CN106074411A - 包含整合酶抑制剂的固体药物组合物 - Google Patents

包含整合酶抑制剂的固体药物组合物 Download PDF

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Publication number
CN106074411A
CN106074411A CN201610500807.0A CN201610500807A CN106074411A CN 106074411 A CN106074411 A CN 106074411A CN 201610500807 A CN201610500807 A CN 201610500807A CN 106074411 A CN106074411 A CN 106074411A
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CN
China
Prior art keywords
superdisintegrant
compressed tablets
iii
tablet
hiv
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.)
Pending
Application number
CN201610500807.0A
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English (en)
Chinese (zh)
Inventor
M.马霍尔
李峰
马德成
S.索特希维拉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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
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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=CN106074411(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of CN106074411A publication Critical patent/CN106074411A/zh
Pending legal-status Critical Current

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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
    • 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
    • A61K9/2004—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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (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)
CN201610500807.0A 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物 Pending CN106074411A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25486909P 2009-10-26 2009-10-26
US61/254869 2009-10-26
CN2010800593740A CN102655752A (zh) 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2010800593740A Division CN102655752A (zh) 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物

Publications (1)

Publication Number Publication Date
CN106074411A true CN106074411A (zh) 2016-11-09

Family

ID=43922462

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2010800593740A Pending CN102655752A (zh) 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物
CN201610500807.0A Pending CN106074411A (zh) 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物

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CN2010800593740A Pending CN102655752A (zh) 2009-10-26 2010-10-21 包含整合酶抑制剂的固体药物组合物

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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)
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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)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
CN111615391A (zh) * 2018-01-19 2020-09-01 吉利德科学公司 比卡格韦的代谢物

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ES2898348T3 (es) 2009-10-26 2022-03-07 Merck Sharp & Dohme Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa
WO2012145446A1 (en) * 2011-04-22 2012-10-26 Merck Sharp & Dohme Corp. Taste-masked formulations of raltegravir
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
CA2885763C (en) * 2012-10-23 2021-04-06 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
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
CN112912067B (zh) * 2018-08-31 2025-04-04 欧普科爱尔兰环球控股有限公司 儿童剂型、制造和使用方法

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CN101068550A (zh) * 2004-12-03 2007-11-07 默克公司 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂
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CN101068550A (zh) * 2004-12-03 2007-11-07 默克公司 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111615391A (zh) * 2018-01-19 2020-09-01 吉利德科学公司 比卡格韦的代谢物
CN111615391B (zh) * 2018-01-19 2023-05-30 吉利德科学公司 比卡格韦的代谢物

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IL219369A (en) 2017-06-29
CO6531485A2 (es) 2012-09-28
US20170231993A1 (en) 2017-08-17
US20120213851A1 (en) 2012-08-23
IN2012DN03377A (enExample) 2015-10-23
CA2777937A1 (en) 2011-05-05
EP3970702A1 (en) 2022-03-23
EP2493312A4 (en) 2013-07-10
CA2777937C (en) 2017-08-29
JP2016034962A (ja) 2016-03-17
EP2493312A1 (en) 2012-09-05
MY162494A (en) 2017-06-15
LT2493312T (lt) 2022-01-10
IL219369A0 (en) 2012-06-28
RU2602865C2 (ru) 2016-11-20
MX2012004903A (es) 2012-06-14
BR112012009857A8 (pt) 2023-04-11
ZA201203012B (en) 2012-12-27
WO2011053504A1 (en) 2011-05-05
BR112012009857A2 (pt) 2015-09-29
PL2493312T3 (pl) 2022-01-03
SI2493312T1 (sl) 2021-12-31
KR20120102063A (ko) 2012-09-17
DK2493312T3 (da) 2021-12-13
EP2493312B1 (en) 2021-10-20
US9649311B2 (en) 2017-05-16
RU2012121857A (ru) 2013-12-10
KR101835893B1 (ko) 2018-04-19
CY1124914T1 (el) 2023-01-05
JP6122639B2 (ja) 2017-04-26
AU2010313571A1 (en) 2012-06-07
MX345227B (es) 2017-01-20
HUE057248T2 (hu) 2022-04-28
AU2010313571B2 (en) 2014-07-31
PT2493312T (pt) 2021-11-25
US10772888B2 (en) 2020-09-15
HRP20211826T1 (hr) 2022-03-04
JP2013508395A (ja) 2013-03-07
ES2898348T3 (es) 2022-03-07
CN102655752A (zh) 2012-09-05
RS62600B1 (sr) 2021-12-31

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Application publication date: 20161109