摘要
目的考察3种促进剂在不同浓度条件下双氯芬酸钠凝胶体外经皮离子导入渗透速率的影响。方法选择聚乙烯醇、聚乙烯吡咯烷酮、羟丙甲基纤维素为基质,制备了分别含有月桂氮酮、肉豆蔻酸异丙酯和油酸的双氯芬酸钠经皮离子导入凝胶,采用改良Franz纵向释放池,以人体皮肤为透皮屏障,进行药物凝胶的离子导入经皮试验。结果3种促进剂均有促进效果,其中肉豆蔻酸异丙酯渗透速率不高,渗透效果不理想;含有不同浓度月桂氮酮的凝胶具有一定渗透速率;含油酸的凝胶的渗透速率较高。结论其中以3%油酸的促进效果最好,在0.2 mA的电流下,渗透速率达到(29.34±0.65)μg.cm-2.h-1。
OBJECTIVE To observe the effects of three transdermal enhancers （azone, isopropyl myristate, oleic acid） in vitro under the condition of iontophoresis with diclofenac sodium as the model drug. To select a better enhancer for the gel formulation. METHODS After gel as the drug carrier was formulated using PVP, PVA and HPMC, the enhancer was incorporated into the gel. The iontophorestic flux of various gels with enhancer in five kinds of concentration （g/g） was compared. The transdermal amount, permeation rate of the gel, and the time lag, enhancement ratio of the enhancers were calculated. RESULTS All of three enhancers had effects on diclofenac sodium. Isopmpyl myristate had only a little effect and the gels with azone in various concentration had better effects. Among the three enhancers, oleic acid was the best. CONCLUSION All of the enhancers own enhancing activities. Compared to the other gel, the gel with 3 % oleic acid is the best one. Its iontophorestic flux is up to （29.34±0.65）μg·cm^-2·h^-1 under the current of 0.2 mA.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第12期921-923,共3页
Chinese Pharmaceutical Journal
基金
浙江省科技厅国际合作项目(001106126)
