Pharmaceutical compositions containing nsaid and bile acids

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/28 (2006.01) A61K 9/00 (2006.01) A61K 9/48 (2006.01) A61K 9/50 (2006.01) A61K 31/16 (2006.01) A61K 31/19 (2006.01) A61K 31/405 (2006.01) A61K 31/54 (2006.01) A61K 45/00 (2006.01)

Patent

CA 2137573

Non-steroidal anti-inflammatory drugs, such as indomethacin, and other pharmaceutically active compounds, are formulated with bile acids or their salts and conjugates. Bile acids previously proposed for use in such formulations have placed an un-acceptable toxic load on the liver and/or cells of the gastrointestinal tract, causing abnormal liver function or cell erosion. In this invention, the bile acid is a low detergent bile acid, such as ursodeoxycholate. Stabilization of the bile acid pool results in enhanced and predictable enterohepatic recycling of NSAIDs (and other drugs) and a reduced risk of toxicity.

Des anti-inflammatoires non stéroïdiens, comme l'indométhacine, et d'autres composés d'usage pharmaceutique sont formulés à partir d'acides biliaires ou de leurs sels et conjugués. Les acides biliaires, dont l'utilisation a déjà été proposée dans de telles formulations, ont imposé une charge toxique inacceptable sur le foie et/ou les cellules du tractus gastro-intestinal, causant un fonctionnement anormal du foie ou l'érosion des cellules. Dans cette invention, l'acide biliaire est un acide biliaire faiblement détersif, comme l'ursodésoxycholate. La stabilisation du pool d'acides biliaires résulte en un recyclage entérohépatique amélioré et prévisible des AINS (et d'autres médicaments) et un risque de toxicité moindre.

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