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IN2012DN03377A - - Google Patents

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Publication number
IN2012DN03377A
IN2012DN03377A IN3377DEN2012A IN2012DN03377A IN 2012DN03377 A IN2012DN03377 A IN 2012DN03377A IN 3377DEN2012 A IN3377DEN2012 A IN 3377DEN2012A IN 2012DN03377 A IN2012DN03377 A IN 2012DN03377A
Authority
IN
India
Prior art keywords
tablets
superdisintegrant
prophylaxis
iii
optionally
Prior art date
Application number
Inventor
Majid Mahjour
Feng Li
Decheng Ma
Sutthilug Sotthivirat
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43922462&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IN2012DN03377(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of IN2012DN03377A publication Critical patent/IN2012DN03377A/en

Links

Classifications

    • 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
    • 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
    • A61K9/2095—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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)

Abstract

Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.
IN3377DEN2012 2009-10-26 2010-10-21 IN2012DN03377A (en)

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 (1)

Publication Number Publication Date
IN2012DN03377A true IN2012DN03377A (en) 2015-10-23

Family

ID=43922462

Family Applications (1)

Application Number Title Priority Date Filing Date
IN3377DEN2012 IN2012DN03377A (en) 2009-10-26 2010-10-21

Country Status (26)

Country Link
US (2) US9649311B2 (en)
EP (2) EP2493312B1 (en)
JP (2) JP6122639B2 (en)
KR (1) KR101835893B1 (en)
CN (2) CN102655752A (en)
AU (1) AU2010313571B2 (en)
BR (1) BR112012009857A8 (en)
CA (1) CA2777937C (en)
CO (1) CO6531485A2 (en)
CY (1) CY1124914T1 (en)
DK (1) DK2493312T3 (en)
ES (1) ES2898348T3 (en)
HR (1) HRP20211826T1 (en)
HU (1) HUE057248T2 (en)
IL (1) IL219369A (en)
IN (1) IN2012DN03377A (en)
LT (1) LT2493312T (en)
MX (1) MX345227B (en)
MY (1) MY162494A (en)
PL (1) PL2493312T3 (en)
PT (1) PT2493312T (en)
RS (1) RS62600B1 (en)
RU (1) RU2602865C2 (en)
SI (1) SI2493312T1 (en)
WO (1) WO2011053504A1 (en)
ZA (1) ZA201203012B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2493312T3 (en) 2009-10-26 2021-12-13 Merck Sharp & Dohme PHARMACEUTICAL SOLID COMPOSITIONS CONTAINING AN INTEGRASE INHIBITOR
CA2833006A1 (en) * 2011-04-22 2012-10-26 Merck Sharp & Dohme Corp. Taste-masked formulations of 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
WO2014064409A1 (en) * 2012-10-23 2014-05-01 Cipla Limited Pharmaceutical antiretroviral composition
WO2015006177A1 (en) * 2013-07-11 2015-01-15 Merck Sharp & Dohme Corp. Formulations for cathepsin k inhibitors with vitamin d
CN105237526B (en) * 2014-06-20 2018-01-23 朱靖华 A kind of anti-hiv drug and preparation method thereof
JP7023054B2 (en) * 2017-04-05 2022-02-21 東和薬品株式会社 Levetiracetam-containing pharmaceutical composition and method for producing the same
WO2019144015A1 (en) * 2018-01-19 2019-07-25 Gilead Sciences, Inc. Metabolites of bictegravir
EP3801532A4 (en) * 2018-06-06 2022-03-23 Merck Sharp & Dohme Corp. Formulations of raltegravir
RU2688235C1 (en) * 2018-06-19 2019-05-21 Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" Pharmaceutical anti-diabetic composition based on substituted thiophene carboxylate and a method for production thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
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 (en) * 1999-07-08 2003-05-09 Prographarm Laboratoires PROCESS FOR THE MANUFACTURE OF MASK TASTE COATED GRANULES AND IMMEDIATE RELEASE OF THE ACTIVE INGREDIENT
AU777824B2 (en) 1999-11-24 2004-11-04 Merck Sharp & Dohme Corp. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors
PL360944A1 (en) 2000-10-12 2004-09-20 Merck & Co, Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
EP1441735B1 (en) 2001-10-26 2006-02-22 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
SI1441734T1 (en) 2001-10-26 2007-08-31 Angeletti P Ist Richerche Bio Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
WO2003086319A2 (en) 2002-04-10 2003-10-23 Merck & Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
WO2004058757A1 (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
DE602004031767D1 (en) 2003-12-31 2011-04-21 Bend Res Inc STABILIZED PHARMACEUTICAL SOLIDS COMPOSITIONS OF MEDIUM SOLUBILITY MEDICAMENTS, POLOXAMERS AND STABILIZING POLYMERS
US7829720B2 (en) 2004-05-04 2010-11-09 Bristol-Myers Squibb Company Process for preparing atazanavir bisulfate and novel forms
WO2006060681A2 (en) 2004-12-03 2006-06-08 Merck & Co., Inc. Pharmaceutical composition containing an anti-nucleating agent
KR101351059B1 (en) * 2004-12-03 2014-02-17 머크 샤프 앤드 돔 코포레이션 Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate controlling composition
BRPI0518741A2 (en) 2004-12-03 2008-12-02 Merck & Co Inc use of a combination of a drug directly metabolised by ugt1a1 or a pharmaceutically acceptable salt thereof and atazanavir or a pharmaceutically acceptable salt thereof, and a pharmaceutical combination for oral administration to a mammal
UA87884C2 (en) 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Potassium salt of an hiv integrase inhibitor
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
JP2010530889A (en) 2007-06-22 2010-09-16 ブリストル−マイヤーズ スクイブ カンパニー Tablet composition containing atazanavir
WO2009009531A2 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives for the treatment of hiv infections
US8372431B2 (en) * 2007-10-26 2013-02-12 Bial-Portela & C.A., S.A. Pharmaceutical composition comprising licarbazepine acetate
DK2493312T3 (en) 2009-10-26 2021-12-13 Merck Sharp & Dohme PHARMACEUTICAL SOLID COMPOSITIONS CONTAINING AN INTEGRASE INHIBITOR

Also Published As

Publication number Publication date
MY162494A (en) 2017-06-15
EP2493312B1 (en) 2021-10-20
SI2493312T1 (en) 2021-12-31
DK2493312T3 (en) 2021-12-13
EP2493312A4 (en) 2013-07-10
KR20120102063A (en) 2012-09-17
CA2777937C (en) 2017-08-29
RS62600B1 (en) 2021-12-31
IL219369A0 (en) 2012-06-28
CN106074411A (en) 2016-11-09
EP3970702A1 (en) 2022-03-23
HUE057248T2 (en) 2022-04-28
US9649311B2 (en) 2017-05-16
JP6122639B2 (en) 2017-04-26
US10772888B2 (en) 2020-09-15
JP2013508395A (en) 2013-03-07
CA2777937A1 (en) 2011-05-05
ZA201203012B (en) 2012-12-27
ES2898348T3 (en) 2022-03-07
LT2493312T (en) 2022-01-10
KR101835893B1 (en) 2018-04-19
JP2016034962A (en) 2016-03-17
RU2012121857A (en) 2013-12-10
BR112012009857A2 (en) 2015-09-29
CO6531485A2 (en) 2012-09-28
AU2010313571B2 (en) 2014-07-31
BR112012009857A8 (en) 2023-04-11
MX2012004903A (en) 2012-06-14
EP2493312A1 (en) 2012-09-05
US20170231993A1 (en) 2017-08-17
HRP20211826T1 (en) 2022-03-04
WO2011053504A1 (en) 2011-05-05
CY1124914T1 (en) 2023-01-05
US20120213851A1 (en) 2012-08-23
CN102655752A (en) 2012-09-05
AU2010313571A1 (en) 2012-06-07
MX345227B (en) 2017-01-20
PT2493312T (en) 2021-11-25
PL2493312T3 (en) 2022-01-03
IL219369A (en) 2017-06-29
RU2602865C2 (en) 2016-11-20

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