丹皮酚作为体外透皮吸收试验指标物质的研究

Study with paeonol as the index substance of transdermal absorption test

目的:建立高效液相色谱-紫外(HPLC-UV)法测定体外透皮吸收实验中丹皮酚的含量的方法,并进行方法学研究,研究以丹皮酚作为体外透皮吸收试验的质控对照体系的可能性。方法:采用体外扩散池法进行透皮吸收试验,以HPLC-UV法检测1,20,100 mg·mL^(-1)的丹皮酚溶液在猪背部和腹部皮肤1,2,4,6,8,12,24 h的累积渗透率,并且考察了20 mg·mL^(-1)丹皮酚溶液在冻融1～5次的猪背部皮肤上各时间点的累积渗透率。结果:丹皮酚在生理盐水中10.38～103.80μg·mL^(-1)线性关系良好,进样精密度良好(RSD=1.7%),在生理盐水中24 h稳定(RSD=1.9%),平均回收率为98.8%,丹皮酚浓度越高累积渗透率越高,猪背部皮肤的透过性优于腹部皮肤,冻融3次以上的皮肤透过性显著降低。结论:丹皮酚透皮吸收性良好,其检测方法简便快速,可作为体外透皮吸收试验的质控对照物质。

OBJECTIVE To establish a HPLC-UV method for determination of paeonol in transdermal absorption test,and perform methodological validation,study the possibility of paeonol as a control system for transdermal absorption test. METHODS The in vitro skin permeation experiment was conducted by using diffusion cells,the cumulative permeability values of 1,20,100 mg·mL^-1 paeonol solutions on the skin of the back and abdomen of the pig were determined by HPLC at 1,2,4,6,8,12 and 24 h. The cumulative permeability of 20 mg·mL^-1 paeonol solution on the skin of the back for 1-5 freezing and thawing cycles at different times were observed. RESULTS The calibration curve was linear over the range of 10. 38^（-1）03. 80 μg·mL^-1. The injection precision was good,the solution was stable for 48 h,and the average recovery was 98. 8%. The cumulative permeability was increased with paeonol concentration. The permeability of the back skin was better than that of the abdomen skin. The permeability of 3 freezing and thawing cycles was significantly decreased. CONCLUSION The paeonol has good transdermal absorption and simple detection method,and can be used as index substance of transdermal absorption test.