Oral preparation comprising specific organic acid, and...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/485 (2006.01) A61K 9/14 (2006.01) A61K 9/20 (2006.01) A61K 9/48 (2006.01) A61K 47/12 (2006.01) A61K 47/16 (2006.01) A61P 1/14 (2006.01) A61P 13/02 (2006.01) A61P 17/04 (2006.01) A61P 25/04 (2006.01) C07D 489/02 (2006.01)

Patent

CA 2687558

Disclosed is a chemically stable oral preparation having an excellent elution property, which comprises a specific morphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient. Specifically disclosed is an oral preparation which comprises a specific morphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient, and additionally contains such an organic acid that 30 mL or more of water is needed for dissolving 1 g of the organic acid at 20~C. Also disclosed is a method for improving the elution property and the chemical stability of an oral preparation comprising a specific morphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient, which comprises adding such an organic acid that 30 mL or more of water is needed for dissolving 1 g of the organic acid at 20~C to the oral preparation.

La présente invention concerne une préparation orale stable sur le plan chimique présentant une excellente propriété d'élution qui renferme un dérivé de morphinane spécifique ou l'un de ses sels d'addition d'acide acceptables sur le plan pharmacologique en tant que principe actif. L'invention concerne spécifiquement une préparation orale qui renferme un dérivé de morphinane spécifique ou l'un de ses sels d'addition d'acide acceptables sur le plan pharmacologique en tant que principe actif et qui contient en outre un acide organique de telle manière que 30 ml d'eau ou plus sont nécessaires pour dissoudre 1 g de l'acide organique à 20 °C. L'invention a également pour objet un procédé d'amélioration de la propriété d'élution et de la stabilité chimique d'une préparation orale renfermant un dérivé de morphinane spécifique ou l'un de ses sels d'addition d'acide acceptables sur le plan pharmacologique en tant que principe actif, qui comprend l'addition d'un acide organique de telle manière que 30 ml d'eau ou plus sont nécessaires pour dissoudre 1 g de l'acide organique à 20 °C à la préparation orale.

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