甲磺酸培氟沙星凝胶基质的研究Studies on pefloxacin mesylate gel matrix
毛世瑞,王蕾,蔡翠芳,毕殿洲
MAO Shi rui; WANG Lei; CAI Cui fang; BI Dian zhou (School of Pharmacy;
摘要(Abstract)：
目的以水溶性的甲磺酸培氟沙星为模型药物 ,研究不同浓度、不同种类的水凝胶基质及穿透促进剂对其释药的影响 ,寻找其规律性。方法分别采用半透膜扩散法和离体皮肤法评价其释药性 ,求出其累计释药量和渗透系数。结果甲磺酸培氟沙星在海藻酸钠、CMC—Na、MC、黄原胶、HPMC凝胶基质中的体外释放均符合Higuchi方程 ,透过离体鼠皮扩散属零级释放过程。以CMC—Na为基质 ,丙二醇和月桂氮卓酮为穿透促进剂 ,结果表明二者对凝胶的透皮吸收皆有促进作用 ,但月桂氮卓酮的效果更明显 ,二者合用有拮抗作用。结论水凝胶基质种类、浓度不同 ,渗透速度不同 ;所采用的研究方法不同 ,释药机理不同 ;药物浓度与渗透系数间无相关性 ;加入丙二醇和月桂氮卓酮对凝胶的透皮吸收有促进作用
Objective The study is to use the hydrosoluble pefloxacin mesylate was used as a model drug to study the effects of hydrogel kinds, concentration and penetrating accelerant on drug release mechanism. Methods Semi permeable membrane diffusion and in vitro skin diffusion, were used to evaluate drug release characteristics, and more, the cumulative release amount and permeability coefficients were calculated. Results The in vitro release of pefloxacin mesylate from sodium alginate, CMC Na, MC, xanthum gum, HPMC followed. The Higuchi equation, respectively, and followed the zero order equation across the rat′s skin. By using CMC Na as the matrix, it was indicated that the propylene glycol and azone were all sorbefacient, the penetrating effect of azone was more evident; but when they were used together, antagonism appeared. Conclusions The results of our study showed that different kinds and different concentrations of hydrogel had different release rates; different research methods resulted in different release mechanisms; there was no correlation between the drug concentration and penetration coefficient; the addition of propylene glycol and azone could facilitate transdermal absorption.
关键词(KeyWords)：
甲磺酸培氟沙星;凝胶基质;透皮吸收;穿透促进剂
pefloxacin mesylate; gel matrix; transdermal absorption; penetrating accelerant
基金项目(Foundation):
作者(Authors):
毛世瑞,王蕾,蔡翠芳,毕殿洲
MAO Shi rui; WANG Lei; CAI Cui fang; BI Dian zhou (School of Pharmacy;
参考文献(References)：
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