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氢化可的松从所选胆固醇N-酰基酯固溶体中的表面张力降低及溶解速率

Surface tension lowering and dissolution rate of hydrocortisone from solid solutions of selected n-acyl esters of cholesterol.

作者信息

Kim K H, Jarowski C I

出版信息

J Pharm Sci. 1977 Nov;66(11):1536-40. doi: 10.1002/jps.2600661108.

Abstract

The dissolution of hydrocortisone into simulated intestinal fluid from lipid delivery systems followed second-order kinetics. As the ratio of hydrocortisone to lipid was increased from 1:1 to 1:6, the dissolution rate decreased. Solvent deposition of solid solutions of hydrocortisone and lipid on lactose resulted in the enhancement of the dissolution rate. For the 1:1 hydrocortisone-lipid solid solutions, the rank order of the dissolution rate was hydrocortisone-cholesteryl stearate, hydrocortisone, hydrocortisone-cholesterol, hydrocortisone-cholesteryl acetate, hydrocortisone-cholesteryl palmitate, hydrocortisone-cholesteryl n-butyrate, hydrocortisone-cholesteryl laurate, and hydrocortisone-cholesteryl n-decylate. A direct correlation was found between the dissolution rate of hydrocortisone and the surface tension lowering of simulated intestinal fluid by the corticoid and various lipids.

摘要

氢化可的松从脂质给药系统溶解到模拟肠液中遵循二级动力学。随着氢化可的松与脂质的比例从1:1增加到1:6,溶解速率降低。氢化可的松和脂质的固溶体在乳糖上的溶剂沉积导致溶解速率提高。对于1:1的氢化可的松 - 脂质固溶体,溶解速率的排序为氢化可的松 - 硬脂酸胆固醇酯、氢化可的松、氢化可的松 - 胆固醇、氢化可的松 - 乙酸胆固醇酯、氢化可的松 - 棕榈酸胆固醇酯、氢化可的松 - 正丁酸胆固醇酯、氢化可的松 - 月桂酸胆固醇酯和氢化可的松 - 正癸酸胆固醇酯。发现氢化可的松的溶解速率与皮质类固醇和各种脂质对模拟肠液表面张力的降低之间存在直接相关性。

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