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目的:建立0.1%他克莫司软膏体外透皮接收液中药物的HPLC测定方法,研究0.1%他克莫司软膏的体外透皮量。方法:采用Kromasil 100-5 C18色谱柱(250mm×4.6mm,5μm);流动相:乙腈-水-磷酸(690∶310∶1);流速:1.0ml/min;检测波长:215nm。体外透皮实验采用自制改良的Franz直立式扩散池,使用实验用离体乳猪皮作为透皮屏障。将自制凝胶与市售凝胶的透皮结果进行对比分析,分别在设定的1h、2h、4h、6h、8h、12h时间点取样测定透皮接收液中他克莫司的浓度,计算累积透皮量。结果:他克莫司的标准曲线方程为A=17408.1203×C+555.4604(r=0.9995),线性范围为2.036～20.36μg/ml,平均回收率为99.15%。结果表明,累积透皮量与时间呈现良好的线性关系,自制乳膏与市售乳膏的透皮结果无显著性差异(P>0.05)。结论:本检测方法操作简便,快速准确,是考察他克莫司软膏的体外透皮性能比较理想的方法。
OBJECTIVE: To establish a HPLC method for the determination of 0.1% tacrolimus ointment in vitro and to study the in vitro transdermal delivery of 0.1% tacrolimus ointment. Methods: Kromasil 100-5 C18 column (250 mm × 4.6 mm, 5 μm) was used. The mobile phase consisted of acetonitrile-water-phosphoric acid (690: 310: 1), the flow rate was 1.0 ml / min and the detection wavelength was 215 nm. In vitro transdermal experiments using self-made modified Franz upright diffusion cell, the experimental use of piglets in vitro as a transdermal barrier. The self-made gels were compared with the transdermal results of the commercially available gels, and the concentration of tacrolimus in the transdermal receiving fluid was sampled and measured at the set time points of 1h, 2h, 4h, 6h, 8h and 12h, respectively Cumulative transdermal volume. Results: The standard curve equation of tacrolimus was A = 17408.1203 × C + 555.4604 (r = 0.9995) with a linear range of 2.036 ~ 20.36μg / ml with an average recovery of 99.15%. The results showed that cumulative transdermal volume showed a good linear relationship with time, there was no significant difference (P> 0.05) between transdermal results of homemade cream and commercial cream. Conclusion: The method is simple, rapid and accurate, which is an ideal method to investigate the in vitro transdermal performance of tacrolimus ointment.