WO2010059038A2 - Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz - Google Patents

Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz Download PDF

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Publication number
WO2010059038A2
WO2010059038A2 PCT/NL2009/000227 NL2009000227W WO2010059038A2 WO 2010059038 A2 WO2010059038 A2 WO 2010059038A2 NL 2009000227 W NL2009000227 W NL 2009000227W WO 2010059038 A2 WO2010059038 A2 WO 2010059038A2
Authority
WO
WIPO (PCT)
Prior art keywords
emtricitabine
efavirenz
tenofovir disoproxil
composition
tenofovir
Prior art date
Application number
PCT/NL2009/000227
Other languages
English (en)
Other versions
WO2010059038A3 (fr
Inventor
Evanthia Dova
Marcel Hoffmann
Samir Kulkarni
Rita Ramos
Original Assignee
Ultimorphix Technologies B.V
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
Application filed by Ultimorphix Technologies B.V filed Critical Ultimorphix Technologies B.V
Priority to US13/129,676 priority Critical patent/US20110288045A1/en
Priority to CA2744211A priority patent/CA2744211A1/fr
Priority to AU2009318202A priority patent/AU2009318202A1/en
Priority to JP2011537381A priority patent/JP2012509320A/ja
Priority to EP09761039A priority patent/EP2365798A2/fr
Priority to CN2009801462062A priority patent/CN102281869A/zh
Publication of WO2010059038A2 publication Critical patent/WO2010059038A2/fr
Publication of WO2010059038A3 publication Critical patent/WO2010059038A3/fr

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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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

Definitions

  • This application relates to products for the treatment of viral infections, in particular
  • Figure 6 shows the HPLC spectrogram with the retention peaks at 3.425, 3.610, 8.573 and 12.624 min which corresponds to the Emtricitabine related compounds.
  • the peaks at retention time of 26.94 and 35.78 minutes are the Tenofovir disoproxil related impurities with a mass of 935 and 1051.1 respectively.

Abstract

La présente invention concerne une méthode et une composition de produit pharmaceutique basées sur le diisopropoxylhémifumarate de Tenofovir, l’Emtricitabine et l’Efavirenz. La composition peut être élaborée suivante un procédé comprenant une étape de granulation humide pour reproduire une forme galénique stable adaptée au traitement du VIH essentiellement en l'absence de produits de dégradation connus.
PCT/NL2009/000227 2008-11-21 2009-11-19 Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz WO2010059038A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
US13/129,676 US20110288045A1 (en) 2008-11-21 2009-11-19 Wet granulation of tenofovir, emtricitabine and efavirenz
CA2744211A CA2744211A1 (fr) 2008-11-21 2009-11-19 Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz
AU2009318202A AU2009318202A1 (en) 2008-11-21 2009-11-19 Wet granulation of Tenofovir, Emtricitabine and Efavirenz
JP2011537381A JP2012509320A (ja) 2008-11-21 2009-11-19 テノフォビル、エムトリシタビン及びエファビレンツの湿式造粒法
EP09761039A EP2365798A2 (fr) 2008-11-21 2009-11-19 Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz
CN2009801462062A CN102281869A (zh) 2008-11-21 2009-11-19 替诺福韦、恩曲他滨和依法韦仑的湿法制粒

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US11692508P 2008-11-21 2008-11-21
US61/116,925 2008-11-21
US17914609P 2009-05-18 2009-05-18
US61/179,146 2009-05-18

Publications (2)

Publication Number Publication Date
WO2010059038A2 true WO2010059038A2 (fr) 2010-05-27
WO2010059038A3 WO2010059038A3 (fr) 2010-07-08

Family

ID=42111508

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/NL2009/000227 WO2010059038A2 (fr) 2008-11-21 2009-11-19 Granulation humide du tenofovir, de l'emtricitabine et de l'efavirenz

Country Status (7)

Country Link
US (1) US20110288045A1 (fr)
EP (1) EP2365798A2 (fr)
JP (1) JP2012509320A (fr)
CN (1) CN102281869A (fr)
AU (1) AU2009318202A1 (fr)
CA (1) CA2744211A1 (fr)
WO (1) WO2010059038A2 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015085976A1 (fr) * 2013-12-09 2015-06-18 Zentiva, K.S. Composition pharmaceutique stable contenant du fumarate de disoproxil de tenofovir
WO2015155673A1 (fr) * 2014-04-08 2015-10-15 Teva Pharmaceutical Industries Ltd Forme pharmaceutique unitaire comprenant de l'emtricitabine, du ténofovir, du darunavir et du ritonavir
WO2015028875A3 (fr) * 2013-08-29 2015-11-19 Teva Pharmaceuticals Industries Ltd. Forme pharmaceutique unitaire comprenant de l'emtricitabine, du ténofovir, du darunavir et du ritonavir et un comprimé monolithique comprenant du darunavir et du ritonavir
EP3326619A1 (fr) * 2016-11-29 2018-05-30 Arven Ilac Sanayi Ve Ticaret A.S. Compositions pharmaceutiques orales solides comprenant du tenofovir et du emtricitabine
CN115524408A (zh) * 2021-06-25 2022-12-27 成都倍特药业股份有限公司 恩曲他滨丙酚替诺福韦片复方制剂中有关物质的检测方法

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2013CH05288A (fr) * 2013-11-18 2015-09-11 Aurobindo Pharma Ltd
KR20170003063A (ko) * 2015-06-30 2017-01-09 한미약품 주식회사 테노포비어 디소프록실 함유 경구용 고형제제 및 그 제조방법
US10561614B2 (en) * 2017-01-27 2020-02-18 Steerlife India Private Limited Tenofovir granules

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006135932A2 (fr) * 2005-06-13 2006-12-21 Gilead Sciences, Inc. Composition d'un produit pharmaceutique, et procede correspondant
US20070099902A1 (en) * 2005-06-13 2007-05-03 Bristol-Myers Squibb & Gilead Sciences, Llc Unitary pharmaceutical dosage form
WO2008007392A2 (fr) * 2006-07-12 2008-01-17 Matrix Laboratories Limited Procédé amélioré destiné à préparer du ténofovir
WO2008143500A1 (fr) * 2007-05-22 2008-11-27 Ultimorphix Technologies B.V. Co-cristaux de tenofovir disoproxil acide hémi-fumarique

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010125572A1 (fr) * 2009-04-29 2010-11-04 Hetero Research Foundation Comprimés et capsules contenant de l'éfavirenz

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006135932A2 (fr) * 2005-06-13 2006-12-21 Gilead Sciences, Inc. Composition d'un produit pharmaceutique, et procede correspondant
US20070099902A1 (en) * 2005-06-13 2007-05-03 Bristol-Myers Squibb & Gilead Sciences, Llc Unitary pharmaceutical dosage form
WO2008007392A2 (fr) * 2006-07-12 2008-01-17 Matrix Laboratories Limited Procédé amélioré destiné à préparer du ténofovir
WO2008143500A1 (fr) * 2007-05-22 2008-11-27 Ultimorphix Technologies B.V. Co-cristaux de tenofovir disoproxil acide hémi-fumarique

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015028875A3 (fr) * 2013-08-29 2015-11-19 Teva Pharmaceuticals Industries Ltd. Forme pharmaceutique unitaire comprenant de l'emtricitabine, du ténofovir, du darunavir et du ritonavir et un comprimé monolithique comprenant du darunavir et du ritonavir
WO2015085976A1 (fr) * 2013-12-09 2015-06-18 Zentiva, K.S. Composition pharmaceutique stable contenant du fumarate de disoproxil de tenofovir
WO2015155673A1 (fr) * 2014-04-08 2015-10-15 Teva Pharmaceutical Industries Ltd Forme pharmaceutique unitaire comprenant de l'emtricitabine, du ténofovir, du darunavir et du ritonavir
EP3326619A1 (fr) * 2016-11-29 2018-05-30 Arven Ilac Sanayi Ve Ticaret A.S. Compositions pharmaceutiques orales solides comprenant du tenofovir et du emtricitabine
WO2018099895A1 (fr) * 2016-11-29 2018-06-07 Arven Ilac Sanayi Ve Ticaret A.S. Compositions pharmaceutiques orales solides comprenant du ténofovir et de l'emtricitabine
CN115524408A (zh) * 2021-06-25 2022-12-27 成都倍特药业股份有限公司 恩曲他滨丙酚替诺福韦片复方制剂中有关物质的检测方法

Also Published As

Publication number Publication date
JP2012509320A (ja) 2012-04-19
WO2010059038A3 (fr) 2010-07-08
CN102281869A (zh) 2011-12-14
EP2365798A2 (fr) 2011-09-21
CA2744211A1 (fr) 2010-05-27
AU2009318202A1 (en) 2011-07-07
US20110288045A1 (en) 2011-11-24

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