CN105687152B - 一种法匹拉韦快速释放药物制剂及制备方法 - Google Patents
一种法匹拉韦快速释放药物制剂及制备方法 Download PDFInfo
- Publication number
- CN105687152B CN105687152B CN201610163419.8A CN201610163419A CN105687152B CN 105687152 B CN105687152 B CN 105687152B CN 201610163419 A CN201610163419 A CN 201610163419A CN 105687152 B CN105687152 B CN 105687152B
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- favipiravir
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- solubilizer
- quick
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- ZCGNOVWYSGBHAU-UHFFFAOYSA-N favipiravir Chemical compound NC(=O)C1=NC(F)=CNC1=O ZCGNOVWYSGBHAU-UHFFFAOYSA-N 0.000 title claims abstract description 46
- 229950008454 favipiravir Drugs 0.000 title claims abstract description 44
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 12
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 12
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 12
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 12
- 239000002904 solvent Substances 0.000 claims abstract description 11
- 239000000314 lubricant Substances 0.000 claims abstract description 8
- 239000000463 material Substances 0.000 claims abstract description 8
- 238000002156 mixing Methods 0.000 claims description 19
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 10
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 9
- 239000002245 particle Substances 0.000 claims description 9
- 239000000741 silica gel Substances 0.000 claims description 9
- 229910002027 silica gel Inorganic materials 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 8
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 7
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 7
- 239000011248 coating agent Substances 0.000 claims description 6
- 238000000576 coating method Methods 0.000 claims description 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 6
- 238000007873 sieving Methods 0.000 claims description 6
- 229960000913 crospovidone Drugs 0.000 claims description 5
- 229940069328 povidone Drugs 0.000 claims description 5
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 4
- 235000021355 Stearic acid Nutrition 0.000 claims description 4
- 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 4
- 239000000203 mixture Substances 0.000 claims description 4
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical group CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 4
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 4
- 229960000502 poloxamer Drugs 0.000 claims description 4
- 229920001983 poloxamer Polymers 0.000 claims description 4
- 239000008117 stearic acid Substances 0.000 claims description 4
- 239000007884 disintegrant Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 abstract description 11
- 239000003795 chemical substances by application Substances 0.000 abstract description 3
- 239000003826 tablet Substances 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 7
- 239000003814 drug Substances 0.000 description 7
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 5
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 5
- 229920002785 Croscarmellose sodium Polymers 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 4
- 238000010298 pulverizing process Methods 0.000 description 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
- 229920002472 Starch Polymers 0.000 description 3
- 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 description 3
- 229960001681 croscarmellose sodium Drugs 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 235000015424 sodium Nutrition 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 229940083575 sodium dodecyl sulfate Drugs 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 229940068968 polysorbate 80 Drugs 0.000 description 2
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- ANRFTTXEGCYVMQ-UHFFFAOYSA-L C(C=CC(=O)[O-])(=O)[O-].[Na+].C(CCCCCCCCCCCCCCCCC)(=O)O.[Na+] Chemical compound C(C=CC(=O)[O-])(=O)[O-].[Na+].C(CCCCCCCCCCCCCCCCC)(=O)O.[Na+] ANRFTTXEGCYVMQ-UHFFFAOYSA-L 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
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 239000007948 fast release tablet Substances 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229950008882 polysorbate Drugs 0.000 description 1
- 102220076495 rs200649587 Human genes 0.000 description 1
- 102220043159 rs587780996 Human genes 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 239000002699 waste material Substances 0.000 description 1
- 238000005550 wet granulation Methods 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
实施例1 | 实施例2 | 实施例3 | 实施例4 | 对比实验1 | 对比实验2 | |
15分钟单点溶出量 | 99.9% | 99.7% | 100.2% | 100.1% | 91.1% | 85.6% |
崩解时限 | 1min | 1min | 1min | 1min | 5min | 6min |
Claims (2)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201610163419.8A CN105687152B (zh) | 2016-03-22 | 2016-03-22 | 一种法匹拉韦快速释放药物制剂及制备方法 |
Applications Claiming Priority (1)
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---|---|---|---|
CN201610163419.8A CN105687152B (zh) | 2016-03-22 | 2016-03-22 | 一种法匹拉韦快速释放药物制剂及制备方法 |
Publications (2)
Publication Number | Publication Date |
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CN105687152A CN105687152A (zh) | 2016-06-22 |
CN105687152B true CN105687152B (zh) | 2020-04-07 |
Family
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CN201610163419.8A Active CN105687152B (zh) | 2016-03-22 | 2016-03-22 | 一种法匹拉韦快速释放药物制剂及制备方法 |
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CN (1) | CN105687152B (zh) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109125271A (zh) * | 2017-06-27 | 2019-01-04 | 北京阜康仁生物制药科技有限公司 | 一种使用流化床制备含有法匹拉韦中间体颗粒的方法 |
CN116898979A (zh) * | 2020-02-01 | 2023-10-20 | 北京四环制药有限公司 | 一种含有法匹拉韦的药物组合物及其制备方法和其应用 |
CN111450063B (zh) * | 2020-04-09 | 2021-10-15 | 广州帝奇医药技术有限公司 | 一种法匹拉韦颗粒制剂及其制备方法 |
RU2731932C1 (ru) * | 2020-05-07 | 2020-09-09 | Общество с ограниченной ответственностью "Кромис" (ООО "Кромис") | Противо-COVID-19 (SARS-CoV-2) вирусная фармацевтическая композиция |
RU2764444C1 (ru) * | 2020-09-07 | 2022-01-17 | Общество с ограниченной ответственностью "Кромис", (ООО "Кромис") | Противо-SARS-CoV-2 вирусная фармацевтическая композиция и ее применение |
WO2021225468A1 (ru) * | 2020-05-07 | 2021-11-11 | Общество с ограниченной ответственностью "Кромис" (ООО "Кромис") | Противо-sars-cov-2 вирусная фармацевтическая композиция и ее применение |
WO2021225467A1 (ru) * | 2020-05-07 | 2021-11-11 | Общество с ограниченной ответственностью "Кромис" (ООО "Кромис") | Пpotиbo-sars-cov-2 вирусная фармацевтическая композиция и ее применение |
RU2751108C1 (ru) * | 2020-06-15 | 2021-07-08 | Общество С Ограниченной Ответственностью "Промомед Рус" | Противовирусная композиция |
CN115551484A (zh) * | 2020-06-19 | 2022-12-30 | 浙江华海药业股份有限公司 | 一种法匹拉韦组合物及其制备方法 |
CN112294818B (zh) * | 2020-10-28 | 2021-08-31 | 浙江海正药业股份有限公司 | 一种快速溶出的法维拉韦药物组合物及制备方法 |
WO2022115055A1 (en) * | 2020-11-27 | 2022-06-02 | Santa Farma Ilac Sanayii A.S. | Immediate release composition of favipiravir |
CN114159400A (zh) * | 2021-11-22 | 2022-03-11 | 山东省药学科学院 | 法匹拉韦包芯片 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102348458A (zh) * | 2009-03-13 | 2012-02-08 | 富山化学工业株式会社 | 含有6-氟-3-羟基-2-吡嗪甲酰胺的片剂和粒状粉剂 |
CN104288154A (zh) * | 2014-09-29 | 2015-01-21 | 成都新恒创药业有限公司 | 一种含有不同粒径范围的法匹拉韦药物组合物 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CZ301763B6 (cs) * | 1998-08-20 | 2010-06-16 | Toyama Chemical Co., Ltd. | Protivirový prostredek a derivát dusíkatého heterocyklického karboxamidu |
-
2016
- 2016-03-22 CN CN201610163419.8A patent/CN105687152B/zh active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102348458A (zh) * | 2009-03-13 | 2012-02-08 | 富山化学工业株式会社 | 含有6-氟-3-羟基-2-吡嗪甲酰胺的片剂和粒状粉剂 |
CN104288154A (zh) * | 2014-09-29 | 2015-01-21 | 成都新恒创药业有限公司 | 一种含有不同粒径范围的法匹拉韦药物组合物 |
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Denomination of invention: The invention relates to a rapid release drug preparation of fapiravir and a preparation method thereof Effective date of registration: 20211217 Granted publication date: 20200407 Pledgee: Shandong Linzi Rural Commercial Bank Co.,Ltd. Pledgor: SHANDONG QIDU PHARMACEUTICAL Co.,Ltd. Registration number: Y2021980015391 |
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Denomination of invention: A Rapid Release Drug Formulation and Preparation Method of Fapiravir Effective date of registration: 20231206 Granted publication date: 20200407 Pledgee: Shandong Linzi Rural Commercial Bank Co.,Ltd. Pledgor: SHANDONG QIDU PHARMACEUTICAL Co.,Ltd. Registration number: Y2023980069709 |
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PC01 | Cancellation of the registration of the contract for pledge of patent right | ||
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Granted publication date: 20200407 Pledgee: Shandong Linzi Rural Commercial Bank Co.,Ltd. Pledgor: SHANDONG QIDU PHARMACEUTICAL Co.,Ltd. Registration number: Y2023980069709 |