DK2729128T3 - Darunavir-formuleringer - Google Patents
Darunavir-formuleringer Download PDFInfo
- Publication number
- DK2729128T3 DK2729128T3 DK12732668.4T DK12732668T DK2729128T3 DK 2729128 T3 DK2729128 T3 DK 2729128T3 DK 12732668 T DK12732668 T DK 12732668T DK 2729128 T3 DK2729128 T3 DK 2729128T3
- Authority
- DK
- Denmark
- Prior art keywords
- darunavir
- dosage form
- oral dosage
- hypromellose
- mixture
- Prior art date
Links
Classifications
-
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/141—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
- A61K9/145—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 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- 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
-
- 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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
-
- 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
- A61K9/20—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
- 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
- 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
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Claims (10)
1. Darunavir-granulatsammensætning, der består af darunavir eller et farmaceutisk acceptabelt salt eller solvat deraf, hypromellose og eventuelt resterende vand fra granuleringen.
2. Darunavir-granulatsammensætning ifølge krav 1, hvor darunavir er til stede i form af dets ethanolat og hypromellose er hypromellose 2910 15 mPa.s.
3. Oral doseringsform, der omfatter ca. 0,4 til 0,6 vægt-% (vægt/vægt) af et smøremiddel, ca. 2 til 4 vægt-% (vægt/vægt) af et opløsningsmiddel, mikrokrystallinsk cellulose og ca. 50 til 90 vægt-% (vægt/vægt) af et darunavir-granulat ifølge krav 1 eller 2, hvor kernen eventuelt er overtrukket med en film.
4. Oral doseringsform ifølge krav 3, hvor kernen yderligere omfatter en ekstra aktiv bestanddel.
5. Oral doseringsform ifølge krav 4, hvor den ekstra aktive bestanddel er en cytochrom P450-inhibitor.
6. Oral doseringsform ifølge et hvilket som helst af ovennævnte krav, der omfatter ca. 0,5 vægt-% (vægt/vægt) af et smøremiddel
7. Oral doseringsform ifølge krav 6, der omfatter ca. 800 mg fri form-ækvivalent af darunavir.
8. Fremgangsmåde til fremstilling af en oral doseringsform ifølge et hvilket som helst af ovennævnte krav, der omfatter trinene: - tilvejebringelse af granuleret darunavir ved; blanding af vand og hypromellose 2910 15 mPa.s, sprøjtning af denne første blanding på et pulver af darunavir eller et farmaceutisk acceptabelt salt eller solvat deraf og tørring af det således opnåede darunavir-granulat, tilvejebringelse af en anden blanding, der omfatter mikrokrystallinsk cellulose og et opløsningsmiddel, tilsætning af granuleret darunavir til blandingen og efterfølgende tørblanding, - tilsætning af et smøremiddel og blanding indtil homogenitet, - komprimering af blandingen til tilvejebringelse af den orale doseringsform, hvilken orale doseringsform herefter eventuelt overtrækkes med en film.
9. Oral doseringsform ifølge et hvilket som helst af kravene 1 til 7 til anvendelse i medicin.
10. Oral doseringsform ifølge et hvilket som helst af kravene 1 til 7 til anvendelse til behandling af HIV-infektion.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11173066 | 2011-07-07 | ||
| PCT/EP2012/063242 WO2013004816A1 (en) | 2011-07-07 | 2012-07-06 | Darunavir formulations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2729128T3 true DK2729128T3 (da) | 2016-11-21 |
Family
ID=46458539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12732668.4T DK2729128T3 (da) | 2011-07-07 | 2012-07-06 | Darunavir-formuleringer |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US20140142174A1 (da) |
| EP (1) | EP2729128B1 (da) |
| JP (1) | JP6101260B2 (da) |
| KR (1) | KR101817991B1 (da) |
| CN (1) | CN103841962B (da) |
| AU (1) | AU2012280277B2 (da) |
| BR (1) | BR112014000195A2 (da) |
| CA (1) | CA2837539C (da) |
| CY (1) | CY1119446T1 (da) |
| DK (1) | DK2729128T3 (da) |
| EA (1) | EA026588B1 (da) |
| ES (1) | ES2598823T3 (da) |
| HR (1) | HRP20161340T1 (da) |
| HU (1) | HUE030341T2 (da) |
| IL (1) | IL229700B (da) |
| LT (1) | LT2729128T (da) |
| MX (1) | MX341976B (da) |
| PL (1) | PL2729128T3 (da) |
| PT (1) | PT2729128T (da) |
| RS (1) | RS55236B1 (da) |
| SI (1) | SI2729128T1 (da) |
| SM (1) | SMT201600380B (da) |
| WO (1) | WO2013004816A1 (da) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014000290B1 (pt) | 2011-07-07 | 2022-05-10 | Gilead Sciences, Inc. | Forma de dosagem oral de combinação de darunavir, processo para preparação de uma forma de dosagem oral e uso de granulado de darunavir |
| CA2918707A1 (en) | 2013-08-29 | 2015-03-05 | Teva Pharmaceuticals Industries Ltd. | Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir and a monolithic tablet comprising darunavir and ritonavir |
| JP5843986B2 (ja) * | 2014-03-25 | 2016-01-13 | アステラス製薬株式会社 | 粒状医薬組成物 |
| EP3129009A1 (en) | 2014-04-08 | 2017-02-15 | Teva Pharmaceutical Industries Ltd | Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir |
| US10512633B2 (en) | 2014-10-26 | 2019-12-24 | King Abdullah University Of Science And Technology | Alkaloids from sponge, scaffolds for the inhibition of human immunodeficiency virus (HIV) |
| WO2019018676A1 (en) | 2017-07-20 | 2019-01-24 | Janssen Sciences Ireland Unlimited Company | COMPOSITIONS COMPRISING DARUNAVIR, COBICISTAT, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE FOR USE IN THE TREATMENT OF HIV |
| WO2020064980A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Sciences Ireland Unlimited Company | Methods of treating and preventing neuropsychiatric and/or neurocognitive complications in patients infected with hiv |
| WO2021180963A1 (en) | 2020-03-13 | 2021-09-16 | Janssen Sciences Ireland Unlimited Company | A protease inhibitor regimen for treating subjects infected with hiv |
| US11311559B2 (en) | 2020-04-20 | 2022-04-26 | Poviva Corp. | Compositions and methods for enhanced delivery of antiviral agents |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5968942A (en) | 1992-08-25 | 1999-10-19 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| DE69415326T2 (de) | 1993-08-24 | 1999-06-02 | Searle & Co | Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen |
| EP2336134B1 (en) | 1998-06-23 | 2016-08-31 | The United States of America, represented by the Secretary, Department of Health and Human Services | Fitness assay and methods for reducing resistance of HIV to therapy |
| AR037797A1 (es) | 2001-12-12 | 2004-12-01 | Tibotec Pharm Ltd | Combinacion de inhibidores de proteasa dependientes del citocromo p450 |
| JP2010531301A (ja) * | 2007-06-25 | 2010-09-24 | テイボテク・フアーマシユーチカルズ | ダルナビル及びエトラビリンを含んでなる組み合わせ調剤 |
| AR069539A1 (es) * | 2007-07-25 | 2010-02-03 | Tibotec Pharm Ltd | Avances respecto de las formulaciones de comprimidos contra el vih |
| GT200800303A (es) * | 2007-12-24 | 2009-09-18 | Combinacion anti-retroviral | |
| EP2477992B1 (en) * | 2009-09-17 | 2016-12-14 | Mylan Laboratories Limited | Processes for the preparation of darunavir and the amorphous form thereof |
-
2012
- 2012-07-06 CA CA2837539A patent/CA2837539C/en active Active
- 2012-07-06 EA EA201490223A patent/EA026588B1/ru unknown
- 2012-07-06 PT PT127326684T patent/PT2729128T/pt unknown
- 2012-07-06 CN CN201280033515.0A patent/CN103841962B/zh active Active
- 2012-07-06 BR BR112014000195A patent/BR112014000195A2/pt not_active Application Discontinuation
- 2012-07-06 US US14/131,272 patent/US20140142174A1/en not_active Abandoned
- 2012-07-06 PL PL12732668T patent/PL2729128T3/pl unknown
- 2012-07-06 MX MX2013015196A patent/MX341976B/es active IP Right Grant
- 2012-07-06 DK DK12732668.4T patent/DK2729128T3/da active
- 2012-07-06 LT LTEP12732668.4T patent/LT2729128T/lt unknown
- 2012-07-06 ES ES12732668.4T patent/ES2598823T3/es active Active
- 2012-07-06 HU HUE12732668A patent/HUE030341T2/en unknown
- 2012-07-06 AU AU2012280277A patent/AU2012280277B2/en active Active
- 2012-07-06 KR KR1020147000084A patent/KR101817991B1/ko active IP Right Grant
- 2012-07-06 WO PCT/EP2012/063242 patent/WO2013004816A1/en active Application Filing
- 2012-07-06 JP JP2014517820A patent/JP6101260B2/ja active Active
- 2012-07-06 RS RS20160872A patent/RS55236B1/sr unknown
- 2012-07-06 SI SI201230742A patent/SI2729128T1/sl unknown
- 2012-07-06 EP EP12732668.4A patent/EP2729128B1/en active Active
-
2013
- 2013-11-28 IL IL229700A patent/IL229700B/en active IP Right Grant
-
2016
- 2016-01-07 US US14/990,621 patent/US20160113949A1/en not_active Abandoned
- 2016-10-13 HR HRP20161340TT patent/HRP20161340T1/hr unknown
- 2016-10-25 CY CY20161101073T patent/CY1119446T1/el unknown
- 2016-10-26 SM SM201600380T patent/SMT201600380B/it unknown
-
2021
- 2021-04-27 US US17/242,218 patent/US20210244749A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HUE030341T2 (en) | 2017-05-29 |
| US20210244749A1 (en) | 2021-08-12 |
| CY1119446T1 (el) | 2018-04-04 |
| ES2598823T3 (es) | 2017-01-30 |
| RS55236B1 (sr) | 2017-02-28 |
| IL229700B (en) | 2018-04-30 |
| AU2012280277B2 (en) | 2017-02-09 |
| EP2729128A1 (en) | 2014-05-14 |
| CN103841962B (zh) | 2016-08-17 |
| KR20140068844A (ko) | 2014-06-09 |
| EP2729128B1 (en) | 2016-07-27 |
| SI2729128T1 (sl) | 2016-11-30 |
| JP6101260B2 (ja) | 2017-03-22 |
| LT2729128T (lt) | 2016-11-10 |
| WO2013004816A1 (en) | 2013-01-10 |
| PT2729128T (pt) | 2016-09-21 |
| MX341976B (es) | 2016-09-07 |
| CN103841962A (zh) | 2014-06-04 |
| HRP20161340T1 (hr) | 2016-12-02 |
| IL229700A0 (en) | 2014-01-30 |
| PL2729128T3 (pl) | 2017-05-31 |
| SMT201600380B (it) | 2017-01-10 |
| MX2013015196A (es) | 2014-08-18 |
| US20160113949A1 (en) | 2016-04-28 |
| AU2012280277A1 (en) | 2013-12-19 |
| KR101817991B1 (ko) | 2018-01-12 |
| CA2837539A1 (en) | 2013-01-10 |
| US20140142174A1 (en) | 2014-05-22 |
| BR112014000195A2 (pt) | 2017-02-21 |
| CA2837539C (en) | 2021-08-10 |
| EA026588B1 (ru) | 2017-04-28 |
| EA201490223A1 (ru) | 2014-06-30 |
| JP2014520786A (ja) | 2014-08-25 |
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