摘要
目的研究醋氯芬酸溶液经离体鼠皮的透过特性,寻找能有效增加醋氯芬酸渗透的促渗剂,用以开发醋氯芬酸经皮给药传递系统。方法测定醋氯芬酸在pH 2.5、3.6、5.0、6.8、7.4 PBS缓冲液中的饱和溶解度;采用水平扩散装置进行醋氯芬酸在pH 2.5、3.6、5.0、6.8、7.4条件下及在乙醇、丙二醇、卡必醇、桉叶油醇、松节油、油酸、氮酮等促渗剂作用下的经皮渗透实验;用HPLC法分析样品。结果随着pH值的增加,醋氯芬酸的溶解度增加,经皮渗透量也呈上升趋势;氮酮、油酸和松节油均可显著增加醋氯芬酸的经皮渗透,促渗顺序为氮酮>油酸>松节油,且主要通过增加表皮基质间的分配系数实现促渗效果。结论醋氯芬酸具有一定的经皮透过性,宜制成经皮给药剂型;油酸、油溶性氮酮可作为其有效的渗透促进剂。
Objective To study the permeability of aceclofenac through the excised rat skin and to develop a new kind of transdermal preparation of aceclofenac by an excellent permeation promoter. Methods The solubility of aceclofenac at different pH was determined, its permeations at different pH and by different enhancers were examined using modified horizontal diffusion cell. Samples were withdrawn at constant internal and analyzed by HPLC. Results The enhancing effects of azone, oleic acid and turpentine were significant, with the order of azone〉oleic acid 〉 turpentine. Conclusions The transdermal formulation of aceclofenac is anticipated to be developed by using oleic acid or azone as the effective enhancers.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2006年第6期344-346,352,共4页
Journal of Shenyang Pharmaceutical University
关键词
醋氯芬酸
经皮渗透
油酸
松节油
氮酮
aceclofenac
permeation enhancers
oleic acid
turpentine
azone
