A method for producing a microparticle

Details A method for producing a microparticle A method for producing a microparticle

A - Human Necessities

61

K

A61K 9/16 (2006.01) A61K 31/38 (2006.01) A61K 31/382 (2006.01) A61K 31/66 (2006.01) A61K 31/67 (2006.01) A61K 47/12 (2006.01) B02C 23/06 (2006.01)

Patent

CA 2267930

This invention provides a method for producing a microparticle which comprises pulverizing a solid preparation comprising a compound represented by formula (I), wherein ring A is an optionally substituted benzene ring; R is a hydrogen atom or an optionally substituted hydrocarbon group; B is an optionally esterified or amidated carboxyl group; X is -CH(OH)- or -CO-; k is 0 or 1; and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof and a biodegradable polymer of .alpha.-hydroxycarboxylic acid in the presence of a pulverizing auxiliary, which can provide microparticles which are less adhesive and involve less aggregation and are thus excellent in drug entrapment ratio and control of drug release in a desired particle size.

L'invention porte sur un procédé de production d'une microparticule, consistant à pulvériser une préparation solide comprenant un composé de formule (I) dans laquelle: le cycle A est un cycle benzénique facultativement substitué; R est un atome d'hydrogène ou un groupe hydrocarbure facultativement substitué, B est un groupe carboxyle facultativement estérifié ou amidé; X est -CH(OH)- ou -CO-; k vaut 0 ou 1; et n vaut 0, 1 ou 2, ou l'un de leurs sels pharmacocompatibles, et sur un polymère biodégradable de l'acide .alpha.-hydroxycarboxylique qui en présence d'un auxiliaire de pulvérisation peut produire des microparticules qui sont moins adhésives, moins enclines à l'agrégation, et de ce fait excellentes du point de vue du taux de capture des médicaments et de la régulation de la libération des médicaments, et cela pour la taille de particules désirée.

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