丹皮酚泡囊乳膏的制备及其体外透皮吸收考察

目的 以泡囊为载体制备丹皮酚乳膏，优化丹皮酚乳膏的制备工艺及制备处方，并考察体外透皮吸收情况。方法 用乙醇注入法制备丹皮酚泡囊；用乳化法制备丹皮酚乳膏；应用控制变量法优化制备工艺；采用正交设计优化制备处方；并采用TP-6型透皮扩散实验仪，以大鼠腹部离体皮肤作为渗透屏障，通过高效液相色谱法测定药物的累计渗透量来考察丹皮酚乳膏体外透皮吸收情况。结果 基于丹皮酚泡囊制得的乳膏在12 h和24 h的累积渗透量分别是丹皮酚原料药的1.1倍和1.2倍，在24 h时皮内药物滞留量是丹皮酚原料药乳膏的1.26倍。结论 基于丹皮酚泡囊制得的乳膏在有效期内各时间段的体外透皮吸收高于原料药乳膏，且丹皮酚泡囊乳膏的皮内滞留量明显高于丹皮酚原料药乳膏。

Preparation of Vesicle-entrapped Paeonol Cream and Evaluation of Its Percutaneous Absorption in Vitro

Objective To prepare vesicle-entrapped paeonol cream, optimize the preparation process and formula of paeonol cream, and to evaluate its percutaneous absorption in vitro. Methods The vesicle-entrapped paeonol was prepared by the ethanol-injection method. Paeonol cream was prepared by emulsion. The preparation process and formula were optimized by variable adjustment and orthogonal design, respectively. In order to investigate the percutaneous absorption of paeonol cream in vitro, the cumulative infiltration of the cream through the abdominal skin excised from the rat on TP-6 percutaneous diffusion cell was measured by high-performance liquid chromatography. Results The cumulative infiltration of the vesicle-entrapped paeonol cream within 12 and 24 hours was 1.1 and 1.2 times that of raw paeonol cream, respectively. The cutaneous retention of vesicle-entrapped paeonol cream within 24 hours was 1.26 times that of raw paeonol cream. Conclusion Compared with raw paeonol cream, vesicle-entrapped paeonol cream has higher percutaneous absorption in vitro within different periods before expiration and substantially higher cutaneous retention.