透明质酸钠对眼用温度敏感原位凝胶体外释放和粘附力的影响  

Effects of sodium hyaluronate on the physicochemical properties of ophthalmic thermosensitive in situ ge1s of diclofenac sodium

作　　者：鞠凤阁[1] 朱照静[1] 马俐丽[1] 

机构地区：[1]重庆医科大学药学院药剂学教研室,重庆400016

出　　处：《中国新药杂志》2009年第13期1237-1242,共6页Chinese Journal of New Drugs

摘　　要：目的:考察透明质酸钠(sodium hyaluronate,SH)对眼用温度敏感原位凝胶胶凝温度、浊点、凝胶溶蚀、药物释放及粘附力的影响,为二者的配伍使用提供依据。方法:采用冷法,制备含不同浓度SH的双氯芬酸钠眼用温度敏感原位凝胶;试管倾斜法测定凝胶的胶凝温度;无膜溶出法考察凝胶的溶蚀及药物释放行为;生物粘附力测定装置测定离体角膜粘附力。结果:随着SH浓度的升高,凝胶的胶凝温度与浊点均降低,凝胶溶蚀速率和药物释放速率减慢,离体角膜粘附力增强;双氯芬酸钠在凝胶中的释放由凝胶溶蚀控制。结论:SH可改善凝胶的理化性质,处方中含0.15%SH的眼用温度敏感原位凝胶角膜粘附性能良好,药物释放较慢,有望在临床中获得应用。Objective ：To study the effects of sodium hyaluronate （SH） on the physicochemical properties of ophthalmic thermosensitive in situ gels of diclofenac sodium （DS）. Methods：The thermosensitive in situ gels composed of different concentrations of SH （0 -0. 15% ,w/w） and poloxamers （P407：P188 = 21%：5% ,w/w） were prepared by the cold method. The gelatin temperature was determined by tube-reverse method. The erosion of the gels and release of DS from the gels were investigated by membrane-free method and RP-HPLC. Bioadhesive forcemeasuring device was used to evaluate the bioadhesive force. Results：Increased SH concentration in gels decreased the gelatin temperatures of poloxamer gels,the cloud points, and drug release rates. The bioadhesive forces rose accordingly. Drug release was controlled by the erosion of the gel matrix. Conclusion ： An optimized formation containing 0. 15% SH showed more desirable characteristics and might have great potential application for future clinical therapy.

关 键 词：泊洛沙姆 透明质酸钠 胶凝温度 凝胶溶蚀 体外释放 生物粘附力 

分 类 号：R943.4[医药卫生—药剂学] R988.1[医药卫生—药学]