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目的研究表面活性剂对尼美舒利缓释片释放的影响。方法制备尼美舒利缓释片,并采用阴离子型表面活性剂十二烷基硫酸钠(SDS)、阳离子型表面活性剂十六烷基三甲基溴化铵(CTAB)和非离子型表面活性剂吐温80(Tween 80)制备尼美舒利胶束,考察缓冲液种类、表面活性剂类型、浓度和离子强度等对尼美舒利平衡溶解度的影响,探讨缓释骨架片体外释放机制。结果与结论在pH 1.2的盐酸溶液、水以及pH 6.8的磷酸盐缓冲液中,CTAB的增溶能力最强,SDS和Tween 80次之;在pH 9.0的Tris缓冲液中,CTAB浓度达到1%时,尼美舒利的平衡溶解度达到谷值。尼美舒利缓释片的体外释放的高低顺序和平衡溶解度的结果类似,且药物的释放速率与时间成正比。
Objective To study the effect of surfactant on the release of nimesulide sustained-release tablets. Methods Nimesulide sustained-release tablets were prepared and characterized by anionic surfactant sodium dodecyl sulfate (SDS), cationic surfactant cetyltrimethylammonium bromide (CTAB) and nonionic surface The effect of buffer type, surfactant type, concentration and ionic strength on the equilibrium solubility of nimesulide was investigated by using Tween 80 as active agent. The in vitro release mechanism of sustained-release matrix tablets . RESULTS AND CONCLUSION CTAB had the strongest solubilization ability in hydrochloric acid solution of pH 1.2, water and phosphate buffer solution of pH 6.8, with SDS and Tween 80 times. The concentration of CTAB in Tris buffer solution at pH 9.0 reached 1% , The equilibrium solubility of nimesulide reached its trough. The order of in vitro release of nimesulide sustained-release tablets was similar to that of equilibrium solubility, and the rate of drug release was proportional to time.