微乳对难溶性药物增溶机理的研究

目的:初步探讨微乳对难溶性药物的增溶机理.方法:经处方筛选及相图研究确定(BL-9/正丁醇3∶1)/油/水比例为9∶1∶40的微乳处方;以二氢吡啶类药物为模型药物,测定其在微乳、胶束和油相中的溶解度及油/水分配系数;根据化学结构,采用计算机软件计算药物的特性参数,并结合模型药物的特性分析微乳增溶难溶性药物的机理.结果:微乳对药物的增溶效果远大于油相和胶束,并随药物的脂溶性和空间结构的改变而变化.结论:微乳可用于增溶难溶性药物,且脂溶性越大,空间位阻越小,增溶效果越明显.

Study on the Mechanism of Lipophilic Drugs Incorporation into Microemulsion System

AIM:To study the mechanism of lipophilic drugs incorporation into O/W microemulsion system.METHOD:The formulation of microemulsion was optimized based on the results of the pseudo-termary phase diagram.The oil/water partition coefficient and the solubility of the dihydropyridines in the microemulsion,micelle and oil phase were measured,respectively.The characteristic parameters of the drugs which were calculated by the computer based on their chemical structures were used to analyze the mechanism of drugs incorporation into O/W microemulsion system.RESULT:The solubility of drugs in the microemulsion was far larger than that in the micelle and oil phase,which was related with its lipophilic and space structure.CONCLUSION:Improvement of the solubility by the microemulsion system is significant for the high lipophilic and low molecular bulk drugs.