Oral pharmaceutical composition of a poorly water-soluble...

A - Human Necessities – 61 – K

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Details

A61K 9/20 (2006.01) A61K 9/48 (2006.01) A61K 31/55 (2006.01) A61K 45/08 (2006.01)

Patent

CA 2654243

Provided in the present invention are improved oral pharmaceutical compositions comprising at least one poorly water soluble active agent, preferably endothelin conversion enzyme (ECE) inhibitor and/or neutral endopeptidase (NEP) inhibitor in an amount greater than 10% w/w of the composition, more preferably, with the alkali system co mprising a mixture of at least two alkaline compounds in the ratio 1:20 to 20:1, the active agent is SLV-306 or its pharmaceutically acceptable salts, esters, hydrates, solvates, isomers or derivatives thereof; a alkali system in an amount greater than 10% w/w of the composition preferably comprising a mixture of at least two alkaline compounds and optionally one or more pharmaceutically acceptable excipients. Also provided are process for preparation of such improved compositions and method of using such composition.

La présente invention concerne des compositions pharmaceutiques améliorées, destinées à une administration par voie orale, comprenant au moins un agent actif peu soluble dans l'eau, de préférence un inhibiteur de l'enzyme de conversion de l'endothéline (ECE) et/ou un inhibiteur de l'endopeptidase neutre (NEP) à hauteur de plus de 10 % poids/poids de la composition, le système alcalin comprenant, mieux encore, un mélange d'au moins deux composés alcalins présents selon un rapport de 1 : 20 à 20 : 1, l'agent actif étant le SLV-306 ou un sel, ester, hydrate, solvate, isomère ou dérivé de celui-ci acceptable sur le plan pharmaceutique ; un système alcalin à hauteur de plus de 10 % poids/poids de la composition comprenant, de préférence, un mélange d'au moins deux composés alcalins et, éventuellement, un ou plusieurs excipients acceptables sur le plan pharmaceutique. L'invention concerne également un procédé de préparation de telles compositions améliorées et un procédé d'utilisation d'une telle composition.

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