| 摘要: |
| 目的：比较驻极体与化学促渗剂对美洛昔康的促渗作用.方法：以美洛昔康贴剂为对照组,以加化学促渗剂的美洛昔康贴剂、驻极体美洛昔康贴剂和加入化学促渗剂的驻极体美洛昔康贴剂为实验组,利用改良的Franz扩散池,用紫外分光光度仪于362 nm处测定各类贴剂中主药的光密度并求算其10 h内的累积渗透量,并与对照组10 h内累积渗透量相比,比较驻极体与化学促渗剂对美洛昔康的体外促渗能力及驻极体与化学促渗剂的协同作用.结果：（1）1%、3%、5%氮酮美洛昔康贴剂作用离体皮肤10 h,其累积渗透量分别为对照组的1.20、1.33、1.26倍（P＜0.05）,促渗能力由大到小依次排序为：3%氮酮＞5%氮酮＞1%氮酮;（2）除20%丙二醇外,化学促渗剂（1%、3%、5%氮酮,10%油酸乙酯,1%薄荷油,30%二甲亚砜）对美洛昔康均有促渗作用;其中以10%油酸乙酯促渗能力最强,为对照组的1.86倍（P＜0.05）;（3）驻极体对美洛昔康的促渗作用优于选用的化学促渗剂,为对照组的2.16倍（P＜0.05）;（4）驻极体可增强化学促渗剂的促渗作用,加入化学促渗剂的驻极体美洛昔康贴剂与加化学促渗剂的美洛昔康贴剂相比,其促渗能力提高到1.14～2.82倍（P＜0.05）.结论：驻极体具有优良的药物透皮吸收促进作用,可作为一种新型促渗方法用于体外透皮 |
| 关键词: 驻极体 美洛昔康 贴剂 化学促渗剂 累积渗透量 |
| DOI：10.3724/SP.J.1008.2007.00709 |
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| 基金项目:国家自然科学基金（50577066）;军队“十一五”科技攻关项目（06H022）. |
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| Comparison of electret and chemical enhancers in enhancing transdermal delivery of meloxicam |
| HOU Xue-mei , CUI Li-li , JIANG Jian , LI Guo-dong , LIANG Yuan yuan , SONG Mao-hai , KONG Yu-xiu , CHENG Liang |
| (1. Department of Inorganic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China; 2. Department of Physics and Mathematics,College of Basic Medical Sciences, Second Military Medical University, Shanghai 200433) |
| Abstract: |
| Objective： To compare the effects of electret and chemical enhancers in enhancing the transdermal delivery of meloxicam. Methods： The study was divided into 4 groups, including meloxicam patch group （control）, chemical enhancer ＋ meloxicam patch group,electret meloxicam patch,and electret ＋ chemical enhancer ＋ meloxicam patch group. The in vitro skin permeation of meloxicam from patches was examined by using a modified Franz diffusion cell. Ultraviolet spectrophotometry （362 nm） was used to analyze the drug concentration in the receptor. The 10 h-cumulated permeation amount of meloxicam from patchs was calculated in 3 experimental groups and were compared with that the control group. The enhancing abilities of electret and chemical enhancers were compared and the synergistic effect of them was assessed. Results： （1） 1 %. 3 % and 5 azones showed 1.20,1.33 ,and 1.26 fold-increases in the 10 h cumulated permeation of meloxiam respectively as compared with control group（P〈0.05）. （2） Most of the chemical enhancers used in thisstudy（1%,3% and 5%azones,10% ethyloleate,1% menthnol,and 300% sulphoxiade） ,except for 20 % propylene glycol,had enhancing effect on transdermal delivery of melocicam. Ethyl oleate（10%） was proven to be the most potent enhancer, showing a 1.86 fold cumulated permeation that of the control group（P〈0. 05） ; （3） Electret was more potent than the chemical enhanrers in promoting meloxieam transdermal delivery, showing a 2. 16-fold cumulated permeation that of control group（P〈0. 05）;（4） Electret improved the enhancing effect of chemical enhancers in this study. The cumulated permeation of meloxicam in electret ＋ chemical enhancer ＋ meloxicam patch group was 1.14-2.82 folds that of the chemical enhancer ＋ meloxicam patch group（P〈0. 05）. Conclusion： Electret has a good promoting effect for transdermal drug delivery and can be used as a novel enhancer in transdermal delivery of drugs |
| Key words: electret meloxicam patch chemical enhancers cumulated permeation amount |
