更昔洛韦左氧氟沙星喷雾剂透皮促进剂的选择

Study on penetration enhancer for the ganciclovir and levofloxacin spray

目的:选择一种能改善更昔洛韦左氧氟沙星喷雾剂透皮能力的适宜透皮促进剂。方法:采用改良型Franz扩散池(垂直式),以pH7.4的磷酸盐缓冲液为吸收液进行体外透皮实验;用高效液相色谱法同时测定更昔洛韦、左氧氟沙星的透皮浓度,计算12h的累积透皮率,并以空白为对照,比较甘油和二甲基亚砜体外透皮的促透皮作用。结果:空白组、甘油组、二甲基亚砜组12h内对更昔洛韦的累积透皮率分别为3.88%,10.17%,10.77%;对左氧氟沙星的12h累积透皮率分别为1.15%,13.31%,14.92%。结论:甘油和二甲基亚砜均能显著提高更昔洛韦左氧氟沙星喷雾剂的透皮渗透能力,二甲基亚砜的促皮吸收能力比甘油略强,但差异无显著性(P>0.05)。综合考虑二者促透皮能力和不良反应,选择甘油作为更昔洛韦左氧氟沙星喷雾剂的透皮促进剂。

OBJECTIVE To choose a better penetration enhancer for the Ganciclovir and Levofloxacin Spray from glycerol and dimethyl sulfoxide. METHODS Modified Franz-type vertical diffusion cells and absorptive solution of phosphate buffer （pH 7. 4） were used. The contents of Ganciclovir and Levofloxacin were determined by HPLC. The cumulative Ratio （CR） were also calculated. RESULTS The 12 h CRs of the blank,glycerol and dimethyl sulfoxide groups were 3. 88%,10. 17%,10. 77% for ganciclovir, 1. 15%, 13. 31%, and 14. 92% for levofloxacin. CONCLUSION Both glycerol and dimethyl Sulfoxide could enhance the CR for the Ganciclovir and Levofloxacin Spray. Compared with the CR of the blank group,P〈0. 05, this re sults indicates that there were significant difference, glycerol was selected as penetration enhancer for the Ganciclovir and Levo floxacin Spray with the consideration of side reaction.