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1. (WO1997015191) WET GRANULATION FORMULATION OF A GROWTH HORMONE SECRETAGOGUE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/015191 International Application No.: PCT/US1996/017196
Publication Date: 01.05.1997 International Filing Date: 23.10.1996
Chapter 2 Demand Filed: 07.05.1997
IPC:
A61K 9/20 (2006.01) ,A61K 31/438 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
20
Pills, lozenges or tablets
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
438
the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
Applicants:
MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue Rahway, NJ 07065, US (AllExceptUS)
ASGHARNEJAD, Mandana [IR/US]; US (UsOnly)
DRAPER, Jerome, P. [US/US]; US (UsOnly)
DUBOST, David, C. [US/US]; US (UsOnly)
KAUFMAN, Michael, J. [US/US]; US (UsOnly)
STOREY, David, E. [GB/US]; US (UsOnly)
Inventors:
ASGHARNEJAD, Mandana; US
DRAPER, Jerome, P.; US
DUBOST, David, C.; US
KAUFMAN, Michael, J.; US
STOREY, David, E.; US
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065, US
Priority Data:
60/005,89727.10.1995US
60/005,90127.10.1995US
9603238.816.02.1996GB
9603834.423.02.1996GB
Title (EN) WET GRANULATION FORMULATION OF A GROWTH HORMONE SECRETAGOGUE
(FR) FORMULATION DE SECRETAGOGUE STIMULANT LA SECRETION DE L'HORMONE DE CROISSANCE, DESTINEE A ETRE GRANULEE PAR VOIE HUMIDE
Abstract:
(EN) The present invention relates to a pharmaceutical composition and a process for the preparation of a tablet containing a growth hormone secretagogue as the active ingredient. The tablet is prepared by forming a powder blend of the active ingredient N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, or a pharmaceutically acceptable salt thereof, in particular the methanesulfonate salt, with a binder/diluent, a first diluent, a second diluent, a first portion of a disintegrant, and a lubricant; wet granulating the powder blend with a solution of ethanol/water to form granules; drying the granules to remove the ethanol/water; adding a second portion of a disintegrant; lubricating the granules; and compressing the dried granules into the desired tablet form. The present invention further relates to a novel amorphous form of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is produced directly as a result of the process of tablet formulation.
(FR) 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.
Designated States: AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0857020US6123964JPH11513989CA2234817AU1996075228