丹参双相载药亚微乳注射液的研制

Preparation and characteristics of Salvia miltiorrhiza biphasic drug-loading lipid microemulsion for injection

目的制备同时含有丹参酮及丹酚酸的静脉注射剂。方法以丹参脂溶性成分丹参酮ⅡA和水溶性成分丹酚酸B作为指标性成分,水溶性提取物与脂溶性提取物质量比10∶1,以中链油作为油相,大豆磷脂作为主要乳化剂,分别将水溶性成分溶于水相,脂溶性成分溶于油相,采用高压均质法制备丹参双相载药亚微乳注射液。结果制剂的外观呈棕褐色,粒径(200±50)nm,zeta电位在-20^-40 mV之间;30 min旋转水浴灭菌后,制剂外观无明显变化,zeta电位略有升高;指标性成分测定结果显示,水溶性成分85%分布在水相中,脂溶性成分90%分布在油相中。结论制备丹参双相载药亚微乳是可行的;脂溶性成分与水溶性成分分别存在于与其性质相适应的油相和水相中。

Objective To investigate the preparation technology of Salvia miltiorrhiza biphasic drug-loading lipid microemulsion and its related physico-chemistry properties. Methods Tanshinone ⅡA and salvianolic acid B were adopted as index ingredients for lipid-soluble components and water-soluble components respectively with ratio of 10： 1. Middle chain triglycerides were selected as oil phase. Liposoluble extractive was dissolved in oil and water-soluble in water. Soybean phospholipid acted as primary emulsifier. High-pressure homogenization was adopted to prepare the biphasic drug-loading lipid microemulsion. Results The lipid microsemulsion presented brown color. Its particle size distribution was about 200 nm and its zeta-potential was between - 20- - 40 mV. After sterilization for 30 min in rotating water-bath, there was no conspicuous alteration of its appearance, but the zeta potential of the microemulsion rose a little. The determination of the index ingredients indicated that 85% of the water-soluble components distributed in aqueous phase, and 90% of the liposoluble components distributed in oil phase. Conclusions It is feasible to prepare Salvia miltiorrhiza biphasic drug-loading lipid microemulsion, the distribution of the two kinds of drug is consistent with their properties.