止痛凝胶膏剂体外透皮行为研究

Study on transdermal behavior of Zhitong cataplasm

该试验旨在测定止痛凝胶膏剂中有效成分的含量,研究其体外透皮吸收特性。以阿魏酸和欧前胡素为指标,用甲醇提取止痛凝胶膏剂中有效成分,以HPLC同时测定2种成分的含量。采用改良的Franz扩散池法,以裸鼠腹皮为体外模型,选择合适的接收液,测定接收液和皮中阿魏酸和欧前胡素的含量。止痛凝胶膏剂中阿魏酸和欧前胡素的质量分数分别为455.10,371.66μg·g-1。以20%乙醇-磷酸盐缓冲液(pH=8)做接收液,止痛凝胶膏剂中阿魏酸和欧前胡素透皮速率分别为1.29,0.15μg·h-1·cm-2,24 h的累积透过量分别为30.03,3.31μg·cm-2,累积透过率分别为41.45%,5.60%,在皮中的滞留量分别为0.69,2.60μg·cm-2,滞留率分别为0.95%,4.40%。止痛凝胶膏剂中,阿魏酸的体外透皮行为接近零级过程,皮肤角质层是其主要限速因素;欧前胡素的体外透皮行为符合Higuchi方程,渗透过程受药物释放和皮肤的限制。

The aim of the present research was to study the transdermal absorbability of ferulic acid and imperatorin in Zhitong cataplasm. Using methanol to extract the effective components, HPLC was established to determine drug content in Zhitong cataplasm. The excised abdominal skin of nude rats was used as the peimeation model Utilizing the modified Franz diffusion cell, the suitable re- ceiving solution was elected. The contents of ferulic acid and imperatorin in Zhitong cataplasm were 455.10,371.66 μg·g^-1, respec- tively. Taken 20% ethanol- PBS（ pH 8） as receiving solution, ferulic acid and imperatorin could be detected maximize, with the stead- y-state infiltration rates of 1.29, 0. 15μg·h^-1·cm^-2, respectively. After 24 h, their penetration quantities were 30. 03 , 3.31 μg·cm^-2 with the penetration rates of 41.45%, 5.60%, respectively. The residual quantities of ferulic acid and imperatorin in skin were 0. 69, 2. 60μg·cm^-2, with the retention rates of 0. 95% , 4.40% , respectively. The in vitro transdermal behavior of ferulic acid in Zhitong cataplasm was close to a zero-order process, with the stratum corneum playing a rate-limiting role; whereas the percutaneous behavior of imperatorin was closer to Higuchi model, where diffusion played an important role in drugs permeation.