KR101835893B1 - 인테그라제 억제제를 함유하는 고형 제약 조성물 - Google Patents

인테그라제 억제제를 함유하는 고형 제약 조성물 Download PDF

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KR101835893B1
KR101835893B1 KR1020127013561A KR20127013561A KR101835893B1 KR 101835893 B1 KR101835893 B1 KR 101835893B1 KR 1020127013561 A KR1020127013561 A KR 1020127013561A KR 20127013561 A KR20127013561 A KR 20127013561A KR 101835893 B1 KR101835893 B1 KR 101835893B1
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raltegravir
tablet
iii
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KR20120102063A (ko
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마지드 마주르
펭 리
데쳉 마
수티러그 소티비라트
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머크 샤프 앤드 돔 코포레이션
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    • 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020127013561A 2009-10-26 2010-10-21 인테그라제 억제제를 함유하는 고형 제약 조성물 Active KR101835893B1 (ko)

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
KR20120102063A KR20120102063A (ko) 2012-09-17
KR101835893B1 true KR101835893B1 (ko) 2018-04-19

Family

ID=43922462

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Application Number Title Priority Date Filing Date
KR1020127013561A Active KR101835893B1 (ko) 2009-10-26 2010-10-21 인테그라제 억제제를 함유하는 고형 제약 조성물

Country Status (26)

Country Link
US (2) US9649311B2 (https=)
EP (2) EP3970702A1 (https=)
JP (2) JP6122639B2 (https=)
KR (1) KR101835893B1 (https=)
CN (2) CN106074411A (https=)
AU (1) AU2010313571B2 (https=)
BR (1) BR112012009857A8 (https=)
CA (1) CA2777937C (https=)
CO (1) CO6531485A2 (https=)
CY (1) CY1124914T1 (https=)
DK (1) DK2493312T3 (https=)
ES (1) ES2898348T3 (https=)
HR (1) HRP20211826T1 (https=)
HU (1) HUE057248T2 (https=)
IL (1) IL219369A (https=)
IN (1) IN2012DN03377A (https=)
LT (1) LT2493312T (https=)
MX (1) MX345227B (https=)
MY (1) MY162494A (https=)
PL (1) PL2493312T3 (https=)
PT (1) PT2493312T (https=)
RS (1) RS62600B1 (https=)
RU (1) RU2602865C2 (https=)
SI (1) SI2493312T1 (https=)
WO (1) WO2011053504A1 (https=)
ZA (1) ZA201203012B (https=)

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IN2012DN03377A (https=) 2009-10-26 2015-10-23 Merck Sharp & Dohme
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
CA2885763C (en) * 2012-10-23 2021-04-06 Cipla Limited Pharmaceutical antiretroviral composition
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
WO2019236395A1 (en) * 2018-06-06 2019-12-12 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
WO2020044314A1 (en) * 2018-08-31 2020-03-05 Opko Ireland Global Holdings, Ltd. Vitamin d pediatric dosage forms, methods of making and using

Citations (3)

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WO2007087188A2 (en) * 2006-01-20 2007-08-02 Merck & Co., Inc. Taste-masked tablets and granules
WO2008043167A1 (en) * 2006-10-12 2008-04-17 Pharmascience Inc. Pharmaceutical compositions comprising intra- and extra- granular fractions
US20080118559A1 (en) 2004-12-03 2008-05-22 Cruanes Maria T Pharmaceutical Composition Containing an Anti-Nucleating Agent

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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
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CA2425440C (en) 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
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CA2551254A1 (en) 2003-12-31 2005-07-21 Pfizer Products Inc. Stabilized pharmaceutical solid compositions of low-solubility drugs, 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
RU2403066C2 (ru) 2004-12-03 2010-11-10 Мерк Шарп Энд Домэ Корп Применение атазанавира для улучшения фармакокинетики лекарственных средств, метаболизируемых ugt1a1
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ES2360336T3 (es) * 2007-06-22 2011-06-03 Bristol-Myers Squibb Company Composiciones en comprimidos que contienen atazanavir.
WO2009009531A2 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives for the treatment of hiv infections
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IN2012DN03377A (https=) * 2009-10-26 2015-10-23 Merck Sharp & Dohme

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
US20080118559A1 (en) 2004-12-03 2008-05-22 Cruanes Maria T Pharmaceutical Composition Containing an Anti-Nucleating Agent
WO2007087188A2 (en) * 2006-01-20 2007-08-02 Merck & Co., Inc. Taste-masked tablets and granules
WO2008043167A1 (en) * 2006-10-12 2008-04-17 Pharmascience Inc. Pharmaceutical compositions comprising intra- and extra- granular fractions

Also Published As

Publication number Publication date
CY1124914T1 (el) 2023-01-05
DK2493312T3 (da) 2021-12-13
MX345227B (es) 2017-01-20
BR112012009857A8 (pt) 2023-04-11
WO2011053504A1 (en) 2011-05-05
US9649311B2 (en) 2017-05-16
EP2493312A1 (en) 2012-09-05
EP2493312B1 (en) 2021-10-20
RU2602865C2 (ru) 2016-11-20
SI2493312T1 (sl) 2021-12-31
EP3970702A1 (en) 2022-03-23
ZA201203012B (en) 2012-12-27
JP2016034962A (ja) 2016-03-17
JP2013508395A (ja) 2013-03-07
CN102655752A (zh) 2012-09-05
IL219369A (en) 2017-06-29
PL2493312T3 (pl) 2022-01-03
IL219369A0 (en) 2012-06-28
PT2493312T (pt) 2021-11-25
ES2898348T3 (es) 2022-03-07
JP6122639B2 (ja) 2017-04-26
KR20120102063A (ko) 2012-09-17
CO6531485A2 (es) 2012-09-28
CA2777937C (en) 2017-08-29
RU2012121857A (ru) 2013-12-10
MX2012004903A (es) 2012-06-14
BR112012009857A2 (pt) 2015-09-29
CN106074411A (zh) 2016-11-09
IN2012DN03377A (https=) 2015-10-23
CA2777937A1 (en) 2011-05-05
AU2010313571A1 (en) 2012-06-07
EP2493312A4 (en) 2013-07-10
US20120213851A1 (en) 2012-08-23
RS62600B1 (sr) 2021-12-31
HUE057248T2 (hu) 2022-04-28
US20170231993A1 (en) 2017-08-17
LT2493312T (lt) 2022-01-10
AU2010313571B2 (en) 2014-07-31
MY162494A (en) 2017-06-15
HRP20211826T1 (hr) 2022-03-04
US10772888B2 (en) 2020-09-15

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