CN109512790A - A kind of prescription and preparation process of oral disnitegration tablet - Google Patents
A kind of prescription and preparation process of oral disnitegration tablet Download PDFInfo
- Publication number
- CN109512790A CN109512790A CN201811626732.6A CN201811626732A CN109512790A CN 109512790 A CN109512790 A CN 109512790A CN 201811626732 A CN201811626732 A CN 201811626732A CN 109512790 A CN109512790 A CN 109512790A
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- China
- Prior art keywords
- prescription
- weight
- preparation process
- oral disnitegration
- disnitegration tablet
- Prior art date
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- 238000002360 preparation method Methods 0.000 title claims abstract description 22
- 239000003814 drug Substances 0.000 claims abstract description 27
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 25
- 239000000203 mixture Substances 0.000 claims abstract description 14
- 239000000463 material Substances 0.000 claims abstract description 11
- 239000002245 particle Substances 0.000 claims abstract description 11
- 239000000853 adhesive Substances 0.000 claims abstract description 9
- 230000001070 adhesive effect Effects 0.000 claims abstract description 9
- 239000000945 filler Substances 0.000 claims abstract description 9
- 229940124597 therapeutic agent Drugs 0.000 claims abstract description 9
- 239000003086 colorant Substances 0.000 claims abstract description 7
- 239000000314 lubricant Substances 0.000 claims abstract description 7
- 238000000034 method Methods 0.000 claims description 14
- 229940079593 drug Drugs 0.000 claims description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- 229920002261 Corn starch Polymers 0.000 claims description 6
- 239000008120 corn starch Substances 0.000 claims description 6
- 229940099112 cornstarch Drugs 0.000 claims description 6
- -1 corrigent Substances 0.000 claims description 6
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims description 4
- 235000015165 citric acid Nutrition 0.000 claims description 4
- 239000008187 granular material Substances 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 3
- 229930195725 Mannitol Natural products 0.000 claims description 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 3
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 3
- 239000000594 mannitol Substances 0.000 claims description 3
- 235000010355 mannitol Nutrition 0.000 claims description 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 3
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 108010011485 Aspartame Proteins 0.000 claims description 2
- SGHZXLIDFTYFHQ-UHFFFAOYSA-L Brilliant Blue Chemical compound [Na+].[Na+].C=1C=C(C(=C2C=CC(C=C2)=[N+](CC)CC=2C=C(C=CC=2)S([O-])(=O)=O)C=2C(=CC=CC=2)S([O-])(=O)=O)C=CC=1N(CC)CC1=CC=CC(S([O-])(=O)=O)=C1 SGHZXLIDFTYFHQ-UHFFFAOYSA-L 0.000 claims description 2
- 235000005979 Citrus limon Nutrition 0.000 claims description 2
- 239000001856 Ethyl cellulose Substances 0.000 claims description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- DQMUQFUTDWISTM-UHFFFAOYSA-N O.[O-2].[Fe+2].[Fe+2].[O-2] Chemical compound O.[O-2].[Fe+2].[Fe+2].[O-2] DQMUQFUTDWISTM-UHFFFAOYSA-N 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 241000220317 Rosa Species 0.000 claims description 2
- 206010039966 Senile dementia Diseases 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[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 UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims description 2
- 239000004376 Sucralose Substances 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- 239000002253 acid Substances 0.000 claims description 2
- 239000003470 adrenal cortex hormone Substances 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 239000003242 anti bacterial agent Substances 0.000 claims description 2
- 230000003266 anti-allergic effect Effects 0.000 claims description 2
- 230000000049 anti-anxiety effect Effects 0.000 claims description 2
- 230000003178 anti-diabetic effect Effects 0.000 claims description 2
- 230000003474 anti-emetic effect Effects 0.000 claims description 2
- 230000003556 anti-epileptic effect Effects 0.000 claims description 2
- 230000002460 anti-migrenic effect Effects 0.000 claims description 2
- 230000001754 anti-pyretic effect Effects 0.000 claims description 2
- 230000002921 anti-spasmodic effect Effects 0.000 claims description 2
- 239000000043 antiallergic agent Substances 0.000 claims description 2
- 229940088710 antibiotic agent Drugs 0.000 claims description 2
- 239000001961 anticonvulsive agent Substances 0.000 claims description 2
- 239000000935 antidepressant agent Substances 0.000 claims description 2
- 229940005513 antidepressants Drugs 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 239000002111 antiemetic agent Substances 0.000 claims description 2
- 229940127218 antiplatelet drug Drugs 0.000 claims description 2
- 239000002221 antipyretic Substances 0.000 claims description 2
- 239000002249 anxiolytic agent Substances 0.000 claims description 2
- 239000000605 aspartame Substances 0.000 claims description 2
- 235000010357 aspartame Nutrition 0.000 claims description 2
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 2
- 229960003438 aspartame Drugs 0.000 claims description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 2
- 235000013539 calcium stearate Nutrition 0.000 claims description 2
- 239000008116 calcium stearate Substances 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 239000002327 cardiovascular agent Substances 0.000 claims description 2
- 229940125692 cardiovascular agent Drugs 0.000 claims description 2
- 239000000812 cholinergic antagonist Substances 0.000 claims description 2
- 229960000913 crospovidone Drugs 0.000 claims description 2
- 208000010643 digestive system disease Diseases 0.000 claims description 2
- 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 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 239000000686 essence Substances 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 239000012530 fluid Substances 0.000 claims description 2
- 238000009472 formulation Methods 0.000 claims description 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 2
- 229960001340 histamine Drugs 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- 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 description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- 239000000845 maltitol Substances 0.000 claims description 2
- 235000010449 maltitol Nutrition 0.000 claims description 2
- 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 description 2
- 229940035436 maltitol Drugs 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 238000002156 mixing Methods 0.000 claims description 2
- 239000003158 myorelaxant agent Substances 0.000 claims description 2
- 229940124636 opioid drug Drugs 0.000 claims description 2
- 239000008188 pellet Substances 0.000 claims description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
- 239000000612 proton pump inhibitor Substances 0.000 claims description 2
- 229940126409 proton pump inhibitor Drugs 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 239000000932 sedative agent Substances 0.000 claims description 2
- 230000001624 sedative effect Effects 0.000 claims description 2
- 210000002027 skeletal muscle Anatomy 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 229940013618 stevioside Drugs 0.000 claims description 2
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 2
- 235000019202 steviosides Nutrition 0.000 claims description 2
- 238000003756 stirring Methods 0.000 claims description 2
- 235000019408 sucralose Nutrition 0.000 claims description 2
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 2
- 150000005846 sugar alcohols Chemical class 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 235000020985 whole grains Nutrition 0.000 claims description 2
- 239000000811 xylitol Substances 0.000 claims description 2
- 235000010447 xylitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 2
- 229960002675 xylitol Drugs 0.000 claims description 2
- 244000248349 Citrus limon Species 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 235000010944 ethyl methyl cellulose Nutrition 0.000 claims 1
- 238000005469 granulation Methods 0.000 claims 1
- 230000003179 granulation Effects 0.000 claims 1
- 229920003087 methylethyl cellulose Polymers 0.000 claims 1
- 239000003176 neuroleptic agent Substances 0.000 claims 1
- 238000005550 wet granulation Methods 0.000 abstract description 6
- 238000007908 dry granulation Methods 0.000 abstract description 3
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 3
- 239000004576 sand Substances 0.000 abstract description 3
- 239000003085 diluting agent Substances 0.000 description 4
- 210000000214 mouth Anatomy 0.000 description 4
- 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 3
- 238000004108 freeze drying Methods 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 210000003296 saliva Anatomy 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 2
- 238000007907 direct compression Methods 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- 239000006104 solid solution Substances 0.000 description 2
- 244000131522 Citrus pyriformis Species 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- 244000179525 Dracocephalum moldavica Species 0.000 description 1
- 235000010700 Dracocephalum moldavica Nutrition 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 229920003081 Povidone K 30 Polymers 0.000 description 1
- 239000004411 aluminium Substances 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 239000000164 antipsychotic agent Substances 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- 230000001055 chewing effect Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000009747 swallowing Effects 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
- A61K9/2095—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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention provides a kind of prescription of oral disnitegration tablet and preparation processes, it is suitable for the pharmaceutical preparation that therapeutic agent weight accounting in prescription is 0.01%-10%, auxiliary material includes filler, interior additional disintegrating agent, adhesive, lubricant and the corrigent being added as needed, colorant in prescription, preparation process is that therapeutic agent and filler, interior plus disintegrating agent, adhesive and other auxiliary materials pass through progress compressing dry granulation after wet granulation is made particle, gained particle and additional disintegrating agent and other auxiliary materials and carries out total mix and are made.Oral disnitegration tablet hardness strength obtained by the present invention is big, disintegration time is fast and in good taste, without sand type, complies fully with country to the quality requirement of oral disnitegration tablet.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of prescription and preparation process of oral disnitegration tablet.
Background technique
Oral disnitegration tablet is a kind of new oral solid pharmaceutical preparation, can be few in oral cavity without chewing, drinking-water in oral cavity
Measure saliva can quick disintegration form solution or suspension, the disintegration time is less than one minute, then swallows work by oral cavity
Enter human gastrointestinal tract with swallowing, and then drug ingedient is absorbed into human recycle system and plays drug effect, oral disnitegration tablet
It is very suitable for dysphagia or medication crowd need to be forced to use, be with a wide range of applications.
According to the literature, [technology of preparing and clinical application [J] medicine Leader of Yang Zhihong oral disnitegration tablet,
2013,32 (11): 1465-1467.] at present the preparation method of oral disnitegration tablet have freeze-drying, direct compression method, wet process
Granulating tabletting process, solid solution method, microencapsulation, as described in document, freeze-drying, solid solution method etc. are due to equipment, work
Skill technical requirements are higher, with high costs, and domestic application is less.Direct compression method prepares oral disnitegration tablet, to the mobility of auxiliary material,
Compressibility etc. is more demanding, and due to most of auxiliary material poorly water-soluble, tablet has insoluble granule residual after Orally disintegrating,
Sand type is serious.
Wet granule compression tablet is made diluent using mannitol soluble easily in water, lactose etc., through wet granulation, is significantly improved
The mobility of particle, compressibility, but to reduce disintegration time, the insoluble type disintegrating agent of a large amount of water and auxiliary material need to be equally added, such as
For example using crosslinked polyvinylpyrrolidone as disintegrating agent, microcrystalline cellulose, lactose are diluent, wet process system in above-mentioned document
Grain tabletting prepares Dracocephalum moldavica total-flavone mouth disintegrated tablet, and when disintegrating agent crosslinked polyvinylpyrrolidone is 10%, diluent crystallite is fine
When dimension element with lactose is 5: 1,10% disintegrating agent, the insoluble type auxiliary material crystallite of water are added in prescription by ifs vitro disintegration time < 1min
Cellulose accounts for diluent ratio up to 80% or more, and mouthfeel is difficult to enable user satisfied.
When preparing oral disnitegration tablet using wet granulation, for example guarantee mouthfeel, with water soluble adjuvant such as sugar or glycitols
When conjunction object is main, since disintegration of the tabletting hardness to piece is affected, often need to reduce tabletting hardness, so that tablet is wrapping
Dress, transport, using easily sliver during splitting out, while tablet also easy to absorb moisture, so that occurring pitted skin, soft within the shelf-life
Change and other issues, thus usually need to increase cost using double aluminium packagings.
The prescription and preparation process of a kind of oral disnitegration tablet of the present patent application, when therapeutic agent weight accounting is in prescription
When 0.01%-10%, with water soluble adjuvant glycitols compound for main filler, using in raw material plus disintegrating agent wet granulation system
After single-size, additional disintegrating agent compressing dry granulation method prepared, gained oral disintegrated preparation hardness is high, appearance uniform beauty
It sees, after meeting saliva of buccal cavity, is soaked by the quick disintegration of additional disintegrating agent at little particle, then through saliva, little particle dispersing and dissolving is mixed
Select liquid or solution, in good taste, no sand type, oral disnitegration tablet obtained by prescription of the present invention and preparation process from character, quality,
Mouthfeel is consistent with product obtained by freeze-drying.
Summary of the invention
Present invention generally provides a kind of prescription of oral disnitegration tablet and preparation processes, when therapeutic agent weight accounting in prescription
When for 0.01%-10%, using in raw material plus disintegrating agent wet granulation be made single-size after, additional disintegrating agent compressing dry granulation method into
Row preparation, oral disnitegration tablet obtained by the prescription and technique have both disintegration and tablet strength, at the same comfortable taste, without gravel
Sense.
In order to achieve the above-mentioned object of the invention, the present invention adopts the following technical scheme that:
A kind of prescription and preparation process of oral disnitegration tablet are grouped as in prescription by the group of following weight fraction containing auxiliary material: being filled out
Fill agent 66-92.5 parts by weight, interior plus disintegrating agent 3-5 parts by weight, adhesive 0.01-1 parts by weight, additional disintegrating agent 2-3 parts by weight,
Lubricant 0.01-1 parts by weight, other auxiliary materials such as corrigent, colorant are added as needed, and parts by weight are corrigent 0.01-1 weight
Measure part, colorant 0.01-0.5 parts by weight.
The filler is made of glycitols compound, cornstarch, microcrystalline cellulose, and its ratio be 4-5:0.1-
1.5:0.1-1.5.Glycitols compound is made of mannitol, xylitol, sorbierite, the one or more of maltitol.
The interior plus disintegrating agent is by crospovidone, sodium carboxymethyl starch, sodium carboxymethylcellulose, cornstarch
One or more compositions.
The adhesive is by PVP K30, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose
One or more compositions.
The additional disintegrating agent is made of cornstarch.
The lubricant is by one of magnesium stearate, calcium stearate or talcum powder or a variety of forms.
The corrigent is by one of Aspartame, Sucralose, stevioside, citric acid, citric acid, essence or more
Kind composition.
The colorant is by one of di-iron trioxide, famille rose, sunset yellow, brilliant blue, lemon yellow or a variety of forms.
A kind of prescription and preparation process of oral disnitegration tablet, it is characterised in that preparation process is wet granulation, including as follows
Step:
1) adhesive of formula ratio is soluble in water, being configured to concentration is 1-5% solution, and placing is swollen it sufficiently；
2) filler, interior plus disintegrating agent, therapeutic agent are sequentially added into method using fast wet granulator by formula ratio, are uniformly mixed,
The adhesive that step 1 is configured is added, stirring prepares particle；
3) particle made is placed in fluid bed dryer or baking oven, dry, dry particl is made in whole grain；
4) additional disintegrating agent being weighed by formula ratio, dry particl obtained by lubricant and step 3) carries out total mix in mixing machine,
Pellet moisture is controlled, and measures total mix granule therapy medicament contg；
5) according to total mix particle drug content, weight of formulation is converted by pharmaceutical specifications, tabletting is carried out using quick tablet press machine, with
15-30KN pressure carries out tabletting, press tablet hardness greater than 3KG.
A kind of prescription and preparation process of oral disnitegration tablet, therapeutic agent includes but is not limited to following drug: being used for maincenter
Drug, antidepressants, antiemetic, cardiovascular drugs, the antihypnotic/antianxiety sedative, antiepileptic, analgesia of nervous system
Medicine/antipyretic, rheumatoid arthritis medicine, antimigraine, opioid drug, the drug for Parkinson's disease, antipsychotic
Agent, antiplatelet drug, skeletal muscle relaxant, anti-senile dementia disease drug, antispasmodic, proton pump inhibitor, 2 antagonist of histamine H,
Gastrointestinal disease aminosalicyclic acid esters, corticosteroid, antidiabetic, antiallergic and antibiotic agent.
Claims (6)
1. the prescription and preparation process of a kind of oral disnitegration tablet, it is characterised in that therapeutic agent weight accounting is 0.01%- in prescription
10%。
2. a kind of prescription and preparation process of oral disnitegration tablet as described in claim 1, it is characterised in that containing auxiliary in prescription
Material is grouped as by the group of following weight fraction: filler 66-92.5 parts by weight, interior plus disintegrating agent 3-5 parts by weight, adhesive
0.01-1 parts by weight, additional disintegrating agent 2-3 parts by weight, lubricant 0.01-1 parts by weight, other auxiliary materials such as corrigent, colorant root
According to needing to add, parts by weight are corrigent 0.01-1 parts by weight, colorant 0.01-0.5 parts by weight.
3. a kind of prescription and preparation process of oral disnitegration tablet as claimed in claim 2, it is characterised in that filler is by sugar alcohol
Class compound, cornstarch, microcrystalline cellulose composition, its ratio be 4-5:0.1-1.5:0.1-1.5；The interior plus disintegrating agent
By one of crospovidone, sodium carboxymethyl starch, sodium carboxymethylcellulose, cornstarch or a variety of form；Described is viscous
Mixture is by one of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose or a variety of forms；It is described additional to collapse
Solution agent is made of cornstarch；The lubricant is by one of magnesium stearate, calcium stearate or talcum powder or a variety of forms；
The corrigent is by one of Aspartame, Sucralose, stevioside, citric acid, citric acid, essence or a variety of forms；
The colorant is by one of di-iron trioxide, famille rose, sunset yellow, brilliant blue, lemon yellow or a variety of forms.
4. a kind of prescription and preparation process of oral disnitegration tablet as claimed in claim 3, it is characterised in that filler glycitols
Compound is made of mannitol, xylitol, sorbierite, the one or more of maltitol.
5. a kind of prescription and preparation process of oral disnitegration tablet as described in claim 1, it is characterised in that preparation process is wet
Method granulation, includes the following steps:
1) adhesive of formula ratio is soluble in water, being configured to concentration is 1-5% solution, and placing is swollen it sufficiently；
2) filler, interior plus disintegrating agent, therapeutic agent are sequentially added into method using fast wet granulator by formula ratio, are uniformly mixed,
The adhesive that step 1 is configured is added, stirring prepares particle；
3) particle made is placed in fluid bed dryer or baking oven, dry, dry particl is made in whole grain；
4) additional disintegrating agent being weighed by formula ratio, dry particl obtained by lubricant and step 3) carries out total mix in mixing machine,
Pellet moisture is controlled, and measures total mix granule therapy medicament contg；
5) according to total mix particle drug content, weight of formulation is converted by pharmaceutical specifications, tabletting is carried out using quick tablet press machine, with
15-30KN pressure carries out tabletting, press tablet hardness greater than 3KG.
6. a kind of prescription and preparation process of oral disnitegration tablet as described in claim 1, therapeutic agent includes but is not limited to such as
Lower drug: for the drug of central nervous system, antidepressants, antiemetic, cardiovascular drugs, antihypnotic/antianxiety sedative,
Antiepileptic, antalgesic/antipyretic, rheumatoid arthritis medicine, antimigraine, opioid drug, for Parkinson's disease
Drug, major tranquilizer, antiplatelet drug, skeletal muscle relaxant, anti-senile dementia disease drug, antispasmodic, proton pump inhibitor,
2 antagonist of histamine H, gastrointestinal disease aminosalicyclic acid esters, corticosteroid, antidiabetic, antiallergic and antibiotic agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811626732.6A CN109512790A (en) | 2018-12-28 | 2018-12-28 | A kind of prescription and preparation process of oral disnitegration tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811626732.6A CN109512790A (en) | 2018-12-28 | 2018-12-28 | A kind of prescription and preparation process of oral disnitegration tablet |
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| CN109512790A true CN109512790A (en) | 2019-03-26 |
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| CN201811626732.6A Pending CN109512790A (en) | 2018-12-28 | 2018-12-28 | A kind of prescription and preparation process of oral disnitegration tablet |
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|---|---|---|---|---|
| CN101411747A (en) * | 2008-11-25 | 2009-04-22 | 广东药学院 | Salvia root polyphenol acid orally disintegrating tablets and preparation method thereof |
| WO2013161823A1 (en) * | 2012-04-24 | 2013-10-31 | 第一三共株式会社 | Orally disintegrating tablet and method for producing same |
| CN104490833A (en) * | 2014-12-11 | 2015-04-08 | 武汉武药科技有限公司 | Ezetimibe orally disintegrating tablet and preparation method thereof |
| CN106880612A (en) * | 2017-02-14 | 2017-06-23 | 万全万特制药（厦门）有限公司 | Ziprasidone HCl oral disintegrating tablet and preparation method thereof |
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2018
- 2018-12-28 CN CN201811626732.6A patent/CN109512790A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101411747A (en) * | 2008-11-25 | 2009-04-22 | 广东药学院 | Salvia root polyphenol acid orally disintegrating tablets and preparation method thereof |
| WO2013161823A1 (en) * | 2012-04-24 | 2013-10-31 | 第一三共株式会社 | Orally disintegrating tablet and method for producing same |
| CN104490833A (en) * | 2014-12-11 | 2015-04-08 | 武汉武药科技有限公司 | Ezetimibe orally disintegrating tablet and preparation method thereof |
| CN106880612A (en) * | 2017-02-14 | 2017-06-23 | 万全万特制药（厦门）有限公司 | Ziprasidone HCl oral disintegrating tablet and preparation method thereof |
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