活血祛瘀巴布剂体外释放度及离体小鼠经皮渗透行为与动力学考察

The Transdermal Release Rate and the Pharmacokinetic Characteristics of Huoxue Quyu Cataplasm In Vitro and in Mice

目的研究活血祛瘀巴布剂中丹参素钠、原儿茶醛、阿魏酸、迷迭香酸与丹酚酸B体外释放度,以及离体小鼠透皮率及动力学方程。方法采用桨碟法进行活血祛瘀巴布剂体外释放度实验;采用改良France扩散池以离体小鼠皮肤为屏障,分别对接受液采用高效液相色谱(HPLC)法测定有效成分。结果活血祛瘀巴布剂丹参素钠、原儿茶醛、阿魏酸、迷迭香酸以及丹酚酸B180 min累积释放度分别为89.40%,86.39%,88.94%,87.19%,90.05%;活血祛瘀巴布剂中丹参素钠、原儿茶醛、阿魏酸、迷迭香酸以及丹酚酸B离体小鼠皮肤24 h透皮率分别为29.83%,28.69%,30.14%,30.03%,30.60%,动力学拟合方程符合Higuchi方程,拟合度均达到0.9。结论活血祛瘀巴布剂释放度良好,透皮率高,动力学方程表明其为骨架型缓释制剂。

Objective To study the in vitro drug release,transdermal rate and the pharmacokinetic characteristics of active component of Huoxue Quyu cataplasm,including Danshensu sodium,protocatechuic aldehyde,ferulic acid,rosmarinic acid and salvianolic acid B.Methods The effective components of the cataplasm were determined by HPLC after the processes of paddle plate and modified France diffussion pool.Results The cumulative releases in 180 min of danshensu sodium,protocatechuic aldehyde,ferulic acid,rosemic acid,and salbutamol acid B in the Huoxue Quyu cataplasm agent reached 89.40%,86.39%,88.94%,87.19%and 90.05%respectively;The skin transdermal rates of danshensu sodium,protocatechuic aldehyde,ferulic acid,rosmarinic acid,and salvianolic acid B isolated mice in 24 hours were 29.83%,28.69%,30.14%,30.03%and 30.60%;The kinetic fitting equation conforms to the Higuchi equation,and the quasi-compatibility degree has reached 0.9 or more.Conclusion The release rate of Huoxue Quyu cataplasm is good and the permeability is high.The kinetic equation shows that it is a skeleton sustained release preparation.