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Pharmaceutical compositions comprising a glucocorticoid or glucocorticoid derivative encapsulated in a liposome

机译:包含包裹在脂质体中的糖皮质激素或糖皮质激素衍生物的药物组合物

摘要

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.
机译:本发明提供了药物组合物,其包含稳定地包封在脂质体中的糖皮质激素或糖皮质激素衍生物。糖皮质激素或糖皮质激素衍生物选自pKa等于或小于11且在pH 7下的logD在-2.5至1.5之间的两亲性弱碱型糖皮质激素或糖皮质激素衍生物。或两亲性弱酸GC或GC衍生物,其pKa大于3.5,且pH 7的logD在-2.5至1.5之间。用多发性硬化和癌症的合适模型在体内显示了本发明的药物组合物的治疗效果。

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