CO6531485A2 - Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa - Google Patents

Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa

Info

Publication number
CO6531485A2
CO6531485A2 CO12068959A CO12068959A CO6531485A2 CO 6531485 A2 CO6531485 A2 CO 6531485A2 CO 12068959 A CO12068959 A CO 12068959A CO 12068959 A CO12068959 A CO 12068959A CO 6531485 A2 CO6531485 A2 CO 6531485A2
Authority
CO
Colombia
Prior art keywords
tablets
integress
inhibitor
pharmaceutical compositions
compositions containing
Prior art date
Application number
CO12068959A
Other languages
English (en)
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=CO6531485(A2) "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 CO6531485A2 publication Critical patent/CO6531485A2/es

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
    • A61K9/2004—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
    • 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
    • A61K9/2072—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

Landscapes

  • 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)

Abstract

Están descritas tabletas comprimidas para administración oral que contienen raltegravir en forma de una sal farmacéuticamente aceptable. Las tabletas comprenden: (A) un componente intragranular que comprende (i) una cantidad efectiva de una sal de metal alcalino de raltegravir, (ii) opcionalmente un primer superdesintegrante, y (iii) un aglutinante; y (B) un componente extragranular el cual comprende (i) un segundo superdesintegrante, (ii) un relleno, y (iii) un lubricante. También están descritos métodos para preparar las tabletas y el uso de las tabletas, opcionalmente en combinación con otros agentes anti-VIH, para la inhibición de la integrasa del VIH, para el tratamiento o la profilaxis de la infección por VIH, o para el tratamiento, retraso en la aparición, o la profilaxis del SIDA.
CO12068959A 2009-10-26 2012-04-26 Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa CO6531485A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US25486909P 2009-10-26 2009-10-26

Publications (1)

Publication Number Publication Date
CO6531485A2 true CO6531485A2 (es) 2012-09-28

Family

ID=43922462

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12068959A CO6531485A2 (es) 2009-10-26 2012-04-26 Composiciones farmacéuticas sólidas que contienen un inhibidor de la integrasa

Country Status (26)

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

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2012DN03377A (es) 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

Family Cites Families (22)

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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
WO2001038332A1 (en) 1999-11-24 2001-05-31 Merck & Co., Inc. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides as hiv protease inhibitors
CA2425440C (en) 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
EP1441734B1 (en) 2001-10-26 2007-02-28 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
NZ533057A (en) 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
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UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
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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
KR101835893B1 (ko) 2018-04-19
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
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 (es) 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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