醋酸曲安奈德益康唑乳膏体外透皮吸收的评价试验

目的建立高效液相色谱(HPLC)法测定醋酸曲安奈德益康唑乳膏体外透皮接收液中药物的含量,验证自制与上市产品体外透皮吸收的一致性。方法采用色谱柱:辛烷基硅烷键合硅胶为填充剂(250mm×4.6mm,5μm);流动相:以0.094%无水己烷磺酸钠(水-乙腈-异丙醇)溶液为流动相A,以0.094%己烷磺酸钠(水-甲醇)溶液为流动相B,梯度洗脱;柱温40℃;检测波长227 nm;流速1.0 mL/min;进样量20μL。体外透皮实验采用改进的Franz立式扩散池,以实验用离体乳猪皮为透皮屏障,对比自制醋酸曲安奈德益康唑乳膏与市售乳膏的透皮效果,分别在一定时间点取样测定透皮接收液中醋酸曲安奈德和硝酸益康唑的浓度,计算其累积透皮吸收量、皮肤残留量及皮肤表面剩余量。结果自制乳膏和市售乳膏12h平均累计渗透量分别为11.1085μg/cm~2、11.7150μg/cm~2;透皮速率分别为1.3733μg/(cm~2·h)、1.4441μg/(cm~2·h);醋酸曲安奈德总体平均回收率分别为100.9%、99.9%;硝酸益康唑总体平均回收率分别为88.8%、86.8%,两者平均累计渗透量和总体平均回收率均无显著性差异(P0.05)。结论自制和市售乳膏在透皮吸收上具有一致性。

Evaluation of Percutaneous Absorption of Triamcinolone Acetonide Acetate and Econazole Nitrate Cream in vitro

Objective To establish an HPLC method for quantitative determination of Triamcinolone Acetonide Acetate and Econazole Nitrate Cream in vitro percutaneous solution,and verify the consistency of the vitro percutaneous absorption of self-made products and market products.Methods Chromatographic column:C8 (250mm × 4.6mm,5 μm);mobile phase:gradient elution:0.094％ anhydrous sodium hexanesulfonate solution (purified water-acetonitrile -isopropyl alcohol) as mobile phase A,with 0.094％ sodium hexanesulfonate solution (purified water-methanol) as mobile phase B;column temperature:40℃C;detection wavelength:227nm;flow rate:1.0 mL/min.Injection:20μL.Improved Franz vertical diffusion cell were used in vitro permeation studies and excised minipig's skins in vitro as transdermal barrier.The concentration of Triamcinolone Acetonide Acetate and Econazole Nitrate in vitro pereutaneous absorption was determined by HPLC to investigate its cumulative permeation quantity at different time respectively,and calculate its cumulative permeation quantity,residual quantity of skin and residual quantity of skin surface to evaluate the transdermal effect of self-made cream and commercial cream.Results For self-made products and market products,12h average cumulative permeation quantity of was 11.1085μ.g/cm2,11.7150μg/cm2respectively;the skin permeation rate was 1.3733 μg/(cm2 · h),1.4441 μg/(cm2 · h) respectively;the overall average recovery rates of Triamcinolone Acetonide Acetate were 100.9％ and 99.9％,and Econazole Nitrate were 88.8％ and 86.8％ respectively.There was no significant difference between the average cumulative permeation quantity and overall average recovery rate of the self -made cream and commercial cream (P ＞ 0.05).Conclusion According to the above analysis result,it can be proved that the self-made cream and commercial cream are consistent in the transdermal absorption.