino acid addition salt examples include salts of glycine, phenylalanine, lysine, aspartic acid, glutamic acid and the like.
- the glucosamine salt is preferable because it is stable to heat and less likely to brown, and is easily absorbed from the intestinal tract after ingestion, and the use of glucosamine hydrochloride is more preferable .
- the granule of the present invention is a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity, more specifically, glucosamine or a salt thereof. And a granule obtained by spray-drying a solution containing chondroitin sulfate or a salt thereof.
- glucosamine or a salt thereof and chondroitin sulfate or a salt thereof collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin
- a solution containing one or more compounds selected from the group consisting of pantothenic acid preferably a compound added to glucosamine or a salt thereof and chondroitin sulfate or a salt thereof is collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof
- Granules obtained by spray-drying a solution that is one or more compounds selected from the group consisting of are also the granules of the present invention.
- the collagen or enzyme-treated product thereof may be any animal-derived one, such as those derived from domestic animals such as pigs, cows, chickens, and seafood.
- the collagen for example, commercially available products such as water-soluble collagen peptide SS, HP fish collagen (manufactured by Kyowa Hakko Bio) may be used.
- the rutin enzyme-treated product in rutin or an enzyme-treated product thereof is a product of rutin and a rutin analog converted to a glycoside by enzymatic treatment. Examples of the rutin analog include quercetin, isoquercitrin, morin, Examples of the enzyme-treated product or enzyme in the enzyme treatment include ⁇ -glucosyl glycosyltransferase.
- ⁇ -Glucosyl glycosyltransferase is an enzyme that hydrolyzes ⁇ -glucoside and adds the resulting sugar directly to another aglycone.
- the origin of the rutin enzyme-treated product is not particularly limited as long as it is a composition having the same composition, but it can be obtained by, for example, a method of treating an extract such as Enju or buckwheat with a glycosyltransferase. Can do. Specifically, it can be obtained by the methods described in JP-A-7-10898, JP-A-2003-33164 and the like.
- Thiamin is a water-soluble vitamin, also called vitamin B1, which is used for the metabolism of carbohydrates and branched chain fatty acids.
- Riboflavin is a water-soluble vitamin, also called vitamin B2 or lactoflavin, which is used for the metabolism and respiration of fats, carbohydrates and proteins.
- Pyridoxine is a water-soluble vitamin that is one of the compounds classified into vitamin B6 and represents a function that promotes red blood cell production.
- Niacin is a water-soluble vitamin, also called vitamin B3, which is a general term for nicotinic acid and nicotinamide, and has functions such as promoting the functions of the circulatory system, digestive system, and nervous system.
- the riboflavin, pyridoxine, niacin and thiamine may be salts of the respective compounds, and the salts may be the same or different, and include hydrochloride, sulfate, nitrate, diarrheal sulfate, etc. preferable.
- Pantothenic acid is D (+)-N- (2,4-dihydroxy-3,3-dimethylbutyryl) - ⁇ -alanine, a water-soluble vitamin contained in the vitamin B group.
- CoA coenzyme A
- Pantothenic acid may be a salt. Examples of the salt include calcium salt and sodium salt, and calcium salt is preferable.
- the thiamine, riboflavin, pyridoxine, niacin and pantothenic acid may be produced by any production method such as a protein hydrolysis method, a chemical synthesis method, an enzymatic method or a fermentation method, or a commercially available product may be used.
- the composition of the present invention is a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tableting properties and fluidity. More specifically, the granule of the present invention contains a lubricant, fluidity. It is a composition obtained by adding one or more compounds selected from the group consisting of an improving agent and additives.
- the lubricant is not particularly limited as long as it can be used for foods and the like, and examples thereof include stearic acid, magnesium stearate, calcium stearate, sucrose fatty acid ester, glycerin fatty acid ester, hardened oil and fat, fine silicon dioxide and the like. It is done.
- the lubricant may be present only on the surface of the tablet or may be dispersed inside the tablet.
- the total proportion of lubricants in the tablet of the present invention is preferably 0.5 to 12% by weight, more preferably 1 to 10% by weight. Two or more kinds of lubricants may be used.
- the fluidity improver is not particularly limited as long as it can be used in foods and the like, and examples thereof include tricalcium phosphate and calcium hydrogen phosphate.
- the proportion of the fluidity improving agent in the tablet of the present invention is preferably 0.1 to 7% by mass, and more preferably 0.5 to 6% by mass.
- additives include disintegrants, sugars, sweeteners, flavors, acidulants, binders, antioxidants, colorants, etc., collagen or enzyme-treated products thereof, rutin or enzyme-treated products thereof, thiamine, Riboflavin, pyridoxine, niacin and pantothenic acid may also be used as additives added to the granules of the present invention.
- disintegrants examples include starch, agar, gelatin powder, crystalline cellulose, calcium carbonate, sodium bicarbonate, calcium citrate, dextran, pectin, low-substituted hydroxypropyl cellulose, croscarmellose sodium, carboxymethyl cellulose, carboxymethyl cellulose sodium.
- the saccharide is not particularly limited as long as it can be used for food and the like, and examples thereof include monosaccharides, disaccharides, sugar alcohols, oligosaccharides, and preferably sugar alcohols.
- monosaccharides include glucose, xylose, galactose, and fructose.
- disaccharide include trehalose, sucrose, lactose, palatinose, and the like.
- sugar alcohol include maltitol, erythritol, sorbitol, xylitol and the like.
- oligosaccharide examples include raffinose, inulooligosaccharide (chicory oligosaccharide), palatinose oligosaccharide and the like.
- the proportion of saccharides in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
- the sweetener is not particularly limited as long as it can be used in foods, and examples thereof include sodium saccharin, dipotassium glycyrrhizin, aspartame, stevia, thaumatin and the like.
- the proportion of the sweetener in the tablet of the present invention is not particularly limited as long as it is within the range of the general use in the preparation. Although it will not restrict
- the proportion of the fragrance in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
- the acidulant is not particularly limited as long as it can be used for foods, and examples thereof include citric acid, tartaric acid, malic acid and the like.
- the proportion of the acidulant in the tablet of the present invention is not particularly limited as long as it is within the range of the general use amount in the preparation.
- the binder is not particularly limited as long as it can be used for foods and the like, and examples thereof include gelatin and pullulan.
- the proportion of the binder in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
- the antioxidant is not particularly limited as long as it can be used in foods and the like, and examples thereof include tocopherol, ascorbic acid, cysteine hydrochloride, L-ascorbic acid stearate, and the like.
- the proportion of the antioxidant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
- the colorant is not particularly limited as long as it can be used for foods, and examples thereof include food yellow No. 5, food red No. 2, food blue No. 2, carotenoid pigment, tomato pigment and the like.
- the proportion of the colorant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
- the tablet of the present invention is a tablet containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof. Specifically, the tablet is obtained by tableting the granule or composition of the present invention.
- Granules of the present invention can be produced by the following steps i-1), i-2) or i-3) and ii). i-1) Glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are heated and stirred in a solvent to dissolve or suspend them to obtain Solution 1.
- i-2) one or more selected from the group consisting of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid
- a compound 2 is added and heated or stirred in a solvent to dissolve or suspend them to obtain a solution 2.
- i-3) One or more compounds selected from the group consisting of collagen or its enzyme-treated product and rutin or its enzyme-treated product are added to glucosamine or its salt and chondroitin sulfate or its salt, and heated and stirred in a solvent.
- Solution 2 is obtained by dissolving or suspending by mixing.
- ii) Spray dry the solution 1 or 2 obtained in i-1), i-2) or i-3) to obtain granules.
- the granule of the present invention can be produced according to the following production steps.
- the solution 1 in the above step represents a solution in which glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are dissolved or suspended in a solvent having a temperature from room temperature to the boiling point of the solvent. And water is preferred. Examples of the alcohol include ethanol and glycerin.
- the total solute content in the solution or suspension may be 1 to 50% by weight, preferably 5 to 45% by weight, and more preferably 10 to 40% by weight.
- the solution 2 in the above step is selected from the group consisting of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid.
- One or more compounds, preferably one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof are dissolved or suspended in a solvent having a temperature from room temperature to the boiling point of the solvent.
- the solvent include water and alcohol, and water is preferred.
- the alcohol include ethanol and glycerin.
- the total solute content in the solution or suspension may be 1 to 50% by weight, preferably 5 to 45% by weight, and more preferably 10 to 40% by weight.
- the suspension may be either uniform or non-uniform, preferably uniform.
- the solute may be partially dissolved in the solvent, and the suspension may be a colloidal solution.
- the content of glucosamine or a salt thereof in the solution 1 or 2 is preferably 15 to 27% by weight, more preferably 18 to 24% by weight with respect to the solution 1 or 2.
- the content of chondroitin sulfate or a salt thereof in the solution 1 or 2 is preferably 1 to 6% by weight, more preferably 1.8 to 4.0% by weight with respect to the solution 1 or 2.
- the total content of one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in solution 2 is 0.2 with respect to solution 2. ⁇ 2 wt% is preferable, and 0.5 to 1.5 wt% is more preferable.
- the content of the total solute in the suspension (when a part is dissolved, the dissolved solute and the undissolved solute are combined into a solute) is 35 to 65% by weight. 40 to 60% by weight is preferable.
- Spray drying is generally used to obtain granules from a compound or mixture in a liquid form, and the granules obtained by the method are sprayed as fine particles of several hundred ⁇ m or less in hot air and dried. Since it is recovered as powder by dropping in the tower, the obtained powder has a property of being nearly spherical and excellent in fluidity and high in water solubility.
- the material used for spray drying is temporarily exposed to hot air, but the exposure time is very short and the temperature does not rise very much due to the latent heat of vaporization of water. Difficult to change due to condensate. Further, in the case of a material that is very sensitive to heat, it is possible to supply cold air instead of hot air. In that case, although a drying capability falls, it is preferable at the point which can implement
- the spray drying in the above step ii) is a method generally used for obtaining a powder from a liquid form, and the liquid composition is sprayed as fine particles of several hundred ⁇ m or less in hot air while being dried. It is recovered as a powder by dropping inside the tower.
- the material used for spray drying is temporarily exposed to hot air, but because the exposure time is very short and the temperature does not rise very much due to the latent heat of vaporization of water, the material is less susceptible to thermal denaturation, Changes due to condensate are also small. Further, in the case of a material that is very sensitive to heat, it is possible to supply cold air instead of hot air. In that case, although a drying capability falls, it is preferable at the point which can implement
- the granules used in the production method of the present invention can be obtained by spray-drying the solution or suspension using a spray dryer under the conditions of an air blowing temperature of 150 to 200 ° C. and an exhaust air temperature of 55 to 85 ° C. it can.
- a solution When spray drying is performed in step ii), it is preferable to use a solution.
- the spraying method of the spray dryer include a nozzle type and a disk type.
- the nozzle type include Pulvis Mini-Spray GB22 (manufactured by Yamato Kagaku Co., Ltd.).
- the disk type include L8. -i type spray dryer (Okawara Kako Co., Ltd.).
- the nozzle diameter is preferably 0.1 to 4.0 mm, and more preferably 0.3 to 3.5 mm.
- the ejection pressure of the nozzle is preferably 10 to 450 kg / cm 2, more preferably 50 to 300 kg / cm 2 .
- the inlet temperature include 100 to 200 ° C., preferably 110 to 195 ° C., and more preferably 120 to 190 ° C.
- the outlet temperature include 40 to 100 ° C, preferably 50 to 90 ° C, and more preferably 60 to 80 ° C.
- the atomizer speed is preferably 20000 to 45000 rpm, more preferably 25000 to 40000 rpm.
- the inlet temperature include 100 to 200 ° C., preferably 110 to 195 ° C., and more preferably 120 to 190 ° C.
- the outlet temperature include 40 to 100 ° C, preferably 50 to 90 ° C, and more preferably 60 to 80 ° C.
- the content of glucosamine or a salt thereof contained in the granules obtained by the production method of the present invention is preferably 65 to 99% by weight, more preferably 70 to 95% by weight as glucosamine or a salt thereof. 75 to 93% by weight is particularly preferable.
- the content of chondroitin sulfate or a salt thereof contained in the granule obtained by the production method of the present invention is preferably 3 to 22% by weight, more preferably 5 to 16% by weight.
- the amount is preferably from 0.1 to 10% by weight, more preferably from 0.5 to 5% by weight, based on the granules of the present invention. 3.
- composition of the present invention can be produced by the following step iii). iii) One or more compounds selected from the group consisting of lubricants, fluidity improvers and additives are added to the granules obtained in step ii) above, preferably mixed.
- Lubricants, fluidity improvers and additives may be in the form of independent powders, or granulated by combining them in advance and using a known wet or dry granulation method. It may be added in the form of For example, mixing is performed using a mixer such as a basket mill, a V-type mixer, a fret mill, a tumbler mixer, or the like. It can be carried out. 4).
- Method for producing sized powder The granule or composition of the present invention also includes a sized powder obtained by sizing the granule or composition obtained by the above method, and the sized powder is obtained in the following step iv). Can be manufactured. iv) The granule or composition obtained in the above step ii) or iii) is sieved to obtain a sized powder.
- the granule or composition obtained in the above step ii) or iii) is put into a sieve and shaken by hand, or passed through a sieve or a granule or composition using a sieving machine.
- the equipment used for the sieving in step iv) include a classifier / vibrating sieve [wet / dry type / net: cartridge type (standard) or inner ring type (standard)] (Dalton), Sato type vibrating sieve. Machine (manufactured by Kanei Sangyo Co., Ltd.).
- the sieve used for the above sieving is not particularly limited, and examples thereof include No. 4 sieve (4750 ⁇ m) to No. 60 sieve (250 ⁇ m), and No. 8 sieve (2360 ⁇ m) to No. 42 sieve (355 ⁇ m). No. 12 sieve (1400 ⁇ m) to No. 32 sieve (500 ⁇ m) are more preferred. 5.
- Method for producing tablet of the present invention The tablet of the present invention can be produced by the following step v). v) Tablets are produced by tableting the granules obtained in ii) above, or the composition obtained in iii), preferably the sized powder obtained in iv).
- the tablet of the present invention can be produced according to the following production steps.
- step v) the granule or composition of the present invention, preferably the sized powder is used as a tableting tablet, and compression-molded by an appropriate method to produce a tablet.
- a compression molding method for example, a conventional method in which a tableting granule is compression molded as it is, or a tableting granule that does not contain a lubricant after preliminarily applying a lubricant to the surface of the punch and the mortar wall. Examples include a so-called external lubrication compression molding method in which compression molding is performed.
- compressors such as a single shot compression molding machine, a rotary compression molding machine, a hydraulic press machine, etc.
- the content of glucosamine or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 60 to 95% by weight, more preferably 65 to 90% by weight as glucosamine or a salt thereof, Particularly preferred is 70 to 88% by weight.
- the content of chondroitin sulfate or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 3 to 20% by weight, more preferably 5 to 15% by weight as chondroitin sulfate or a salt thereof.
- the amount is preferably 0.1 to 10% by weight, more preferably 0.5 to 5% by weight.
- the tablet obtained by the production method of the present invention contains the granule of the present invention in an amount of preferably 80 to 99% by weight, more preferably 85 to 96% by weight.
- the shape of the tablet obtained by the production method of the present invention is not particularly limited, but for example, a round tablet, a triangular tablet, a cannonball tablet and the like are preferable.
- the size of the tablet of the present invention is not particularly limited, but is preferably 0.1 to 2 g in mass and 0.3 to 2.0 cm in diameter, for example.
- the tablet obtained by the production method of the present invention preferably has a hardness that does not cause, for example, cracking or breakage.
- the hardness of the tablet is generally measured as a breaking strength in the diameter direction of the tablet with a tablet hardness meter, and the value is preferably 3 to 20 kgf, more preferably 5 to 18 kgf. Particularly preferred is ⁇ 16 kgf.
- the hardness of the tablet can be measured by a commercially available tablet breaking strength measuring machine, for example, TH-203CP type (manufactured by Toyama Sangyo Co., Ltd.).
- a very small amount of lubricant is applied in advance to the die of the compression molding machine, and the mixture containing no lubricant is compression molded with a compression molding machine having the tooling coated with the lubricant.
- a tablet having a desired hardness can be produced without causing a tableting trouble.
- tableting obstacles include sticking (a phenomenon in which powder adheres to the heel), binding (a phenomenon in which friction between the die and the tablet increases), capping (a phenomenon in which the tablet peels off in a cap shape), and lamination (a tablet is layered). Phenomenon).
- the tablet obtained by the production method of the present invention may be a sugar-coated tablet or a coated tablet coated with sugar, sugar alcohol or the like, for example, in order to improve moisture resistance, storage stability and the like.
- a sugar-coated tablet or a coated tablet coated with sugar, sugar alcohol or the like for example, in order to improve moisture resistance, storage stability and the like.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [Malinker ridge 40S ⁇ (Yaizu Suisan Chemical Co., Ltd.) 52 g were dissolved in 1116 mL of purified water and 25 wt% An aqueous solution was obtained. Using this aqueous solution, spray-dry and granulate with a spray dryer [L8-i type spray dryer (Okawara Kako Co., Ltd.)] with the atomizer speed of 35000 rpm, inlet temperature of 180 ° C and outlet temperature of 70 ° C. Of 250 to 300 g was obtained.
- a spray dryer [L8-i type spray dryer (Okawara Kako Co., Ltd.)] with the atomizer speed of 35000 rpm, inlet temperature of 180 ° C and outlet temperature of 70 ° C. Of 250 to 300 g was obtained.
- sucrose fatty acid ester DK [DK ester F20W20 (Daiichi Kogyo Seiyaku Co., Ltd.) 10 g and tribasic calcium phosphate ⁇ [tribasic calcium phosphate (Taihei Chemical Industry Co., Ltd.)] ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇
- the mixture was thoroughly mixed to obtain a composition, which was sieved using a No. 16 sieve (1000 ⁇ m) sieve to obtain 200 g of sized powder.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g, Shark cartilage extract powder [Malinkin ridge 40S ⁇ (Yaizu Suisan Chemical Co., Ltd.)] 40 g and collagen [Water-soluble fish collagen (manufactured by Kyowa Hakko Bio) )] 12 g was dissolved in 1116 mL of purified water to obtain an aqueous solution having a total solute of 25 wt%. Next, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 900 kgf, and 20 tablets showing a hardness of 11.2 kgf were obtained.
- Glucosamine hydrochloride [Glucosamine FM (Kyowa Hakko Bio Inc.) 320 g, Shark cartilage extract powder ⁇ [Malinkin ridge 40S ⁇ (Yaizu Suisan Chemical Co., Ltd.)] 40 g and enzyme-treated rutin ⁇ [ ⁇ G rutin PS (Toyo Seiki Co., Ltd.) )] 12 g was dissolved in 1116 mL of purified water to obtain an aqueous solution having a total solute of 25 wt%.
- aqueous solution after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 1000 kgf to obtain 20 tablets having a hardness of 11.5 kgf. It was.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [SCP (NB) (manufactured by Maruha Nichiro)] 52 were dissolved in 1116 mL of purified water to obtain a 25 wt% aqueous solution. .
- SCP shark cartilage extract powder
- aqueous solution after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 950 kgf, and 20 tablets showing a hardness of 9.5 kgf were obtained. It was.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] ⁇ ⁇ ⁇ and shark cartilage extract powder ⁇ [Malinkin Tiridge 40S (manufactured by Yaizu Suisan Chemical Co., Ltd.)] 32 g were dissolved in 1116 mL of purified water An aqueous solution was obtained. Using the aqueous solution, after obtaining granules, a composition and a sized powder in the same manner as in Example 1, compression molding was performed with a tableting pressure of 1250 kgf to obtain 20 tablets showing a hardness of 10.7 kgf. It was.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [Malinkin Tiridge 40S (Yaizu Suisan Chemical Co., Ltd.) 40 g were dissolved in 1080 mL of purified water and 25 wt% An aqueous solution was obtained. Using this aqueous solution, 250 to 300 g of granules were obtained in the same manner as in Example 1.
- 180 g contains collagen [water-soluble fish collagen (manufactured by Kyowa Hakko Bio)] 6, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 and tribasic calcium phosphate ⁇ [third Calcium phosphate cocoon (produced by Taihei Chemical Sangyo Co., Ltd.)] 4 ⁇ g was added and mixed thoroughly in a polyethylene bag to obtain a composition. g was obtained. The sized powder was subjected to compression molding at a tableting pressure of 1000 kgf by the method of Example 1. As a result, 20 tablets of 350 mg per tablet showing a hardness of 10.5 kgf were obtained.
- Example 6 A 25% by weight aqueous solution of glucosamine and chondroitin sulfate was obtained in the same manner as in Example 6. Using this aqueous solution, 250 to 300 g of granules were obtained in the same manner as in Example 1.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g, shark cartilage extract powder [chondroitin HG-40 for shark cartilage food (manufactured by Nippon Yakuhin)] and enzyme-treated rutin [ ⁇ G rutin PS (Toyo Seika Co., Ltd.) 12 g) was dissolved in 1116 mL of purified water to obtain a 25 wt% aqueous solution. Using this aqueous solution, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 850 kgf to obtain 20 tablets showing a hardness of 9.5 kgf.
- Example 2 The sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1 to obtain 20 tablets of 350 mg per tablet having a hardness of 6.6 kgf.
- Comparative Example 2 A 25% by weight aqueous solution of glucosamine hydrochloride was obtained in the same manner as in Comparative Example 1. Granules were obtained by the same method as in Example 1 using the aqueous solution.
- the sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1, and 20 tablets of 350 mg per tablet showing a hardness of 6.9 kgf were obtained.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g and shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g were suspended in 93 mL of purified water. Obtained.
- the suspension is dried for 15 hours with a freeze dryer [STD and BTD Eco tray dryer (manufactured by FTSSYSTEMS)] set at a vacuum of 20 mT or less, a cooler temperature of -80 ° C, and a shelf temperature of 30 ° C.
- a freeze dryer [STD and BTD Eco tray dryer (manufactured by FTSSYSTEMS)] set at a vacuum of 20 mT or less, a cooler temperature of -80 ° C, and a shelf temperature of 30 ° C.
- sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku)]
- Tricalcium phosphate Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.)]
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 80 g, Shark cartilage extract powder [Marinlinkerid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g and tricalcium phosphate [Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.) 1 g) is thoroughly mixed in a polyethylene bag, and the mixed powder is sieved using a No. 24 sieve (750 ⁇ m).
- a fluidized bed granulator [fluid granulation coating equipment FL-MINI type (Freund 20 g of purified water was sprayed on the mixed powder after sieving and granulated to obtain granules.
- To 47 g of the granules add 2.5 g of sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] and 0.5 g of tribasic calcium phosphate [Tribasic calcium phosphate (Taihei Chemical Sangyo Co., Ltd.)]. Mix thoroughly.
- the mixed powder was sieved using a No. 16 sieve (1000 ⁇ m) to obtain a sized powder.
- Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g, Shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 10 g, collagen [Water-soluble fish collagen (Kyowa Hakko Bio Co., Ltd.) )] 3 g and tricalcium phosphate [tricalcium phosphate (produced by Taihei Chemical Industrial Co., Ltd.)] 1 g were thoroughly mixed in a polyethylene bag.
- the tablet hardness in Examples and Comparative Examples of the present application represents the average value of the tablet hardness of 5 tablets randomly selected from the manufactured tablets in each of Examples 1-8 and Comparative Examples 1-7.
- Tables 1 to 3 show the results.
- the units of the numerical values of the spray-dried components and additional components in Table 1 below, the freeze-dried components and additional components in Table 2 and the granulated components and additional components in Table 3 are all by weight.
- G in Tables 1 to 3 below represents glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] ⁇
- A represents shark cartilage extract powder [Malinkin ridge 40S (manufactured by Yaizu Suisan Chemical Co., Ltd.)]
- B represents shark cartilage extract powder [SCP (NB) (manufactured by Maruha Nichiro)]
- C represents shark cartilage extract powder [chondroitin HG-40 for shark cartilage food (manufactured by Nippon Pharmaceutical)]
- D represents collagen [water-soluble Fish collagen cocoon (manufactured by Kyowa Hakko Bio)]
- E represents enzyme-treated rutin [ ⁇ G rutin PS (manufactured by Toyo Seika Co., Ltd.)] ⁇
- F represents sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku) H) represents tricalcium phosphat
- glucosamine or a salt thereof and chondroitin sulfate or a salt thereof containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof improved in tableting property and fluidity are used to increase the glucosamine or a salt thereof and chondroitin sulfate or a salt thereof. It was found that tablets containing were obtained.
- granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity and a tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof and a production thereof A method is provided.
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Abstract
After a solution or suspension is obtained by adding glucosamine or a salt thereof, chondroitin sulfate or a salt thereof, and other components as needed, granules or a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are obtained by spray-drying the solution or suspension. Tablets containing high amounts of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are obtained by tableting the granules or composition.
Description
本発明は、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒および組成物、ならびにグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤およびそれらの製造方法に関する。
The present invention relates to granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, as well as tablets containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, and their It relates to a manufacturing method.
グルコサミンは、動物体内では、軟骨や結合組織などにムコ多糖の構成成分として広く分布している単分子のアミノ糖で、具体的にはグルコースの2位の水酸基がアミノ基に置換した2-アミノグルコースである。また、カニやエビなどの甲殻類のキチンにも多く含まれている。
グルコサミンは、軟骨細胞により生産され、軟骨成分の生成を促進する。従って、グルコサミンは変形性関節症等の関節炎に有効とされ、栄養補給用サプリメントとして市販されている。 Glucosamine is a monomolecular amino sugar widely distributed as a component of mucopolysaccharide in cartilage and connective tissues in the animal body. Specifically, 2-amino acid in which the hydroxyl group at the 2-position of glucose is substituted with an amino group. Glucose. It is also abundant in crustacean chitin such as crabs and shrimps.
Glucosamine is produced by chondrocytes and promotes the production of cartilage components. Therefore, glucosamine is effective for arthritis such as osteoarthritis and is commercially available as a supplement for nutritional supplementation.
グルコサミンは、軟骨細胞により生産され、軟骨成分の生成を促進する。従って、グルコサミンは変形性関節症等の関節炎に有効とされ、栄養補給用サプリメントとして市販されている。 Glucosamine is a monomolecular amino sugar widely distributed as a component of mucopolysaccharide in cartilage and connective tissues in the animal body. Specifically, 2-amino acid in which the hydroxyl group at the 2-position of glucose is substituted with an amino group. Glucose. It is also abundant in crustacean chitin such as crabs and shrimps.
Glucosamine is produced by chondrocytes and promotes the production of cartilage components. Therefore, glucosamine is effective for arthritis such as osteoarthritis and is commercially available as a supplement for nutritional supplementation.
しかし、グルコサミンおよびその塩の結晶粉末は流動性が悪く、打錠機の臼への均一な充填が悪くなり、キャッピング、ラミネーション等の打錠障害の発生頻度が高まったり、錠剤の重量にバラツキが生じたりする等の問題があった。
一方、グルコサミンまたはその塩の結晶末を粉砕物とすることで、結着性の高い粉砕品を取得し、当該結着性の高い結晶と結着性の低い結晶末との両方を使用することで、タブレット用組成物の流動性を向上させ、打錠障害の発生頻度を低く抑えることができる(特許文献1)。しかし、該グルコサミン結晶粉砕物含有組成物は、流動性が実用上不十分である。 However, the crystal powder of glucosamine and its salts has poor fluidity, the uniform filling of the tablet machine into a die, and the occurrence of tableting troubles such as capping and lamination increases, and the tablet weight varies. There was a problem that occurred.
On the other hand, a pulverized product of glucosamine or a salt thereof is used to obtain a pulverized product with high binding properties, and both the crystal with high binding properties and the crystal powder with low binding properties are used. Thus, the fluidity of the tablet composition can be improved and the occurrence frequency of tableting troubles can be kept low (Patent Document 1). However, the glucosamine crystal pulverized product-containing composition has insufficient practical fluidity.
一方、グルコサミンまたはその塩の結晶末を粉砕物とすることで、結着性の高い粉砕品を取得し、当該結着性の高い結晶と結着性の低い結晶末との両方を使用することで、タブレット用組成物の流動性を向上させ、打錠障害の発生頻度を低く抑えることができる(特許文献1)。しかし、該グルコサミン結晶粉砕物含有組成物は、流動性が実用上不十分である。 However, the crystal powder of glucosamine and its salts has poor fluidity, the uniform filling of the tablet machine into a die, and the occurrence of tableting troubles such as capping and lamination increases, and the tablet weight varies. There was a problem that occurred.
On the other hand, a pulverized product of glucosamine or a salt thereof is used to obtain a pulverized product with high binding properties, and both the crystal with high binding properties and the crystal powder with low binding properties are used. Thus, the fluidity of the tablet composition can be improved and the occurrence frequency of tableting troubles can be kept low (Patent Document 1). However, the glucosamine crystal pulverized product-containing composition has insufficient practical fluidity.
また、グルコサミンに、グルコサミン以外の、デンプン、多糖類、単糖などの糖類を含有する溶液を噴霧した後、又は噴霧しつつ、造粒加工することによって、打錠加工に適した物性を有するグルコサミン顆粒が得られる (特許文献2)。
一方、コンドロイチン硫酸は、関節炎等に効果があり、コンドロイチン硫酸を含有する医薬品が市販されている。また、コンドロイチン硫酸、およびグルコサミンを含有し、人や動物の結合組織の治療用組成物が報告されている (特許文献3)。グルコサミンおよびコンドロイチン硫酸の投与による結合組織の治療に対する相乗効果が知られている。 Also, after spraying a solution containing saccharides such as starch, polysaccharides, and monosaccharides other than glucosamine on glucosamine, or by spraying, glucosamine has physical properties suitable for tableting. Granules are obtained (Patent Document 2).
On the other hand, chondroitin sulfate is effective for arthritis and the like, and pharmaceuticals containing chondroitin sulfate are commercially available. In addition, a composition for treating connective tissues of humans and animals containing chondroitin sulfate and glucosamine has been reported (Patent Document 3). Synergistic effects on the treatment of connective tissue by administration of glucosamine and chondroitin sulfate are known.
一方、コンドロイチン硫酸は、関節炎等に効果があり、コンドロイチン硫酸を含有する医薬品が市販されている。また、コンドロイチン硫酸、およびグルコサミンを含有し、人や動物の結合組織の治療用組成物が報告されている (特許文献3)。グルコサミンおよびコンドロイチン硫酸の投与による結合組織の治療に対する相乗効果が知られている。 Also, after spraying a solution containing saccharides such as starch, polysaccharides, and monosaccharides other than glucosamine on glucosamine, or by spraying, glucosamine has physical properties suitable for tableting. Granules are obtained (Patent Document 2).
On the other hand, chondroitin sulfate is effective for arthritis and the like, and pharmaceuticals containing chondroitin sulfate are commercially available. In addition, a composition for treating connective tissues of humans and animals containing chondroitin sulfate and glucosamine has been reported (Patent Document 3). Synergistic effects on the treatment of connective tissue by administration of glucosamine and chondroitin sulfate are known.
しかし、市販のグルコサミンサプリメントの多くは、グルコサミンの打錠性向上のために賦形剤を含有しており、そのためコンドロイチン硫酸およびグルコサミンの含量は低くならざるを得ない。
スプレードライで得られた顆粒を打錠に用いている例として、ナプロキセンまたはナプロキセンナトリウム、崩壊剤、結合剤からなる混合スラリーをスプレードライすることで、球状および多孔性でかつ流動性に優れたサイズの均一な粒子を与えること、および高度に圧縮可能であることが報告されている (特許文献4)。 However, many commercially available glucosamine supplements contain excipients to improve tableting properties of glucosamine, and therefore the contents of chondroitin sulfate and glucosamine must be lowered.
As an example of using granules obtained by spray-drying for tableting, spray-dried mixed slurry consisting of naproxen or naproxen sodium, a disintegrant, and a binder makes it spherical, porous, and excellent in fluidity Are reported to be uniform and highly compressible (Patent Document 4).
スプレードライで得られた顆粒を打錠に用いている例として、ナプロキセンまたはナプロキセンナトリウム、崩壊剤、結合剤からなる混合スラリーをスプレードライすることで、球状および多孔性でかつ流動性に優れたサイズの均一な粒子を与えること、および高度に圧縮可能であることが報告されている (特許文献4)。 However, many commercially available glucosamine supplements contain excipients to improve tableting properties of glucosamine, and therefore the contents of chondroitin sulfate and glucosamine must be lowered.
As an example of using granules obtained by spray-drying for tableting, spray-dried mixed slurry consisting of naproxen or naproxen sodium, a disintegrant, and a binder makes it spherical, porous, and excellent in fluidity Are reported to be uniform and highly compressible (Patent Document 4).
一方、スプレードライを用いて顆粒を製造することにより、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒および組成物が得られること、ならびにそれら顆粒または組成物を用いることによりグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤が得られることは知られていない。
On the other hand, by producing granules using spray drying, granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity can be obtained, and the granules or compositions thereof It is not known that tablets containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof can be obtained by using the product.
本発明の目的は、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒および組成物、ならびにグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤およびそれらの製造方法を提供することにある。
An object of the present invention is to provide granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, and tablets containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof It is in providing the manufacturing method of them.
本発明は以下の(1)~(19)に関する。
(1)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液1と略す)をスプレードライして得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(2)溶液1が、さらにコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液2と略す)である(1)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(3)溶液2に含有される化合物が、コラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物である(2)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(4)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するグルコサミンまたはその塩の含有量が60~95重量%である(1)~(3)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(5)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコンドロイチン硫酸またはその塩の含有量が3~20重量%である(1)~(4)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(6)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である(2)~(5)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(7)(1)~(6)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に、滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加して得られる組成物。
(8)(1)~(7)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物を打錠して得られる錠剤。
(9)錠剤に対する錠剤中のグルコサミンまたはその塩の含有量が60~95重量%である(8)に記載の錠剤。
(10)錠剤に対する錠剤中のコンドロイチン硫酸またはその塩の含有量が3~20重量%である(8)または(9)に記載の錠剤。
(11)錠剤に対する錠剤中のコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である(8)~(10)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤。
(12)溶液1または2をスプレードライする工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒の製造方法。
(13)溶液1または2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物の製造方法。
(14)溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である(12)または(13)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。
(15)溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が、1~6重量%である(12)~(14)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。
(16)溶液1または溶液2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒を用いて打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(17)溶液1または溶液2をスプレードライする工程、該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加し混合する工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物を打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(18)溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である(16)または(17)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(19)溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が1~6重量%である(16)~(18)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 The present invention relates to the following (1) to (19).
(1) Glucosamine or a salt thereof and chondroitin sulfate obtained by spray-drying a solution or suspension containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof (hereinafter, the solution or suspension is abbreviated as Solution 1) or Granules containing the salt.
(2) Solution 1 or suspension containing one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid A granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (1) which is a liquid (hereinafter, the solution or suspension is abbreviated as solution 2).
(3) The glucosamine or a salt thereof and chondroitin according to (2), wherein the compound contained in the solution 2 is one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof Granules containing sulfuric acid or a salt thereof.
(4) The glucosamine or salt thereof according to any one of (1) to (3), wherein the content of glucosamine or salt thereof is 60 to 95% by weight with respect to granules containing glucosamine or salt thereof and chondroitin sulfate or salt thereof And a granule containing chondroitin sulfate or a salt thereof.
(5) Glucosamine or a salt thereof according to any one of (1) to (4), wherein the content of chondroitin sulfate or a salt thereof is 3 to 20% by weight with respect to granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof Granules containing a salt and chondroitin sulfate or a salt thereof.
(6) One selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid for granules containing glucosamine or its salt and chondroitin sulfate or its salt A granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (2) to (5), wherein the total content of the above compounds is 0.1 to 10% by weight.
(7) The granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (1) to (6) is selected from the group consisting of a lubricant, a fluidity improver and an additive. A composition obtained by adding two or more compounds.
(8) A tablet obtained by tableting a granule or composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (1) to (7).
(9) The tablet according to (8), wherein the content of glucosamine or a salt thereof in the tablet is 60 to 95% by weight.
(10) The tablet according to (8) or (9), wherein the content of chondroitin sulfate or a salt thereof in the tablet is 3 to 20% by weight.
(11) The total content of one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in the tablet is 0.1 to A tablet containing 10% by weight of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (8) to (10).
(12) A method for producing granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising a step of spray-drying the solution 1 or 2.
(13) A step of spray-drying solution 1 or 2 and a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt obtained in the step are selected from the group consisting of a lubricant, a fluidity improver and an additive. A method for producing a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising the step of adding one or more compounds.
(14) Granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (12) or (13), wherein the content of glucosamine or a salt thereof contained in solution 1 or 2 is 15 to 27% by weight A method for producing the composition.
(15) The glucosamine or salt thereof and the chondroitin sulfate or salt thereof according to any one of (12) to (14), wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight A method for producing granules or compositions containing.
(16) A step of spray-drying solution 1 or solution 2 and a step of tableting using granules containing glucosamine or a salt thereof and chondroitin sulfate obtained in the step or glucosamine or a salt thereof and chondroitin sulfate or The manufacturing method of the tablet containing the salt.
(17) A step of spray-drying solution 1 or solution 2 and a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt obtained in the step selected from the group consisting of a lubricant, a fluidity improver and an additive And a step of tableting a composition containing glucosamine or a salt thereof and chondroitin sulfate obtained in the step, and a chondroitin sulfate or salt thereof. A method for producing tablets containing
(18) A tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (16) or (17), wherein the content of glucosamine or a salt thereof in solution 1 or 2 is 15 to 27% by weight Production method.
(19) The glucosamine or salt thereof and the chondroitin sulfate or salt thereof according to any one of (16) to (18), wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight. The manufacturing method of the tablet to contain.
(1)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液1と略す)をスプレードライして得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(2)溶液1が、さらにコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液2と略す)である(1)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(3)溶液2に含有される化合物が、コラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物である(2)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(4)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するグルコサミンまたはその塩の含有量が60~95重量%である(1)~(3)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(5)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコンドロイチン硫酸またはその塩の含有量が3~20重量%である(1)~(4)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(6)グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である(2)~(5)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。
(7)(1)~(6)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に、滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加して得られる組成物。
(8)(1)~(7)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物を打錠して得られる錠剤。
(9)錠剤に対する錠剤中のグルコサミンまたはその塩の含有量が60~95重量%である(8)に記載の錠剤。
(10)錠剤に対する錠剤中のコンドロイチン硫酸またはその塩の含有量が3~20重量%である(8)または(9)に記載の錠剤。
(11)錠剤に対する錠剤中のコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である(8)~(10)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤。
(12)溶液1または2をスプレードライする工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒の製造方法。
(13)溶液1または2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物の製造方法。
(14)溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である(12)または(13)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。
(15)溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が、1~6重量%である(12)~(14)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。
(16)溶液1または溶液2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒を用いて打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(17)溶液1または溶液2をスプレードライする工程、該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加し混合する工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物を打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(18)溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である(16)または(17)に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。
(19)溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が1~6重量%である(16)~(18)のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 The present invention relates to the following (1) to (19).
(1) Glucosamine or a salt thereof and chondroitin sulfate obtained by spray-drying a solution or suspension containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof (hereinafter, the solution or suspension is abbreviated as Solution 1) or Granules containing the salt.
(2) Solution 1 or suspension containing one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid A granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (1) which is a liquid (hereinafter, the solution or suspension is abbreviated as solution 2).
(3) The glucosamine or a salt thereof and chondroitin according to (2), wherein the compound contained in the solution 2 is one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof Granules containing sulfuric acid or a salt thereof.
(4) The glucosamine or salt thereof according to any one of (1) to (3), wherein the content of glucosamine or salt thereof is 60 to 95% by weight with respect to granules containing glucosamine or salt thereof and chondroitin sulfate or salt thereof And a granule containing chondroitin sulfate or a salt thereof.
(5) Glucosamine or a salt thereof according to any one of (1) to (4), wherein the content of chondroitin sulfate or a salt thereof is 3 to 20% by weight with respect to granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof Granules containing a salt and chondroitin sulfate or a salt thereof.
(6) One selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid for granules containing glucosamine or its salt and chondroitin sulfate or its salt A granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (2) to (5), wherein the total content of the above compounds is 0.1 to 10% by weight.
(7) The granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (1) to (6) is selected from the group consisting of a lubricant, a fluidity improver and an additive. A composition obtained by adding two or more compounds.
(8) A tablet obtained by tableting a granule or composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (1) to (7).
(9) The tablet according to (8), wherein the content of glucosamine or a salt thereof in the tablet is 60 to 95% by weight.
(10) The tablet according to (8) or (9), wherein the content of chondroitin sulfate or a salt thereof in the tablet is 3 to 20% by weight.
(11) The total content of one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in the tablet is 0.1 to A tablet containing 10% by weight of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of (8) to (10).
(12) A method for producing granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising a step of spray-drying the solution 1 or 2.
(13) A step of spray-drying solution 1 or 2 and a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt obtained in the step are selected from the group consisting of a lubricant, a fluidity improver and an additive. A method for producing a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising the step of adding one or more compounds.
(14) Granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (12) or (13), wherein the content of glucosamine or a salt thereof contained in solution 1 or 2 is 15 to 27% by weight A method for producing the composition.
(15) The glucosamine or salt thereof and the chondroitin sulfate or salt thereof according to any one of (12) to (14), wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight A method for producing granules or compositions containing.
(16) A step of spray-drying solution 1 or solution 2 and a step of tableting using granules containing glucosamine or a salt thereof and chondroitin sulfate obtained in the step or glucosamine or a salt thereof and chondroitin sulfate or The manufacturing method of the tablet containing the salt.
(17) A step of spray-drying solution 1 or solution 2 and a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt obtained in the step selected from the group consisting of a lubricant, a fluidity improver and an additive And a step of tableting a composition containing glucosamine or a salt thereof and chondroitin sulfate obtained in the step, and a chondroitin sulfate or salt thereof. A method for producing tablets containing
(18) A tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to (16) or (17), wherein the content of glucosamine or a salt thereof in solution 1 or 2 is 15 to 27% by weight Production method.
(19) The glucosamine or salt thereof and the chondroitin sulfate or salt thereof according to any one of (16) to (18), wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight. The manufacturing method of the tablet to contain.
本発明により、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒および組成物、ならびにグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤およびそれらの製造方法を提供することができる。
According to the present invention, granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tabletability and fluidity, and tablets containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof and A manufacturing method can be provided.
以下、本発明を詳細に説明する。
本発明で用いられるグルコサミンは、例えば、発酵生産する方法、エビ・カニから抽出する方法等により取得することができる。また、グルコサミンは、各社の市販品を購入することにより入手することもできる。
グルコサミンを発酵生産する方法としては、例えば、植物を原料として微生物発酵により製造する方法等が挙げられ、好ましくは、Metabolic Engineering. 7 (3), 2005, 201-214に記載の方法が挙げられる。 Hereinafter, the present invention will be described in detail.
The glucosamine used in the present invention can be obtained by, for example, a method for producing by fermentation, a method for extracting from shrimp or crab, and the like. Glucosamine can also be obtained by purchasing a commercial product from each company.
Examples of the method for fermentative production of glucosamine include a method of producing glucosamine by microbial fermentation using a plant as a raw material, and a method described in Metabolic Engineering. 7 (3), 2005, 201-214 is preferable.
本発明で用いられるグルコサミンは、例えば、発酵生産する方法、エビ・カニから抽出する方法等により取得することができる。また、グルコサミンは、各社の市販品を購入することにより入手することもできる。
グルコサミンを発酵生産する方法としては、例えば、植物を原料として微生物発酵により製造する方法等が挙げられ、好ましくは、Metabolic Engineering. 7 (3), 2005, 201-214に記載の方法が挙げられる。 Hereinafter, the present invention will be described in detail.
The glucosamine used in the present invention can be obtained by, for example, a method for producing by fermentation, a method for extracting from shrimp or crab, and the like. Glucosamine can also be obtained by purchasing a commercial product from each company.
Examples of the method for fermentative production of glucosamine include a method of producing glucosamine by microbial fermentation using a plant as a raw material, and a method described in Metabolic Engineering. 7 (3), 2005, 201-214 is preferable.
グルコサミンをエビ・カニから抽出する方法としては、例えば、エビやカニの殻を原料としてキチンを抽出し、これを加水分解後、精製し、乾燥して調製する方法等が挙げられ、好ましくは特開2004-359908、US3683076等に記載の方法が挙げられる。
市販されているグルコサミンとしては、例えば、発酵グルコサミンK(協和発酵バイオ社製)、グルコサミンFM(協和発酵バイオ社製)を挙げられる。 Examples of the method for extracting glucosamine from shrimp and crab include a method of extracting chitin from shrimp and crab shells, hydrolyzing it, purifying it, and drying it. The methods described in Kaikai 2004-359908, US3683076 and the like can be mentioned.
Examples of commercially available glucosamine include fermented glucosamine K (manufactured by Kyowa Hakko Bio) and glucosamine FM (manufactured by Kyowa Hakko Bio).
市販されているグルコサミンとしては、例えば、発酵グルコサミンK(協和発酵バイオ社製)、グルコサミンFM(協和発酵バイオ社製)を挙げられる。 Examples of the method for extracting glucosamine from shrimp and crab include a method of extracting chitin from shrimp and crab shells, hydrolyzing it, purifying it, and drying it. The methods described in Kaikai 2004-359908, US3683076 and the like can be mentioned.
Examples of commercially available glucosamine include fermented glucosamine K (manufactured by Kyowa Hakko Bio) and glucosamine FM (manufactured by Kyowa Hakko Bio).
本発明で用いるグルコサミンまたはその塩は、市販のグルコサミンまたはその塩でもよいし、またはキチンの加水分解および精製により得られるグルコサミン等をそのまま用いる、上記製造法後に乾燥工程を省略した未乾燥のグルコサミンまたはその塩を用いる、もしくは、グルコサミンまたはその塩を粉砕して用いる方法でもよい。グルコサミンまたはその塩の粉砕方法は、外力による圧縮、衝撃またはせん断や、粒子自身の慣性力による衝突または摩擦のいずれの原理を用いてもよく、例えば、ボールミル、ローラーミル、高速回転ミル、ジェットミル等を用いる粉砕方法等が挙げられる。
Glucosamine or a salt thereof used in the present invention may be a commercially available glucosamine or a salt thereof, or glucosamine obtained by hydrolysis and purification of chitin, etc. A method of using the salt or pulverizing glucosamine or a salt thereof may be used. The pulverization method of glucosamine or a salt thereof may use any of the principles of compression, impact or shear by external force, and collision or friction by the inertial force of the particle itself, for example, ball mill, roller mill, high-speed rotary mill, jet mill. And the like.
ボールミルとしては、例えば、転動ボールミル、遊星ミル等が挙げられ、ローラーミルとしては、例えば、堅式ローラーミル、ロールクラッシャー、高圧ロールプレス等が挙げられ、高速回転ミルとしては、例えば、ハンマーミル、ピンミル、ケージミル等が挙げられる。
本発明におけるコンドロイチン硫酸またはその塩は、例えば、化学的に合成する方法、または抽出する方法等により取得することができる。また、コンドロイチン硫酸は、各社の市販品を購入することにより入手することもできる。 Examples of the ball mill include a rolling ball mill and a planetary mill. Examples of the roller mill include a solid roller mill, a roll crusher, and a high-pressure roll press. Examples of the high-speed rotation mill include a hammer mill. , Pin mill, cage mill and the like.
The chondroitin sulfate or a salt thereof in the present invention can be obtained by, for example, a chemical synthesis method or an extraction method. Moreover, chondroitin sulfate can also be obtained by purchasing a commercial product of each company.
本発明におけるコンドロイチン硫酸またはその塩は、例えば、化学的に合成する方法、または抽出する方法等により取得することができる。また、コンドロイチン硫酸は、各社の市販品を購入することにより入手することもできる。 Examples of the ball mill include a rolling ball mill and a planetary mill. Examples of the roller mill include a solid roller mill, a roll crusher, and a high-pressure roll press. Examples of the high-speed rotation mill include a hammer mill. , Pin mill, cage mill and the like.
The chondroitin sulfate or a salt thereof in the present invention can be obtained by, for example, a chemical synthesis method or an extraction method. Moreover, chondroitin sulfate can also be obtained by purchasing a commercial product of each company.
コンドロイチン硫酸を化学的に合成する方法としては、例えば特開2003-199583に記載の方法等が挙げられる。
コンドロイチン硫酸を抽出する方法としては、例えば特開2014-009164に記載の方法等が挙げられる。
該抽出する方法等により取得することができるコンドロイチン硫酸は、どのような生物に由来するものでもよく、例えば、エイやサメ、ウシ、クジラ、ウサギ、ヒツジ、カブトガニ、ブタ、イカ等の動物を挙げることができる。 Examples of the method for chemically synthesizing chondroitin sulfate include the method described in JP-A-2003-199583.
Examples of the method for extracting chondroitin sulfate include the method described in JP-A-2014-009164.
The chondroitin sulfate that can be obtained by the extraction method and the like may be derived from any organism, and examples include animals such as rays, sharks, cows, whales, rabbits, sheep, horseshoe crabs, pigs, squids, and the like. be able to.
コンドロイチン硫酸を抽出する方法としては、例えば特開2014-009164に記載の方法等が挙げられる。
該抽出する方法等により取得することができるコンドロイチン硫酸は、どのような生物に由来するものでもよく、例えば、エイやサメ、ウシ、クジラ、ウサギ、ヒツジ、カブトガニ、ブタ、イカ等の動物を挙げることができる。 Examples of the method for chemically synthesizing chondroitin sulfate include the method described in JP-A-2003-199583.
Examples of the method for extracting chondroitin sulfate include the method described in JP-A-2014-009164.
The chondroitin sulfate that can be obtained by the extraction method and the like may be derived from any organism, and examples include animals such as rays, sharks, cows, whales, rabbits, sheep, horseshoe crabs, pigs, squids, and the like. be able to.
コンドロイチン硫酸の市販品としては、例えば、サメ軟骨、サメヒレ軟骨等の原料から抽出して粉末化したコンドロイチン硫酸を含有するサメ軟骨抽出粉末等が挙げられ、例えばマリンカーティリッジ40S(焼津水産化学工業社製)、SCP(NB)(マルハニチロ社製)、サメ軟骨食品用コンドロイチンHG-40 (日本薬品社製)等が挙げられる。
グルコサミンの塩およびコンドロイチンの塩としては、それぞれ同一または異なって、酸付加塩、金属塩、アンモニウム塩、有機アミン付加塩、アミノ酸付加塩等があげられる。 Commercially available products of chondroitin sulfate include, for example, shark cartilage extract powder containing chondroitin sulfate extracted from raw materials such as shark cartilage and shark fin cartilage. ), SCP (NB) (manufactured by Maruha Nichiro), chondroitin HG-40 for shark cartilage food (manufactured by Nippon Pharmaceutical Co., Ltd.), and the like.
The salt of glucosamine and the salt of chondroitin are the same or different and include acid addition salts, metal salts, ammonium salts, organic amine addition salts, amino acid addition salts, and the like.
グルコサミンの塩およびコンドロイチンの塩としては、それぞれ同一または異なって、酸付加塩、金属塩、アンモニウム塩、有機アミン付加塩、アミノ酸付加塩等があげられる。 Commercially available products of chondroitin sulfate include, for example, shark cartilage extract powder containing chondroitin sulfate extracted from raw materials such as shark cartilage and shark fin cartilage. ), SCP (NB) (manufactured by Maruha Nichiro), chondroitin HG-40 for shark cartilage food (manufactured by Nippon Pharmaceutical Co., Ltd.), and the like.
The salt of glucosamine and the salt of chondroitin are the same or different and include acid addition salts, metal salts, ammonium salts, organic amine addition salts, amino acid addition salts, and the like.
酸付加塩としては、例えば、塩酸塩、硫酸塩、硝酸塩、リン酸塩等の無機酸塩、酢酸塩、マレイン酸塩、フマル酸塩、クエン酸塩、リンゴ酸塩、乳酸塩、α-ケトグルタル酸塩、グルコン酸塩、カプリル酸塩等の有機酸塩等があげられる。
金属塩としては、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩、マグネシウム塩、カルシウム塩等のアルカリ土類金属塩、アルミニウム塩、亜鉛塩等があげられる。 Examples of the acid addition salt include inorganic acid salts such as hydrochloride, sulfate, nitrate, and phosphate, acetate, maleate, fumarate, citrate, malate, lactate, α-ketoglutar And organic acid salts such as acid salts, gluconates and caprylates.
Examples of the metal salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as magnesium salt and calcium salt, aluminum salt, zinc salt and the like.
金属塩としては、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩、マグネシウム塩、カルシウム塩等のアルカリ土類金属塩、アルミニウム塩、亜鉛塩等があげられる。 Examples of the acid addition salt include inorganic acid salts such as hydrochloride, sulfate, nitrate, and phosphate, acetate, maleate, fumarate, citrate, malate, lactate, α-ketoglutar And organic acid salts such as acid salts, gluconates and caprylates.
Examples of the metal salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as magnesium salt and calcium salt, aluminum salt, zinc salt and the like.
アンモニウム塩としては、例えば、アンモニウム、テトラメチルアンモニウム等の塩があげられる。
有機アミン付加塩としては、例えば、モルホリン、ピペリジン等の塩があげられる。 アミノ酸付加塩としては、例えば、グリシン、フェニルアラニン、リジン、アスパラギン酸、グルタミン酸等の塩があげられる。 Examples of the ammonium salt include salts such as ammonium and tetramethylammonium.
Examples of organic amine addition salts include salts of morpholine, piperidine and the like. Examples of the amino acid addition salt include salts of glycine, phenylalanine, lysine, aspartic acid, glutamic acid and the like.
有機アミン付加塩としては、例えば、モルホリン、ピペリジン等の塩があげられる。 アミノ酸付加塩としては、例えば、グリシン、フェニルアラニン、リジン、アスパラギン酸、グルタミン酸等の塩があげられる。 Examples of the ammonium salt include salts such as ammonium and tetramethylammonium.
Examples of organic amine addition salts include salts of morpholine, piperidine and the like. Examples of the amino acid addition salt include salts of glycine, phenylalanine, lysine, aspartic acid, glutamic acid and the like.
本発明におけるグルコサミンとグルコサミンの塩を比較すると、グルコサミンの塩の方が、熱に安定で褐変し難いこと、および経口摂取した後、腸管から吸収され易いため好ましく、グルコサミン塩酸塩の使用がより好ましい。
1.本発明の顆粒、組成物および錠剤
本発明の顆粒は、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒であり、より具体的にはグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する溶液をスプレードライすることにより得られる顆粒である。さらに、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に加え、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を含有する溶液、好ましくはグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に加えられる化合物が、コラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物である溶液をスプレードライすることにより得られる顆粒もまた、本発明の顆粒である。 Comparing the glucosamine and glucosamine salts in the present invention, the glucosamine salt is preferable because it is stable to heat and less likely to brown, and is easily absorbed from the intestinal tract after ingestion, and the use of glucosamine hydrochloride is more preferable .
1. Granule, composition and tablet of the present invention The granule of the present invention is a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity, more specifically, glucosamine or a salt thereof. And a granule obtained by spray-drying a solution containing chondroitin sulfate or a salt thereof. Furthermore, in addition to glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin And a solution containing one or more compounds selected from the group consisting of pantothenic acid, preferably a compound added to glucosamine or a salt thereof and chondroitin sulfate or a salt thereof is collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof Granules obtained by spray-drying a solution that is one or more compounds selected from the group consisting of are also the granules of the present invention.
1.本発明の顆粒、組成物および錠剤
本発明の顆粒は、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒であり、より具体的にはグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する溶液をスプレードライすることにより得られる顆粒である。さらに、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に加え、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を含有する溶液、好ましくはグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に加えられる化合物が、コラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物である溶液をスプレードライすることにより得られる顆粒もまた、本発明の顆粒である。 Comparing the glucosamine and glucosamine salts in the present invention, the glucosamine salt is preferable because it is stable to heat and less likely to brown, and is easily absorbed from the intestinal tract after ingestion, and the use of glucosamine hydrochloride is more preferable .
1. Granule, composition and tablet of the present invention The granule of the present invention is a granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity, more specifically, glucosamine or a salt thereof. And a granule obtained by spray-drying a solution containing chondroitin sulfate or a salt thereof. Furthermore, in addition to glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin And a solution containing one or more compounds selected from the group consisting of pantothenic acid, preferably a compound added to glucosamine or a salt thereof and chondroitin sulfate or a salt thereof is collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof Granules obtained by spray-drying a solution that is one or more compounds selected from the group consisting of are also the granules of the present invention.
コラーゲンまたはその酵素処理物は、豚、牛、鶏等の家畜由来、魚介類由来のもの等、動物由来のものであればいずれでもよい。また、コラーゲンとしては、例えば、水溶性コラーゲンペプチドSS、HPフィッシュコラーゲン(以上、協和発酵バイオ社製)等、市販のものを用いてもよい。
ルチンまたはその酵素処理物における、ルチンの酵素処理物は、ルチンおよびルチン類縁体を酵素処理によって配糖体化したものであり、該ルチン類縁体としては、例えば、ケルセチン、イソクエルシトリン、モリン、ミリシトリン、ミリセチン等が挙げられ、酵素処理物または酵素処理における該酵素としては、例えば、α-グルコシル糖転移酵素等が挙げられる。 The collagen or enzyme-treated product thereof may be any animal-derived one, such as those derived from domestic animals such as pigs, cows, chickens, and seafood. As the collagen, for example, commercially available products such as water-soluble collagen peptide SS, HP fish collagen (manufactured by Kyowa Hakko Bio) may be used.
The rutin enzyme-treated product in rutin or an enzyme-treated product thereof is a product of rutin and a rutin analog converted to a glycoside by enzymatic treatment. Examples of the rutin analog include quercetin, isoquercitrin, morin, Examples of the enzyme-treated product or enzyme in the enzyme treatment include α-glucosyl glycosyltransferase.
ルチンまたはその酵素処理物における、ルチンの酵素処理物は、ルチンおよびルチン類縁体を酵素処理によって配糖体化したものであり、該ルチン類縁体としては、例えば、ケルセチン、イソクエルシトリン、モリン、ミリシトリン、ミリセチン等が挙げられ、酵素処理物または酵素処理における該酵素としては、例えば、α-グルコシル糖転移酵素等が挙げられる。 The collagen or enzyme-treated product thereof may be any animal-derived one, such as those derived from domestic animals such as pigs, cows, chickens, and seafood. As the collagen, for example, commercially available products such as water-soluble collagen peptide SS, HP fish collagen (manufactured by Kyowa Hakko Bio) may be used.
The rutin enzyme-treated product in rutin or an enzyme-treated product thereof is a product of rutin and a rutin analog converted to a glycoside by enzymatic treatment. Examples of the rutin analog include quercetin, isoquercitrin, morin, Examples of the enzyme-treated product or enzyme in the enzyme treatment include α-glucosyl glycosyltransferase.
α-グルコシル糖転移酵素はα-グルコシドを加水分解し、生じた糖をそのまま別のアグリコンに付加させる酵素を表す。
ルチンの酵素処理物は、同様の配合組成を有する組成物であれば、その由来については特に制限はないが、例えば、エンジュ、ソバ等の抽出物を糖転移酵素で処理する方法等によって得ることができる。具体的には特開平7-10898、特開2003-33164等に記載の方法で得ることができる。 α-Glucosyl glycosyltransferase is an enzyme that hydrolyzes α-glucoside and adds the resulting sugar directly to another aglycone.
The origin of the rutin enzyme-treated product is not particularly limited as long as it is a composition having the same composition, but it can be obtained by, for example, a method of treating an extract such as Enju or buckwheat with a glycosyltransferase. Can do. Specifically, it can be obtained by the methods described in JP-A-7-10898, JP-A-2003-33164 and the like.
ルチンの酵素処理物は、同様の配合組成を有する組成物であれば、その由来については特に制限はないが、例えば、エンジュ、ソバ等の抽出物を糖転移酵素で処理する方法等によって得ることができる。具体的には特開平7-10898、特開2003-33164等に記載の方法で得ることができる。 α-Glucosyl glycosyltransferase is an enzyme that hydrolyzes α-glucoside and adds the resulting sugar directly to another aglycone.
The origin of the rutin enzyme-treated product is not particularly limited as long as it is a composition having the same composition, but it can be obtained by, for example, a method of treating an extract such as Enju or buckwheat with a glycosyltransferase. Can do. Specifically, it can be obtained by the methods described in JP-A-7-10898, JP-A-2003-33164 and the like.
チアミンは、ビタミンB1とも呼ばれる水溶性ビタミンで、糖質および分岐鎖脂肪酸の代謝に用いられるものを表す。
リボフラビンは、ビタミンB2、ラクトフラビンとも呼ばれる水溶性ビタミンで、脂肪、炭水化物およびタンパク質の代謝や呼吸に用いられるものを表す。
ピリドキシンとはビタミンB6に分類される化合物のひとつである水溶性ビタミンで、赤血球生産の促進等の機能を持つものを表す。 Thiamin is a water-soluble vitamin, also called vitamin B1, which is used for the metabolism of carbohydrates and branched chain fatty acids.
Riboflavin is a water-soluble vitamin, also called vitamin B2 or lactoflavin, which is used for the metabolism and respiration of fats, carbohydrates and proteins.
Pyridoxine is a water-soluble vitamin that is one of the compounds classified into vitamin B6 and represents a function that promotes red blood cell production.
リボフラビンは、ビタミンB2、ラクトフラビンとも呼ばれる水溶性ビタミンで、脂肪、炭水化物およびタンパク質の代謝や呼吸に用いられるものを表す。
ピリドキシンとはビタミンB6に分類される化合物のひとつである水溶性ビタミンで、赤血球生産の促進等の機能を持つものを表す。 Thiamin is a water-soluble vitamin, also called vitamin B1, which is used for the metabolism of carbohydrates and branched chain fatty acids.
Riboflavin is a water-soluble vitamin, also called vitamin B2 or lactoflavin, which is used for the metabolism and respiration of fats, carbohydrates and proteins.
Pyridoxine is a water-soluble vitamin that is one of the compounds classified into vitamin B6 and represents a function that promotes red blood cell production.
ナイアシンとはニコチン酸とニコチン酸アミドの総称でビタミンB3とも呼ばれる水溶性ビタミンであり、循環系、消化系、神経系の働きを促進する等の機能をもつものを表す。
上記リボフラビン、ピリドキシン、ナイアシンおよびチアミンは、各化合物の塩であってもよく、塩としては、それぞれ、同一または異なって、塩酸塩、硫酸塩、硝酸塩、セシル硫酸塩等が挙げられ、塩酸塩が好ましい。 Niacin is a water-soluble vitamin, also called vitamin B3, which is a general term for nicotinic acid and nicotinamide, and has functions such as promoting the functions of the circulatory system, digestive system, and nervous system.
The riboflavin, pyridoxine, niacin and thiamine may be salts of the respective compounds, and the salts may be the same or different, and include hydrochloride, sulfate, nitrate, cecil sulfate, etc. preferable.
上記リボフラビン、ピリドキシン、ナイアシンおよびチアミンは、各化合物の塩であってもよく、塩としては、それぞれ、同一または異なって、塩酸塩、硫酸塩、硝酸塩、セシル硫酸塩等が挙げられ、塩酸塩が好ましい。 Niacin is a water-soluble vitamin, also called vitamin B3, which is a general term for nicotinic acid and nicotinamide, and has functions such as promoting the functions of the circulatory system, digestive system, and nervous system.
The riboflavin, pyridoxine, niacin and thiamine may be salts of the respective compounds, and the salts may be the same or different, and include hydrochloride, sulfate, nitrate, cecil sulfate, etc. preferable.
パントテン酸は、D(+)-N-(2,4-ジヒドロキシ-3,3-ジメチルブチリル)-β-アラニンであり、ビタミンB群に含まれる水溶性ビタミンで、CoA(補酵素A)の構成成分として、糖代謝や脂肪酸代謝に関わる物質のことを表す。パントテン酸は、塩であってもよく、塩としては例えば、カルシウム塩、ナトリウム塩等が挙げられ、カルシウム塩が好ましい。
上記チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸は、蛋白質加水分解法、化学合成法、酵素法又は発酵法など、いずれの製造方法で製造されたものでもよいし、市販品を用いることもできる。 Pantothenic acid is D (+)-N- (2,4-dihydroxy-3,3-dimethylbutyryl) -β-alanine, a water-soluble vitamin contained in the vitamin B group. CoA (coenzyme A) It represents a substance involved in sugar metabolism and fatty acid metabolism. Pantothenic acid may be a salt. Examples of the salt include calcium salt and sodium salt, and calcium salt is preferable.
The thiamine, riboflavin, pyridoxine, niacin and pantothenic acid may be produced by any production method such as a protein hydrolysis method, a chemical synthesis method, an enzymatic method or a fermentation method, or a commercially available product may be used.
上記チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸は、蛋白質加水分解法、化学合成法、酵素法又は発酵法など、いずれの製造方法で製造されたものでもよいし、市販品を用いることもできる。 Pantothenic acid is D (+)-N- (2,4-dihydroxy-3,3-dimethylbutyryl) -β-alanine, a water-soluble vitamin contained in the vitamin B group. CoA (coenzyme A) It represents a substance involved in sugar metabolism and fatty acid metabolism. Pantothenic acid may be a salt. Examples of the salt include calcium salt and sodium salt, and calcium salt is preferable.
The thiamine, riboflavin, pyridoxine, niacin and pantothenic acid may be produced by any production method such as a protein hydrolysis method, a chemical synthesis method, an enzymatic method or a fermentation method, or a commercially available product may be used.
本発明の組成物は、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物であり、より具体的には本発明の顆粒に滑沢剤、流動性改善剤、および添加物からなる群より選ばれる1つ以上の化合物を添加して得られる組成物である。
滑沢剤としては、食品等に使用できるものであれば特に制限されないが、例えば、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、ショ糖脂肪酸エステル、グリセリン脂肪酸エステル、硬化油脂、微粒二酸化ケイ素等が挙げられる。滑沢剤は、錠剤の表面のみにあっても、錠剤内部に分散していてもよい。本発明の錠剤中で滑沢剤が占める割合は、合計で0.5~12重量%が好ましく、1~10重量%がより好ましい。また、2種類以上の滑沢剤を用いても良い。 The composition of the present invention is a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tableting properties and fluidity. More specifically, the granule of the present invention contains a lubricant, fluidity. It is a composition obtained by adding one or more compounds selected from the group consisting of an improving agent and additives.
The lubricant is not particularly limited as long as it can be used for foods and the like, and examples thereof include stearic acid, magnesium stearate, calcium stearate, sucrose fatty acid ester, glycerin fatty acid ester, hardened oil and fat, fine silicon dioxide and the like. It is done. The lubricant may be present only on the surface of the tablet or may be dispersed inside the tablet. The total proportion of lubricants in the tablet of the present invention is preferably 0.5 to 12% by weight, more preferably 1 to 10% by weight. Two or more kinds of lubricants may be used.
滑沢剤としては、食品等に使用できるものであれば特に制限されないが、例えば、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、ショ糖脂肪酸エステル、グリセリン脂肪酸エステル、硬化油脂、微粒二酸化ケイ素等が挙げられる。滑沢剤は、錠剤の表面のみにあっても、錠剤内部に分散していてもよい。本発明の錠剤中で滑沢剤が占める割合は、合計で0.5~12重量%が好ましく、1~10重量%がより好ましい。また、2種類以上の滑沢剤を用いても良い。 The composition of the present invention is a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof with improved tableting properties and fluidity. More specifically, the granule of the present invention contains a lubricant, fluidity. It is a composition obtained by adding one or more compounds selected from the group consisting of an improving agent and additives.
The lubricant is not particularly limited as long as it can be used for foods and the like, and examples thereof include stearic acid, magnesium stearate, calcium stearate, sucrose fatty acid ester, glycerin fatty acid ester, hardened oil and fat, fine silicon dioxide and the like. It is done. The lubricant may be present only on the surface of the tablet or may be dispersed inside the tablet. The total proportion of lubricants in the tablet of the present invention is preferably 0.5 to 12% by weight, more preferably 1 to 10% by weight. Two or more kinds of lubricants may be used.
流動性改善剤としては、食品等に使用できるものであれば特に制限されないが、例えば、第三リン酸カルシウム、リン酸水素カルシウム等があげられる。本発明の錠剤中で流動性改善剤が占める割合は、0.1~7質量%が好ましく、0.5~6質量%がより好ましい。
添加物としては、例えば、崩壊剤、糖類、甘味料、香料、酸味料、結合剤、抗酸化剤、着色剤等が挙げられ、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸も本発明の顆粒に添加する添加物として用いてもよい。 The fluidity improver is not particularly limited as long as it can be used in foods and the like, and examples thereof include tricalcium phosphate and calcium hydrogen phosphate. The proportion of the fluidity improving agent in the tablet of the present invention is preferably 0.1 to 7% by mass, and more preferably 0.5 to 6% by mass.
Examples of additives include disintegrants, sugars, sweeteners, flavors, acidulants, binders, antioxidants, colorants, etc., collagen or enzyme-treated products thereof, rutin or enzyme-treated products thereof, thiamine, Riboflavin, pyridoxine, niacin and pantothenic acid may also be used as additives added to the granules of the present invention.
添加物としては、例えば、崩壊剤、糖類、甘味料、香料、酸味料、結合剤、抗酸化剤、着色剤等が挙げられ、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸も本発明の顆粒に添加する添加物として用いてもよい。 The fluidity improver is not particularly limited as long as it can be used in foods and the like, and examples thereof include tricalcium phosphate and calcium hydrogen phosphate. The proportion of the fluidity improving agent in the tablet of the present invention is preferably 0.1 to 7% by mass, and more preferably 0.5 to 6% by mass.
Examples of additives include disintegrants, sugars, sweeteners, flavors, acidulants, binders, antioxidants, colorants, etc., collagen or enzyme-treated products thereof, rutin or enzyme-treated products thereof, thiamine, Riboflavin, pyridoxine, niacin and pantothenic acid may also be used as additives added to the granules of the present invention.
崩壊剤としては、例えば、デンプン、寒天、ゼラチン末、結晶セルロース、炭酸カルシウム、炭酸水素ナトリウム、クエン酸カルシウム、デキストラン、ペクチン、低置換度ヒドロキシプロピルセルロース、クロスカルメロースナトリウム、カルボキシメチルセルロース、カルボキシメチルセルロースナトリウム、カルボキシメチルセルロースカルシウム、カルボキシメチルスターチナトリウム、低置換度カルボキシメチルスターチナトリウム、クロスポビドン等が挙げられる。
Examples of disintegrants include starch, agar, gelatin powder, crystalline cellulose, calcium carbonate, sodium bicarbonate, calcium citrate, dextran, pectin, low-substituted hydroxypropyl cellulose, croscarmellose sodium, carboxymethyl cellulose, carboxymethyl cellulose sodium. Carboxymethyl cellulose calcium, sodium carboxymethyl starch, sodium carboxymethyl starch having a low degree of substitution, crospovidone and the like.
糖類としては、食品等に使用できるものであれば特に制限されないが、例えば、単糖類、二糖類、糖アルコール、オリゴ糖等があげられ、好ましくは糖アルコールがあげられる。
単糖類としては、例えば、グルコース、キシロース、ガラクトース、フラクトース等が挙げられる。二糖類としては、例えば、トレハロース、蔗糖、乳糖、パラチノース等が挙げられる。糖アルコールとしては、例えばマルチトール、エリスリトール、ソルビトール、キシリトール等が挙げられる。オリゴ糖としては、例えばラフィノース、イヌロオリゴ糖 (チコリオリゴ糖)、パラチノースオリゴ糖等が挙げられる。本発明の錠剤中で糖類が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The saccharide is not particularly limited as long as it can be used for food and the like, and examples thereof include monosaccharides, disaccharides, sugar alcohols, oligosaccharides, and preferably sugar alcohols.
Examples of monosaccharides include glucose, xylose, galactose, and fructose. Examples of the disaccharide include trehalose, sucrose, lactose, palatinose, and the like. Examples of the sugar alcohol include maltitol, erythritol, sorbitol, xylitol and the like. Examples of the oligosaccharide include raffinose, inulooligosaccharide (chicory oligosaccharide), palatinose oligosaccharide and the like. The proportion of saccharides in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
単糖類としては、例えば、グルコース、キシロース、ガラクトース、フラクトース等が挙げられる。二糖類としては、例えば、トレハロース、蔗糖、乳糖、パラチノース等が挙げられる。糖アルコールとしては、例えばマルチトール、エリスリトール、ソルビトール、キシリトール等が挙げられる。オリゴ糖としては、例えばラフィノース、イヌロオリゴ糖 (チコリオリゴ糖)、パラチノースオリゴ糖等が挙げられる。本発明の錠剤中で糖類が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The saccharide is not particularly limited as long as it can be used for food and the like, and examples thereof include monosaccharides, disaccharides, sugar alcohols, oligosaccharides, and preferably sugar alcohols.
Examples of monosaccharides include glucose, xylose, galactose, and fructose. Examples of the disaccharide include trehalose, sucrose, lactose, palatinose, and the like. Examples of the sugar alcohol include maltitol, erythritol, sorbitol, xylitol and the like. Examples of the oligosaccharide include raffinose, inulooligosaccharide (chicory oligosaccharide), palatinose oligosaccharide and the like. The proportion of saccharides in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
甘味料としては、食品等に使用できるものであれば特に制限されないが、例えば、サッカリンナトリウム、グリチルリチン二カリウム、アスパルテーム、ステビア、ソーマチン等が挙げられる。本発明の錠剤中で甘味剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。
香料としては、食品に使用できるものであれば特に制限されないが、例えばレモンフレーバー、レモンライムフレーバー、グレープフルーツフレーバー、アップルフレーバー等が挙げられる。本発明の錠剤中で香料が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The sweetener is not particularly limited as long as it can be used in foods, and examples thereof include sodium saccharin, dipotassium glycyrrhizin, aspartame, stevia, thaumatin and the like. The proportion of the sweetener in the tablet of the present invention is not particularly limited as long as it is within the range of the general use in the preparation.
Although it will not restrict | limit especially as a fragrance | flavor if it can be used for a foodstuff, For example, lemon flavor, lemon-lime flavor, grapefruit flavor, apple flavor etc. are mentioned. The proportion of the fragrance in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
香料としては、食品に使用できるものであれば特に制限されないが、例えばレモンフレーバー、レモンライムフレーバー、グレープフルーツフレーバー、アップルフレーバー等が挙げられる。本発明の錠剤中で香料が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The sweetener is not particularly limited as long as it can be used in foods, and examples thereof include sodium saccharin, dipotassium glycyrrhizin, aspartame, stevia, thaumatin and the like. The proportion of the sweetener in the tablet of the present invention is not particularly limited as long as it is within the range of the general use in the preparation.
Although it will not restrict | limit especially as a fragrance | flavor if it can be used for a foodstuff, For example, lemon flavor, lemon-lime flavor, grapefruit flavor, apple flavor etc. are mentioned. The proportion of the fragrance in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
酸味料としては、食品等に使用できるものであれば特に制限されないが、例えば、クエン酸、酒石酸、リンゴ酸等があげられる。本発明の錠剤中で酸味料が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。
結合剤としては、食品等に使用できるものであれば特に制限されないが、例えば、ゼラチン、プルラン等があげられる。本発明の錠剤中で結合剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The acidulant is not particularly limited as long as it can be used for foods, and examples thereof include citric acid, tartaric acid, malic acid and the like. The proportion of the acidulant in the tablet of the present invention is not particularly limited as long as it is within the range of the general use amount in the preparation.
The binder is not particularly limited as long as it can be used for foods and the like, and examples thereof include gelatin and pullulan. The proportion of the binder in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
結合剤としては、食品等に使用できるものであれば特に制限されないが、例えば、ゼラチン、プルラン等があげられる。本発明の錠剤中で結合剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The acidulant is not particularly limited as long as it can be used for foods, and examples thereof include citric acid, tartaric acid, malic acid and the like. The proportion of the acidulant in the tablet of the present invention is not particularly limited as long as it is within the range of the general use amount in the preparation.
The binder is not particularly limited as long as it can be used for foods and the like, and examples thereof include gelatin and pullulan. The proportion of the binder in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
抗酸化剤としては、食品等に使用できるものであれば特に制限されないが、例えば、トコフェロール、アスコルビン酸、塩酸システイン、L-アスコルビン酸ステアリン酸エステル等があげられる。本発明の錠剤中で抗酸化剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。
着色剤としては、食品等に使用できるものであれば特に制限はされないが、例えば、食用黄色5号、食用赤色2号、食用青色2号、カロチノイド色素、トマト色素等があげられる。本発明の錠剤中で着色剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The antioxidant is not particularly limited as long as it can be used in foods and the like, and examples thereof include tocopherol, ascorbic acid, cysteine hydrochloride, L-ascorbic acid stearate, and the like. The proportion of the antioxidant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
The colorant is not particularly limited as long as it can be used for foods, and examples thereof include food yellow No. 5, food red No. 2, food blue No. 2, carotenoid pigment, tomato pigment and the like. The proportion of the colorant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
着色剤としては、食品等に使用できるものであれば特に制限はされないが、例えば、食用黄色5号、食用赤色2号、食用青色2号、カロチノイド色素、トマト色素等があげられる。本発明の錠剤中で着色剤が占める割合は、製剤における一般的な使用の量の範囲内であれば特に限定されない。 The antioxidant is not particularly limited as long as it can be used in foods and the like, and examples thereof include tocopherol, ascorbic acid, cysteine hydrochloride, L-ascorbic acid stearate, and the like. The proportion of the antioxidant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
The colorant is not particularly limited as long as it can be used for foods, and examples thereof include food yellow No. 5, food red No. 2, food blue No. 2, carotenoid pigment, tomato pigment and the like. The proportion of the colorant in the tablet of the present invention is not particularly limited as long as it is within the range of general use in the preparation.
本発明の錠剤は、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤であり、具体的には本発明の顆粒または組成物を打錠することにより得られる錠剤である。
2.本発明の顆粒の製造方法
本発明における顆粒は以下の工程i-1)、i-2)またはi-3)およびii)で製造することができる。
i-1) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を溶媒中で加熱・撹拌混合を行うことでそれらを溶解または懸濁させ溶液1を得る。
i-2) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を加えて溶媒中で加熱・撹拌混合を行うことでそれらを溶解または懸濁させ溶液2を得る。
i-3) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に、コラーゲンまたはその酵素処理物、およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物を加えて溶媒中で加熱・撹拌混合を行うことで溶解または懸濁させ溶液2を得る。およびii) i-1)、i-2)またはi-3)で得られる溶液1または2をスプレードライして顆粒を得る。 The tablet of the present invention is a tablet containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof. Specifically, the tablet is obtained by tableting the granule or composition of the present invention.
2. Process for Producing Granules of the Present Invention Granules of the present invention can be produced by the following steps i-1), i-2) or i-3) and ii).
i-1) Glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are heated and stirred in a solvent to dissolve or suspend them to obtain Solution 1.
i-2) one or more selected from the group consisting of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid A compound 2 is added and heated or stirred in a solvent to dissolve or suspend them to obtain a solution 2.
i-3) One or more compounds selected from the group consisting of collagen or its enzyme-treated product and rutin or its enzyme-treated product are added to glucosamine or its salt and chondroitin sulfate or its salt, and heated and stirred in a solvent. Solution 2 is obtained by dissolving or suspending by mixing. And ii) Spray dry the solution 1 or 2 obtained in i-1), i-2) or i-3) to obtain granules.
2.本発明の顆粒の製造方法
本発明における顆粒は以下の工程i-1)、i-2)またはi-3)およびii)で製造することができる。
i-1) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を溶媒中で加熱・撹拌混合を行うことでそれらを溶解または懸濁させ溶液1を得る。
i-2) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に、コラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を加えて溶媒中で加熱・撹拌混合を行うことでそれらを溶解または懸濁させ溶液2を得る。
i-3) グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩に、コラーゲンまたはその酵素処理物、およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物を加えて溶媒中で加熱・撹拌混合を行うことで溶解または懸濁させ溶液2を得る。およびii) i-1)、i-2)またはi-3)で得られる溶液1または2をスプレードライして顆粒を得る。 The tablet of the present invention is a tablet containing a high content of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof. Specifically, the tablet is obtained by tableting the granule or composition of the present invention.
2. Process for Producing Granules of the Present Invention Granules of the present invention can be produced by the following steps i-1), i-2) or i-3) and ii).
i-1) Glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are heated and stirred in a solvent to dissolve or suspend them to obtain Solution 1.
i-2) one or more selected from the group consisting of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid A compound 2 is added and heated or stirred in a solvent to dissolve or suspend them to obtain a solution 2.
i-3) One or more compounds selected from the group consisting of collagen or its enzyme-treated product and rutin or its enzyme-treated product are added to glucosamine or its salt and chondroitin sulfate or its salt, and heated and stirred in a solvent. Solution 2 is obtained by dissolving or suspending by mixing. And ii) Spray dry the solution 1 or 2 obtained in i-1), i-2) or i-3) to obtain granules.
具体的には、本発明の顆粒は、以下の製造工程に従って製造することができる。
上記工程における溶液1とは、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を室温から溶媒の沸点までの温度の溶媒に溶解または懸濁させたものを表し、溶媒としては、例えば水、アルコール等が挙げられ、水が好ましい。アルコールとしては、例えば、エタノール、グリセリン等が挙げられる。上記溶液中または懸濁液中の全溶質の含有量としては、1~50重量%が挙げられ、5~45重量%が好ましく、10~40重量%がより好ましい。 Specifically, the granule of the present invention can be produced according to the following production steps.
The solution 1 in the above step represents a solution in which glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are dissolved or suspended in a solvent having a temperature from room temperature to the boiling point of the solvent. And water is preferred. Examples of the alcohol include ethanol and glycerin. The total solute content in the solution or suspension may be 1 to 50% by weight, preferably 5 to 45% by weight, and more preferably 10 to 40% by weight.
上記工程における溶液1とは、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を室温から溶媒の沸点までの温度の溶媒に溶解または懸濁させたものを表し、溶媒としては、例えば水、アルコール等が挙げられ、水が好ましい。アルコールとしては、例えば、エタノール、グリセリン等が挙げられる。上記溶液中または懸濁液中の全溶質の含有量としては、1~50重量%が挙げられ、5~45重量%が好ましく、10~40重量%がより好ましい。 Specifically, the granule of the present invention can be produced according to the following production steps.
The solution 1 in the above step represents a solution in which glucosamine or a salt thereof and chondroitin sulfate or a salt thereof are dissolved or suspended in a solvent having a temperature from room temperature to the boiling point of the solvent. And water is preferred. Examples of the alcohol include ethanol and glycerin. The total solute content in the solution or suspension may be 1 to 50% by weight, preferably 5 to 45% by weight, and more preferably 10 to 40% by weight.
上記工程における溶液2とは、グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩、ならびにコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物、好ましくはコラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群より選ばれる1つ以上の化合物を室温から溶媒の沸点までの温度の溶媒に溶解または懸濁させたものを表し、溶媒としては、例えば水、アルコール等が挙げられ、水が好ましい。アルコールとしては、例えば、エタノール、グリセリン等が挙げられる。上記溶液中または懸濁液中の全溶質の含有量としては、1~50重量%が挙げられ、5~45重量%が好ましく、10~40重量%がより好ましい。
The solution 2 in the above step is selected from the group consisting of glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid. One or more compounds, preferably one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof are dissolved or suspended in a solvent having a temperature from room temperature to the boiling point of the solvent. Examples of the solvent include water and alcohol, and water is preferred. Examples of the alcohol include ethanol and glycerin. The total solute content in the solution or suspension may be 1 to 50% by weight, preferably 5 to 45% by weight, and more preferably 10 to 40% by weight.
懸濁液は均一または不均一のどちらでもよく、均一が望ましい。また、溶質が溶媒に一部溶解していてもよく、さらに懸濁液はコロイド溶液でもかまわない。
溶液1または2におけるグルコサミンまたはその塩の含有量は、溶液1または2に対して15~27重量%が好ましく、18~24重量%がより好ましい。
溶液1または2におけるコンドロイチン硫酸またはその塩の含有量は、溶液1または2に対して1~6重量%が好ましく、1.8~4.0重量%がより好ましい。 The suspension may be either uniform or non-uniform, preferably uniform. The solute may be partially dissolved in the solvent, and the suspension may be a colloidal solution.
The content of glucosamine or a salt thereof in the solution 1 or 2 is preferably 15 to 27% by weight, more preferably 18 to 24% by weight with respect to the solution 1 or 2.
The content of chondroitin sulfate or a salt thereof in the solution 1 or 2 is preferably 1 to 6% by weight, more preferably 1.8 to 4.0% by weight with respect to the solution 1 or 2.
溶液1または2におけるグルコサミンまたはその塩の含有量は、溶液1または2に対して15~27重量%が好ましく、18~24重量%がより好ましい。
溶液1または2におけるコンドロイチン硫酸またはその塩の含有量は、溶液1または2に対して1~6重量%が好ましく、1.8~4.0重量%がより好ましい。 The suspension may be either uniform or non-uniform, preferably uniform. The solute may be partially dissolved in the solvent, and the suspension may be a colloidal solution.
The content of glucosamine or a salt thereof in the solution 1 or 2 is preferably 15 to 27% by weight, more preferably 18 to 24% by weight with respect to the solution 1 or 2.
The content of chondroitin sulfate or a salt thereof in the solution 1 or 2 is preferably 1 to 6% by weight, more preferably 1.8 to 4.0% by weight with respect to the solution 1 or 2.
溶液2におけるコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量は、溶液2に対して0.2~2重量%が好ましく、0.5~1.5重量%がより好ましい。
懸濁液中の全溶質の含有量(一部が溶解している場合は、溶解している溶質および溶解していない溶質を合わせて溶質とする)としては、35~65重量%が挙げられ、40~60重量%が好ましい。 スプレードライは液状形態の化合物または混合物から顆粒を得るために一般に用いられ、当該方法で得られる顆粒は、液状の組成物が熱風中に数100 μm以下の微小な粒子として噴霧され、乾燥されながら塔内を落下していくことで粉末として回収されるため、得られた粉末は、球形に近く流動性に優れ、水溶性が高いという性質を有している。 The total content of one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in solution 2 is 0.2 with respect to solution 2. ˜2 wt% is preferable, and 0.5 to 1.5 wt% is more preferable.
The content of the total solute in the suspension (when a part is dissolved, the dissolved solute and the undissolved solute are combined into a solute) is 35 to 65% by weight. 40 to 60% by weight is preferable. Spray drying is generally used to obtain granules from a compound or mixture in a liquid form, and the granules obtained by the method are sprayed as fine particles of several hundred μm or less in hot air and dried. Since it is recovered as powder by dropping in the tower, the obtained powder has a property of being nearly spherical and excellent in fluidity and high in water solubility.
懸濁液中の全溶質の含有量(一部が溶解している場合は、溶解している溶質および溶解していない溶質を合わせて溶質とする)としては、35~65重量%が挙げられ、40~60重量%が好ましい。 スプレードライは液状形態の化合物または混合物から顆粒を得るために一般に用いられ、当該方法で得られる顆粒は、液状の組成物が熱風中に数100 μm以下の微小な粒子として噴霧され、乾燥されながら塔内を落下していくことで粉末として回収されるため、得られた粉末は、球形に近く流動性に優れ、水溶性が高いという性質を有している。 The total content of one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in solution 2 is 0.2 with respect to solution 2. ˜2 wt% is preferable, and 0.5 to 1.5 wt% is more preferable.
The content of the total solute in the suspension (when a part is dissolved, the dissolved solute and the undissolved solute are combined into a solute) is 35 to 65% by weight. 40 to 60% by weight is preferable. Spray drying is generally used to obtain granules from a compound or mixture in a liquid form, and the granules obtained by the method are sprayed as fine particles of several hundred μm or less in hot air and dried. Since it is recovered as powder by dropping in the tower, the obtained powder has a property of being nearly spherical and excellent in fluidity and high in water solubility.
また、スプレードライに用いられる素材は一時的に熱風に曝されるが、曝されている時間が非常に短いことと水の蒸発潜熱のためあまり温度が上がらないことから、素材の熱変性が起きにくく、復水による変化も小さい。さらに、非常に熱に弱い素材の場合、熱風の代わりに冷風を供給することも可能である。その場合、乾燥能力は落ちるが、よりマイルドな乾燥を実現できる点で好ましい。
In addition, the material used for spray drying is temporarily exposed to hot air, but the exposure time is very short and the temperature does not rise very much due to the latent heat of vaporization of water. Difficult to change due to condensate. Further, in the case of a material that is very sensitive to heat, it is possible to supply cold air instead of hot air. In that case, although a drying capability falls, it is preferable at the point which can implement | achieve milder drying.
上記工程ii)におけるスプレードライとは、液状形態のものから粉末を得るために一般に用いられる方法であり、液状の組成物が熱風中に数100 μm以下の微小な粒子として噴霧され、乾燥されながら塔内を落下していくことで粉末として回収される。スプレードライに用いられる素材は一時的に熱風に曝されるが、曝されている時間が非常に短いことと水の蒸発潜熱のためあまり温度が上がらないことから、素材の熱変性が起きにくく、復水による変化も小さいものである。また、非常に熱に弱い素材の場合、熱風の代わりに冷風を供給する場合も可能である。その場合、乾燥能力は落ちるが、よりマイルドな乾燥を実現できる点で好ましい。
The spray drying in the above step ii) is a method generally used for obtaining a powder from a liquid form, and the liquid composition is sprayed as fine particles of several hundred μm or less in hot air while being dried. It is recovered as a powder by dropping inside the tower. The material used for spray drying is temporarily exposed to hot air, but because the exposure time is very short and the temperature does not rise very much due to the latent heat of vaporization of water, the material is less susceptible to thermal denaturation, Changes due to condensate are also small. Further, in the case of a material that is very sensitive to heat, it is possible to supply cold air instead of hot air. In that case, although a drying capability falls, it is preferable at the point which can implement | achieve milder drying.
次いでスプレードライヤーを用いて、送風温度150~200 ℃および排風温度55~85 ℃の条件にて、溶液または懸濁液のスプレードライを行うことで本発明の製造方法に用いる顆粒を得ることができる。
上記工程ii)でスプレードライをする際には、溶液を用いる方が好ましい。
スプレードライヤーの噴霧方式としては、例えば、ノズル式、ディスク式等が挙げられ、ノズル式としては、例えば、Pulvis Mini-Spray GB22 (ヤマト科学社製) 等が挙げられ、ディスク式としては、例えばL8-i型スプレードライヤー (大川原化工機社製) 等が挙げられる。 Next, the granules used in the production method of the present invention can be obtained by spray-drying the solution or suspension using a spray dryer under the conditions of an air blowing temperature of 150 to 200 ° C. and an exhaust air temperature of 55 to 85 ° C. it can.
When spray drying is performed in step ii), it is preferable to use a solution.
Examples of the spraying method of the spray dryer include a nozzle type and a disk type. Examples of the nozzle type include Pulvis Mini-Spray GB22 (manufactured by Yamato Kagaku Co., Ltd.). Examples of the disk type include L8. -i type spray dryer (Okawara Kako Co., Ltd.).
上記工程ii)でスプレードライをする際には、溶液を用いる方が好ましい。
スプレードライヤーの噴霧方式としては、例えば、ノズル式、ディスク式等が挙げられ、ノズル式としては、例えば、Pulvis Mini-Spray GB22 (ヤマト科学社製) 等が挙げられ、ディスク式としては、例えばL8-i型スプレードライヤー (大川原化工機社製) 等が挙げられる。 Next, the granules used in the production method of the present invention can be obtained by spray-drying the solution or suspension using a spray dryer under the conditions of an air blowing temperature of 150 to 200 ° C. and an exhaust air temperature of 55 to 85 ° C. it can.
When spray drying is performed in step ii), it is preferable to use a solution.
Examples of the spraying method of the spray dryer include a nozzle type and a disk type. Examples of the nozzle type include Pulvis Mini-Spray GB22 (manufactured by Yamato Kagaku Co., Ltd.). Examples of the disk type include L8. -i type spray dryer (Okawara Kako Co., Ltd.).
ノズル式の場合、ノズルの径としては0.1~4.0 mmが好ましく、0.3~3.5 mmがより好ましい。ノズルの噴出圧力としては10~450 kg/cm2が好ましく、50~300 kg/cm2がより好ましい。入り口温度としては100~200 ℃が挙げられ、110~195 ℃が好ましく、120~190 ℃がより好ましい。出口温度としては40~100 ℃が挙げられ、50~90 ℃が好ましく、60~80 ℃がより好ましい。
In the case of the nozzle type, the nozzle diameter is preferably 0.1 to 4.0 mm, and more preferably 0.3 to 3.5 mm. The ejection pressure of the nozzle is preferably 10 to 450 kg / cm 2, more preferably 50 to 300 kg / cm 2 . Examples of the inlet temperature include 100 to 200 ° C., preferably 110 to 195 ° C., and more preferably 120 to 190 ° C. Examples of the outlet temperature include 40 to 100 ° C, preferably 50 to 90 ° C, and more preferably 60 to 80 ° C.
ディスク式の場合、アトマイザ回転数としては、20000~45000 rpmが好ましく、25000~40000 rpmがより好ましい。入り口温度としては100~200 ℃が挙げられ、110~195 ℃が好ましく、120~190 ℃がより好ましい。出口温度としては40~100 ℃が挙げられ、50~90 ℃が好ましく、60~80 ℃がより好ましい。
本発明の製造方法で得られる顆粒に含まれるグルコサミンまたはその塩の含有量としては、グルコサミンまたはその塩として、65~99重量%であることが好ましく、70~95重量%であることがより好ましく、75~93重量%であることが特に好ましい。 In the case of a disk type, the atomizer speed is preferably 20000 to 45000 rpm, more preferably 25000 to 40000 rpm. Examples of the inlet temperature include 100 to 200 ° C., preferably 110 to 195 ° C., and more preferably 120 to 190 ° C. Examples of the outlet temperature include 40 to 100 ° C, preferably 50 to 90 ° C, and more preferably 60 to 80 ° C.
The content of glucosamine or a salt thereof contained in the granules obtained by the production method of the present invention is preferably 65 to 99% by weight, more preferably 70 to 95% by weight as glucosamine or a salt thereof. 75 to 93% by weight is particularly preferable.
本発明の製造方法で得られる顆粒に含まれるグルコサミンまたはその塩の含有量としては、グルコサミンまたはその塩として、65~99重量%であることが好ましく、70~95重量%であることがより好ましく、75~93重量%であることが特に好ましい。 In the case of a disk type, the atomizer speed is preferably 20000 to 45000 rpm, more preferably 25000 to 40000 rpm. Examples of the inlet temperature include 100 to 200 ° C., preferably 110 to 195 ° C., and more preferably 120 to 190 ° C. Examples of the outlet temperature include 40 to 100 ° C, preferably 50 to 90 ° C, and more preferably 60 to 80 ° C.
The content of glucosamine or a salt thereof contained in the granules obtained by the production method of the present invention is preferably 65 to 99% by weight, more preferably 70 to 95% by weight as glucosamine or a salt thereof. 75 to 93% by weight is particularly preferable.
本発明の製造方法で得られる顆粒に含まれるコンドロイチン硫酸またはその塩の含有量としては、好ましくは3~22重量%含有し、さらに好ましくは5~16重量%含有する。
本発明の製造方法で得られる顆粒に含まれるコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の総含有量は、本発明の顆粒に対して0.1~10重量%が好ましく、0.5~5重量%がより好ましい。
3.本発明の組成物の製造方法
本発明の組成物は、以下の工程iii)で製造することができる。
iii) 上記工程ii)で得られる顆粒に、滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加し、好ましくは混合する。 The content of chondroitin sulfate or a salt thereof contained in the granule obtained by the production method of the present invention is preferably 3 to 22% by weight, more preferably 5 to 16% by weight.
Total content of one or more compounds selected from the group consisting of collagen or enzyme-treated product thereof, rutin or enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid contained in the granule obtained by the production method of the present invention The amount is preferably from 0.1 to 10% by weight, more preferably from 0.5 to 5% by weight, based on the granules of the present invention.
3. Production method of the composition of the present invention The composition of the present invention can be produced by the following step iii).
iii) One or more compounds selected from the group consisting of lubricants, fluidity improvers and additives are added to the granules obtained in step ii) above, preferably mixed.
本発明の製造方法で得られる顆粒に含まれるコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の総含有量は、本発明の顆粒に対して0.1~10重量%が好ましく、0.5~5重量%がより好ましい。
3.本発明の組成物の製造方法
本発明の組成物は、以下の工程iii)で製造することができる。
iii) 上記工程ii)で得られる顆粒に、滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加し、好ましくは混合する。 The content of chondroitin sulfate or a salt thereof contained in the granule obtained by the production method of the present invention is preferably 3 to 22% by weight, more preferably 5 to 16% by weight.
Total content of one or more compounds selected from the group consisting of collagen or enzyme-treated product thereof, rutin or enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid contained in the granule obtained by the production method of the present invention The amount is preferably from 0.1 to 10% by weight, more preferably from 0.5 to 5% by weight, based on the granules of the present invention.
3. Production method of the composition of the present invention The composition of the present invention can be produced by the following step iii).
iii) One or more compounds selected from the group consisting of lubricants, fluidity improvers and additives are added to the granules obtained in step ii) above, preferably mixed.
滑沢剤、流動性改善剤および添加物は、それぞれ独立した粉体の形態であってもよいし、予めこれらを組み合わせて、公知の湿式または乾式造粒方法等を用いて造粒した顆粒状の形態にして添加してもよい。
混合は、例えば、バスケットミル、V型混合機、フレットミル、タンブラー混合機等の混合機を用いて行われるか、またはポリエチレン袋内に、混合させる成分を加えて手で上下左右に振っても行うことができる。
4.整粒末の製造方法
本発明の顆粒または組成物には、上記方法で得られる顆粒または組成物を整粒して得られる整粒末も含まれ、該整粒末は以下の工程iv)で製造することができる。
iv) 上記工程ii)またはiii)で得られる顆粒または組成物を篩過して整粒末を得る。 Lubricants, fluidity improvers and additives may be in the form of independent powders, or granulated by combining them in advance and using a known wet or dry granulation method. It may be added in the form of
For example, mixing is performed using a mixer such as a basket mill, a V-type mixer, a fret mill, a tumbler mixer, or the like. It can be carried out.
4). Method for producing sized powder The granule or composition of the present invention also includes a sized powder obtained by sizing the granule or composition obtained by the above method, and the sized powder is obtained in the following step iv). Can be manufactured.
iv) The granule or composition obtained in the above step ii) or iii) is sieved to obtain a sized powder.
混合は、例えば、バスケットミル、V型混合機、フレットミル、タンブラー混合機等の混合機を用いて行われるか、またはポリエチレン袋内に、混合させる成分を加えて手で上下左右に振っても行うことができる。
4.整粒末の製造方法
本発明の顆粒または組成物には、上記方法で得られる顆粒または組成物を整粒して得られる整粒末も含まれ、該整粒末は以下の工程iv)で製造することができる。
iv) 上記工程ii)またはiii)で得られる顆粒または組成物を篩過して整粒末を得る。 Lubricants, fluidity improvers and additives may be in the form of independent powders, or granulated by combining them in advance and using a known wet or dry granulation method. It may be added in the form of
For example, mixing is performed using a mixer such as a basket mill, a V-type mixer, a fret mill, a tumbler mixer, or the like. It can be carried out.
4). Method for producing sized powder The granule or composition of the present invention also includes a sized powder obtained by sizing the granule or composition obtained by the above method, and the sized powder is obtained in the following step iv). Can be manufactured.
iv) The granule or composition obtained in the above step ii) or iii) is sieved to obtain a sized powder.
工程iv)の篩過としては、上記工程ii) またはiii)で得られた顆粒または組成物を篩に入れて、手で振動させて篩過する方法、または篩機を用いて顆粒または組成物を篩過する方法等が挙げられる。
工程iv)の篩過に用いられる機器としては、例えば、分級機・振動ふるい[湿式・乾式/網:カートリッジ式(標準)または内リング式(標準)](ダルトン社製)、佐藤式振動ふるい機(晃栄産業社製)等が挙げられる。 As the sieving in step iv), the granule or composition obtained in the above step ii) or iii) is put into a sieve and shaken by hand, or passed through a sieve or a granule or composition using a sieving machine. And the like.
Examples of the equipment used for the sieving in step iv) include a classifier / vibrating sieve [wet / dry type / net: cartridge type (standard) or inner ring type (standard)] (Dalton), Sato type vibrating sieve. Machine (manufactured by Kanei Sangyo Co., Ltd.).
工程iv)の篩過に用いられる機器としては、例えば、分級機・振動ふるい[湿式・乾式/網:カートリッジ式(標準)または内リング式(標準)](ダルトン社製)、佐藤式振動ふるい機(晃栄産業社製)等が挙げられる。 As the sieving in step iv), the granule or composition obtained in the above step ii) or iii) is put into a sieve and shaken by hand, or passed through a sieve or a granule or composition using a sieving machine. And the like.
Examples of the equipment used for the sieving in step iv) include a classifier / vibrating sieve [wet / dry type / net: cartridge type (standard) or inner ring type (standard)] (Dalton), Sato type vibrating sieve. Machine (manufactured by Kanei Sangyo Co., Ltd.).
上記篩過の際に用いる篩いとしては特に限定されず、例えば4号篩(4750 μm)~60号篩(250 μm)等が挙げられ、8号篩 (2360 μm)~42号篩 (355 μm)が好ましく、12号篩 (1400 μm)~32号篩 (500 μm)がより好ましい。
5.本発明の錠剤の製造方法
本発明の錠剤は以下の工程v)により製造することができる。
v) 上記ii)で得られる顆粒、またはiii)で得られる組成物、好ましくはiv)で得られる整粒末を打錠して錠剤を製造する。 The sieve used for the above sieving is not particularly limited, and examples thereof include No. 4 sieve (4750 μm) to No. 60 sieve (250 μm), and No. 8 sieve (2360 μm) to No. 42 sieve (355 μm). No. 12 sieve (1400 μm) to No. 32 sieve (500 μm) are more preferred.
5. Method for producing tablet of the present invention The tablet of the present invention can be produced by the following step v).
v) Tablets are produced by tableting the granules obtained in ii) above, or the composition obtained in iii), preferably the sized powder obtained in iv).
5.本発明の錠剤の製造方法
本発明の錠剤は以下の工程v)により製造することができる。
v) 上記ii)で得られる顆粒、またはiii)で得られる組成物、好ましくはiv)で得られる整粒末を打錠して錠剤を製造する。 The sieve used for the above sieving is not particularly limited, and examples thereof include No. 4 sieve (4750 μm) to No. 60 sieve (250 μm), and No. 8 sieve (2360 μm) to No. 42 sieve (355 μm). No. 12 sieve (1400 μm) to No. 32 sieve (500 μm) are more preferred.
5. Method for producing tablet of the present invention The tablet of the present invention can be produced by the following step v).
v) Tablets are produced by tableting the granules obtained in ii) above, or the composition obtained in iii), preferably the sized powder obtained in iv).
具体的には、本発明の錠剤は、以下の製造工程に従って製造することができる。
工程v)では、本発明の顆粒または組成物、好ましくは整粒末を打錠用粒として適当な方法により圧縮成形して錠剤を製造する。圧縮成形する方法としては、例えば、打錠用粒をそのまま圧縮成形する通例の方法や、あらかじめ滑沢剤を杵表面および臼壁に塗布してから、滑沢剤を含有しない打錠用粒を圧縮成形する、いわゆる外部滑沢圧縮成形方法等が挙げられる。 Specifically, the tablet of the present invention can be produced according to the following production steps.
In step v), the granule or composition of the present invention, preferably the sized powder is used as a tableting tablet, and compression-molded by an appropriate method to produce a tablet. As a compression molding method, for example, a conventional method in which a tableting granule is compression molded as it is, or a tableting granule that does not contain a lubricant after preliminarily applying a lubricant to the surface of the punch and the mortar wall. Examples include a so-called external lubrication compression molding method in which compression molding is performed.
工程v)では、本発明の顆粒または組成物、好ましくは整粒末を打錠用粒として適当な方法により圧縮成形して錠剤を製造する。圧縮成形する方法としては、例えば、打錠用粒をそのまま圧縮成形する通例の方法や、あらかじめ滑沢剤を杵表面および臼壁に塗布してから、滑沢剤を含有しない打錠用粒を圧縮成形する、いわゆる外部滑沢圧縮成形方法等が挙げられる。 Specifically, the tablet of the present invention can be produced according to the following production steps.
In step v), the granule or composition of the present invention, preferably the sized powder is used as a tableting tablet, and compression-molded by an appropriate method to produce a tablet. As a compression molding method, for example, a conventional method in which a tableting granule is compression molded as it is, or a tableting granule that does not contain a lubricant after preliminarily applying a lubricant to the surface of the punch and the mortar wall. Examples include a so-called external lubrication compression molding method in which compression molding is performed.
圧縮成形時に用いる機器としては、例えば単発式圧縮成型機、ロータリー圧縮成形機、油圧プレス機等の圧縮機等を用いることができる。
本発明の製造方法で得られる錠剤に含まれるグルコサミンまたはその塩含有量としては、グルコサミンまたはその塩として、60~95重量%であることが好ましく、65~90重量%であることがより好ましく、70~88重量%であることが特に好ましい。 As an apparatus used at the time of compression molding, compressors, such as a single shot compression molding machine, a rotary compression molding machine, a hydraulic press machine, etc. can be used, for example.
The content of glucosamine or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 60 to 95% by weight, more preferably 65 to 90% by weight as glucosamine or a salt thereof, Particularly preferred is 70 to 88% by weight.
本発明の製造方法で得られる錠剤に含まれるグルコサミンまたはその塩含有量としては、グルコサミンまたはその塩として、60~95重量%であることが好ましく、65~90重量%であることがより好ましく、70~88重量%であることが特に好ましい。 As an apparatus used at the time of compression molding, compressors, such as a single shot compression molding machine, a rotary compression molding machine, a hydraulic press machine, etc. can be used, for example.
The content of glucosamine or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 60 to 95% by weight, more preferably 65 to 90% by weight as glucosamine or a salt thereof, Particularly preferred is 70 to 88% by weight.
本発明の製造方法で得られる錠剤に含まれるコンドロイチン硫酸またはその塩の含有量としては、コンドロイチン硫酸またはその塩として、3~20重量%が好ましく、5~15重量%がより好ましい。
本発明の製造方法で得られる錠剤に含まれるコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量は、0.1~10重量%が好ましく、0.5~5重量%がより好ましい。 The content of chondroitin sulfate or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 3 to 20% by weight, more preferably 5 to 15% by weight as chondroitin sulfate or a salt thereof.
Total content of one or more compounds selected from the group consisting of collagen or enzyme-treated product thereof, rutin or enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid contained in the tablet obtained by the production method of the present invention The amount is preferably 0.1 to 10% by weight, more preferably 0.5 to 5% by weight.
本発明の製造方法で得られる錠剤に含まれるコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量は、0.1~10重量%が好ましく、0.5~5重量%がより好ましい。 The content of chondroitin sulfate or a salt thereof contained in the tablet obtained by the production method of the present invention is preferably 3 to 20% by weight, more preferably 5 to 15% by weight as chondroitin sulfate or a salt thereof.
Total content of one or more compounds selected from the group consisting of collagen or enzyme-treated product thereof, rutin or enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid contained in the tablet obtained by the production method of the present invention The amount is preferably 0.1 to 10% by weight, more preferably 0.5 to 5% by weight.
本発明の製造方法により得られる錠剤は、錠剤中に、本発明の顆粒を、好ましくは80~99重量%、さらに好ましくは85~96重量%含む。
本発明の製造方法で得られる錠剤の形状は、特に制限されないが、例えば丸錠、三角錠、砲丸錠等が好ましい。本発明の錠剤の大きさは、特に制限されないが、例えば質量で0.1~2 g、直径で0.3~2.0 cmであるのが好ましい。 The tablet obtained by the production method of the present invention contains the granule of the present invention in an amount of preferably 80 to 99% by weight, more preferably 85 to 96% by weight.
The shape of the tablet obtained by the production method of the present invention is not particularly limited, but for example, a round tablet, a triangular tablet, a cannonball tablet and the like are preferable. The size of the tablet of the present invention is not particularly limited, but is preferably 0.1 to 2 g in mass and 0.3 to 2.0 cm in diameter, for example.
本発明の製造方法で得られる錠剤の形状は、特に制限されないが、例えば丸錠、三角錠、砲丸錠等が好ましい。本発明の錠剤の大きさは、特に制限されないが、例えば質量で0.1~2 g、直径で0.3~2.0 cmであるのが好ましい。 The tablet obtained by the production method of the present invention contains the granule of the present invention in an amount of preferably 80 to 99% by weight, more preferably 85 to 96% by weight.
The shape of the tablet obtained by the production method of the present invention is not particularly limited, but for example, a round tablet, a triangular tablet, a cannonball tablet and the like are preferable. The size of the tablet of the present invention is not particularly limited, but is preferably 0.1 to 2 g in mass and 0.3 to 2.0 cm in diameter, for example.
本発明の製造方法で得られる錠剤は、例えば、かけ、くずれ等が生じない硬度を有しているのが好ましい。錠剤の硬度は、一般的に錠剤硬度計で錠剤の直径方向の破壊強度として測定されるが、その値は3~20 kgfであるのが好ましく、5~18 kgfであるのがより好ましく、7~16 kgfであるのが特に好ましい。
錠剤の硬度は、市販の錠剤破壊強度測定機、例えば、TH-203CP型(富山産業社製)等により測定できる。 The tablet obtained by the production method of the present invention preferably has a hardness that does not cause, for example, cracking or breakage. The hardness of the tablet is generally measured as a breaking strength in the diameter direction of the tablet with a tablet hardness meter, and the value is preferably 3 to 20 kgf, more preferably 5 to 18 kgf. Particularly preferred is ˜16 kgf.
The hardness of the tablet can be measured by a commercially available tablet breaking strength measuring machine, for example, TH-203CP type (manufactured by Toyama Sangyo Co., Ltd.).
錠剤の硬度は、市販の錠剤破壊強度測定機、例えば、TH-203CP型(富山産業社製)等により測定できる。 The tablet obtained by the production method of the present invention preferably has a hardness that does not cause, for example, cracking or breakage. The hardness of the tablet is generally measured as a breaking strength in the diameter direction of the tablet with a tablet hardness meter, and the value is preferably 3 to 20 kgf, more preferably 5 to 18 kgf. Particularly preferred is ˜16 kgf.
The hardness of the tablet can be measured by a commercially available tablet breaking strength measuring machine, for example, TH-203CP type (manufactured by Toyama Sangyo Co., Ltd.).
本発明の製造方法では、圧縮成形機の杵臼にあらかじめ極微量の滑沢剤を塗布し、滑沢剤が塗布された杵臼を有する圧縮成形機で滑沢剤を含有しない混合物を圧縮成形する、いわゆる外部滑沢圧縮成形方法を用いても打錠障害を生じることなく所望の硬度を有する錠剤を製造することができる。
上記打錠障害としては、例えば、スティッキング (杵に粉末が付着する現象)、バインディング (臼と錠剤の摩擦が大きくなる現象)、キャッピング (錠剤が帽子状に剥離する現象)、ラミネーション (錠剤が層状に剥離する現象) 等が挙げられる。 In the production method of the present invention, a very small amount of lubricant is applied in advance to the die of the compression molding machine, and the mixture containing no lubricant is compression molded with a compression molding machine having the tooling coated with the lubricant. Even if a so-called external lubrication compression molding method is used, a tablet having a desired hardness can be produced without causing a tableting trouble.
Examples of tableting obstacles include sticking (a phenomenon in which powder adheres to the heel), binding (a phenomenon in which friction between the die and the tablet increases), capping (a phenomenon in which the tablet peels off in a cap shape), and lamination (a tablet is layered). Phenomenon).
上記打錠障害としては、例えば、スティッキング (杵に粉末が付着する現象)、バインディング (臼と錠剤の摩擦が大きくなる現象)、キャッピング (錠剤が帽子状に剥離する現象)、ラミネーション (錠剤が層状に剥離する現象) 等が挙げられる。 In the production method of the present invention, a very small amount of lubricant is applied in advance to the die of the compression molding machine, and the mixture containing no lubricant is compression molded with a compression molding machine having the tooling coated with the lubricant. Even if a so-called external lubrication compression molding method is used, a tablet having a desired hardness can be produced without causing a tableting trouble.
Examples of tableting obstacles include sticking (a phenomenon in which powder adheres to the heel), binding (a phenomenon in which friction between the die and the tablet increases), capping (a phenomenon in which the tablet peels off in a cap shape), and lamination (a tablet is layered). Phenomenon).
本発明の製造方法で得られる錠剤は、さらに、防湿性、保存安定性等の向上のため、例えば糖、糖アルコール等によりコーティングされた糖衣錠又はコーティング錠であってもよい。
以下に、実施例に基づいて本発明をより詳細に説明するが、本発明はこれらに限定されるものではない。 The tablet obtained by the production method of the present invention may be a sugar-coated tablet or a coated tablet coated with sugar, sugar alcohol or the like, for example, in order to improve moisture resistance, storage stability and the like.
Hereinafter, the present invention will be described in more detail based on examples, but the present invention is not limited thereto.
以下に、実施例に基づいて本発明をより詳細に説明するが、本発明はこれらに限定されるものではない。 The tablet obtained by the production method of the present invention may be a sugar-coated tablet or a coated tablet coated with sugar, sugar alcohol or the like, for example, in order to improve moisture resistance, storage stability and the like.
Hereinafter, the present invention will be described in more detail based on examples, but the present invention is not limited thereto.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 gおよびサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 52 gを精製水1116 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、アトマイザ回転数35000 rpm、入り口温度180 ℃および出口温度70 ℃の条件に設定したスプレードライヤー [L8-i型スプレードライヤー (大川原化工機社製)] で、スプレードライして顆粒を250~300g得た。当該顆粒のうち186 gにショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えて、ポリエチレン袋内で充分に混合して組成物得て、これを16号篩 (1000 μm) を用いて篩過して整粒末を200 g得た。当該整粒末を単発式圧縮成型機 [竪型成形機6B-2M (菊水製作所社製)]を用いて、1000 kgfの打錠圧で圧縮成型を行って8.2 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [Malinker ridge 40S 焼 (Yaizu Suisan Chemical Co., Ltd.) 52 g were dissolved in 1116 mL of purified water and 25 wt% An aqueous solution was obtained. Using this aqueous solution, spray-dry and granulate with a spray dryer [L8-i type spray dryer (Okawara Kako Co., Ltd.)] with the atomizer speed of 35000 rpm, inlet temperature of 180 ° C and outlet temperature of 70 ° C. Of 250 to 300 g was obtained. Add sucrose fatty acid ester DK [DK ester F20W20 (Daiichi Kogyo Seiyaku Co., Ltd.) 10 g and tribasic calcium phosphate 第三 [tribasic calcium phosphate (Taihei Chemical Industry Co., Ltd.)] の う ち の う ちThe mixture was thoroughly mixed to obtain a composition, which was sieved using a No. 16 sieve (1000 μm) sieve to obtain 200 g of sized powder. Per tablet showing a hardness of 8.2 kgf by compressing the sized powder using a single compression molding machine 竪 [Type 6B-2M (manufactured by Kikusui Seisakusho)] with a tableting pressure of 1000 kgf 20 tablets of 350 mg were obtained.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 40 gおよびコラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 12 gを精製水1116 mLに溶解して全溶質が25重量%の水溶液を得た。次に実施例1と同様の方法により顆粒、組成物および整粒末を得た後に、900 kgfの打錠圧で圧縮成形を行い、11.2 kgfの硬度を示す錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g, Shark cartilage extract powder [Malinkin ridge 40S 焼 (Yaizu Suisan Chemical Co., Ltd.)] 40 g and collagen [Water-soluble fish collagen (manufactured by Kyowa Hakko Bio) )] 12 g was dissolved in 1116 mL of purified water to obtain an aqueous solution having a total solute of 25 wt%. Next, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 900 kgf, and 20 tablets showing a hardness of 11.2 kgf were obtained.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 40 gおよび酵素処理ルチン [αGルチンPS (東洋精糖社製)] 12 gを精製水1116 mLに溶解して全溶質が25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒、組成物および整粒末を得た後に、1000 kgfの打錠圧で圧縮成形を行い、11.5 kgfの硬度を示す錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (Kyowa Hakko Bio Inc.) 320 g, Shark cartilage extract powder マ [Malinkin ridge 40S 焼 (Yaizu Suisan Chemical Co., Ltd.)] 40 g and enzyme-treated rutin α [αG rutin PS (Toyo Seiki Co., Ltd.) )] 12 g was dissolved in 1116 mL of purified water to obtain an aqueous solution having a total solute of 25 wt%. Using the aqueous solution, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 1000 kgf to obtain 20 tablets having a hardness of 11.5 kgf. It was.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320g、サメ軟骨抽出粉末[SCP(NB) (マルハニチロ社製)] 52 gを精製水1116 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒、組成物および整粒末を得た後に、950 kgfの打錠圧で圧縮成形を行い、9.5 kgfの硬度を示す錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [SCP (NB) (manufactured by Maruha Nichiro)] 52 were dissolved in 1116 mL of purified water to obtain a 25 wt% aqueous solution. . Using the aqueous solution, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 950 kgf, and 20 tablets showing a hardness of 9.5 kgf were obtained. It was.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 340 gおよびサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 32 gを精製水1116 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒、組成物および整粒末を得た後に、1250 kgfの打錠圧で圧縮成形を行い、10.7 kgfの硬度を示す錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] お よ び and shark cartilage extract powder マ [Malinkin Tiridge 40S (manufactured by Yaizu Suisan Chemical Co., Ltd.)] 32 g were dissolved in 1116 mL of purified water An aqueous solution was obtained. Using the aqueous solution, after obtaining granules, a composition and a sized powder in the same manner as in Example 1, compression molding was performed with a tableting pressure of 1250 kgf to obtain 20 tablets showing a hardness of 10.7 kgf. It was.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 gおよびサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 40 gを精製水1080 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を250~300 g得た。当該顆粒のうち180 gにコラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 6 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えて、ポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末200 gを得た。当該整粒末を実施例1の方法により1000 kgfの打錠圧で圧縮成型を行った結果、10.5 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g and shark cartilage extract powder [Malinkin Tiridge 40S (Yaizu Suisan Chemical Co., Ltd.) 40 g were dissolved in 1080 mL of purified water and 25 wt% An aqueous solution was obtained. Using this aqueous solution, 250 to 300 g of granules were obtained in the same manner as in Example 1. Of these granules, 180 g contains collagen [water-soluble fish collagen (manufactured by Kyowa Hakko Bio)] 6, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 and tribasic calcium phosphate 第三 [third Calcium phosphate cocoon (produced by Taihei Chemical Sangyo Co., Ltd.)] 4 混合 g was added and mixed thoroughly in a polyethylene bag to obtain a composition. g was obtained. The sized powder was subjected to compression molding at a tableting pressure of 1000 kgf by the method of Example 1. As a result, 20 tablets of 350 mg per tablet showing a hardness of 10.5 kgf were obtained.
実施例6と同様の方法によりグルコサミンおよびコンドロイチン硫酸の25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を250~300 g得た。当該顆粒のうち180 gに酵素処理ルチン [αGルチンPS (東洋精糖社製)] 6 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えて、ポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末200 gを得た。当該整粒末を実施例1と同様の方法により1000 kgfの打錠圧で圧縮成型を行った結果、10.9 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
A 25% by weight aqueous solution of glucosamine and chondroitin sulfate was obtained in the same manner as in Example 6. Using this aqueous solution, 250 to 300 g of granules were obtained in the same manner as in Example 1. Of these granules, 180 に g were treated with enzyme-treated rutin α [αG rutin PS (Toyo Seika Co., Ltd.)] 6, sucrose fatty acid ester DK [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 and tricalcium phosphate [Third Calcium phosphate cocoon (produced by Taihei Chemical Sangyo Co., Ltd.)] 4 混合 g was added and mixed thoroughly in a polyethylene bag to obtain a composition. g was obtained. The sized powder was subjected to compression molding at a tableting pressure of 1000 kgf in the same manner as in Example 1. As a result, 20 tablets of 350 mg per tablet showing a hardness of 10.9 kgf were obtained.
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 g、サメ軟骨抽出粉末 [サメ軟骨食品用コンドロイチンHG-40 (日本薬品社製)] 40 gおよび酵素処理ルチン [αGルチンPS (東洋精糖社製)] 12 gを精製水1116 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒、組成物および整粒末を得た後に、850 kgfの打錠圧で圧縮成形を行い、9.5 kgfの硬度を示す錠剤を20錠得た。
[比較例1]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 gを精製水960 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を得た。当該顆粒160 gに対して、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 26 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えてポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1と同様の方法により1500 kgfの打錠圧で圧縮成形を行い、6.6 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例2]
比較例1と同様の方法によりグルコサミン塩酸塩の25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を得た。当該顆粒160 gに対して、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 20 g、酵素処理ルチン [αGルチンPS (東洋精糖社製)] 6 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えてポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1との方法により1500 kgfの打錠圧で圧縮成形を行い、6.9 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例3]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 gおよびサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)]13 gを精製水93 mLに懸濁して懸濁液を得た。次いで、真空度 20 mT以下、冷却機温度-80 ℃および棚温度30 ℃の条件に設定したフリーズドライヤー [STD及びBTD Eco トレイドライヤー (FTSSYSTEMS社製)] で、上記懸濁液を15時間乾燥させて顆粒を得た。当該顆粒46.5 gにショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gを加えて、ポリエチレン袋内で充分に混合し、本混合末を16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1000 kgfの打錠圧で圧縮成形を行い、8.2 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例4]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 13 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合し、当該混合末を24号篩 (750 μm) を用いて篩過し、流動層造粒機 [流動造粒コーティング装置 FL-MINI型 (フロイント産業社製)] を用いて、20 gの精製水を篩過後の混合末に噴霧して造粒し、顆粒を得た。当該顆粒47 gにショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)]を0.5 g加えて、ポリエチレン袋内で充分に混合した。当該混合末を、16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1700 kgfの打錠圧で圧縮成形を行い、6.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例5]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 10 g、コラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 3 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒および整粒末を得た後、1800 kgfの打錠圧で圧縮成形を行い、6.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例6]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 10 g、酵素処理ルチン [αGルチンPS (東洋精糖社製)] 3 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒および整粒末を得た後、1700 kgfの打錠圧で圧縮成形を行い、5.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例7]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒を得た後、当該顆粒40.5 gにサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 5 g、コラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 1.5 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 0.5 gを加えて、ポリエチレン袋内で充分に混合した。当該混合末を16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1800 kgfの打錠圧で圧縮成形を行い、5.5 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。 Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g, shark cartilage extract powder [chondroitin HG-40 for shark cartilage food (manufactured by Nippon Yakuhin)] and enzyme-treated rutin [αG rutin PS (Toyo Seika Co., Ltd.) 12 g) was dissolved in 1116 mL of purified water to obtain a 25 wt% aqueous solution. Using this aqueous solution, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 850 kgf to obtain 20 tablets showing a hardness of 9.5 kgf. It was.
[Comparative Example 1]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g was dissolved in 960 mL of purified water to obtain a 25 wt% aqueous solution. Granules were obtained by the same method as in Example 1 using the aqueous solution. Shark cartilage extract powder [Marinty ridge 40S (Yaizu Suisan Chemical Co., Ltd.)] 26 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 g Calcium triphosphate [Tricalcium phosphate (manufactured by Taihei Chemical Industrial Co., Ltd.)] Add 4 g and mix well in a polyethylene bag to obtain a composition, which is sieved using a No. 16 sieve (1000 μm). A sized powder was obtained. The sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1 to obtain 20 tablets of 350 mg per tablet having a hardness of 6.6 kgf.
[Comparative Example 2]
A 25% by weight aqueous solution of glucosamine hydrochloride was obtained in the same manner as in Comparative Example 1. Granules were obtained by the same method as in Example 1 using the aqueous solution. Shark cartilage extract powder [Malinker ridge 40S (Yaizui Sui Chemical Co., Ltd.)] 20 g, enzyme-treated rutin [αG rutin PS (Toyo Seiki Co., Ltd.)] 6 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 g and tricalcium phosphate [Tribasic calcium phosphate (Taihei Chemical Industrial Co., Ltd.)] 4 g were added and mixed well in a polyethylene bag to obtain a composition. This was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1, and 20 tablets of 350 mg per tablet showing a hardness of 6.9 kgf were obtained.
[Comparative Example 3]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g and shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g were suspended in 93 mL of purified water. Obtained. Next, the suspension is dried for 15 hours with a freeze dryer [STD and BTD Eco tray dryer (manufactured by FTSSYSTEMS)] set at a vacuum of 20 mT or less, a cooler temperature of -80 ° C, and a shelf temperature of 30 ° C. To obtain granules. Add 2.5 g of sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku)] and 1 g of tricalcium phosphate [Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.)] to 46.5 g of the granules. The mixed powder was thoroughly mixed, and the mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1000 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 8.2 kgf were obtained.
[Comparative Example 4]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 80 g, Shark cartilage extract powder [Marinlinkerid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g and tricalcium phosphate [Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.) 1 g) is thoroughly mixed in a polyethylene bag, and the mixed powder is sieved using a No. 24 sieve (750 μm). A fluidized bed granulator [fluid granulation coating equipment FL-MINI type (Freund 20 g of purified water was sprayed on the mixed powder after sieving and granulated to obtain granules. To 47 g of the granules, add 2.5 g of sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] and 0.5 g of tribasic calcium phosphate [Tribasic calcium phosphate (Taihei Chemical Sangyo Co., Ltd.)]. Mix thoroughly. The mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1700 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 6.0 kgf were obtained.
[Comparative Example 5]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g, Shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 10 g, collagen [Water-soluble fish collagen (Kyowa Hakko Bio Co., Ltd.) )] 3 g and tricalcium phosphate [tricalcium phosphate (produced by Taihei Chemical Industrial Co., Ltd.)] 1 g were thoroughly mixed in a polyethylene bag. After obtaining granules and sized powder by the same process as in Comparative Example 4, compression molding was performed with a tableting pressure of 1800 kgf to obtain 20 tablets of 350 mg per tablet having a hardness of 6.0 kgf.
[Comparative Example 6]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g, Shark cartilage extract powder [Marinlinkerid 40S (Yaizu Suisan Chemical Co., Ltd.)] 10 g, enzyme-treated rutin [αG rutin PS (manufactured by Toyo Seiki Co., Ltd.) )] 3 g and tricalcium phosphate [tricalcium phosphate (produced by Taihei Chemical Industrial Co., Ltd.)] 1 g were thoroughly mixed in a polyethylene bag. After obtaining granules and sized powder by the same process as in Comparative Example 4, compression molding was performed with a tableting pressure of 1700 kgf to obtain 20 tablets of 350 mg per tablet having a hardness of 5.0 kgf.
[Comparative Example 7]
80 g of glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] and 1 g of tricalcium phosphate [tricalcium phosphate (manufactured by Taihei Chemical Industrial Co., Ltd.)] were thoroughly mixed in a polyethylene bag. After obtaining granules by the same process as in Comparative Example 4, 50.5 g of shark cartilage extract powder [Malinker ridge 40S (Yaizui Suisan Chemical Co., Ltd.)] and collagen [water-soluble fish collagen (Kyowa Hakko Bio) 1.5 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 2.5 g and tribasic calcium phosphate [tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.)] 0.5 g Mix well within. The mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1800 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 5.5 kgf were obtained.
[比較例1]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 320 gを精製水960 mLに溶解して25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を得た。当該顆粒160 gに対して、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 26 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えてポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1と同様の方法により1500 kgfの打錠圧で圧縮成形を行い、6.6 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例2]
比較例1と同様の方法によりグルコサミン塩酸塩の25重量%の水溶液を得た。該水溶液を用いて、実施例1と同様の方法により顆粒を得た。当該顆粒160 gに対して、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 20 g、酵素処理ルチン [αGルチンPS (東洋精糖社製)] 6 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 10 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 4 gを加えてポリエチレン袋内で充分に混合して組成物を得て、これを16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1との方法により1500 kgfの打錠圧で圧縮成形を行い、6.9 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例3]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 gおよびサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)]13 gを精製水93 mLに懸濁して懸濁液を得た。次いで、真空度 20 mT以下、冷却機温度-80 ℃および棚温度30 ℃の条件に設定したフリーズドライヤー [STD及びBTD Eco トレイドライヤー (FTSSYSTEMS社製)] で、上記懸濁液を15時間乾燥させて顆粒を得た。当該顆粒46.5 gにショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gを加えて、ポリエチレン袋内で充分に混合し、本混合末を16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1000 kgfの打錠圧で圧縮成形を行い、8.2 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例4]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 13 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合し、当該混合末を24号篩 (750 μm) を用いて篩過し、流動層造粒機 [流動造粒コーティング装置 FL-MINI型 (フロイント産業社製)] を用いて、20 gの精製水を篩過後の混合末に噴霧して造粒し、顆粒を得た。当該顆粒47 gにショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)]を0.5 g加えて、ポリエチレン袋内で充分に混合した。当該混合末を、16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1700 kgfの打錠圧で圧縮成形を行い、6.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例5]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 10 g、コラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 3 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒および整粒末を得た後、1800 kgfの打錠圧で圧縮成形を行い、6.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例6]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 g、サメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 10 g、酵素処理ルチン [αGルチンPS (東洋精糖社製)] 3 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒および整粒末を得た後、1700 kgfの打錠圧で圧縮成形を行い、5.0 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。
[比較例7]
グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] 80 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 1 gをポリエチレン袋内で充分に混合した。比較例4と同様の工程により顆粒を得た後、当該顆粒40.5 gにサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] 5 g、コラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] 1.5 g、ショ糖脂肪酸エステル [DKエステルF20W (第一工業製薬社製)] 2.5 gおよび第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] 0.5 gを加えて、ポリエチレン袋内で充分に混合した。当該混合末を16号篩 (1000 μm) を用いて篩過して整粒末を得た。当該整粒末を実施例1~8と同様にして1800 kgfの打錠圧で圧縮成形を行い、5.5 kgfの硬度を示す1錠あたり350 mgの錠剤を20錠得た。 Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g, shark cartilage extract powder [chondroitin HG-40 for shark cartilage food (manufactured by Nippon Yakuhin)] and enzyme-treated rutin [αG rutin PS (Toyo Seika Co., Ltd.) 12 g) was dissolved in 1116 mL of purified water to obtain a 25 wt% aqueous solution. Using this aqueous solution, after obtaining granules, a composition and a sized powder by the same method as in Example 1, compression molding was performed with a tableting pressure of 850 kgf to obtain 20 tablets showing a hardness of 9.5 kgf. It was.
[Comparative Example 1]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 320 g was dissolved in 960 mL of purified water to obtain a 25 wt% aqueous solution. Granules were obtained by the same method as in Example 1 using the aqueous solution. Shark cartilage extract powder [Marinty ridge 40S (Yaizu Suisan Chemical Co., Ltd.)] 26 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 g Calcium triphosphate [Tricalcium phosphate (manufactured by Taihei Chemical Industrial Co., Ltd.)] Add 4 g and mix well in a polyethylene bag to obtain a composition, which is sieved using a No. 16 sieve (1000 μm). A sized powder was obtained. The sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1 to obtain 20 tablets of 350 mg per tablet having a hardness of 6.6 kgf.
[Comparative Example 2]
A 25% by weight aqueous solution of glucosamine hydrochloride was obtained in the same manner as in Comparative Example 1. Granules were obtained by the same method as in Example 1 using the aqueous solution. Shark cartilage extract powder [Malinker ridge 40S (Yaizui Sui Chemical Co., Ltd.)] 20 g, enzyme-treated rutin [αG rutin PS (Toyo Seiki Co., Ltd.)] 6 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 10 g and tricalcium phosphate [Tribasic calcium phosphate (Taihei Chemical Industrial Co., Ltd.)] 4 g were added and mixed well in a polyethylene bag to obtain a composition. This was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1500 kgf in the same manner as in Example 1, and 20 tablets of 350 mg per tablet showing a hardness of 6.9 kgf were obtained.
[Comparative Example 3]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g and shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g were suspended in 93 mL of purified water. Obtained. Next, the suspension is dried for 15 hours with a freeze dryer [STD and BTD Eco tray dryer (manufactured by FTSSYSTEMS)] set at a vacuum of 20 mT or less, a cooler temperature of -80 ° C, and a shelf temperature of 30 ° C. To obtain granules. Add 2.5 g of sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku)] and 1 g of tricalcium phosphate [Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.)] to 46.5 g of the granules. The mixed powder was thoroughly mixed, and the mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1000 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 8.2 kgf were obtained.
[Comparative Example 4]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 80 g, Shark cartilage extract powder [Marinlinkerid 40S (Yaizu Suisan Chemical Co., Ltd.)] 13 g and tricalcium phosphate [Tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.) 1 g) is thoroughly mixed in a polyethylene bag, and the mixed powder is sieved using a No. 24 sieve (750 μm). A fluidized bed granulator [fluid granulation coating equipment FL-MINI type (Freund 20 g of purified water was sprayed on the mixed powder after sieving and granulated to obtain granules. To 47 g of the granules, add 2.5 g of sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] and 0.5 g of tribasic calcium phosphate [Tribasic calcium phosphate (Taihei Chemical Sangyo Co., Ltd.)]. Mix thoroughly. The mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1700 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 6.0 kgf were obtained.
[Comparative Example 5]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g, Shark cartilage extract powder [Marin tilid 40S (Yaizu Suisan Chemical Co., Ltd.)] 10 g, collagen [Water-soluble fish collagen (Kyowa Hakko Bio Co., Ltd.) )] 3 g and tricalcium phosphate [tricalcium phosphate (produced by Taihei Chemical Industrial Co., Ltd.)] 1 g were thoroughly mixed in a polyethylene bag. After obtaining granules and sized powder by the same process as in Comparative Example 4, compression molding was performed with a tableting pressure of 1800 kgf to obtain 20 tablets of 350 mg per tablet having a hardness of 6.0 kgf.
[Comparative Example 6]
Glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio Inc.)] 80 g, Shark cartilage extract powder [Marinlinkerid 40S (Yaizu Suisan Chemical Co., Ltd.)] 10 g, enzyme-treated rutin [αG rutin PS (manufactured by Toyo Seiki Co., Ltd.) )] 3 g and tricalcium phosphate [tricalcium phosphate (produced by Taihei Chemical Industrial Co., Ltd.)] 1 g were thoroughly mixed in a polyethylene bag. After obtaining granules and sized powder by the same process as in Comparative Example 4, compression molding was performed with a tableting pressure of 1700 kgf to obtain 20 tablets of 350 mg per tablet having a hardness of 5.0 kgf.
[Comparative Example 7]
80 g of glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] and 1 g of tricalcium phosphate [tricalcium phosphate (manufactured by Taihei Chemical Industrial Co., Ltd.)] were thoroughly mixed in a polyethylene bag. After obtaining granules by the same process as in Comparative Example 4, 50.5 g of shark cartilage extract powder [Malinker ridge 40S (Yaizui Suisan Chemical Co., Ltd.)] and collagen [water-soluble fish collagen (Kyowa Hakko Bio) 1.5 g, sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku Co., Ltd.)] 2.5 g and tribasic calcium phosphate [tricalcium phosphate (Taihei Chemical Industrial Co., Ltd.)] 0.5 g Mix well within. The mixed powder was sieved using a No. 16 sieve (1000 μm) to obtain a sized powder. The sized powder was subjected to compression molding at a tableting pressure of 1800 kgf in the same manner as in Examples 1 to 8, and 20 tablets of 350 mg per tablet showing a hardness of 5.5 kgf were obtained.
なお本願実施例および比較例における錠剤の硬度は、実施例1~8および比較例1~7の各製造において、製造した錠剤のうちランダムに選んだ5錠の錠剤硬度の平均値を表し、下記表1~3にその結果を示す。
下記表1中のスプレードライ成分および追加成分、表2中のフリーズドライ成分および追加成分ならびに表3中の造粒成分および追加成分の数値の単位は全て重量%である。 The tablet hardness in Examples and Comparative Examples of the present application represents the average value of the tablet hardness of 5 tablets randomly selected from the manufactured tablets in each of Examples 1-8 and Comparative Examples 1-7. Tables 1 to 3 show the results.
The units of the numerical values of the spray-dried components and additional components in Table 1 below, the freeze-dried components and additional components in Table 2 and the granulated components and additional components in Table 3 are all by weight.
下記表1中のスプレードライ成分および追加成分、表2中のフリーズドライ成分および追加成分ならびに表3中の造粒成分および追加成分の数値の単位は全て重量%である。 The tablet hardness in Examples and Comparative Examples of the present application represents the average value of the tablet hardness of 5 tablets randomly selected from the manufactured tablets in each of Examples 1-8 and Comparative Examples 1-7. Tables 1 to 3 show the results.
The units of the numerical values of the spray-dried components and additional components in Table 1 below, the freeze-dried components and additional components in Table 2 and the granulated components and additional components in Table 3 are all by weight.
下記表1~3中のGは、グルコサミン塩酸塩 [グルコサミンFM (協和発酵バイオ社製)] を表し、Aはサメ軟骨抽出粉末 [マリンカーティリッジ40S (焼津水産化学工業社製)] を表し、Bは、サメ軟骨抽出粉末[SCP(NB) (マルハニチロ社製)] を表し、Cはサメ軟骨抽出粉末 [サメ軟骨食品用コンドロイチンHG-40 (日本薬品社製)]、Dは、コラーゲン [水溶性フィッシュコラーゲン (協和発酵バイオ社製)] を表し、Eは、酵素処理ルチン [αGルチンPS (東洋精糖社製)] を表し、Fは、ショ糖脂肪酸エステル[DKエステルF20W (第一工業製薬社製)] を表し、Hは、第三リン酸カルシウム [第三リン酸カルシウム (太平化学産業社製)] を表す。
G in Tables 1 to 3 below represents glucosamine hydrochloride [Glucosamine FM (manufactured by Kyowa Hakko Bio)] 、, A represents shark cartilage extract powder [Malinkin ridge 40S (manufactured by Yaizu Suisan Chemical Co., Ltd.)] B represents shark cartilage extract powder [SCP (NB) (manufactured by Maruha Nichiro)], C represents shark cartilage extract powder [chondroitin HG-40 for shark cartilage food (manufactured by Nippon Pharmaceutical)], D represents collagen [water-soluble Fish collagen cocoon (manufactured by Kyowa Hakko Bio)], E represents enzyme-treated rutin [αG rutin PS (manufactured by Toyo Seika Co., Ltd.)] 、, and F represents sucrose fatty acid ester [DK ester F20W (Daiichi Kogyo Seiyaku) H) represents tricalcium phosphate cocoon [tricalcium phosphate cocoon (manufactured by Taihei Chemical Industrial Co., Ltd.)].
下記表1~3中の「キャッピング」における○は、当該実施例または比較例の製造において、20錠打錠した際に1錠もキャッピングが発生しなかったことを表し、×は、20錠打錠した際に1錠以上キャッピングが発生したことを表す。
下記表1~3中の「流動性」における○は、単発式圧縮成型機において、篩過した混合末の充填時に、1回のすり切りで篩過した混合末がスムーズに充填されたことを示し、×は、単発式圧縮成型機において、少なくとも1回のすり切りでは、篩過した混合末がスムーズに充填されなかったことを示す。 In Tables 1 to 3 below, “Capping” indicates that no capping occurred when 20 tablets were tableted in the production of the examples or comparative examples, and × indicates 20 tablets. Indicates that one or more tablets have been capped when locked.
In the following Tables 1 to 3, “◯” in “fluidity” indicates that in a single-press compression molding machine, when the mixed powder passed through the sieve was filled, the mixed powder passed through the sieving was filled smoothly. , X indicates that in a single-shot compression molding machine, the sieved mixed powder was not smoothly filled by at least one grinding.
下記表1~3中の「流動性」における○は、単発式圧縮成型機において、篩過した混合末の充填時に、1回のすり切りで篩過した混合末がスムーズに充填されたことを示し、×は、単発式圧縮成型機において、少なくとも1回のすり切りでは、篩過した混合末がスムーズに充填されなかったことを示す。 In Tables 1 to 3 below, “Capping” indicates that no capping occurred when 20 tablets were tableted in the production of the examples or comparative examples, and × indicates 20 tablets. Indicates that one or more tablets have been capped when locked.
In the following Tables 1 to 3, “◯” in “fluidity” indicates that in a single-press compression molding machine, when the mixed powder passed through the sieve was filled, the mixed powder passed through the sieving was filled smoothly. , X indicates that in a single-shot compression molding machine, the sieved mixed powder was not smoothly filled by at least one grinding.
上記実施例1~8で得られた錠剤について、少なくともグルコサミン塩酸塩およびサメ軟骨抽出粉末を水に溶解してスプレードライした実施例1~8では流動性が十分であり、キャッピングまたはラミネーションを生じることなく錠剤が得られた。一方、グルコサミンのみをスプレードライした比較例1および2ならびに流動層造粒で造粒成分を造粒した比較例4~7では、流動性は十分であったが、キャッピングが生じた。また、グルコサミン塩酸塩およびサメ軟骨抽出粉末をフリーズドライした比較例3は、キャッピングは生じなかったが、流動性が不十分であった。
For the tablets obtained in Examples 1-8 above, at least glucosamine hydrochloride and shark cartilage extract powder were dissolved in water and spray-dried, and in Examples 1-8, the fluidity was sufficient and capping or lamination occurred. A tablet was obtained. On the other hand, in Comparative Examples 1 and 2 in which only glucosamine was spray-dried and in Comparative Examples 4 to 7 in which the granulated components were granulated by fluidized bed granulation, the fluidity was sufficient, but capping occurred. In Comparative Example 3 in which glucosamine hydrochloride and shark cartilage extract powder were freeze-dried, capping did not occur, but fluidity was insufficient.
従って、本願発明により、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒、組成物およびそれらを用いることによりグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤が得られることが分かった。
Therefore, according to the present invention, glucosamine or a salt thereof and chondroitin sulfate or a salt thereof containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof improved in tableting property and fluidity are used to increase the glucosamine or a salt thereof and chondroitin sulfate or a salt thereof. It was found that tablets containing were obtained.
本発明により、打錠性および流動性が向上したグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒および組成物、ならびにグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を高含有する錠剤およびその製造方法が提供される。
According to the present invention, granules and compositions containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof having improved tableting properties and fluidity, and a tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof and a production thereof A method is provided.
Claims (19)
- グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液1と略す)をスプレードライして得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 Glucosamine or a salt thereof and chondroitin sulfate or a salt thereof obtained by spray-drying a solution or suspension containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof (hereinafter, the solution or suspension is abbreviated as Solution 1) Contains granules.
- 溶液1が、さらにコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物を含有する溶液または懸濁液(以下当該溶液または懸濁液を溶液2と略す)である請求項1に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 Solution 1 is a solution or suspension containing one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof, rutin or an enzyme-treated product thereof, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid (hereinafter referred to as “the solution 1”). 2. The granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to claim 1, wherein the solution or suspension is abbreviated as solution 2.
- 溶液2に含有される化合物が、コラーゲンまたはその酵素処理物およびルチンまたはその酵素処理物からなる群から選ばれる1つ以上の化合物である請求項2に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 The glucosamine or a salt thereof and chondroitin sulfate or the compound thereof according to claim 2, wherein the compound contained in the solution 2 is one or more compounds selected from the group consisting of collagen or an enzyme-treated product thereof and rutin or an enzyme-treated product thereof. Granules containing salt.
- グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するグルコサミンまたはその塩の含有量が60~95重量%である請求項1~3のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 The glucosamine or a salt thereof and the chondroitin sulfate or the glucosamine or a salt thereof and the chondroitin sulfate or the glucosamine or a salt thereof and the chondroitin sulfate or the glucosamine or the salt thereof and the chondroitin sulfate or the salt thereof according to any one of claims 1 to 3, wherein the content of the glucosamine or the salt thereof is 60 to 95% by weight. Granules containing salt.
- グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコンドロイチン硫酸またはその塩の含有量が3~20重量%である請求項1~4のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 The glucosamine or a salt thereof and chondroitin sulfate or the chondroitin sulfate or the chondroitin sulfate according to any one of claims 1 to 4, wherein the content of the chondroitin sulfate or the salt thereof relative to the granule containing glucosamine or the salt thereof and the chondroitin sulfate or the salt thereof is 3 to 20% by weight. Granules containing the salt.
- グルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に対するコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である請求項2~5のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒。 One or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid for granules containing glucosamine or its salt and chondroitin sulfate or its salt The granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of claims 2 to 5, wherein the total content of
- 請求項1~6のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に、滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加して得られる組成物。 7. The granule containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of claims 1 to 6, and at least one compound selected from the group consisting of a lubricant, a fluidity improver and an additive A composition obtained by addition.
- 請求項1~7のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物を打錠して得られる錠剤。 A tablet obtained by tableting the granule or composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of claims 1 to 7.
- 錠剤に対する錠剤中のグルコサミンまたはその塩の含有量が60~95重量%である請求項8に記載の錠剤。 The tablet according to claim 8, wherein the content of glucosamine or a salt thereof in the tablet relative to the tablet is 60 to 95% by weight.
- 錠剤に対する錠剤中のコンドロイチン硫酸またはその塩の含有量が3~20重量%である請求項8または9に記載の錠剤。 The tablet according to claim 8 or 9, wherein the content of chondroitin sulfate or a salt thereof in the tablet relative to the tablet is 3 to 20% by weight.
- 錠剤に対する錠剤中のコラーゲンまたはその酵素処理物、ルチンまたはその酵素処理物、チアミン、リボフラビン、ピリドキシン、ナイアシンおよびパントテン酸からなる群から選ばれる1つ以上の化合物の合計含有量が0.1~10重量%である請求項8~10のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤。 The total content of one or more compounds selected from the group consisting of collagen or its enzyme-treated product, rutin or its enzyme-treated product, thiamine, riboflavin, pyridoxine, niacin and pantothenic acid in the tablet relative to the tablet is 0.1 to 10% by weight A tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of claims 8 to 10.
- 溶液1または2をスプレードライする工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒の製造方法。 A method for producing granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising a step of spray-drying solution 1 or 2.
- 溶液1または2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物の製造方法。 One or more selected from the group consisting of a lubricant, a fluidity improver, and an additive in the granule containing the step of spray-drying solution 1 or 2 and glucosamine or a salt thereof and chondroitin sulfate obtained in the step A method for producing a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising the step of adding the compound of:
- 溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である請求項12または13に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。 14. The method for producing granules or a composition containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to claim 12 or 13, wherein the content of glucosamine or a salt thereof contained in the solution 1 or 2 is 15 to 27% by weight. .
- 溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が、1~6重量%である請求項12~14のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒または組成物の製造方法。 The granule or glucosamine or salt thereof and chondroitin sulfate or salt thereof according to any one of claims 12 to 14, wherein the content of chondroitin sulfate or salt thereof contained in the solution 1 or 2 is 1 to 6% by weight. A method for producing the composition.
- 溶液1または溶液2をスプレードライする工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒を用いて打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 Glucosamine or a salt thereof and chondroitin sulfate or a salt thereof comprising a step of spray-drying solution 1 or solution 2 and a tableting step using granules containing glucosamine or a salt thereof and chondroitin sulfate or the salt obtained in the step The manufacturing method of the tablet to contain.
- 溶液1または溶液2をスプレードライする工程、該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する顆粒に滑沢剤、流動性改善剤および添加物からなる群より選ばれる1つ以上の化合物を添加し混合する工程ならびに該工程で得られるグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する組成物を打錠する工程を含むグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 A step of spray-drying solution 1 or solution 2, one selected from the group consisting of a lubricant, a fluidity improver and an additive in granules containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof obtained in the step Containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof, comprising a step of adding and mixing the above compound and a step of tableting a composition containing glucosamine or a salt thereof and chondroitin sulfate or the salt obtained in the step Tablet manufacturing method.
- 溶液1または2に含まれるグルコサミンまたはその塩の含有量が15~27重量%である請求項16または17に記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 18. The method for producing a tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to claim 16 or 17, wherein the content of glucosamine or a salt thereof contained in Solution 1 or 2 is 15 to 27% by weight.
- 溶液1または2に含まれるコンドロイチン硫酸またはその塩の含有量が1~6重量%である請求項16~18のいずれかに記載のグルコサミンまたはその塩およびコンドロイチン硫酸またはその塩を含有する錠剤の製造方法。 The production of a tablet containing glucosamine or a salt thereof and chondroitin sulfate or a salt thereof according to any one of claims 16 to 18, wherein the content of chondroitin sulfate or a salt thereof contained in the solution 1 or 2 is 1 to 6% by weight. Method.
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JP2003299497A (en) * | 2002-02-05 | 2003-10-21 | Masayoshi Kachi | Mucopolysaccharide and method for producing the same |
JP2005515174A (en) * | 2001-11-07 | 2005-05-26 | フィンツェルベルグ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニエ コマンデット ゲゼルシャフト | Method for preparing dry extracts |
US20060228487A1 (en) * | 2005-04-11 | 2006-10-12 | J. Rettenmaier & Söehne GmbH + Co. KG | Methods of combining active agents with augmented microcrystalline cellulose |
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JP2003299497A (en) * | 2002-02-05 | 2003-10-21 | Masayoshi Kachi | Mucopolysaccharide and method for producing the same |
US20060228487A1 (en) * | 2005-04-11 | 2006-10-12 | J. Rettenmaier & Söehne GmbH + Co. KG | Methods of combining active agents with augmented microcrystalline cellulose |
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JP2018035143A (en) * | 2016-08-25 | 2018-03-08 | 大正製薬株式会社 | tablet |
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