摘要
目的研究8-甲氧基补骨脂素(8-MOP)微乳及其微乳凝胶的在体透皮性能。方法以SD大鼠为实验动物,对8-MOP微乳、8-MOP微乳凝胶和市售8-MOP溶液分别进行在体透皮实验,于不同时间点眼眶取血,HPLC法测定血样及鼠皮中药物含量。结果 8-MOP微乳组的AUC_(0~24)是溶液组的2.9倍,药物皮肤滞留量是后者的4.9倍,即相对提高了滞留量;微乳组和微乳凝胶组之间的AUC_(0~24)、AUC_(0~∞)和皮肤滞留量差异均无统计学意义;微乳凝胶组的AUC_(0~24)是溶液组的2.85倍,但药物皮肤滞留量差异并无统计学意义(P>0.05)。结论与市售8-MOP溶液剂相比,8-MOP微乳能提高药物的滞留透过比,制备成微乳凝胶后,降低了药物的皮肤滞留性。
Objective To determine the in vivo transdermal properties of 8-MOP microemusion （ 8-MOP ME ） and its microemulsion-based hydrogel （ 8-MOP MBH ） . Methods SD rats were used and in vivo transdermal study of 8-MOP ME, MBH and commercially available solution were performed. After topical administration preparation, blood samples were withdrawn from the fossa orbitalis of the rats at predetermined time intervals. The 8-MOP in the rat plasma and skin was determined by HPLC. Results The A UC（0 - 24） values from 8-MOP ME and MBH were 2.9 and 2.85 times, and were greater than the AUGo_ 2a~ values from the commercially available 8-MOP solution. The skin residual amount from ME was 4.9 times greater than the solution. The 8-MOP ME resulted in an increased 8-MOP skin residual amount, but the 8-MOP MBH did not. Conclusion 8-MOP ME can promote the drug localization into the skin, while similar function is not found in 8-MOP MBH.
出处
《中南药学》
CAS
2017年第12期1691-1694,共4页
Central South Pharmacy
关键词
8-甲氧基补骨脂素
微乳
微乳凝胶
经皮给药
8-methoxsalen
microemulsion
microemulsion-based hydrogel
percutaneous administration
