CA2777937C - Solid pharmaceutical compositions containing an integrase inhibitor - Google Patents
Solid pharmaceutical compositions containing an integrase inhibitor Download PDFInfo
- Publication number
- CA2777937C CA2777937C CA2777937A CA2777937A CA2777937C CA 2777937 C CA2777937 C CA 2777937C CA 2777937 A CA2777937 A CA 2777937A CA 2777937 A CA2777937 A CA 2777937A CA 2777937 C CA2777937 C CA 2777937C
- Authority
- CA
- Canada
- Prior art keywords
- range
- amount
- employed
- superdisintegrant
- compressed tablet
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- 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
- A61K9/2004—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
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
- A61J3/10—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
-
- 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
-
- 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
- A61K9/2013—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
- A61K9/2095—Tabletting processes
-
- 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
- A61K2121/00—Preparations for use in therapy
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25486909P | 2009-10-26 | 2009-10-26 | |
| US61/254,869 | 2009-10-26 | ||
| PCT/US2010/053507 WO2011053504A1 (en) | 2009-10-26 | 2010-10-21 | Solid pharmaceutical compositions containing an integrase inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2777937A1 CA2777937A1 (en) | 2011-05-05 |
| CA2777937C true CA2777937C (en) | 2017-08-29 |
Family
ID=43922462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2777937A Active CA2777937C (en) | 2009-10-26 | 2010-10-21 | Solid pharmaceutical compositions containing an integrase inhibitor |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US9649311B2 (enExample) |
| EP (2) | EP3970702A1 (enExample) |
| JP (2) | JP6122639B2 (enExample) |
| KR (1) | KR101835893B1 (enExample) |
| CN (2) | CN102655752A (enExample) |
| AU (1) | AU2010313571B2 (enExample) |
| BR (1) | BR112012009857A8 (enExample) |
| CA (1) | CA2777937C (enExample) |
| CO (1) | CO6531485A2 (enExample) |
| CY (1) | CY1124914T1 (enExample) |
| DK (1) | DK2493312T3 (enExample) |
| ES (1) | ES2898348T3 (enExample) |
| HR (1) | HRP20211826T1 (enExample) |
| HU (1) | HUE057248T2 (enExample) |
| IL (1) | IL219369A (enExample) |
| IN (1) | IN2012DN03377A (enExample) |
| LT (1) | LT2493312T (enExample) |
| MX (1) | MX345227B (enExample) |
| MY (1) | MY162494A (enExample) |
| PL (1) | PL2493312T3 (enExample) |
| PT (1) | PT2493312T (enExample) |
| RS (1) | RS62600B1 (enExample) |
| RU (1) | RU2602865C2 (enExample) |
| SI (1) | SI2493312T1 (enExample) |
| WO (1) | WO2011053504A1 (enExample) |
| ZA (1) | ZA201203012B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2010313571B2 (en) | 2009-10-26 | 2014-07-31 | Merck Sharp & Dohme Llc | Solid pharmaceutical compositions containing an integrase inhibitor |
| EP2699094A4 (en) * | 2011-04-22 | 2014-12-17 | Merck Sharp & Dohme | TASTE-MASKED FORMULATIONS BY RALTEGRAVIR |
| US20150166520A1 (en) * | 2012-07-20 | 2015-06-18 | Merck Sharp & Dohme Corp. | Amido-substituted pyrimidinone derivatives useful for the treatment of hiv infection |
| WO2014064711A2 (en) * | 2012-10-22 | 2014-05-01 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
| EP2911674A1 (en) | 2012-10-23 | 2015-09-02 | Cipla Limited | Pharmaceutical antiretroviral composition |
| US20160166529A1 (en) * | 2013-07-11 | 2016-06-16 | Merck Sharp & Dohme Corp. | Formulations for Cathepsin K Inhibitors with Vitamin D |
| CN105237526B (zh) * | 2014-06-20 | 2018-01-23 | 朱靖华 | 一种抗艾滋病毒药物及其制备方法 |
| JP7023054B2 (ja) * | 2017-04-05 | 2022-02-21 | 東和薬品株式会社 | レベチラセタム含有医薬組成物及びその製造方法 |
| CN111615391B (zh) * | 2018-01-19 | 2023-05-30 | 吉利德科学公司 | 比卡格韦的代谢物 |
| US20210290548A1 (en) * | 2018-06-06 | 2021-09-23 | Merck Sharp & Dohme Corp. | Formulations of raltegravir |
| RU2688235C1 (ru) * | 2018-06-19 | 2019-05-21 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" | Фармацевтическая противодиабетическая композиция на основе замещенного тиофенкарбоксилата и способ её получения |
| EP3843706A1 (en) * | 2018-08-31 | 2021-07-07 | OPKO Ireland Global Holdings, Ltd. | Vitamin d pediatric dosage forms, methods of making and using |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9109862D0 (en) | 1991-05-08 | 1991-07-03 | Beecham Lab Sa | Pharmaceutical formulations |
| US6087383A (en) | 1998-01-20 | 2000-07-11 | Bristol-Myers Squibb Company | Bisulfate salt of HIV protease inhibitor |
| GB9922963D0 (en) | 1999-09-28 | 1999-12-01 | Pfizer Ltd | Polymorphic salt |
| FR2795962B1 (fr) * | 1999-07-08 | 2003-05-09 | Prographarm Laboratoires | Procede de fabrication de granules enrobes a gout masque et liberation immediate du principe actif |
| ES2295068T3 (es) | 1999-11-24 | 2008-04-16 | MERCK & CO., INC. | Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih. |
| EP1326865B1 (en) | 2000-10-12 | 2009-05-06 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| CA2463975A1 (en) | 2001-10-26 | 2003-05-01 | Maria Emilia Di Francesco | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| DE122009000048I1 (de) | 2001-10-26 | 2010-04-08 | Angeletti P Ist Richerche Bio | N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase |
| EP1499391A2 (en) | 2002-04-10 | 2005-01-26 | Merck & Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
| WO2004058756A1 (en) | 2002-12-27 | 2004-07-15 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors |
| US20070148232A1 (en) | 2003-12-31 | 2007-06-28 | Pfizer Inc. | Stabilized pharmaceutical solid compositions of low-solubility drugs and poloxamers, and stabilizing polymers |
| US7829720B2 (en) | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
| UA87884C2 (uk) | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| RU2382648C2 (ru) * | 2004-12-03 | 2010-02-27 | Мерк Энд Ко., Инк. | Фармацевтический состав карбоксамидных ингибиторов интегразы вич, содержащий композицию с контролируемой скоростью высвобождения |
| BRPI0518741A2 (pt) | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| EP3165220B2 (en) * | 2004-12-03 | 2024-11-13 | Merck Sharp & Dohme LLC | Pharmaceutical composition containing an anti-nucleating agent |
| WO2007087188A2 (en) * | 2006-01-20 | 2007-08-02 | Merck & Co., Inc. | Taste-masked tablets and granules |
| CA2563690C (en) * | 2006-10-12 | 2014-10-07 | Pharmascience Inc. | Pharmaceutical compositions comprising intra- and extra- granular fractions |
| KR20100033378A (ko) | 2007-06-22 | 2010-03-29 | 브리스톨-마이어스 스큅 컴퍼니 | 아타자나비르를 함유하는 정제 조성물 |
| US7687509B2 (en) * | 2007-07-09 | 2010-03-30 | Concert Pharmaceuticals Inc. | Pyrimidinecarboxamide derivatives |
| US8372431B2 (en) * | 2007-10-26 | 2013-02-12 | Bial-Portela & C.A., S.A. | Pharmaceutical composition comprising licarbazepine acetate |
| AU2010313571B2 (en) * | 2009-10-26 | 2014-07-31 | Merck Sharp & Dohme Llc | Solid pharmaceutical compositions containing an integrase inhibitor |
-
2010
- 2010-10-21 AU AU2010313571A patent/AU2010313571B2/en active Active
- 2010-10-21 BR BR112012009857A patent/BR112012009857A8/pt active IP Right Grant
- 2010-10-21 CN CN2010800593740A patent/CN102655752A/zh active Pending
- 2010-10-21 KR KR1020127013561A patent/KR101835893B1/ko active Active
- 2010-10-21 RS RS20211443A patent/RS62600B1/sr unknown
- 2010-10-21 EP EP21202505.0A patent/EP3970702A1/en active Pending
- 2010-10-21 CN CN201610500807.0A patent/CN106074411A/zh active Pending
- 2010-10-21 DK DK10827338.4T patent/DK2493312T3/da active
- 2010-10-21 US US13/503,939 patent/US9649311B2/en active Active
- 2010-10-21 WO PCT/US2010/053507 patent/WO2011053504A1/en not_active Ceased
- 2010-10-21 MX MX2012004903A patent/MX345227B/es active IP Right Grant
- 2010-10-21 LT LTEPPCT/US2010/053507T patent/LT2493312T/lt unknown
- 2010-10-21 IN IN3377DEN2012 patent/IN2012DN03377A/en unknown
- 2010-10-21 SI SI201032094T patent/SI2493312T1/sl unknown
- 2010-10-21 HU HUE10827338A patent/HUE057248T2/hu unknown
- 2010-10-21 ES ES10827338T patent/ES2898348T3/es active Active
- 2010-10-21 EP EP10827338.4A patent/EP2493312B1/en active Active
- 2010-10-21 PT PT108273384T patent/PT2493312T/pt unknown
- 2010-10-21 JP JP2012535360A patent/JP6122639B2/ja active Active
- 2010-10-21 CA CA2777937A patent/CA2777937C/en active Active
- 2010-10-21 MY MYPI2012001823A patent/MY162494A/en unknown
- 2010-10-21 HR HRP20211826TT patent/HRP20211826T1/hr unknown
- 2010-10-21 RU RU2012121857/15A patent/RU2602865C2/ru active
- 2010-10-21 PL PL10827338T patent/PL2493312T3/pl unknown
-
2012
- 2012-04-23 IL IL219369A patent/IL219369A/en active IP Right Grant
- 2012-04-24 ZA ZA2012/03012A patent/ZA201203012B/en unknown
- 2012-04-26 CO CO12068959A patent/CO6531485A2/es unknown
-
2015
- 2015-09-25 JP JP2015188605A patent/JP2016034962A/ja active Pending
-
2017
- 2017-04-10 US US15/483,030 patent/US10772888B2/en active Active
-
2021
- 2021-12-14 CY CY20211101099T patent/CY1124914T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20151005 |
|
| MPN | Maintenance fee for patent paid |
Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 15TH ANNIV.) - STANDARD Year of fee payment: 15 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20250908 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20250908 |