United States Patent:  6,057,289

Assignee:  Pharmasolutions, Inc. (Cranbury, NJ)

Filed:  April 30, 1999

The present invent is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of cyclosporin in association with a pharmaceutical carrier, said carrier comprising a drug solubilizing effective amount of a fatty acid having 6-22 carbon atoms and a non-ionic surfactant.

SUMMARY OF THE INVENTION

The present invention is directed to a pharmaceutically acceptable carrier to be used in association with cyclosporin, said pharmaceutically acceptable carrier preferably having similar lipophilicity to the cyclosporin, thereby providing maximal solubility for the drug. In an embodiment thereof, the present invention encompasses this pharmaceutically acceptable carrier associated with a pharmaceutically effective amount of cyclosporin, said carrier comprising (a) a cyclosporin solubilizing agent consisting essentially of C₆ -C₂₂ fatty acids present in an amount sufficient to solubilize the cyclosporin therein and (b) a water soluble non-ionic surfactant, said surfactant being present in an amount sufficient to form an emulsion, and more preferably a fine emulsion and most preferably a microemulsion when in contact with an aqueous medium, especially the aqueous medium found in mammals. The present invention is also directed to a pharmaceutical composition comprising the carrier described hereinabove and the cyclosporin. Moreover, the present invention is also directed to a method of enhancing the solubility of cyclosporin in a pharmaceutical composition containing same, comprising thoroughly mixing the cyclosporin with a cyclosporin solubilizing agent consisting essentially of fatty acids, containing 6-22 carbon atoms. Moreover, the present invention is directed to a method of forming a pharmaceutical composition containing cyclosporin as the active therapeutic agent capable of forming an emulsion and more preferably a fine emulsion and most preferably a microemulsion when in contact with water or an aqueous system, which method comprises thoroughly mixing the cyclosporin with the carrier as defined herein to form an emulsion, preferably a fine emulsion and most preferably a microemulsion, when in contact with an aqueous medium.

Claim 1 of 28 Claims

1. A pharmaceutical composition comprising a pharmaceutically effective amount of cyclosporin in association with a pharmaceutical carrier, said carrier comprising (a) a cyclosporin solubilizing agent consisting essentially of a solubilizing effective amount of a fatty acid of C₆ -C₂₂ carbon atoms, and (b) a non-ionic surfactant having an HLB value greater than 10, said non-ionic surfactant being present with the cyclosporin solubilizing agent and cyclosporin in an amount sufficient to form an emulsion when brought into contact with an aqueous medium in a mammal.

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