CA2777937C - Solid pharmaceutical compositions containing an integrase inhibitor - Google Patents

Solid pharmaceutical compositions containing an integrase inhibitor Download PDF

Info

Publication number
CA2777937C
CA2777937C CA2777937A CA2777937A CA2777937C CA 2777937 C CA2777937 C CA 2777937C CA 2777937 A CA2777937 A CA 2777937A CA 2777937 A CA2777937 A CA 2777937A CA 2777937 C CA2777937 C CA 2777937C
Authority
CA
Canada
Prior art keywords
range
amount
employed
superdisintegrant
compressed tablet
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.)
Active
Application number
CA2777937A
Other languages
English (en)
French (fr)
Other versions
CA2777937A1 (en
Inventor
Majid Mahjour
Feng Li
Decheng Ma
Sutthilug Sotthivirat
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
Merck Sharp and Dohme LLC
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=CA2777937(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of CA2777937A1 publication Critical patent/CA2777937A1/en
Application granted granted Critical
Publication of CA2777937C publication Critical patent/CA2777937C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS 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
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/10Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered 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)
CA2777937A 2009-10-26 2010-10-21 Solid pharmaceutical compositions containing an integrase inhibitor Active CA2777937C (en)

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
CA2777937A1 CA2777937A1 (en) 2011-05-05
CA2777937C true CA2777937C (en) 2017-08-29

Family

ID=43922462

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2777937A Active CA2777937C (en) 2009-10-26 2010-10-21 Solid pharmaceutical compositions containing an integrase inhibitor

Country Status (26)

Country Link
US (2) US9649311B2 (2)
EP (2) EP2493312B1 (2)
JP (2) JP6122639B2 (2)
KR (1) KR101835893B1 (2)
CN (2) CN106074411A (2)
AU (1) AU2010313571B2 (2)
BR (1) BR112012009857A8 (2)
CA (1) CA2777937C (2)
CO (1) CO6531485A2 (2)
CY (1) CY1124914T1 (2)
DK (1) DK2493312T3 (2)
ES (1) ES2898348T3 (2)
HR (1) HRP20211826T1 (2)
HU (1) HUE057248T2 (2)
IL (1) IL219369A (2)
IN (1) IN2012DN03377A (2)
LT (1) LT2493312T (2)
MX (1) MX345227B (2)
MY (1) MY162494A (2)
PL (1) PL2493312T3 (2)
PT (1) PT2493312T (2)
RS (1) RS62600B1 (2)
RU (1) RU2602865C2 (2)
SI (1) SI2493312T1 (2)
WO (1) WO2011053504A1 (2)
ZA (1) ZA201203012B (2)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9649311B2 (en) 2009-10-26 2017-05-16 Merck Sharp & Dohme Corp. Solid pharmaceutical compositions containing an integrase inhibitor
AU2012245524A1 (en) * 2011-04-22 2013-10-24 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
AU2013336491B2 (en) 2012-10-23 2018-08-02 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 (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
EP3801532B1 (en) * 2018-06-06 2025-11-05 Merck Sharp & Dohme LLC 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
JP7603000B2 (ja) 2018-08-31 2024-12-19 オプコ アイルランド グローバル ホールディングス リミテッド ビタミンd小児用剤形、製造方法および使用方法

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 (fr) * 1999-07-08 2003-05-09 Prographarm Laboratoires Procede de fabrication de granules enrobes a gout masque et liberation immediate du principe actif
US6642237B1 (en) 1999-11-24 2003-11-04 Merck & Co., Inc. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
PL360944A1 (en) 2000-10-12 2004-09-20 Merck & Co, Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
AU2003220186A1 (en) 2002-04-10 2003-10-27 Merck And Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
NZ540729A (en) 2002-12-27 2008-03-28 Angeletti P Ist Richerche Bio Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds 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
EP1904067B2 (en) 2004-12-03 2017-10-11 Merck Sharp & Dohme Corp. Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition
BRPI0518741A2 (pt) 2004-12-03 2008-12-02 Merck & Co Inc uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero
EP1819323B2 (en) * 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
UA87884C2 (uk) 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
WO2007087188A2 (en) 2006-01-20 2007-08-02 Merck & Co., Inc. Taste-masked tablets and granules
CA2563690C (en) * 2006-10-12 2014-10-07 Pharmascience Inc. Pharmaceutical compositions comprising intra- and extra- granular fractions
DE602008005316D1 (de) 2007-06-22 2011-04-14 Bristol Myers Squibb Co Tablettierte atazanavirhaltige zusammensetzungen
US7687509B2 (en) * 2007-07-09 2010-03-30 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives
US8372431B2 (en) * 2007-10-26 2013-02-12 Bial-Portela & C.A., S.A. Pharmaceutical composition comprising licarbazepine acetate
US9649311B2 (en) * 2009-10-26 2017-05-16 Merck Sharp & Dohme Corp. Solid pharmaceutical compositions containing an integrase inhibitor

Also Published As

Publication number Publication date
BR112012009857A2 (pt) 2015-09-29
IL219369A (en) 2017-06-29
EP2493312A1 (en) 2012-09-05
CN106074411A (zh) 2016-11-09
ZA201203012B (en) 2012-12-27
EP3970702A1 (en) 2022-03-23
AU2010313571A1 (en) 2012-06-07
LT2493312T (lt) 2022-01-10
KR101835893B1 (ko) 2018-04-19
CO6531485A2 (es) 2012-09-28
SI2493312T1 (sl) 2021-12-31
KR20120102063A (ko) 2012-09-17
JP2016034962A (ja) 2016-03-17
US10772888B2 (en) 2020-09-15
DK2493312T3 (da) 2021-12-13
EP2493312B1 (en) 2021-10-20
WO2011053504A1 (en) 2011-05-05
CY1124914T1 (el) 2023-01-05
MX2012004903A (es) 2012-06-14
US9649311B2 (en) 2017-05-16
CN102655752A (zh) 2012-09-05
US20120213851A1 (en) 2012-08-23
MY162494A (en) 2017-06-15
RU2602865C2 (ru) 2016-11-20
RU2012121857A (ru) 2013-12-10
JP6122639B2 (ja) 2017-04-26
BR112012009857A8 (pt) 2023-04-11
IL219369A0 (en) 2012-06-28
CA2777937A1 (en) 2011-05-05
ES2898348T3 (es) 2022-03-07
IN2012DN03377A (2) 2015-10-23
AU2010313571B2 (en) 2014-07-31
HUE057248T2 (hu) 2022-04-28
MX345227B (es) 2017-01-20
US20170231993A1 (en) 2017-08-17
JP2013508395A (ja) 2013-03-07
PL2493312T3 (pl) 2022-01-03
EP2493312A4 (en) 2013-07-10
PT2493312T (pt) 2021-11-25
RS62600B1 (sr) 2021-12-31
HRP20211826T1 (hr) 2022-03-04

Similar Documents

Publication Publication Date Title
CA2777937C (en) Solid pharmaceutical compositions containing an integrase inhibitor
RU2456989C2 (ru) Твердые лекарственные формы, содержащие тадалафил
US20210093575A1 (en) Immediate release formulations and dosage forms of gamma-hydroxybutyrate
AU2010352575B2 (en) Immediate release formulations and dosage forms of gamma-hydroxybutyrate
JP7836361B2 (ja) パーキンソン病治療薬の安定化方法
JP2017523149A (ja) エドキサバンの医薬組成物
EP4436553A1 (en) An orodispersible pharmaceutical dosage form of edoxaban
WO2013014454A1 (en) New (trimethoxyphenylamino)pyrimidinyl formulations
EP4183390A1 (en) An orodispersible pharmaceutical dosage form of edoxaban
EP3801532B1 (en) Formulations of raltegravir
WO2006134610A1 (en) Efavirenz pharmaceutical composition having enhanced dissolution profile
JP6328138B2 (ja) N−[5−[2−(3,5−ジメトキシフェニル)エチル]−2h−ピラゾール−3−イル]−4−[(3r,5s)−3,5−ジメチルピペラジン−1−イル]ベンズアミドの医薬製剤
HK40069975A (en) Solid pharmaceutical compositions containing an integrase inhibitor
EP3334419A1 (en) Solid pharmaceutical composition of abacavir, lamivudine, and efavirenz
JP2012502042A (ja) Hiv結合阻害剤の最適な送達のための安定な医薬組成物

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20151005

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 15TH ANNIV.) - STANDARD

Year of fee payment: 15

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250908

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250908