HRP20151357T1 - Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa - Google Patents
Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa Download PDFInfo
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- HRP20151357T1 HRP20151357T1 HRP20151357TT HRP20151357T HRP20151357T1 HR P20151357 T1 HRP20151357 T1 HR P20151357T1 HR P20151357T T HRP20151357T T HR P20151357TT HR P20151357 T HRP20151357 T HR P20151357T HR P20151357 T1 HRP20151357 T1 HR P20151357T1
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- particles
- pharmaceutical composition
- compound
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- 239000002245 particle Substances 0.000 title claims 13
- 239000007787 solid Substances 0.000 title claims 8
- 239000008177 pharmaceutical agent Substances 0.000 title 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 9
- 239000000377 silicon dioxide Substances 0.000 claims 6
- 239000011148 porous material Substances 0.000 claims 4
- 235000012239 silicon dioxide Nutrition 0.000 claims 4
- 208000036142 Viral infection Diseases 0.000 claims 2
- 229910002011 hydrophilic fumed silica Inorganic materials 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- XQSPYNMVSIKCOC-NTSWFWBYSA-N Emtricitabine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1 XQSPYNMVSIKCOC-NTSWFWBYSA-N 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 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 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- JUZYLCPPVHEVSV-LJQANCHMSA-N elvitegravir Chemical compound COC1=CC=2N([C@H](CO)C(C)C)C=C(C(O)=O)C(=O)C=2C=C1CC1=CC=CC(Cl)=C1F JUZYLCPPVHEVSV-LJQANCHMSA-N 0.000 claims 1
- 229960003586 elvitegravir Drugs 0.000 claims 1
- 229960000366 emtricitabine Drugs 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims 1
- 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 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Classifications
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- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Plant Substances (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (22)
1. Kompozicija se sastoji od mnoštva čestica čvrstog nosača gdje svaka od njih sadrži silicij dioksid i gdje svaka ima površinu i/ili pore; i spoj formule (I):
[image]
ili njegovu farmaceutski prihvatljivu sol u porama ili na površini čestica čvrstog nosača.
2. Kompozicija prema patentnom zahtjevu 1 gdje čestice silicij dioksida imaju srednju vrijednost presjeka čestica od 10 do 120 mikrona i BET površinu od 40 do 400 m2/g.
3. Kompozicija prema patentnom zahtjevu 2 gdje su čestice silicij dioksida hidrofilna pirogena silika .
4. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 3 gdje postotak težine spoja u formuli (I) iznosi do 50% ± 10% čestica čvrstog nosača.
5. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 4 gdje spoj formule (I) ima obogaćenu koncentraciju od 99 ± 1% stereoizomera formule (Ia):
[image]
6. Metoda sadrži kombinirani spoj formule (I):
[image]
odgovarajućeg rastvarača, i mnoštva čestica čvrstog nosača od kojih svaka sadrži silicij dioksid kako bi se dobila mješavina.
7. Tableta sadrži: 1) spoj formule (I):
[image]
ili njegovu farmaceutski prihvatljivu sol i 2) mnoštvo čestica čvrstog nosača od kojih svaka sadrži silicij dioksid.
8. Tableta prema patentnom zahtjevu 7 gdje mnoštvo čestica čvrstog nosača sadrži mnoštvo silika čestica od kojih svaka ima površinu i pore, i koje imaju srednju vrijednost presjeka čestica 10 do 120 μm i BET površinu od 40 do 400 m2/g.
9. Tableta prema patentnim zahtjevima 7 ili 8 koja dalje sadrži drugi terapeutski agens.
10. Tableta prema patentnom zahtjevu 7 koja dalje sadrži 3) mikrokristalnu celulozu; 4) hidroksipropil celulozu; 5) natrij kroskarmelozu; i 6) magnezij stearat.
11. Tableta prema bilo kojem od patentnih zahtjeva od 7 do 10 gdje spoj formule (I) ima obogaćenu koncentraciju od 99 ± 1% stereoizomera formule (Ia):
[image]
12. Farmaceutska kompozicija sadrži kvaternarnu kombinaciju spoja formule (Ia)/tenofovir disoproksil fumarat/emtricitabin/elvitegravir, i mnoštvo čestica čvrstog nosača od kojih svaka sadrži silicij dioksid, gdje je spoj formule (Ia):
[image]
13. Farmaceutska kompozicija prema patentnom zahtjevu 12 gdje čestice silicij dioksida imaju srednju vrijednost presjeka čestica od 10 do 120 μm i BET površinu od 40 to 400 m2/g.
14. Farmaceutska kompozicija prema patentnom zahtjevu 13 gdje su čestice silicij dioksida hidrofilna pirogena silika.
15. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 14 gdje čestice silicij dioksida imaju srednju vrijednost presjeka zrna od 20 do 40 μm.
16. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 15 gdje čestice silicij dioksida imaju BET površinu od najmanje 150 m2/g.
17. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 16 gdje je spoj formule (Ia) obloženo u porama i na površini čestica silicij dioksida.
18. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 17 gdje odnos težine spoja formule (Ia) do težine čestica silicij dioksida iznosi 1 ± 0.05%.
19. Farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 13 do 18 koja je formulirana kao tableta.
20. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 5, tableta prema bilo kojem od patentnih zahtjeva od 7 do 11, ili farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 19 za upotrebu pri medicinskoj terapiji.
21. Kompozicija prema bilo kojem od patentnih zahtjeva od 1 do 5, tableta prema bilo kojem od patentnih zahtjeva od 7 do 11, ili farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva od 12 do 19 za upotrebu u liječenju virusnih infekcija.
22. Kompozicija za upotrebu kako je naznačeno u patentnom zahtjevu 21, ili tableta za upotrebu kako je naznačeno u patentnom zahtjevu 21, ili farmaceutska kompozicija za upotrebu kako je naznačeno u patentnom zahtjevu 21, gdje je virusna infekcija HIV.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US4993508P | 2008-05-02 | 2008-05-02 | |
US15065209P | 2009-02-06 | 2009-02-06 | |
US15065509P | 2009-02-06 | 2009-02-06 | |
PCT/US2009/042607 WO2009135179A2 (en) | 2008-05-02 | 2009-05-01 | The use of solid carrier particles to improve the processability of a pharmaceutical agent |
EP09739981.0A EP2296633B1 (en) | 2008-05-02 | 2009-05-01 | The use of solid carrier particles to improve the processability of a pharmaceutical agent |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20151357T1 true HRP20151357T1 (hr) | 2016-01-29 |
Family
ID=40809930
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20151357TT HRP20151357T1 (hr) | 2008-05-02 | 2015-12-09 | Upotreba äśestica äśvrstog nosaäśa kako bi se poboljšala procesabilnost farmaceutskog agensa |
Country Status (27)
Country | Link |
---|---|
US (1) | US10039718B2 (hr) |
EP (2) | EP3006032A1 (hr) |
JP (2) | JP5722213B2 (hr) |
KR (2) | KR101784647B1 (hr) |
CN (3) | CN102123700A (hr) |
AP (1) | AP3089A (hr) |
AU (3) | AU2009242451C1 (hr) |
BR (1) | BRPI0911871A8 (hr) |
CA (1) | CA2720856C (hr) |
CO (1) | CO6321225A2 (hr) |
CY (1) | CY1117067T1 (hr) |
DK (1) | DK2296633T3 (hr) |
EA (2) | EA201591353A1 (hr) |
EC (1) | ECSP10010636A (hr) |
ES (1) | ES2553897T3 (hr) |
HK (2) | HK1153670A1 (hr) |
HR (1) | HRP20151357T1 (hr) |
HU (1) | HUE026380T2 (hr) |
IL (2) | IL208614A (hr) |
MX (2) | MX2010011963A (hr) |
NZ (1) | NZ588978A (hr) |
PL (1) | PL2296633T3 (hr) |
PT (1) | PT2296633E (hr) |
SG (2) | SG190618A1 (hr) |
SI (1) | SI2296633T1 (hr) |
WO (1) | WO2009135179A2 (hr) |
ZA (1) | ZA201008007B (hr) |
Families Citing this family (28)
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EP2049506B2 (en) | 2006-07-07 | 2024-05-08 | Gilead Sciences, Inc. | Modulators of pharmacokinetic properties of therapeutics |
LT2487166T (lt) * | 2007-02-23 | 2016-11-10 | Gilead Sciences, Inc. | Terapinių agentų farmakokinetinių savybių moduliatoriai |
WO2009006203A1 (en) * | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
JP5547066B2 (ja) * | 2007-06-29 | 2014-07-09 | ギリアード サイエンシーズ, インコーポレイテッド | 治療用組成物およびその使用 |
SG190618A1 (en) | 2008-05-02 | 2013-06-28 | Gilead Sciences Inc | The use of solid carrier particles to improve the processability of a pharmaceutical agent |
UA108738C2 (uk) | 2009-04-03 | 2015-06-10 | Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки | |
ME01980B (me) | 2010-11-19 | 2015-05-20 | Gilead Sciences Inc | Terapeutske kompozicije koje sadrže rilpivirin hcl i tenofovir dizoproksil fumarat |
EP2705027B1 (en) | 2011-05-02 | 2015-06-03 | Gilead Sciences, Inc. | Amorphous solid salts of Cobicistat (GS-9350) |
ES2651212T3 (es) * | 2011-07-07 | 2018-01-25 | Janssen Sciences Ireland Uc | Formulaciones combinadas de darunavir |
US8754065B2 (en) | 2011-08-16 | 2014-06-17 | Gilead Sciences, Inc. | Tenofovir alafenamide hemifumarate |
WO2013106732A1 (en) | 2012-01-12 | 2013-07-18 | Gilead Sciences, Inc. | Pharmaceutical compositions and methods for their preparation |
KR20140128392A (ko) | 2012-02-03 | 2014-11-05 | 길리애드 사이언시즈, 인코포레이티드 | 제약 작용제를 제조하기 위한 방법 및 중간체 |
EP2819644A1 (en) | 2012-03-01 | 2015-01-07 | Gilead Sciences, Inc. | Spray dried formulations |
JP2015534973A (ja) | 2012-10-23 | 2015-12-07 | シプラ・リミテッド | 抗レトロウイルス医薬組成物 |
WO2014105777A1 (en) | 2012-12-26 | 2014-07-03 | Assia Chemical Industries Ltd. | Cobicostat dichlohydrate salt |
DE102013205347A1 (de) * | 2013-03-26 | 2014-10-02 | Hilti Aktiengesellschaft | Additiv-Zusammensetzung für Amin-Härter, deren Verwendung sowie diese enthaltende Amin-Härterzusammensetzung |
CN103230403A (zh) * | 2013-04-23 | 2013-08-07 | 苏州谷力生物科技有限公司 | 一种抗艾滋病毒的组合型药物片剂 |
AU2014356067A1 (en) | 2013-11-29 | 2016-06-16 | Mylan Laboratories Ltd. | Amorphous cobicistat solid dispersion |
WO2015145324A1 (en) * | 2014-03-25 | 2015-10-01 | Mylan Laboratories Ltd | Process for the preparation of cobicistat |
US20160145344A1 (en) * | 2014-10-20 | 2016-05-26 | University Of Southern California | Murine and human innate lymphoid cells and lung inflammation |
US10166185B2 (en) * | 2015-06-09 | 2019-01-01 | J. Rettenmaier & Söhne Gmbh + Co Kg | Excipient and oral solid dosage forms for oily drugs |
WO2016201119A1 (en) * | 2015-06-09 | 2016-12-15 | J. Rettenmaier & Söhne Gmbh + Co Kg | Excipient and oral solid dosage forms for oily drugs |
TW201728582A (zh) | 2016-01-28 | 2017-08-16 | 基利科學股份有限公司 | 結晶型 |
US20190175511A1 (en) | 2016-08-08 | 2019-06-13 | Hetero Labs Limited | A Multi-Class Anti-Retroviral Composition |
WO2018029561A1 (en) | 2016-08-08 | 2018-02-15 | Hetero Labs Limited | Anti-retroviral compositions |
WO2020122242A1 (ja) * | 2018-12-14 | 2020-06-18 | 富士フイルム株式会社 | 医薬組成物及びその製造方法 |
CN110251476B (zh) * | 2019-08-01 | 2022-08-09 | 海思科制药(眉山)有限公司 | 一种恩曲他滨替诺福韦药物组合物 |
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