CA2234817A1 - Formulation de secretagogue stimulant la secretion de l'hormone de croissance, destinee a etre granulee par voie humide - Google Patents

Formulation de secretagogue stimulant la secretion de l'hormone de croissance, destinee a etre granulee par voie humide Download PDF

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Publication number
CA2234817A1
CA2234817A1 CA 2234817 CA2234817A CA2234817A1 CA 2234817 A1 CA2234817 A1 CA 2234817A1 CA 2234817 CA2234817 CA 2234817 CA 2234817 A CA2234817 A CA 2234817A CA 2234817 A1 CA2234817 A1 CA 2234817A1
Authority
CA
Canada
Prior art keywords
weight
active ingredient
diluent
carbonyl
piperdin
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.)
Abandoned
Application number
CA 2234817
Other languages
English (en)
Inventor
Mandana Asgharnejad
Jerome P. Draper
David C. Dubost
Michael J. Kaufman
David E. Storey
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 and Co Inc
Original Assignee
Individual
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
Priority claimed from GBGB9603238.8A external-priority patent/GB9603238D0/en
Priority claimed from GBGB9603834.4A external-priority patent/GB9603834D0/en
Application filed by Individual filed Critical Individual
Publication of CA2234817A1 publication Critical patent/CA2234817A1/fr
Abandoned legal-status Critical Current

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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne une composition pharmaceutique et un procédé permettant de préparer un comprimé contenant, comme principe actif, un sécretagogue stimulant la sécrétion de l'hormone de croissance. Pour préparer le comprimé on procède aux étapes suivantes: on forme un mélange en poudre constitué du principe actif, à savoir du N-[1(R)-[(1,2-dihydro-1-méthanesulfonyl-spiro[3H-indol-3,4'-piperdin]-1'-yl)carbonyl]-2-(phénylméthyl-oxy)éthyl]-2-amino-2-méthyl-propanamide, ou un sel pharmaceutiquement acceptable de celui-ci, en particulier du méthanesulfonate, et d'un liant/diluant, d'un premier diluant, d'un second diluant, d'une première partie d'un désintégrant, et d'un lubrifiant; on granule par voie humide ledit mélange en poudre avec une solution éthanol/eau pour former des granules; on fait sécher les granules pour enlever la solution éthanol/eau; on ajoute une seconde partie d'un désintégrant; on lubrifie les granules; et on comprime les granules séchés pour leur donner la forme de comprimé désirée. La présente invention concerne également une nouvelle forme amorphe du composé méthanesulfonate de N-[1(R)-[1,2-dihydro-1-méthanesulfonyl-spiro[3H-indol-3,4'-piperdin]-1-yl)carbonyl]-2-(phénylméthyl-oxy)éthyl]-2-amino-2-méthylpropanamide qui constitue le produit directe du procédé de préparation du comprimé selon l'invention.
CA 2234817 1995-10-27 1996-10-23 Formulation de secretagogue stimulant la secretion de l'hormone de croissance, destinee a etre granulee par voie humide Abandoned CA2234817A1 (fr)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US589795P 1995-10-27 1995-10-27
US590195P 1995-10-27 1995-10-27
US60/005,901 1995-10-27
US60/005,897 1995-10-27
GB9603238.8 1996-02-16
GBGB9603238.8A GB9603238D0 (en) 1996-02-16 1996-02-16 Wet granulation formulation of a growth hormone secretagogue
GBGB9603834.4A GB9603834D0 (en) 1996-02-23 1996-02-23 Amorphous form of a growth hormone secretagogue
GB9603834.4 1996-02-23

Publications (1)

Publication Number Publication Date
CA2234817A1 true CA2234817A1 (fr) 1997-05-01

Family

ID=27451404

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2234817 Abandoned CA2234817A1 (fr) 1995-10-27 1996-10-23 Formulation de secretagogue stimulant la secretion de l'hormone de croissance, destinee a etre granulee par voie humide

Country Status (5)

Country Link
EP (1) EP0857020A4 (fr)
JP (1) JPH11513989A (fr)
AU (1) AU7522896A (fr)
CA (1) CA2234817A1 (fr)
WO (1) WO1997015191A1 (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU759022B2 (en) 1999-02-18 2003-04-03 Kaken Pharmaceutical Co., Ltd. Novel amide derivatives as growth hormone secretagogues
CN1635898A (zh) * 1999-07-26 2005-07-06 贝勒医学院 超级活性的猪生长激素释放激素类似物
WO2001034684A1 (fr) * 1999-11-12 2001-05-17 R.P. Scherer Technologies, Inc. Granules de cellulose microcristalline a effet amortisseur
EP1313473A2 (fr) * 2000-08-30 2003-05-28 Pfizer Products Inc. Formulations a liberation prolongee pour les secretagogues de l'hormone de croissance
JP5328071B2 (ja) * 2001-04-10 2013-10-30 サン・ファーマ・アドバンスド・リサーチ・カンパニー・リミテッド 時限パルス放出組成物
DE60315514T3 (de) † 2002-12-20 2012-04-26 F. Hoffmann-La Roche Ag Hochdosierte ibandronat-formulierung
US7476653B2 (en) 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
UY29527A1 (es) * 2005-05-13 2006-12-29 Schering Ag Composicinn farmaccutica que contienen gestrgenos y/o estrngenos y 5-metil - (6s) - tetrhidrofolato.
CU23558A1 (es) 2006-02-28 2010-07-20 Ct Ingenieria Genetica Biotech Compuestos análogos a los secretagogos peptidicos de la hormona de crecimiento
KR20090107088A (ko) 2007-02-09 2009-10-12 트랜자임 파르마 인크 거대고리 그렐린 수용체 조절제 및 이의 사용 방법
ES2758624T3 (es) * 2009-02-12 2020-05-06 Fuji Chem Ind Co Ltd Composición de partículas desintegrantes y material de desintegración rápida moldeado por compresión que comprende la misma
US9119832B2 (en) 2014-02-05 2015-09-01 The Regents Of The University Of California Methods of treating mild brain injury
WO2017075535A1 (fr) 2015-10-28 2017-05-04 Oxeia Biopharmaceuticals, Inc. Méthodes de traitement de troubles neurodégénératifs
US11969416B1 (en) 2022-11-03 2024-04-30 Lumos Pharma, Inc. Compactable oral formulations of ibutamoren

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5578593A (en) * 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs promote release of growth hormone
BR9407869A (pt) * 1993-10-19 1996-10-29 Merck & Co Inc Combinaçao composiçao farmacêutica e processo para o tratamento de osteoporose

Also Published As

Publication number Publication date
JPH11513989A (ja) 1999-11-30
WO1997015191A1 (fr) 1997-05-01
EP0857020A1 (fr) 1998-08-12
AU7522896A (en) 1997-05-15
EP0857020A4 (fr) 1999-01-07

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Legal Events

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FZDE Dead