油酸-吐温20、丙二醇系统对盐酸利多卡因透皮吸收的作用

The Effects of Lidocaine Hydrocholoride Emulsion Transdermal Penetration by the Oleic Acid-tween20,Propylene Glycol System

目的观察以丙二醇(PGL)、油酸(OA)为透皮促进系统,吐温20为油酸增溶剂的乳剂盐酸利多卡因的时间依赖性累积透皮量,选出透皮吸收最佳的配方。方法运用析因设计方法研究不同比例的丙二醇、油酸、吐温20对盐酸利多卡因经皮渗透作用。采用三元相图方法确定增溶剂吐温20的用量。结果油酸与吐温最佳比率为1∶9;5%的丙二醇与5%的油酸、15%的丙二醇与3%的油酸对盐酸利多卡因的渗透促进作用最强;两者存在着显著的相互作用;盐酸利多卡因单位面积的累积透皮量与时间的线性关系良好。结论多元透皮促进系统的合理配方对盐酸利多卡因表面麻醉剂具有良好的透皮促进作用。

Objective To study the accumulated amount of lidocaine hydrocholoride transport through isolated rats skin depending on different time by each formula of oleic acid ＋ tween20 ＋ propylene glycol （ OA ＋ Tween20 ＋ PGL） as penetration enhancers system, Methods To adopt factorial analysis design ; （ OA ＋ Tween20） and PGL as 2 factors 3 levels respectively, establishing the list of factorial analysis ; Using Franz cell as experimental diffusion instrument ; abdominal skins of SD rats as transdermal barrier, At different time to draw the liquid from the receptor to test the concentration of lidocaine hydrocholoride , Using the technique of 3D diagram of solubilization to determine the optimal ratio between oleic acid and tween20; the orthogonal range analysis had also been performed to describe the effects on the penetration of lidocaine hydrocholoride between OA and PGL, Results The ratio of OA to tween20 was 1 ： 9 ;The optiomal formulas were 5% （PG） ＋ 5% （OA） 与 15% （PG） ＋ 3% （OA） which possess 393.190 （μg/cm2h） and 357.588 （μg/cm2h） respectively, Each Q - t has good nature of linear regression; each level of PGL and OA exists remarkable difference（ P = 0.000 -0.022）. Propylene glycol and oleic acid exists marked interaction in permeation of lidocaine hydrocholoride （ P 〈 0,001 ） ; OA had more marked effects on the penetration of lidocaine hydrocholoride, than PGL , Conclusion Between PGL and OA exists marked interaction to promoting permeation of lidocaine hydrocholoride and proving that PGL works well in coordination with OA at reseanable formulas.