利多卡因醇质体的组方研究及其包封率测定

Investigation on Optimal Formula of Lidocaine Ethosome and Determination of Its Entrapment Efficiency

目的:研究制备5%利多卡因醇质体的最佳组方,并对其包封率进行测定。方法:采用正交实验设计设定5%利多卡因醇质体的组方并采用超声注入法进行制备;结合透析袋平衡透析法及高效液相色谱(HPLC)法测定各组方醇质体的包封率,以包封率为评价指标筛选出最佳组方。结果:5%利多卡因醇质体的最佳组方构成为:5%的利多卡因、35%的无水乙醇、5%蛋黄卵磷脂、0.2%的胆固醇及54.8%的超纯水;所制备5%利多卡因醇质体的包封率为(52.85±0.36)%。结论:本研究所采用的制备5%利多卡因及其包封率测定的方法简便、快速、准确,所制备的利多卡因醇质体的包封率较为理想,从而为相关后续研究奠定了基础。

Objective：To obtain optimal formula of 5% lidocaine ethosome with high entrapment efficiency. Methods：The orthogonal test was used to design the formula of 5% lidocaine ethosome which was prepared with ultrasonic injection method.The balanced dialysis with high performance liquid chromatogram（HPLC） analysis methods were used to determine the entrapment efficiency of lidocaine ethosome.The optimal formula of 5% lidocaine ethosome was selected by the highest entrapment efficiency. Results：The optimal formula of 5% lidocaine ethosome was 35% anhydrous ethanol、5% egg phosphatide and 0.2% cholesterol.The entrapment efficiency was 52.85±0.36%. Conclusion：The preparation technique was with ease and convenient,and entrapment efficiency determination method of 5% lidocaine ethosome were accurate.The entrapment efficiency of lidocaine ethosome was ideal which will facilitate the research work in the next stage.