表没食子儿茶没食子酸酯软膏透皮吸收处方筛选

Prescription screening of EGCG ointment in the percutaneous absorption

目的建立表没食子儿茶素没食子酸酯(epigallocatechin gallate,EGCG)的高效液相色谱(high performaence liquid chromatograply,HPLC)测定方法,测定不同处方EGCG软膏在体外透皮吸收过程中接收液和皮肤中EGCG浓度,为EGCG软膏处方工艺优化提供参考依据。方法以裸鼠离体皮肤作为渗透屏障,以EGCG为检测指标,采用HPLC测定接收液和皮肤中药物浓度。色谱条件:色谱柱5C_(18)-MS-Ⅱ(4.6ID×250 mm),流动相乙腈:0.05%磷酸水溶液=18:82,流速:1 mL/min,检测波长:280 nm,柱温:30℃,进样量:20μL。结果在本实验中,皮肤中所含杂质不对样品测定产生干扰,线性关系良好(R^2=0.999),方法绝对回收率大于80%。三个批次的受检样品中,样品20150902P茶多酚软膏的皮肤中药物浓度最接近于国外进口的HPV对照软膏;接收池中样品未见吸收峰。结论样品20150902P茶多酚软膏的皮肤中药物浓度最接近于国外进口的HPV对照软膏,其处方最适于EGCG软膏透皮吸收。

Objective HPLC determination method was established to determine the EGCG concentration in the receiving solution and skin of different prescription EGCG ointment in the process of percutaneous absorption in vitro, and to provide reference basis for optimization of EGCG ointment. Methods Using the isolated skin of nude mice was as a permeability barrier, taking EGCG was as detection index, and using HPLC to determine drug concentration in the receiving solution and skin. Chromatographic condition： chromatographic column5C 18 -MS-Ⅱ（4.6ID×250 mm）, Mobile phase： acetonitrile：0.05% phosphoric acid aqueous solution =18∶82, flow rate： 1 mL/min, detection wavelength： 280 nm, Column temperature： 30℃. sample volume： 20 μL. Results In this experiment, the impurities contained in the skin do not interfere with the determination of the samples, the linear relationship is good （ R 2 =0.999）, and the absolute recovery rate is greater than 80%. In the three batches of samples tested,the drug concentration of Sample 20150902P tea polyphenol ointment in the skin is the most close to foreign import HPV control ointment,and no absorption peak was found in the receiving pool. Conclusion The drug concentration of Sample 20150902P tea polyphenol ointment in the skin is the most close to foreign import HPV control ointment,and the best for EGCG ointment penetration.