利多卡因巴布剂体外透皮吸收研究

Study on Percutaneous Permeability of Lidocaine Cataplasms in Vitro

目的:本研究采用小型猪皮作为透皮试验模型,比较利多卡因巴布剂自制品和市售参比制剂的体外透皮吸收效果。方法:建立高效液相色谱法测定利多卡因巴布剂中药物的体外透皮吸收量。色谱条件为:色谱柱为Elite Hypersil ODS2(5μm,4.6 mm×150 mm);流动相为醋酸盐缓冲液(930 mL水中加入冰醋酸10 mL,以1 mol/L的Na OH溶液调pH至6.0)-甲醇(50∶50);流速:1.0 mL/min;检测波长为254 nm;进样量为20μL。体外透皮实验采用改良的Franz扩散池,以小型猪皮作为透皮试验模型,分别在2 h、4 h、6 h、8 h、10 h和12 h取样测定透皮接收液中利多卡因的浓度,计算累积透过率。结果:自制品和市售参比制剂12 h平均累积透过率分别为195.61μg/cm^2和197.90μg/cm^2,不同时段透皮吸收累积量差异无统计学意义。结论:利多卡因巴布剂自制品和市售参比制剂的体外透皮吸收效果基本一致。

Objective： In this study, small pigskin was used as a transdermal test model to compare the transdermal absorption of lidocaine gel self-made products and commercial reference preparations in vitro. Methods： To establish a HPLC method for determination of transdermal absorption of lidocaine gel in vitro. The chromatographic conditions were as follows： the column was Elite Hypersil ODS2（5 μm, 4.6 mm×150 mm）; the mobile phase was acetate buffer（10 mL glacial acetic acid was added to 930 mL water and adjusted to 6.0 with 1 mol/L NaOH solution） 50∶50）; flow rate： 1.0 mL/min; detection wavelength was 254 nm; injection volume was 20 μL. In vitro transdermal experiment using modified Franz diffusion cell, small pigskin as a transdermal test model, respectively, at 2 h, 4 h, 6 h, 8 h, 10 h and 12 h sample was measured transdermally received lidocaine concentration, calculated cumulative Through rate. Results： The average cumulative transmittivities of self-made and commercially available reference preparations at 12 h were 195.61 μg/cm^2 and 197.90 μg/cm^2, respectively. There was no significant difference in transdermal absorption accumulation at different time points. Conclusion： The effects of transdermal absorption of lidocaine gel self-made products and reference formulations in vitro are basically the same.