BR112012009857A8 - Composições farmacêuticas sólidas contendo um inibidor de integrase - Google Patents
Composições farmacêuticas sólidas contendo um inibidor de integraseInfo
- Publication number
- BR112012009857A8 BR112012009857A8 BR112012009857A BR112012009857A BR112012009857A8 BR 112012009857 A8 BR112012009857 A8 BR 112012009857A8 BR 112012009857 A BR112012009857 A BR 112012009857A BR 112012009857 A BR112012009857 A BR 112012009857A BR 112012009857 A8 BR112012009857 A8 BR 112012009857A8
- Authority
- BR
- Brazil
- Prior art keywords
- pharmaceutical compositions
- compositions containing
- solid pharmaceutical
- integrase inhibitor
- tablets
- 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
- A61K31/33—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
- 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
- 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
- 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
- A61K9/2004—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
- 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)
- 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)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Inorganic Chemistry (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Nutrition Science (AREA)
- Physiology (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)
Abstract
COMPOSIÇÕES FARMACÊUTICAS SÓLIDAS CONTENDO UM INIBIDOR DE INTEGRASE Os tabletes comprimidos para administração oral contendo raltegravir na forma de um sal farmaceuticamente aceitável são descritos. A tabela compreende: (A) um componente intragranular que compreende (i) uma quantidade eficaz de um sal de metal alcalino de raltegravir, (ii) opcionalmente um primeiro superdesintegrante e (iii) um aglutinante e (B) um componente extragranular que compreende (i) um segundo superdesinegrante, (ii) uma carga e (iii) um lubrificante. Os métodos para a preparação de tabletes e para o uso de tabletes, opcionalmente em combinações com outras agentes anti-HIV, para a inibição de HIV integrasse, para o tratamento ou profilaxia de Infecção de HIV ou para o tratamento, atraso no início ou profilaxia da AIDS também são descritos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25486909P | 2009-10-26 | 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 |
---|---|
BR112012009857A2 BR112012009857A2 (pt) | 2015-09-29 |
BR112012009857A8 true BR112012009857A8 (pt) | 2023-04-11 |
Family
ID=43922462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112012009857A BR112012009857A8 (pt) | 2009-10-26 | 2010-10-21 | Composições farmacêuticas sólidas contendo um inibidor de integrase |
Country Status (26)
Country | Link |
---|---|
US (2) | US9649311B2 (pt) |
EP (2) | EP3970702A1 (pt) |
JP (2) | JP6122639B2 (pt) |
KR (1) | KR101835893B1 (pt) |
CN (2) | CN106074411A (pt) |
AU (1) | AU2010313571B2 (pt) |
BR (1) | BR112012009857A8 (pt) |
CA (1) | CA2777937C (pt) |
CO (1) | CO6531485A2 (pt) |
CY (1) | CY1124914T1 (pt) |
DK (1) | DK2493312T3 (pt) |
ES (1) | ES2898348T3 (pt) |
HR (1) | HRP20211826T1 (pt) |
HU (1) | HUE057248T2 (pt) |
IL (1) | IL219369A (pt) |
IN (1) | IN2012DN03377A (pt) |
LT (1) | LT2493312T (pt) |
MX (1) | MX345227B (pt) |
MY (1) | MY162494A (pt) |
PL (1) | PL2493312T3 (pt) |
PT (1) | PT2493312T (pt) |
RS (1) | RS62600B1 (pt) |
RU (1) | RU2602865C2 (pt) |
SI (1) | SI2493312T1 (pt) |
WO (1) | WO2011053504A1 (pt) |
ZA (1) | ZA201203012B (pt) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT2493312T (pt) | 2009-10-26 | 2021-11-25 | Merck Sharp & Dohme | Composições farmacêuticas sólidas contendo um inibidor de integrase |
JP2014512386A (ja) * | 2011-04-22 | 2014-05-22 | メルク・シャープ・アンド・ドーム・コーポレーション | 味がマスクされたラルテグラビル製剤 |
WO2014014933A1 (en) * | 2012-07-20 | 2014-01-23 | Merck Sharp & Dohme Corp. | Hiv treatment with amido-substituted pyrimidinone derivatives |
WO2014064711A2 (en) * | 2012-10-22 | 2014-05-01 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
MX364901B (es) * | 2012-10-23 | 2019-05-10 | Cipla Ltd | Composicion farmaceutica antirretroviral. |
EP3019468A4 (en) * | 2013-07-11 | 2017-01-11 | 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 |
EP3740209A1 (en) * | 2018-01-19 | 2020-11-25 | Gilead Sciences, Inc. | Metabolites of bictegravir |
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 |
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 |
DE60036961T2 (de) | 1999-11-24 | 2008-08-28 | Merck & Co., Inc. | Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer |
CZ20031028A3 (cs) | 2000-10-12 | 2003-08-13 | Merck & Co., Inc. | Aza- a polyazanaftalenylkarboxamidy |
GEP20063848B (en) | 2001-10-26 | 2006-06-12 | Inst Di Richerche Di Biolog Moltcolare P Angeletti Spa | N-substituted hydroxypyrimi-dinone carboxamide inhibitors of hiv integrase |
US7232819B2 (en) | 2001-10-26 | 2007-06-19 | Istituto Di Ricerche Di Biologia P. Angeletti S.P.A. | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
EP1499391A2 (en) | 2002-04-10 | 2005-01-26 | Merck & Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
US7414045B2 (en) | 2002-12-27 | 2008-08-19 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors |
ATE500819T1 (de) | 2003-12-31 | 2011-03-15 | Bend Res Inc | Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren |
US7829720B2 (en) | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
CA2588466A1 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
UA87884C2 (uk) | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
NZ555120A (en) * | 2004-12-03 | 2009-11-27 | Merck & Co Inc | Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate controlling composition |
TR201907729T4 (tr) * | 2004-12-03 | 2019-06-21 | Merck Sharp & Dohme | Bir anti-çekirdekleştirici ajan içeren farmasötik bileşim. |
US20090136570A1 (en) * | 2006-01-20 | 2009-05-28 | Bhagwant Rege | Taste-Masked Tablets and Granules |
CA2563690C (en) * | 2006-10-12 | 2014-10-07 | Pharmascience Inc. | Pharmaceutical compositions comprising intra- and extra- granular fractions |
EP2178511B1 (en) * | 2007-06-22 | 2011-03-02 | Bristol-Myers Squibb Company | Tableted compositions containing atazanavir |
CA2702317A1 (en) * | 2007-07-09 | 2009-01-15 | Concert Pharmaceuticals, Inc. | Novel pyrimidinecarboxamide derivatives |
US8372431B2 (en) * | 2007-10-26 | 2013-02-12 | Bial-Portela & C.A., S.A. | Pharmaceutical composition comprising licarbazepine acetate |
PT2493312T (pt) | 2009-10-26 | 2021-11-25 | Merck Sharp & Dohme | Composições farmacêuticas sólidas contendo um inibidor de integrase |
-
2010
- 2010-10-21 PT PT108273384T patent/PT2493312T/pt unknown
- 2010-10-21 RU RU2012121857/15A patent/RU2602865C2/ru active
- 2010-10-21 RS RS20211443A patent/RS62600B1/sr unknown
- 2010-10-21 CN CN201610500807.0A patent/CN106074411A/zh active Pending
- 2010-10-21 LT LTEPPCT/US2010/053507T patent/LT2493312T/lt unknown
- 2010-10-21 CN CN2010800593740A patent/CN102655752A/zh active Pending
- 2010-10-21 ES ES10827338T patent/ES2898348T3/es active Active
- 2010-10-21 US US13/503,939 patent/US9649311B2/en active Active
- 2010-10-21 DK DK10827338.4T patent/DK2493312T3/da active
- 2010-10-21 AU AU2010313571A patent/AU2010313571B2/en active Active
- 2010-10-21 WO PCT/US2010/053507 patent/WO2011053504A1/en active Application Filing
- 2010-10-21 HR HRP20211826TT patent/HRP20211826T1/hr unknown
- 2010-10-21 HU HUE10827338A patent/HUE057248T2/hu unknown
- 2010-10-21 PL PL10827338T patent/PL2493312T3/pl unknown
- 2010-10-21 MY MYPI2012001823A patent/MY162494A/en unknown
- 2010-10-21 EP EP21202505.0A patent/EP3970702A1/en active Pending
- 2010-10-21 JP JP2012535360A patent/JP6122639B2/ja active Active
- 2010-10-21 MX MX2012004903A patent/MX345227B/es active IP Right Grant
- 2010-10-21 EP EP10827338.4A patent/EP2493312B1/en active Active
- 2010-10-21 IN IN3377DEN2012 patent/IN2012DN03377A/en unknown
- 2010-10-21 KR KR1020127013561A patent/KR101835893B1/ko active IP Right Grant
- 2010-10-21 CA CA2777937A patent/CA2777937C/en active Active
- 2010-10-21 BR BR112012009857A patent/BR112012009857A8/pt not_active Application Discontinuation
- 2010-10-21 SI SI201032094T patent/SI2493312T1/sl 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
Also Published As
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B25A | Requested transfer of rights approved |
Owner name: SCHERING CORPORATION (US) |
|
B25D | Requested change of name of applicant approved |
Owner name: MERCK SHARP AND DOHME CORP (US) |
|
B25G | Requested change of headquarter approved |
Owner name: MERCK SHARP AND DOHME CORP (US) |
|
B15K | Others concerning applications: alteration of classification |
Ipc: A61K 31/425 (2006.01), A01N 43/78 (2006.01) |
|
B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
B09B | Patent application refused [chapter 9.2 patent gazette] | ||
B12B | Appeal against refusal [chapter 12.2 patent gazette] | ||
B25A | Requested transfer of rights approved |
Owner name: MERCK SHARP AND DOHME LLC (US) |