HPLC法测定苯甲酸雌二醇贴片中药物的含量及其体外透皮释放量

Determination of content of estradiol benzoate in estradiol benzoate patches by HPLC and its skin permeation behavior in vitro

文中采用高效液相色谱法测定苯甲酸雌二醇贴片中苯甲酸雌二醇 (EB)的含量和体外透皮释放量。色谱柱为Nova PakC1 8(4 μm) 3 9mm× 1 95mm ,流动相为甲醇与水 ,体积比为 80∶2 0 ,使用紫外吸收检测器 ,检测波长为2 30nm。EB体外透皮释放实验采用单室Franz扩散池 ,测定结果为 :EB质量浓度在 4～ 1 4 μg/mL范围内呈线性 ,平均回收率为 95 2 % ,RSD为 2 85 % ,最小检出量为 0 0 1 5 μg ,日内和日间RSD分别为 0 81 % (n =5 )和 1 7%(n =5 ) ;体外透皮释放量与时间呈良好线性关系 ,相关因数为 0 993。本方法测定EB贴片药物含量操作简便 ,快速准确 ,体外药物透皮释放近似按零级速率释放 。

HPLC was used to determine the content of estradiol benzoate(EB) in an estradiol benzoate transdermal delivery system and that released by its skin permeation in vitro, with Nova Pak C 18 (4?μm) 3 9?mm×195?mm, methanol and water (80∶20) as mobile phase, and UV detector at 230?nm. The EB transcutaneous permeation in vitro was studied with Franz diffusion one cell apparatus. The result showed that the linear range of EB permeation was 4～14?μg/mL; average recovery of EB was 95 2%(RSD=2 85%) ; the detection limit was 0 015?μg; the precision of RSD was 0 81% in one day( n =5)and 1 7%( n =5)between days; the drug permeation rate with the time was in good linear, r =0 993. A simple, rapid and accurate way was provided to determine the content of estradiol benzoate in the patches. The transcutaneous permeation of EB in vitro followed zero order rules. Skin was the main resistance against the release of the drug.