利多卡因微乳制备及体外透皮吸收研究

Study on Lidocaine Microemulsion Preparation and In Vitro Transdermal Absorption

目的制备利多卡因微乳透皮载药系统,并对其理化性质及体外透皮行为进行考察。方法分别以油酸乙酯为油相,吐温-80为表面活性剂,无水乙醇为助表面活性剂,用水滴定的方法制备利多卡因微乳,绘制伪三元相图确定Km值,采用单纯网格法优化微乳,以稳态渗透速率和累积透皮量为指标,采用改良的Franz扩散池考察利多卡因微乳的体外透皮过程,并对其形态、粒径大小等进行了考察。结果优化微乳处方为油酸乙酯-吐温80-无水乙醇-重蒸水-利多卡因(3∶20∶7∶68∶2),微乳为淡黄色透明液体,平均粒径为78 nm。结论利多卡因微乳质量稳定,具有较好的透皮能力,可以为利多卡因经皮给药剂型选择提供参考。

Objective To prepare the transdermal drug delivery system of lidoeaine microemulsion and investigate the physioehemical property and in vitro transdermal behavior. Methods Ethylis oleate was as oil phase, Tween 80 as surfactant and absolute ethyl alcohol as cosurfaetant. Water titration method was used to prepare lidocaine mieroemulsion. The pseudo - ternary phase diagram was drawn and Km value was determined. The simplex grid method was used to optimize microemulsion. The steady state infiltration rate and cumulative transdermal amount were taken as indexes. The modified Franz diffuser was adopted to inves- tigate the in vitro transdermal process of lidocaine microemulsion, as well as its morphology and particle size. Results The prescription of optimized microemulsion ： ethylis oleate ： Tween 80 ： absolute ethyl alcohol ： heavy stem water：lidocaine = 3： 20： 7： 68：2. The microemulsion was light yellow transparent liquid,78 nm in mean diameter. Conclusion Lidocaine microemulsion is stable in quality and good in transdermal ability. It pro- vides the reference to the option of lidocaine percutaneous delivery.