CN102143692A - 赤藓醇的压片 - Google Patents
赤藓醇的压片 Download PDFInfo
- Publication number
- CN102143692A CN102143692A CN2009801345764A CN200980134576A CN102143692A CN 102143692 A CN102143692 A CN 102143692A CN 2009801345764 A CN2009801345764 A CN 2009801345764A CN 200980134576 A CN200980134576 A CN 200980134576A CN 102143692 A CN102143692 A CN 102143692A
- Authority
- CN
- China
- Prior art keywords
- tablet
- composition
- erythrite
- sorbite
- granulated
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims abstract description 62
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims abstract description 40
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims abstract description 26
- 238000000034 method Methods 0.000 claims abstract description 26
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims abstract description 11
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000000811 xylitol Substances 0.000 claims abstract description 11
- 235000010447 xylitol Nutrition 0.000 claims abstract description 11
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract description 11
- 229960002675 xylitol Drugs 0.000 claims abstract description 11
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims abstract description 10
- 239000001768 carboxy methyl cellulose Substances 0.000 claims abstract description 10
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims abstract description 10
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims abstract description 10
- 239000000845 maltitol Substances 0.000 claims abstract description 10
- 235000010449 maltitol Nutrition 0.000 claims abstract description 10
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims abstract description 10
- 229940035436 maltitol Drugs 0.000 claims abstract description 10
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims abstract description 9
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims abstract description 9
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims abstract description 9
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 9
- 239000000905 isomalt Substances 0.000 claims abstract description 9
- 235000010439 isomalt Nutrition 0.000 claims abstract description 9
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 9
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 9
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 9
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 claims abstract description 7
- 241000360590 Erythrites Species 0.000 claims description 39
- 238000007906 compression Methods 0.000 claims description 24
- 230000006835 compression Effects 0.000 claims description 24
- 239000000853 adhesive Substances 0.000 claims description 18
- 230000001070 adhesive effect Effects 0.000 claims description 18
- 238000005469 granulation Methods 0.000 claims description 16
- 230000003179 granulation Effects 0.000 claims description 16
- 229920002472 Starch Polymers 0.000 claims description 9
- 238000007873 sieving Methods 0.000 claims description 9
- 239000008107 starch Substances 0.000 claims description 9
- 235000019698 starch Nutrition 0.000 claims description 9
- 235000013305 food Nutrition 0.000 claims description 8
- 239000000314 lubricant Substances 0.000 claims description 8
- 239000002537 cosmetic Substances 0.000 claims description 5
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 abstract description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 abstract 1
- 239000004386 Erythritol Substances 0.000 abstract 1
- 229920000881 Modified starch Polymers 0.000 abstract 1
- 229940105329 carboxymethylcellulose Drugs 0.000 abstract 1
- 235000019414 erythritol Nutrition 0.000 abstract 1
- 229940009714 erythritol Drugs 0.000 abstract 1
- 229960002160 maltose Drugs 0.000 abstract 1
- 239000000600 sorbitol Substances 0.000 abstract 1
- 229960002920 sorbitol Drugs 0.000 abstract 1
- 235000010356 sorbitol Nutrition 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 67
- 239000000047 product Substances 0.000 description 29
- 239000007788 liquid Substances 0.000 description 19
- 239000002245 particle Substances 0.000 description 19
- 239000000843 powder Substances 0.000 description 17
- 239000004744 fabric Substances 0.000 description 13
- 238000001035 drying Methods 0.000 description 12
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 8
- 238000002360 preparation method Methods 0.000 description 8
- 239000012530 fluid Substances 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 239000007910 chewable tablet Substances 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 238000000227 grinding Methods 0.000 description 5
- 238000002288 cocrystallisation Methods 0.000 description 4
- 235000009508 confectionery Nutrition 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 239000000796 flavoring agent Substances 0.000 description 4
- 235000013355 food flavoring agent Nutrition 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 239000000654 additive Substances 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 210000000214 mouth Anatomy 0.000 description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 238000012216 screening Methods 0.000 description 3
- 150000005846 sugar alcohols Chemical class 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 235000012222 talc Nutrition 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 238000010998 test method Methods 0.000 description 3
- -1 this Chemical compound 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 239000003905 agrochemical Substances 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 238000004040 coloring Methods 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000007884 disintegrant Substances 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 238000000855 fermentation Methods 0.000 description 2
- 230000004151 fermentation Effects 0.000 description 2
- 239000003337 fertilizer Substances 0.000 description 2
- 238000007542 hardness measurement Methods 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 239000003595 mist Substances 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 229960005489 paracetamol Drugs 0.000 description 2
- 229920000728 polyester Polymers 0.000 description 2
- 230000008092 positive effect Effects 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 238000005406 washing Methods 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 238000004438 BET method Methods 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 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 description 1
- 239000005913 Maltodextrin Substances 0.000 description 1
- 229920002774 Maltodextrin Polymers 0.000 description 1
- RCEAADKTGXTDOA-UHFFFAOYSA-N OS(O)(=O)=O.CCCCCCCCCCCC[Na] Chemical compound OS(O)(=O)=O.CCCCCCCCCCCC[Na] RCEAADKTGXTDOA-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 230000001055 chewing effect Effects 0.000 description 1
- 235000015111 chews Nutrition 0.000 description 1
- 239000003599 detergent Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003292 glue Substances 0.000 description 1
- 235000001497 healthy food Nutrition 0.000 description 1
- 238000005984 hydrogenation reaction Methods 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007483 microbial process Effects 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 238000010606 normalization Methods 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 235000019809 paraffin wax Nutrition 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical class CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000000376 reactant Substances 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000010008 shearing Methods 0.000 description 1
- BTURAGWYSMTVOW-UHFFFAOYSA-M sodium dodecanoate Chemical compound [Na+].CCCCCCCCCCCC([O-])=O BTURAGWYSMTVOW-UHFFFAOYSA-M 0.000 description 1
- 229940082004 sodium laurate Drugs 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 239000000273 veterinary drug Substances 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/08—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing solids as carriers or diluents
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
- A23L27/30—Artificial sweetening agents
-
- 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
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
- A23L27/30—Artificial sweetening agents
- A23L27/33—Artificial sweetening agents containing sugars or derivatives
- A23L27/34—Sugar alcohols
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
- A23P10/00—Shaping or working of foodstuffs characterised by the products
- A23P10/20—Agglomerating; Granulating; Tabletting
- A23P10/28—Tabletting; Making food bars by compression of a dry powdered mixture
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/10—General cosmetic use
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/59—Mixtures
- A61K2800/592—Mixtures of compounds complementing their respective functions
- A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0216—Solid or semisolid forms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0216—Solid or semisolid forms
- A61K8/022—Powders; Compacted Powders
- A61K8/0225—Granulated powders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- C—CHEMISTRY; METALLURGY
- C05—FERTILISERS; MANUFACTURE THEREOF
- C05F—ORGANIC FERTILISERS NOT COVERED BY SUBCLASSES C05B, C05C, e.g. FERTILISERS FROM WASTE OR REFUSE
- C05F11/00—Other organic fertilisers
-
- C—CHEMISTRY; METALLURGY
- C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
- C11D—DETERGENT COMPOSITIONS; USE OF SINGLE SUBSTANCES AS DETERGENTS; SOAP OR SOAP-MAKING; RESIN SOAPS; RECOVERY OF GLYCEROL
- C11D3/00—Other compounding ingredients of detergent compositions covered in group C11D1/00
- C11D3/16—Organic compounds
- C11D3/20—Organic compounds containing oxygen
- C11D3/2003—Alcohols; Phenols
- C11D3/2065—Polyhydric alcohols
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Birds (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Emergency Medicine (AREA)
- Wood Science & Technology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Nutrition Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pest Control & Pesticides (AREA)
- Environmental Sciences (AREA)
- Zoology (AREA)
- Dentistry (AREA)
- Toxicology (AREA)
- Plant Pathology (AREA)
- Agronomy & Crop Science (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- General Preparation And Processing Of Foods (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Cephalosporin Compounds (AREA)
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Abstract
将比表面积大于0.25m2/g,优选大于0.3m2/g的赤藓醇与选自下面的物质一起进行造粒:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇及其混合物。制备了片剂,并且描述了相应的方法。
Description
技术领域
本发明涉及适于压片的含有赤藓醇的组合物的制备。
背景技术
在目前关注的无糖和/或低热量产物的使用中,用于药物、糖果或者食品应用的片剂大部分是用糖醇,例如木糖醇、麦芽糖醇、山梨糖醇、甘露醇和赤藓醇制成的。
该片剂不但含有药物或者反应物,它还包含其他的充当填充料的成分,例如 乳糖或者磷酸酯;润滑剂,例如滑石、硬脂酸或者石腊和崩解剂,例如羧甲基纤维素或者淀粉。用于糖果目的时,该片剂经常包含低浓度的香味剂和着色剂。
在欧洲专利EP0497439中已经描述了喷雾干燥的赤藓醇的直接压缩。该片剂总是用麦芽糖糊精作为粘合剂来制备的。
欧洲专利申请EP0528604公开了共结晶的山梨糖醇和木糖醇以及由其制造的片剂。
EP0896528涉及多元醇组合物,其具有通过喷雾干燥或者流化床造粒获得的高浓度的不吸湿性多元醇。
EP0922464涉及一种制备基于赤藓醇的可快速崩解的压模材料的方法。通过直接压模来获得片剂。如此获得的可快速崩解的压模材料在置于口腔或者水中时,被赋予了优异的崩解性和溶解性。
EP0913148涉及一种制备含有赤藓醇的组合物的方法,该组合物适于作为压片的赋形剂。该合适的组合物是通过赤藓醇和第二多元醇例如山梨糖醇的共结晶来制备的。就这样使用赤藓醇,并且在共结晶之前与山梨糖醇进行混合。在该共结晶之后,将该产物进行研磨和压片。该方法不包括造粒步骤。
另外关注的是,使用具有提高的比表面积的赤藓醇作为片剂中的赋形剂。
发明内容
本发明涉及一种可压缩的组合物,其是由比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇和选自下面的粘合剂组成:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇,及其混合物,并且特征在于将该组合物进行造粒。
本发明还涉及一种可咀嚼的片剂,其包含前述可压缩的组合物。
此外,本发明涉及一种制备本发明的可压缩的组合物的方法,并且其包括下面的步骤:
a)取比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇,
b)加入选自下面的粘合剂:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇及其混合物,
c)造粒,
d)任选地湿筛分造粒产物,
e)干燥该造粒产物,
f)任选筛分该造粒产物。
本发明还描述了一种制备本发明的片剂的方法,并且其包括下面的步骤:
a)取根据本发明所制备的造粒产物,
b)与润滑剂进行共混,
c)在5-30kN的压缩力下压片。
最后本发明涉及片剂在食品、饲料、制药和化妆品应用中的用途。
具体实施方式
本发明涉及一种可压缩的组合物,其是由比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇和选自下面的粘合剂组成:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇,及其混合物,并且特征在于将该组合物进行造粒。
赤藓醇是一种丁糖醇,其可以经由化学方法,优选碳水化合物的氢化,和/或微生物方法或者发酵法来获得,优选发酵法。任何赤藓醇都是合适的,只要它的比表面积大于0.25m2/g即可。没有任何的限制,比表面积大于0.25m2/g的赤藓醇的合适来源是如WO2009016133所述而制备的微粉化赤藓醇,或者是涡轮研磨的赤藓醇等等,或者细微级的赤藓醇,条件是它的比表面积大于0.25m2/g。
该比表面积是用BET方法来测量。
出乎意料地,已经发现比表面积对于随后的造粒具有积极的作用,即使用液体形式的粘合剂也是如此。比表面积越大,造粒进行的越好。造粒是这样一种方法,在其中制造初级粉末粒子,来形成称作颗粒的更大的实体。该造粒能够防止粉末混合物成分的分离,改善该粉末混合物的流动性,和改善该粉末混合物的压实特性。
造粒方法可以分为两种基本类型,即,湿法(其在该方法过程中使用液体)和干法(在其中不使用液体)。湿法造粒是最经常使用的,并且涉及许多步骤,其包括:在粒化流体的存在下,使用低剪切或者高剪切混合器或者流化床,通过搅拌附聚(粒化)活性成分的干燥初级粉末粒子和赋形剂,湿筛分(湿过筛)来除去较大的团块,干燥该造粒产物,以及研磨或者筛分(过筛)该干燥的粒化产物,来实现具有期望的颗粒尺寸分布的粒化产物。所获得的粒子随后可以压片。
此外,赤藓醇的体积平均直径(参见Ph.Eur.Vl)小于100μm,优选小于50μm,更优选小于40μm。将粘合剂例如预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖或者其混合物以干燥的形式加入,而将粘合剂例如山梨糖醇以液体形式加入。粘合剂例如麦芽糖醇、异麦芽酮糖醇、木糖醇或者其混合物可以以干燥或者液体形式加入。优选的粘合剂是液体山梨糖醇,其干物质浓度为至少50%,优选60%,更优选至少70%。
赤藓醇与粘合剂的比例是50%:50%,优选70%:30%,最高达90%:10%干重。优选地,使用液体山梨糖醇作为粘合剂时,赤藓醇与山梨糖醇的比例是50%:50%,优选70%:30%,最高达90%:10%干重。
该组合物进一步的特征在于,它在65%的相对湿度和25℃的吸湿量低于3%,优选低于2.7%。
此外,本发明涉及在食品应用、饲料、制药应用、化妆品、洗涤剂、肥料或者农用化学产品中的用途。实际上,非限制性地,本发明的可压缩组合物可以与定影液一起用于食品、动物饲料、健康食品、饮食产品、兽药中,与肥料、与植物颗粒、与植物种子或者种粒和任何被人和/或动物摄入的其他产品或者可受益于本发明的可压缩组合物的性能提高的任何其他产品一起用于农用化学品产品中。本发明的可压缩组合物可以用作添加剂的载体,所述添加剂基于酶或者微生物、去污片、维生素、香味剂、香料、酸、甜味剂或者具有医学或者非医学应用的不同活性成分。最后可以施用添加剂的混合物。
本发明还涉及一种可咀嚼的片剂,其包含前述的可压缩组合物。作为此处使用的,术语“片剂”包括任何片剂,特别是处于任何形式,形状并具有任何物理,化学或者感官性能的片剂,和用于任何给药,指示和应用途径的片剂。根据本发明所生产的片剂是可咀嚼的片剂。本发明的可咀嚼片剂是软片剂,其中在吞咽之前,在口中咀嚼帮助粉碎该片剂粒子和释放活性成分、香味剂、芳香剂等等。可咀嚼的片剂剂型可以是一种软药丸、片剂、胶和最近的“咀嚼片”。片剂硬度和脆性是包含活性成分并且具有令人期望的咀嚼性能的可咀嚼片剂的非常重要的性能。
所述的片剂可以用于食品、饲料、化妆品、洗涤剂和/或制药应用中。该可咀嚼片剂明显不同于在口腔或者水中快速崩解的片剂,并且具有不同的使用目的。
作为片剂形成中的润滑剂,可以根据需要加入硬脂酸镁、硬脂酸钙、硬脂酸、脂肪酸糖酯,和/或滑石等等。此外,可以根据需要加入表面活性剂例如十二烷基硫酸钠、丙二醇、十二烷基磺酸钠、油酸磺酸钠,和混合有硬脂酸盐和滑石的月桂酸钠、硬脂酰富马酸钠、脂肪酸糖酯等等。
根据Ph.Eur.Vl,如此获得的片剂在5-30kN的压缩力下的脆性是0.3-0.7%,优选是0.3-0.5%。优选这些片剂具有至少1 cm2的表面积和350mg的重量,高达2 cm2的表面积和1090mg的重量。
这些片剂的拉伸强度可以表示为压缩力的函数。在5-30kN的压缩力下可获得1.5-3.10N/mm2,甚至高达3.60N/mm2的拉伸强度。在20kN的拉伸强度是至少2.5 N/mm2,优选至少2.8 N/mm2,更优选至少2.9 N/mm2,至少3.0N/mm2,至少3.1 N/mm2,至少3.2 N/mm2,最优选至少3.5 N/mm2。该片剂在15 kN的压缩力下的硬度至少是110N,优选至少130N,更优选至少145 N。优选该片剂具有至少1 cm2的表面积和350mg的重量,高达2 cm2的表面积和1090mg的重量。
本发明的可咀嚼片剂在5-30kN的压缩力下的脆性是0.3-0.7%,并且在5-30kN的压缩力下可获得1.5-3.10N/mm2,甚至高达3.60N/mm2的拉伸强度。
此外,本发明涉及一种制备本发明的可压缩组合物的方法,并且其包括下面的步骤:
a)取比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇,
b)加入选自下面的粘合剂:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇及其混合物,
c)造粒,
d)任选湿筛分造粒产物,
e)干燥该造粒产物,
f)任选筛分该造粒产物。
在该方法中,优选赤藓醇进一步具有小于100μm,优选小于50μm,更优选小于40μm的体积平均直径。当用更粗糙的原料来开始时,在该方法中包括研磨步骤,优选涡轮研磨,来获得小于100μm,优选小于50μm,更优选小于40μm的体积平均直径。如此获得的产物的比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g,并且它对于随后的造粒具有积极的作用。粘合剂例如预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖或者其混合物是以干燥的形式加入的,而粘合剂例如山梨糖醇是以液体形式加入的。粘合剂例如麦芽糖醇、异麦芽酮糖醇、木糖醇或者其混合物可以以干燥或者液体形式加入。优选该粘合剂是液体山梨糖醇,并且它是以至少50%,优选至少60%,更优选至少70%的干物质浓度加入的。根据体积平均直径和共混物的含水量,对产物进行筛分和/或干燥。
本发明方法的步骤c)中所形成的颗粒任选通过预定尺寸的筛网进行压制。优选将筛选机用于这种筛分。同时或者其后,干燥所述产物。
任何干燥机类型都可以用于干燥该颗粒,但是优选将流化床用于此目的。充分干燥的产物是在典型的造粒机中进行造粒的。
本发明还描述了一种制备本发明的片剂的方法,并且它包括下面的步骤:
a)取根据本发明所制备的造粒产物,
b)与润滑剂进行共混,
c)在5-30kN的压缩力下压片。
该造粒产物(=可压缩组合物)进一步与合适的润滑剂(优选是硬脂酸镁)进行共混,并且在压片机中进行压片。
最后本发明涉及片剂在食品、饲料、制药和化妆品应用中的用途。
如果制备片剂来用于食品(糖果)应用中,则通常加入含有高达约99%(w/w)的赤藓醇的可压缩组合物和芳香剂、着色剂、香味剂和润滑剂。如果制备片剂来用于药物应用中,则加入活性成分例如药物,并且根据需要加入填料、润滑剂或者崩解剂。
本发明在下文中将以一系列非限定性的实施例进行说明。
实施例
评价颗粒和片剂性能的方法
该颗粒是通过它们的体积平均直径(尺寸分布)来表征的。使用下面的测量方法。
尺寸分布。尺寸分布是根据European Pharmacopoeia Vl测试方法2.9.31,使用Sympatec GmbH(德国)的激光粒度仪(型号Helos KF-Rodos T4.1)来测定的。粒度是通过激光衍射来分析的。
片剂是通过它们的硬度和脆性来表征的。对于每个压缩力来说,分析10个片剂的硬度和19个片剂的脆性,并且计算平均值。使用下面的测量方法。
硬度。硬度(即,直径压碎强度)是如下来测量的:根据European Pharmacopoeia Vl测试方法2.9.8的片剂的压碎阻力,使用常规的药物硬度测试仪(硬度测试仪型号Multicheck V,获自Erweka GmbH(德国))来测量的。为了比较不同尺寸的片剂的值,归一化断裂区域的断裂强度。该归一化值(单位N/mm2)在这里称作拉伸强度(Ts),并且如下来计算:
Ts =2H/πTD,
其中H是片剂的硬度,T是厚度,D是直径。对于每个压缩力来说,分析10个片剂的硬度(H),厚度(T)和直径(D)。
脆性。脆性测量是根据European Pharmacopoeia Vl测试方法2.9.7的未包覆片剂的脆性来测定的。
实施例1A
将粗赤藓醇产物(Cargill C*PharmEridex16956)在Bauermeister涡轮研磨机UTL中以1mm筛网进行研磨,并且获得了体积平均直径为30μm的粉末。
该体积平均直径是用激光衍射来测量。该赤藓醇的比表面积是0.40m2/g。
将500g的研磨过的赤藓醇粉末在高剪切混合器(Pro-C-ept-Mi-Pro,切碎机:3000rpm,叶轮:1200rpm)中进行60秒的干混。
以9.5g/min的速度逐滴加入79.17g的液体山梨糖醇(70%的干物质)(Cargill C*PharmSorbidex NC16205)。在加入该液体山梨糖醇之后,将该共混物连续混合60秒。
将该造粒粉末在2mm筛网上手动湿过筛。
将该湿过筛的颗粒在流化床(Aeromatic-Fielder GEA-Strea-1)中在70℃的温度下干燥30分钟。
将该干燥的颗粒在造粒机(Erweka(FGS + AR400E)中在0.500mm的筛网上以100转/分钟的速度过筛5-10分钟。
然后将该干燥的过筛颗粒与3%的硬脂酸镁在Pharmatech Equipment中以28 rpm的速度共混。
实施例1B
将粗赤藓醇产物(Cargill ZeroseTM16952)在Bauermeister涡轮研磨机UTL中以1mm筛网进行研磨,并且获得了体积平均直径为20μm的粉末。该体积平均直径是用激光衍射来测量。该赤藓醇的比表面积是0.45m2/g。
将500g的研磨过的赤藓醇粉末在高剪切混合器(Pro-C-ept-Mi-Pro,切碎机:3000rpm,叶轮:1200rpm)中进行60秒的干混。
以9.5g/min的速度逐滴加入79.17g的液体山梨糖醇(70%的干物质)(Cargill C*PharmSorbidex NC16205)。在加入该液体山梨糖醇之后,将该共混物连续混合60秒。
将该造粒粉末在2mm筛网上手动湿过筛。
将该湿过筛的颗粒在流化床(Aeromatic-Fielder GEA-Strea-1)中在70℃的温度下干燥30分钟。
将该干燥的颗粒在造粒机(Erweka(FGS + AR400E)中在0.500mm的筛网上以100转/分钟的速度过筛5-10分钟。
然后将该干燥的过筛颗粒与3%的硬脂酸镁在Pharmatech Equipment中以28 rpm的速度共混。
实施例2A
然后将实施例1A中所获得的造粒产物在压片机(Korsch-PH100)中在5 kN-30kN的压缩力下进行压片。
该片剂的表面积是1 cm2,该片剂的直径是11.3mm,重量是350mg。
如下来分析如此获得的片剂:
脆性比较
压缩力(kN) | 实施例2A的产物% | 与EP0913148的实施例1的产物比较% |
5 | 0.49 | 1.85 |
10 | 0.38 | 1.05 |
15 | 0.52 | 0.91 |
20 | 0.44 | 0.96 |
25 | 0.63 | 0.86 |
30 | 0.55 | 0.94 |
拉伸强度比较
压缩力(kN) | 实施例2A的产物(N/mm2) | 与EP0913148的实施例1的产物比较(N/mm2) |
5 | 1.55 | 0.99 |
10 | 2.35 | 1.99 |
15 | 2.87 | 2.46 |
20 | 2.69 | 2.66 |
25 | 2.47 | 2.62 |
30 | 2.45 | 2.53 |
硬度比较
压缩力(kN) | 实施例2A的产物(N) | 与EP0913148的实施例1的产物比较(N) |
5 | 78 | 50 |
10 | 113 | 94 |
15 | 133 | 114 |
20 | 133 | 122 |
25 | 118 | 121 |
30 | 117 | 117 |
实施例2B
然后将实施例1B中所获得的造粒产物在压片机(Korsch-PH100)中在5 kN-30kN的压缩力下进行压片。
该片剂的表面积是1 cm2,该片剂的直径是11.3mm,重量是350mg。
如下来分析如此获得的片剂:
脆性比较
压缩力(kN) | 实施例2B的产物(%) | 与EP0913148的实施例1的产物比较(%) |
5 | 0.56 | 1.85 |
15 | 0.34 | 0.91 |
20 | 0.27 | 0.96 |
25 | 0.39 | 0.86 |
30 | 0.38 | 0.94 |
拉伸强度比较
压缩力(kN) | 实施例2B的产物(N/mm2) | 与EP0913148的实施例1的产物比较(N/mm2) |
5 | 1.00 | 0.99 |
10 | 2.30 | 1.99 |
15 | 3.03 | 2.46 |
20 | 3.31 | 2.66 |
25 | 3.64 | 2.62 |
30 | 3.53 | 2.53 |
硬度比较
压缩力(kN) | 实施例2B的产物(N) | 与EP0913148的实施例1的产物比较(N) |
5 | 51 | 50 |
10 | 111 | 94 |
15 | 143 | 114 |
20 | 155 | 122 |
25 | 169 | 121 |
30 | 165 | 117 |
实施例3A
将粗赤藓醇产物(Cargill C*PharmEridex16956)在Bauermeister涡轮研磨机UTL中以1mm筛网进行研磨,并且获得了体积平均直径为30μm的粉末。
该体积平均直径是用激光衍射来测量。该赤藓醇的比表面积是0.45m2/g。
将250g的研磨过的赤藓醇粉末在高剪切混合器(Pro-C-ept-Mi-Pro,切碎机:3000rpm,叶轮:1200rpm)中与250g扑热息痛(微粉)进行60秒的干混。
以9.5g/min的速度逐滴加入74.42g的液体山梨糖醇(70%的干物质)(Cargill C*PharmSorbidex NC16205)。在加入该液体山梨糖醇之后,将该共混物连续混合60秒。
将该造粒粉末在2mm筛网上手动湿过筛。
将该湿过筛的颗粒在流化床(Aeromatic-Fielder GEA-Strea-1)中在70℃的温度干燥30分钟。
将该干燥的颗粒在造粒机(Erweka(FGS + AR400E)中在0.500mm的筛网上以100转/分钟的速度过筛5-10分钟。
然后将该干燥的过筛颗粒与3%的硬脂酸镁在Pharmatech Equipment中以28 rpm的速度共混。
实施例3B
将粗赤藓醇产物(Cargill ZeroseTM16952)在Bauermeister涡轮研磨机UTL中以1mm筛网进行研磨,并且获得了体积平均直径为20μm的粉末。
将250g的研磨过的赤藓醇粉末在高剪切混合器(Pro-C-ept-Mi-Pro,切碎机:3000rpm,叶轮:1200rpm)中与250g扑热息痛(微粉)进行60秒的干混。
以9.5g/min的速度逐滴加入74.42g的液体山梨糖醇(70%的干物质)(Cargill C*PharmSorbidex NC16205)。在加入该液体山梨糖醇之后,将该共混物连续混合60秒。
将该造粒粉末在2mm筛网上手动湿过筛。
将该湿过筛的颗粒在流化床(Aeromatic-Fielder GEA-Strea-1)中在70℃的温度干燥30分钟。
将该干燥的颗粒在造粒机(Erweka(FGS + AR400E)中在0.500mm的筛网上以100转/分钟的速度过筛5-10分钟。
然后将该干燥的过筛颗粒与3%的硬脂酸镁在Pharmatech Equipment中以28 rpm的速度共混。
实施例4A
然后将实施例3A中所获得的造粒产物在压片机(Korsch-PH100)中在10 kN-30kN的压缩力下进行压片,并且在20kN的压缩力下产生了1.8N/mm2的拉伸强度。
该片剂的表面积是2cm2,该片剂的直径是16mm,重量是1090mg。
实施例4B
然后将实施例3B中所获得的造粒产物在压片机(Korsch-PH100)中在10 kN-30kN的压缩力下进行压片,并且在20kN的压缩力下产生了2.7N/mm2的拉伸强度。
该片剂的表面积是1cm2,该片剂的直径是11.3mm,重量是350mg。
Claims (11)
1. 可压缩的组合物,其由比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇和选自下面的粘合剂组成:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇,及其混合物,特征在于将该组合物进行造粒。
2. 根据权利要求1的组合物,其特征在于赤藓醇的体积平均直径小于100μm,优选小于50μm,更优选小于40μm。
3. 根据权利要求1或者2的组合物,其特征在于赤藓醇和山梨糖醇的存在比例是50%:50%到90%:10%的干重。
4. 根据权利要求1-3中任一项的组合物,其特征在于它在65%的相对湿度和25℃时的吸湿量低于3%,优选低于2.7%。
5. 可咀嚼的片剂,其包含根据权利要求1-4中任一项的组合物。
6. 根据权利要求5的片剂,其特征在于在5-30kN的压缩力下,它的脆性为0.3-0.7%,优选为0.3-0.5%。
7. 根据权利要求6的片剂,其特征在于它在20kN下的拉伸强度至少为2.5 N/mm2,优选至少2.8 N/mm2,更优选至少3.3 N/mm2。
8. 用于制备根据权利要求1-4中任一项的可压缩组合物的方法,其包括:
a)取比表面积大于0.25m2/g,优选大于0.3m2/g,更优选大于0.4m2/g的赤藓醇,
b)加入选自下面的粘合剂:预凝胶化淀粉、微晶纤维素、羧甲基纤维素、麦芽糖、山梨糖醇、麦芽糖醇、木糖醇、异麦芽酮糖醇及其混合物,
c)造粒,
d)任选湿筛分造粒产物,
e)干燥该造粒产物,
f)任选筛分该造粒产物。
9. 用于制备根据权利要求5-7中任一项的片剂的方法,其包括:
a)取根据权利要求8的方法的造粒产物,
b)与润滑剂进行共混,
c)在5-30kN的压缩力下压片。
10. 根据权利要求9的方法,其特征在于在步骤a)和/或 b)中加入活性成分。
11. 根据权利要求5-7中任一项的可咀嚼的片剂在食品、饲料、制药和化妆品应用中的用途。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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EP08015598.9 | 2008-09-04 | ||
EP08015598 | 2008-09-04 | ||
PCT/EP2009/005460 WO2010025796A1 (en) | 2008-09-04 | 2009-07-28 | Tabletting of ervthritol |
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CN102143692A true CN102143692A (zh) | 2011-08-03 |
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US (2) | US20110250247A1 (zh) |
EP (1) | EP2334202B1 (zh) |
JP (1) | JP5718231B2 (zh) |
KR (1) | KR101651702B1 (zh) |
CN (1) | CN102143692A (zh) |
AT (1) | ATE543393T1 (zh) |
BR (1) | BRPI0919183B8 (zh) |
CA (1) | CA2735037C (zh) |
DK (1) | DK2334202T3 (zh) |
ES (1) | ES2377869T3 (zh) |
HR (1) | HRP20120121T1 (zh) |
PL (1) | PL2334202T3 (zh) |
PT (1) | PT2334202E (zh) |
RU (1) | RU2498636C2 (zh) |
SI (1) | SI2334202T1 (zh) |
WO (1) | WO2010025796A1 (zh) |
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CN109414051A (zh) * | 2016-06-28 | 2019-03-01 | 株式会社日本抗菌总和研究所 | 赋形剂和片剂 |
CN110868997A (zh) * | 2017-06-30 | 2020-03-06 | 欧莱雅 | 固体清洁化妆品组合物 |
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BR112012030652A2 (pt) * | 2010-06-01 | 2016-08-16 | Cargill Inc | comprimidos que podem ser dispersos oralmente de eritritol e isomalte |
WO2013156543A1 (en) * | 2012-04-20 | 2013-10-24 | Dsm Ip Assets B.V. | Solid, color-stable l-ascorbic acid compositions |
PT3148513T (pt) * | 2014-05-29 | 2020-05-27 | Novartis Ag | Formulação de ceritinib |
FR3023128B1 (fr) * | 2014-07-01 | 2017-11-10 | Roquette Freres | Nouvelle composition edulcorante |
US10632076B2 (en) | 2016-11-18 | 2020-04-28 | Fertin Pharma A/S | Tablet comprising separate binder and erythritol |
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US11351103B2 (en) * | 2016-11-18 | 2022-06-07 | Johnson & Johnson Consumer Inc. | Method of providing oral care benefits |
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US11058633B2 (en) | 2018-05-17 | 2021-07-13 | Fertin Pharma A/S | Disintegrating oral tablet suitable for active pharmaceutical ingredients |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN109414051A (zh) * | 2016-06-28 | 2019-03-01 | 株式会社日本抗菌总和研究所 | 赋形剂和片剂 |
CN110868997A (zh) * | 2017-06-30 | 2020-03-06 | 欧莱雅 | 固体清洁化妆品组合物 |
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Publication number | Publication date |
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ES2377869T3 (es) | 2012-04-02 |
EP2334202B1 (en) | 2012-02-01 |
KR101651702B1 (ko) | 2016-08-26 |
US20110250247A1 (en) | 2011-10-13 |
SI2334202T1 (sl) | 2012-04-30 |
DK2334202T3 (da) | 2012-03-05 |
HRP20120121T1 (hr) | 2012-03-31 |
PT2334202E (pt) | 2012-02-28 |
KR20110085976A (ko) | 2011-07-27 |
JP5718231B2 (ja) | 2015-05-13 |
WO2010025796A1 (en) | 2010-03-11 |
JP2012501630A (ja) | 2012-01-26 |
BRPI0919183B1 (pt) | 2020-05-05 |
ATE543393T1 (de) | 2012-02-15 |
PL2334202T3 (pl) | 2012-04-30 |
BRPI0919183B8 (pt) | 2021-05-25 |
BRPI0919183A2 (pt) | 2015-08-18 |
RU2498636C2 (ru) | 2013-11-20 |
US20150320034A1 (en) | 2015-11-12 |
EP2334202A1 (en) | 2011-06-22 |
CA2735037A1 (en) | 2010-03-11 |
RU2011112805A (ru) | 2012-10-10 |
CA2735037C (en) | 2016-07-12 |
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