Enhanced delivery of immunosuppressive drug compositions for...

A - Human Necessities – 61 – K

Patent

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A61K 31/436 (2006.01) A61K 9/72 (2006.01) A61P 37/06 (2006.01)

Patent

CA 2678455

The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non- polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

La présente invention concerne les compositions et procédés pour la fabrication et l'utilisation d'un agrégat nanostructuré substantiellement amorphe à dissolution rapide et à haute efficacité pour l'administration pulmonaire de tacrolimus et une matrice stabilisante comprenant, de manière facultative, un surfactant polymérique ou non polymérique, un saccharide polymérique ou non polymérique ou les deux, dans laquelle l'agrégat comprend une surface supérieure à 5 m2/g, comme mesuré par l'analyse BET et exhibe une sursaturation pour au moins 0,5 heures si une quantité correspondante à 11 à 15 fois la solubilité cristalline aqueuse du tacrolimus est ajoutée au fluide simulé du poumon.

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