Sustained release preparation containing metal salt of a...

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/34 (2006.01) A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 9/52 (2006.01) A61K 38/18 (2006.01) A61K 38/19 (2006.01) A61K 38/21 (2006.01) A61K 38/27 (2006.01) A61K 38/28 (2006.01)

Patent

CA 2196184

A sustained-release preparation containing a water-insoluble or slightly water- soluble polyvalent metal salt of a water-soluble peptide type of physiologically active substance except for an endothelin antagonist and a biodegradable polymer. The present invention is a sustained-release preparation that is highly efficient in incorporating a water-soluble peptide type of physiologically active substance except for an endothelin antagonist and suppresses initital burst of the water- soluble peptide type of physiologically active substance except for an endothelin antagonist. The sustained-release preparation of the present invention is capable of releasing the water-soluble peptide type of physiologically active substance except for an endothelin antagonist while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble peptide type of physiologically active substance except for an endothelin antagonist in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity.

Préparation à libération prolongée renfermant un sel métal polyvalent, insoluble ou légèrement soluble dans l'eau, d'un type peptidique soluble dans l'eau d'une substance physiologiquement active sauf par rapport à l'antagoniste de l'endothéline, ainsi qu'un polymère biodégradable. L'invention concerne une préparation à libération prolongée dans laquelle il est possible d'incorporer de manière très efficace un type peptidique soluble dans l'eau d'une substance physiologiquement active sauf vis-à-vis d'un antagoniste de l'endothéline et qui permet d'éviter la libération initiale brutale du type peptidique. Cette préparation est capable de libérer le type peptidique hydrosoluble de substance physiologiquement active excepté vis-à-vis d'un antagoniste de l'endothéline et de conserver sa bioactivité après administration in vivo. En outre, ledit type peptidique hydrosoluble de substance physiologiquement active excepté vis-à-vis d'un antagoniste de l'endothéline, contenu dans la préparation est maintenu stable sur une longue période, avec une faible perte de bioactivité.

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