RU2018123620A - Фармацевтические композиции, содержащие доравирин, тенофовира дизопроксила фумарат и ламивудин - Google Patents
Фармацевтические композиции, содержащие доравирин, тенофовира дизопроксила фумарат и ламивудин Download PDFInfo
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- RU2018123620A RU2018123620A RU2018123620A RU2018123620A RU2018123620A RU 2018123620 A RU2018123620 A RU 2018123620A RU 2018123620 A RU2018123620 A RU 2018123620A RU 2018123620 A RU2018123620 A RU 2018123620A RU 2018123620 A RU2018123620 A RU 2018123620A
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- pharmaceutical composition
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- magnesium stearate
- croscarmellose sodium
- composition according
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- 239000008194 pharmaceutical composition Substances 0.000 title claims 20
- 229960004556 tenofovir Drugs 0.000 title claims 7
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 title claims 7
- VZCYOOQTPOCHFL-OWOJBTEDSA-L fumarate(2-) Chemical compound [O-]C(=O)\C=C\C([O-])=O VZCYOOQTPOCHFL-OWOJBTEDSA-L 0.000 title 1
- SGOIRFVFHAKUTI-ZCFIWIBFSA-N tenofovir (anhydrous) Chemical compound N1=CN=C2N(C[C@@H](C)OCP(O)(O)=O)C=NC2=C1N SGOIRFVFHAKUTI-ZCFIWIBFSA-N 0.000 title 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 34
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 17
- 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 17
- 229960001681 croscarmellose sodium Drugs 0.000 claims 17
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 17
- 235000019359 magnesium stearate Nutrition 0.000 claims 17
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 11
- 239000008108 microcrystalline cellulose Substances 0.000 claims 11
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 11
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 11
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 10
- ZIAOVIPSKUPPQW-UHFFFAOYSA-N 3-chloro-5-[1-[(4-methyl-5-oxo-1h-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)pyridin-3-yl]oxybenzonitrile Chemical group N1C(=O)N(C)C(CN2C(C(OC=3C=C(C=C(Cl)C=3)C#N)=C(C=C2)C(F)(F)F)=O)=N1 ZIAOVIPSKUPPQW-UHFFFAOYSA-N 0.000 claims 9
- 229950003141 doravirine Drugs 0.000 claims 9
- 229960001627 lamivudine Drugs 0.000 claims 9
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 9
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims 9
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 6
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 6
- 239000000314 lubricant Substances 0.000 claims 6
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 5
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 4
- 229920002472 Starch Polymers 0.000 claims 4
- 239000007884 disintegrant Substances 0.000 claims 4
- 239000007888 film coating Substances 0.000 claims 4
- 238000009501 film coating Methods 0.000 claims 4
- 229960001021 lactose monohydrate Drugs 0.000 claims 4
- 229940032147 starch Drugs 0.000 claims 4
- 239000008107 starch Substances 0.000 claims 4
- 235000019698 starch Nutrition 0.000 claims 4
- 239000006185 dispersion Substances 0.000 claims 3
- 239000007941 film coated tablet Substances 0.000 claims 3
- 229960003943 hypromellose Drugs 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000006187 pill Substances 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims 3
- GUBGYTABKSRVRQ-DCSYEGIMSA-N Beta-Lactose 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-DCSYEGIMSA-N 0.000 claims 2
- 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 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 2
- 235000021355 Stearic acid Nutrition 0.000 claims 2
- 229960004977 anhydrous lactose Drugs 0.000 claims 2
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 2
- 229960003563 calcium carbonate Drugs 0.000 claims 2
- 235000010216 calcium carbonate Nutrition 0.000 claims 2
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 2
- 229960000913 crospovidone Drugs 0.000 claims 2
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 2
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 2
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 2
- 239000001095 magnesium carbonate Substances 0.000 claims 2
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims 2
- 229960001708 magnesium carbonate Drugs 0.000 claims 2
- 235000014380 magnesium carbonate Nutrition 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 229960001855 mannitol Drugs 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 239000000377 silicon dioxide Substances 0.000 claims 2
- 235000012239 silicon dioxide Nutrition 0.000 claims 2
- 229960001866 silicon dioxide Drugs 0.000 claims 2
- 229920003109 sodium starch glycolate Polymers 0.000 claims 2
- 229940079832 sodium starch glycolate Drugs 0.000 claims 2
- 239000008109 sodium starch glycolate Substances 0.000 claims 2
- 239000008117 stearic acid Substances 0.000 claims 2
- 239000000454 talc Substances 0.000 claims 2
- 229910052623 talc Inorganic materials 0.000 claims 2
- 229940033134 talc Drugs 0.000 claims 2
- 235000012222 talc Nutrition 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000004203 carnauba wax Substances 0.000 claims 1
- 235000013869 carnauba wax Nutrition 0.000 claims 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 1
- 230000003179 granulation Effects 0.000 claims 1
- 238000005469 granulation Methods 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 229960002900 methylcellulose Drugs 0.000 claims 1
- 238000005498 polishing Methods 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
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- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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Claims (22)
1. Фармацевтическая композиция, которая представляет собой двухслойную таблетку, содержащую аморфный дисперсионный состав доравирина в первом слое и ламивудин и тенофовира дизопроксила фумарат во втором слое.
2. Фармацевтическая композиция по п. 1, в которой аморфный дисперсионный состав доравирина содержит доравирин и полимер.
3. Фармацевтическая композиция по п. 2, в которой полимер выбран из группы, состоящей из ацетосукцината гидроксипропилметилцеллюлозы, фталата гидроксипропилметилцеллюлозы, ацетофталата целлюлозы, ацетотримеллитата целлюлозы, ацетофталата метилцеллюлозы, ацетофталата гидроксипропилцеллюлозы, ацетотерефталата целлюлозы, ацетоизофталата целлюлозы, поливинилпирролидинона и сополимеров поливинилпирролидинона и поливинилацетата.
4. Фармацевтическая композиция по п. 3, в которой полимер представляет собой ацетосукцинат гидроксипропилметилцеллюлозы.
5. Фармацевтическая композиция по п. 1, в которой первый слой содержит аморфный дисперсионный состав доравирина, вещество, обеспечивающее скольжение, разбавители, разрыхлители и смазывающие вещества.
6. Фармацевтическая композиция по п. 5, в которой первый слой содержит вещество, обеспечивающее скольжение, которое выбран из группы, состоящей из коллоидного диоксида кремния, диоксида кремния, талька и крахмала; разбавители, которые являются выбранными из группы, состоящей из лактозы, безводной лактозы, моногидрата лактозы, маннита, микрокристаллической целлюлозы, двухосновного фосфата кальция, карбоната кальция и карбоната магния; разрыхлители, которые являются выбранными из группы, состоящей из кроскармеллозы натрия, крахмала, кросповидона и крахмал-гликолята натрия; и смазывающие вещества, которые являются выбранными из группы, состоящей из стеарата магния, стеариновой кислоты или стеарилфумарата натрия.
7. Фармацевтическая композиция по п. 6, в которой первый слой содержит вещество, обеспечивающее скольжение, которое представляет собой коллоидный диоксид кремния; разбавитель, который представляет собой микрокристаллическую целлюлозу; разрыхлитель, который представляет собой кроскармеллозу натрия; и смазывающее вещество, которое представляет собой стеарат магния.
8. Фармацевтическая композиция по п. 1, в которой второй слой содержит ламивудин, тенофовира дизопроксила фумарат, вещество, обеспечивающее скольжение, разбавители, разрыхлители и смазывающие вещества.
9. Фармацевтическая композиция по п. 8, в которой второй слой содержит вещество, обеспечивающее скольжение, которое является выбранным из группы, состоящей из коллоидного диоксида кремния, диоксида кремния, талька и крахмала; разбавители, которые являются выбранными из группы, состоящей из лактозы, безводной лактозы, моногидрата лактозы, маннита, микрокристаллической целлюлозы, двухосновного фосфата кальция, карбоната кальция и карбоната магния; разрыхлители, которые являются выбранными из группы, состоящей из кроскармеллозы натрия, крахмала, кросповидона и крахмал-гликолята натрия; смазывающие вещества, которые являются выбранными из группы, состоящей из стеарата магния, стеариновой кислоты и стеарилфумарата натрия.
10. Фармацевтическая композиция по п. 9, в которой второй слой содержит вещество, обеспечивающее скольжение, которое представляет собой коллоидный диоксид кремния; разбавитель, который представляет собой микрокристаллическую целлюлозу; разрыхлитель, который представляет собой кроскармеллозу натрия; и смазывающие вещества, которые представляют собой стеарат магния и стеарилфумарат натрия.
11. Фармацевтическая композиция по п. 1, в которой ламивудин и тенофовира дизопроксила фумарат подвергаются совместному гранулированию.
12. Фармацевтическая композиция по п. 1, в которой ламивудин и тенофовира дизопроксила фумарат подвергаются гранулированию по отдельности.
13. Фармацевтическая композиция по п. 1, содержащая пленочное покрытие.
14. Фармацевтическая композиция по п. 1, содержащая добавку для полировки.
15. Фармацевтическая композиция по п. 1, содержащая 50 мг доравирина, 150 мг ламивудина и 150 мг тенофовира дизопроксила фумарата.
16. Фармацевтическая композиция по п. 1, содержащая 100 мг доравирина, 300 мг ламивудина и 300 мг тенофовира дизопроксила фумарата.
17. Фармацевтическая композиция по п. 1, содержащая:
[мг]
18. Фармацевтическая композиция по п. 1, содержащая:
[мг]
19. Фармацевтическая композиция по п. 1, содержащая:
[мг]
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| US62/261,953 | 2015-12-02 | ||
| PCT/US2016/063894 WO2017095761A1 (en) | 2015-12-02 | 2016-11-29 | Pharmaceutical compositions containing doravirine, tenofovir disoproxil fumarate and lamivudine |
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| CN110769856A (zh) * | 2017-04-18 | 2020-02-07 | 希普拉有限公司 | 用于治疗逆转录病毒感染的组合疗法 |
| BR112020015759A2 (pt) * | 2018-02-02 | 2020-12-08 | Genentech, Inc. | Composto farmacêutico, sais do mesmo, formulações do mesmo e métodos para produzir e usar o mesmo |
| CN113288905A (zh) * | 2021-07-14 | 2021-08-24 | 石家庄龙泽制药股份有限公司 | 含多替拉韦钠、拉米夫定和富马酸诺福韦酯的药物组合物 |
| CN115554248B (zh) * | 2022-08-25 | 2023-09-22 | 平阳润德医院有限公司 | 一种治疗小儿巨细胞病毒感染性肝炎的肠溶型中药制剂及其制备方法 |
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| US5922695A (en) | 1996-07-26 | 1999-07-13 | Gilead Sciences, Inc. | Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability |
| DE602006015721D1 (de) * | 2005-12-14 | 2010-09-02 | Cipla Ltd | Pharmazeutische kombination aus nucleotid und nucleosid-reverse-transkriptase-hemmern (wie tenofovir und lamivudin) in verschiedenen teilen der dosiereinheit |
| JP2010529196A (ja) * | 2007-06-12 | 2010-08-26 | コンサート ファーマシューティカルズ インコーポレイテッド | アザペプチド誘導体 |
| WO2009106960A2 (en) * | 2008-02-27 | 2009-09-03 | Aurobindo Pharma Limited | Stable compositions of lamivudine, tenofovir and efavirenz |
| EP2295038B1 (en) | 2009-09-11 | 2013-05-29 | AiCuris GmbH & Co. KG | Solid dispersion comprising an anti-HIV agent |
| RS54017B1 (sr) | 2010-03-30 | 2015-10-30 | Merck Canada Inc. | Ne-nukleozidni inhibitori reverzne transkriptaze |
| WO2012164241A1 (en) * | 2011-05-30 | 2012-12-06 | Cipla Limited | Pharmaceutical antiretroviral composition |
| EP2958563A2 (en) | 2013-02-20 | 2015-12-30 | AbbVie Inc. | Tablet dosage form comprising ritonavir and lopinavir |
| MX375870B (es) * | 2013-11-22 | 2025-03-07 | Merck Sharp & Dohme Llc | Composicion de un inhibidor de la transcriptasa inversa sin nucleosido. |
| WO2015179448A1 (en) * | 2014-05-21 | 2015-11-26 | Gilead Sciences, Inc. | Therapeutic compounds |
| DK3383397T3 (da) * | 2015-12-02 | 2021-11-08 | Merck Sharp & Dohme | Farmaceutiske sammensætninger indeholdende doravirin, tenofovirdisoproxilfumarat og lamivudin |
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