Liposomal compositions of glucocorticoid and glucocorticoid...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 31/573 (2006.01)

Patent

CA 2579695

The present invention provides pharmaceutical compositions comprising a glucocorticoid or glucocorticoid derivative stably encapsulated in a liposome. The glucocorticoid or glucocorticoid derivative is selected from an amphipathic weak base glucocorticoid or glucocorticoid derivative having a pKa equal or below 11 and a logD at pH 7 in the range between -2.5 and 1.5; or an amphipathic weak acid GC or GC derivative having a pKa above 3.5 and a logD at pH 7 in the range between -2.5 and 1.5. The therapeutic effect of the pharmaceutical composition of the invention was exhibited in vivo with appropriate models of multiple sclerosis and cancer.

L'invention concerne des compositions pharmaceutiques comprenant un glucocorticoïde ou un dérivé de glucocorticoïde encapsulé de manière stable dans un liposome. Le glucocorticoïde ou le dérivé de glucocorticoïde est sélectionné entre un glucocorticoïde ou un dérivé de glucocorticoïde bipolaires faiblement basiques présentant un pKa inférieur ou égal à 11 et un logD, à pH 7, compris entre 2,5 et 1,5; et un glucocorticoïde ou un dérivé de glucocorticoïde bipolaires faiblement acides présentant un pKa supérieur à 3,5 et un logD, à pH 7, compris entre 2.5 et 1,5. L'effet thérapeutique de cette composition pharmaceutique a été démontré in vivo dans des modèles appropriés de sclérose en plaque et de cancer.

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