CN106727384A - A kind of tuber of dwarf lilyturf oligosaccharides sustained release tablets and preparation method thereof - Google Patents
A kind of tuber of dwarf lilyturf oligosaccharides sustained release tablets and preparation method thereof Download PDFInfo
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- CN106727384A CN106727384A CN201710044013.2A CN201710044013A CN106727384A CN 106727384 A CN106727384 A CN 106727384A CN 201710044013 A CN201710044013 A CN 201710044013A CN 106727384 A CN106727384 A CN 106727384A
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- tuber
- oligosaccharides
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- dwarf lilyturf
- release tablets
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- 229920001542 oligosaccharide Polymers 0.000 title claims abstract description 49
- 150000002482 oligosaccharides Chemical class 0.000 title claims abstract description 49
- 239000007939 sustained release tablet Substances 0.000 title claims abstract description 45
- 238000002360 preparation method Methods 0.000 title claims abstract description 39
- 240000002948 Ophiopogon intermedius Species 0.000 title claims abstract 11
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 26
- 239000000314 lubricant Substances 0.000 claims abstract description 20
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 16
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 16
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 15
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims abstract description 15
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 13
- 238000013268 sustained release Methods 0.000 claims abstract description 13
- 239000012730 sustained-release form Substances 0.000 claims abstract description 13
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 12
- 239000008101 lactose Substances 0.000 claims abstract description 12
- 229920002472 Starch Polymers 0.000 claims abstract description 9
- 239000011159 matrix material Substances 0.000 claims abstract description 9
- 239000008107 starch Substances 0.000 claims abstract description 9
- 235000019698 starch Nutrition 0.000 claims abstract description 9
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 7
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000001768 carboxy methyl cellulose Substances 0.000 claims abstract description 7
- 229920003064 carboxyethyl cellulose Polymers 0.000 claims abstract description 7
- 239000000945 filler Substances 0.000 claims abstract description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 7
- 239000000741 silica gel Substances 0.000 claims abstract description 7
- 229910002027 silica gel Inorganic materials 0.000 claims abstract description 7
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims abstract description 7
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims abstract description 7
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000000843 powder Substances 0.000 claims abstract description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 36
- 235000019441 ethanol Nutrition 0.000 claims description 22
- 239000000463 material Substances 0.000 claims description 17
- 239000003826 tablet Substances 0.000 claims description 15
- 238000005469 granulation Methods 0.000 claims description 14
- 230000003179 granulation Effects 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 7
- MYKOKMFESWKQRX-UHFFFAOYSA-N 10h-anthracen-9-one;sulfuric acid Chemical compound OS(O)(=O)=O.C1=CC=C2C(=O)C3=CC=CC=C3CC2=C1 MYKOKMFESWKQRX-UHFFFAOYSA-N 0.000 claims description 6
- 229920002678 cellulose Polymers 0.000 claims description 5
- 239000001913 cellulose Substances 0.000 claims description 5
- 235000010980 cellulose Nutrition 0.000 claims description 5
- 238000001514 detection method Methods 0.000 claims description 5
- -1 hydroxypropyl Chemical group 0.000 claims description 5
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 4
- 239000012043 crude product Substances 0.000 claims description 4
- 238000010828 elution Methods 0.000 claims description 4
- 238000004821 distillation Methods 0.000 claims description 3
- 239000000706 filtrate Substances 0.000 claims description 3
- 239000012467 final product Substances 0.000 claims description 3
- 238000004108 freeze drying Methods 0.000 claims description 3
- 239000000499 gel Substances 0.000 claims description 3
- 238000005119 centrifugation Methods 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 238000011068 loading method Methods 0.000 claims description 2
- 238000001556 precipitation Methods 0.000 claims description 2
- 239000000047 product Substances 0.000 claims description 2
- 238000010992 reflux Methods 0.000 claims description 2
- 239000013049 sediment Substances 0.000 claims description 2
- 238000000967 suction filtration Methods 0.000 claims description 2
- 238000005406 washing Methods 0.000 claims description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 238000004587 chromatography analysis Methods 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 239000012153 distilled water Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 27
- 229940079593 drug Drugs 0.000 abstract description 23
- 239000008280 blood Substances 0.000 abstract description 8
- 210000004369 blood Anatomy 0.000 abstract description 8
- 230000000694 effects Effects 0.000 abstract description 7
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 238000001727 in vivo Methods 0.000 abstract description 2
- 244000248557 Ophiopogon japonicus Species 0.000 description 41
- 239000003405 delayed action preparation Substances 0.000 description 11
- 230000007774 longterm Effects 0.000 description 4
- 229920005654 Sephadex Polymers 0.000 description 2
- 239000012507 Sephadex™ Substances 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000002218 hypoglycaemic effect Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- 230000002588 toxic effect Effects 0.000 description 2
- 229940123208 Biguanide Drugs 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920002527 Glycogen Polymers 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 241001262617 Japonica Species 0.000 description 1
- 241000234280 Liliaceae Species 0.000 description 1
- 102100024295 Maltase-glucoamylase Human genes 0.000 description 1
- 229920003091 Methocel™ Polymers 0.000 description 1
- 241001448424 Ophiopogon Species 0.000 description 1
- 229930195210 Ophiopogon Natural products 0.000 description 1
- 229940100389 Sulfonylurea Drugs 0.000 description 1
- 241000209140 Triticum Species 0.000 description 1
- 235000021307 Triticum Nutrition 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 108010028144 alpha-Glucosidases Proteins 0.000 description 1
- 150000004283 biguanides Chemical class 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- DQYBDCGIPTYXML-UHFFFAOYSA-N ethoxyethane;hydrate Chemical compound O.CCOCC DQYBDCGIPTYXML-UHFFFAOYSA-N 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000003595 mist Substances 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000000837 restrainer Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 150000005856 steroid saponins Chemical class 0.000 description 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/896—Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
- A61K36/8968—Ophiopogon (Lilyturf)
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to a kind of tuber of dwarf lilyturf oligosaccharides sustained release tablets and preparation method thereof.Sustained release tablets of the invention are made up of 0.01 0.02 parts of 1 part of active component tuber of dwarf lilyturf oligosaccharides, 0.5 1.5 parts of sustained-release matrix material, 0.3 0.6 parts of filler and lubricant according to the mass fraction.The described preferred hydroxypropyl methyl cellulose of sustained-release matrix material, sodium carboxymethylcellulose or carboxyethyl cellulose.Described filler includes microcrystalline cellulose, lactose or starch.Described lubricant includes magnesium stearate, superfine silica gel powder or talcum powder.Compared with prior art, tuber of dwarf lilyturf oligosaccharides effectively and stably can be in vivo discharged after this sustained release tablets is taken, effective blood drug concentration and time can be maintained, " peak valley " phenomenon of blood concentration can be avoided again.On the premise of curative effect is ensured, it is possible to decrease the side effect caused by blood concentration is too high, and preparation process is simple, it is adaptable to industrialized production.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to a kind of tuber of dwarf lilyturf oligosaccharides sustained release tablets and preparation method thereof.
Background technology
The tuber of dwarf lilyturf is the Liliaceae Ophiopogon plant tuber of dwarf lilyturf (ophiopogon japonicas (thunb.) Ker-Gawl.
Dry tuber, with promoting production of body fluid and nourishing the lung, replenishing the vital essence and removing heat function.The tuber of dwarf lilyturf mainly contains steroid saponin, polysaccharide and homoisoflavone class etc.
Composition.Research finds that ophiopogonpolysaccharide has significant hypoglycemic effect, the pancreas islet β that its hypoglycemic mechanism may be damaged with improvement
Cell function, β cellular damages are reduced, suppressed decomposition of glycogen, prevented the absorption of glucose enteron aisle relevant.Effectively control is high at this stage
The medicine of blood sugar is generally Western medicine, sulfonylurea drugs, biguanides, alpha-glucosidase restrainer as used by treatment diabetes
Deng, although hyperglycaemia can be effectively controlled, but its toxic and side effect is big, unsuitable long-term use.We early-stage Study show that the tuber of dwarf lilyturf is few
The sugared extract component as the Chinese medicine tuber of dwarf lilyturf, with persistently, curative effect stabilization, toxic and side effect is small, can for action temperature during disease preventing and treating
Long-term use.After medication, insoluble drug release slowly to reach long-acting, reduces medicining times to sustained-release tablet, improves patient's
Compliance.The peak valley phenomenon common to ordinary preparation can be avoided simultaneously, it is ensured that the safety and effectiveness of medication.However, both at home and abroad still
No-trump tuber of dwarf lilyturf oligosaccharides prepares the precedent as sustained release tablets.
The content of the invention
Blood concentration fluctuation is big, medicining times are more etc. is caused the invention aims to solve ordinary tablet half-life short
Technical problem, there is provided one kind improves patient medication compliance, is more suitable for the wheat of the patient for treating diabetes long-term prescription
Winter oligosaccharides sustained release tablets.
Sustained release tablets of the invention are according to the mass fraction by 1 part of active component tuber of dwarf lilyturf oligosaccharides, sustained-release matrix material 0.5-1.5
Part, filler 0.3-0.6 parts and lubricant 0.01-0.02 parts be made.
Described sustained-release matrix material is hydrophilic gel sustained-release matrix material.It is preferred that hydroxypropyl methyl cellulose, carboxymethyl
The mixture of one or more in sodium cellulosate or carboxyethyl cellulose.Between most preferred viscosity 4000-15000mPa.s
Hydroxypropyl methyl cellulose.
Described filler includes one or more in microcrystalline cellulose, lactose or starch.
Described lubricant includes one or more in magnesium stearate, superfine silica gel powder or talcum powder.
Another object of the present invention is to provide a kind of preparation of the tuber of dwarf lilyturf oligosaccharides sustained release tablets suitable for industrialized production
Method.
Compared with prior art, the invention has the advantages that:Drug release rate experiment display, the tuber of dwarf lilyturf of the invention
The rate of release of oligosaccharides sustained release tablets reaches medicament slow release preparation requirement, with slow releasing function.Can effectively and stably exist after taking
Release tuber of dwarf lilyturf oligosaccharides, can maintain effective blood drug concentration and time in vivo, and " peak valley " phenomenon of blood concentration can be avoided again.Protecting
On the premise of card curative effect, it is possible to decrease the side effect caused by blood concentration is too high, daily medication 1-2 times is adapted to need
Want the patient of long-term prescription.And preparation process is simple, it is adaptable to industrialized production.
Specific embodiment
Below in conjunction with specific embodiment, the present invention is further elaborated.
The drug release determination of this experiment is according to Pharmacopoeia of People's Republic of China 2015 edition four (0931 dissolution rate and releases
Determination method).
Embodiment 1
1st, the preparation of tuber of dwarf lilyturf oligosaccharides:Tuber of dwarf lilyturf medicinal material is shredded, 10 times of 95% alcohol refluxs of volume are filtered after 2 hours, abandon filter
Liquid, the band ethanol of medicinal material 95% is volatilized, plus 10 times of volume pure water, 100 DEG C of water-baths are extracted 2 times, and suction filtration is collected filtrate and is concentrated under reduced pressure
It is 1.2g/ml to density, adds 80% ethanol, stand 12 hours, ethanol is abandoned after sugar is separated out, respectively with absolute ethyl alcohol, nothing
Water ether, acetone washing, 55 DEG C of drying sediments, obtain final product thick oligosaccharides.Thick oligosaccharides is dissolved in water, concentration is gone precipitation, made for centrifugation
With Sephadex G-75 chromatographic columns, to distill water elution, Anthrone-sulfuricacid method detection is collected, and merges eluting peak, freeze-drying system
Obtain tuber of dwarf lilyturf oligosaccharides crude product.Gained crude product is dissolved in water, concentration is 0.01g/ml, uses Sephadex G-15 chromatographic columns, loading body
Product is 0.018 times of column volume, and with 0.88 times of distillation water elution of column volume, flow velocity is 0.0009 times of column volume/minute, anthrone-
Sulfuric acid process detects, collects the position and be designated as position 1;It is further continued for 0.3 times of distillation water elution of column volume, flow velocity is 0.0009 times
Column volume/minute, Anthrone-sulfuricacid method detection, collects the position and is designated as position 2;Take the freeze-drying of position 2.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 90g, carboxyethyl cellulose 15g, sodium carboxymethylcellulose
15g, lactose 10g, starch 10g, microcrystalline cellulose 10g, magnesium stearate 0.75g, superfine silica gel powder 0.75g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 2
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 100g, carboxyethyl cellulose 20g, lactose 10g, starch
20g, magnesium stearate 0.75g, superfine silica gel powder 0.75g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 3
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxymethyl-propyl cellulose 85g, sodium carboxymethylcellulose 65g, lactose 10g, crystallite
Cellulose 10g, magnesium stearate 1.5g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 4
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, sodium carboxymethylcellulose 40g, carboxyethyl cellulose 40g, starch 30g, microcrystalline cellulose
Plain 30g, magnesium stearate 1.0g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 5
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 90g, starch 60g, magnesium stearate 1.5g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 6
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, carboxyethyl cellulose 50g, starch 60g, superfine silica gel powder 2.0g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 7
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, sodium carboxymethylcellulose 70g, microcrystalline cellulose 60g, magnesium stearate 1.5g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 8
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 120g, lactose 50g, magnesium stearate 1g, talcum powder 1g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 9
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 80g, sodium carboxymethylcellulose 20g, lactose 50g, micro mist
Silica gel 1g, talcum powder 1g
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Prepare 1000
Piece.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively labelled amount
10~30%, 30~60%, more than 80%, reach the requirement of sustained release preparation release.
Embodiment 10
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 60g, lactose 20g, starch 20g, microcrystalline cellulose 20g,
Talcum powder 2g
Preparation method:By tuber of dwarf lilyturf oligosaccharides and viscosity for 15000mPa.s hydroxypropyl methyl celluloses are well mixed, crystallite is added
Cellulose is well mixed, and uses 95% alcohol granulation, dries, plus compressing tablet after lubricant.Prepare 1000.By drug release determination,
Its result shows the sustained release tablets 2 hours, 4 hours burst sizes with 8 hours be respectively labelled amount 10~30%, 30~60%,
More than 80%, reach the requirement of sustained release preparation release.
Embodiment 11
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 90g, lactose 60g, magnesium stearate 2g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Wherein, hydroxyl
It is 15000mPa.s that propyl methocel uses viscosity, prepares 1000.By drug release determination, its result shows the sustained release
Piece 2 hours, 4 hours burst sizes with 8 hours are respectively 10~30%, 30~60%, more than the 80% of labelled amount, reach sustained release
The requirement of preparation release.
Embodiment 12
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 110g, lactose 40g, magnesium stearate 2g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Wherein hydroxypropyl
It is 4000mPa.s that ylmethyl cellulose uses viscosity, prepares 1000.By drug release determination, its result shows the sustained release tablets 2
Hour, 4 hours burst sizes with 8 hours are respectively 10~30%, 30~60%, more than the 80% of labelled amount, reach sustained release system
The requirement of agent release.
Embodiment 13
1st, tuber of dwarf lilyturf oligosaccharides prepare it is same as Example 1.
2nd, the preparation of sustained release tablets
Formula:Tuber of dwarf lilyturf oligosaccharides 100g, hydroxypropyl methyl cellulose 100g, lactose 50g, magnesium stearate 2g.
Preparation method:Above-mentioned material is well mixed jointly, 95% alcohol granulation, dried, plus compressing tablet after lubricant.Wherein viscosity
It is the hydroxypropyl methyl cellulose 65g of 4000mPa.s, viscosity is the hydroxypropyl methyl cellulose 35g of 15000mPa.s, is prepared
1000.By drug release determination, its result shows the sustained release tablets 2 hours, and 4 hours burst sizes with 8 hours are respectively sign
10~30%, 30~60%, more than the 80% of amount, reaches the requirement of sustained release preparation release.
Claims (7)
1. a kind of tuber of dwarf lilyturf oligosaccharides sustained release tablets, it is characterised in that:Described sustained release tablets are few by the active component tuber of dwarf lilyturf according to the mass fraction
1 part of sugar, 0.5-1.5 parts, filler 0.3-0.6 parts and lubricant 0.01-0.02 parts of sustained-release matrix material are made.
2. sustained release tablets as claimed in claim 1, it is characterised in that:Described sustained-release matrix material is hydrophilic gel sustained release bone
Frame material.
3. sustained release tablets as claimed in claim 2, it is characterised in that:Described hydrophilic gel sustained-release matrix material includes hydroxypropyl
One or more in ylmethyl cellulose, sodium carboxymethylcellulose or carboxyethyl cellulose.
4. sustained release tablets as claimed in claim 3, it is characterised in that:The viscosity of described hydroxypropyl methyl cellulose is
Between 4000-15000mPa.s.
5. sustained release tablets as claimed in claim 1, it is characterised in that:Described filler include microcrystalline cellulose, lactose or
In starch one or more.
6. sustained release tablets as claimed in claim 1, it is characterised in that:Described lubricant includes magnesium stearate, superfine silica gel powder
Or one or more in talcum powder.
7. the preparation method of sustained release tablets as claimed in claim 1, it is characterised in that comprise the following steps:
(1) preparation of tuber of dwarf lilyturf oligosaccharides:Tuber of dwarf lilyturf medicinal material is shredded, 10 times of 95% alcohol refluxs of volume are filtered after 2 hours, abandon filtrate,
The band ethanol of medicinal material 95% is volatilized, plus 10 times of volume pure water, 100 DEG C of water-baths are extracted 2 times, and suction filtration is collected filtrate and is concentrated under reduced pressure into close
It is 1.2g/ml to spend, and adds 80% ethanol, stands 12 hours, ethanol is abandoned after sugar is separated out, respectively with absolute ethyl alcohol, anhydrous second
Ether, acetone washing, 55 DEG C of drying sediments, obtain final product thick oligosaccharides;Thick oligosaccharides is dissolved in water, concentration goes precipitation for centrifugation, and chromatography is washed
De-, Anthrone-sulfuricacid method detection is collected, and merges eluting peak, and freeze-drying obtains tuber of dwarf lilyturf oligosaccharides crude product;Crude product is dissolved in water, concentration is
0.01g/ml, chromatography, loading volume is 0.018 times of column volume, and with 0.88 times of distillation water elution of column volume, flow velocity is 0.0009
Times column volume/minute, Anthrone-sulfuricacid method detection is collected the position and is designated as position 1;It is further continued for 0.3 times of distilled water of column volume
Wash-out, flow velocity is 0.0009 times of column volume/minute, and Anthrone-sulfuricacid method detection is collected the position and is designated as position 2;Take position 2 cold
Lyophilized dry i.e. prepared target product tuber of dwarf lilyturf oligosaccharides, its molecular weight is between 500~2500;
(2) obtained tuber of dwarf lilyturf oligosaccharides, sustained-release matrix material, filler are well mixed by proportioning is common, 95% alcohol granulation is done
It is dry, plus compressing tablet is obtained final product after lubricant.
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Cited By (1)
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CN101428007A (en) * | 2008-12-04 | 2009-05-13 | 上海天赐福生物工程有限公司 | Process for producing diabecron sustained release tablet |
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CN101428007A (en) * | 2008-12-04 | 2009-05-13 | 上海天赐福生物工程有限公司 | Process for producing diabecron sustained release tablet |
CN103006605A (en) * | 2012-09-24 | 2013-04-03 | 浙江莎普爱思药业股份有限公司 | Bendazac lysine sustained release preparation as well as preparation method and application of preparation |
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