A process for preparing formulations of lipophilic active...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/19 (2006.01) A61K 31/352 (2006.01)

Patent

CA 2585314

The present invention is related to a method for the preparation of a pharmaceutical composition comprising a lipophilic compound and a glass of a sugar, a sugar alcohol, a mixture of sugars or a mixture of sugars alcohols, wherein the lipo philic compound is incorporated in the sugar glass, characterized in that a. said lipophilic compound is dissolved in an organic solvent that is miscible with water and said sugar, sugar alcohol, mixture of sugars or mixture of sugar alcohols is dissolved in water; b. the dissolved lipophilic compound and the dissolved sugar, sugar alcohol, mixture of sugars or mixture of sugar alcohols are mixed in such a way that a homogeneous mixture is obtained; c. said mixture is spray freeze dried. The invention is further related to pharmaceutical formulations formed containing lipophilic compounds such as .DELTA.9-tetrahydrocannabinol, diazepam and cyclosporin A.

La présente invention décrit une méthode d'élaboration d~une préparation pharmaceutique comprenant un composé lipophile et un verre d~un sucre, d~un polyol sucré, d'un mélange de sucres ou d'un mélange de polyols sucrés. Ledit composé lipophile est incorporé dans le verre de sucre. Ladite préparation est caractérisée en ce que : a. ledit composé lipophile est dissous dans un solvant organique miscible à l~eau et ledit sucre, polyol sucré, mélange de sucre ou mélange de polyols sucrés est dissous dans l~eau ; b. ledit composé lipophile dissout et ledit sucre, polyol sucré, mélange de sucre ou mélange de polyols sucrés dissous sont mélangés de façon à obtenir un mélange homogène ; c. ledit mélange est lyophilisé par pulvérisation. La présente invention décrit également des formules pharmaceutiques contenant des composés lipophiles tels que le .DELTA.9-tétrahydrocannabinol, le diazépame et la cyclosporine A.

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