盐酸川芎嗪眼用原位温敏凝胶的制备及体外释药特性研究

目的：制备盐酸川芎嗪眼用原位温敏凝胶并对其体外释药特性进行考察。方法采用泊洛沙姆407和泊洛沙姆188为温敏基质制备眼用温敏凝胶，采用无膜溶出模型，研究药物在某一时间的累积释放百分率与时间的变化，对曲线进行拟合分析，研究川芎嗪的体外释放特性。结果所制得凝胶为均匀稍带黏性的澄清溶液，该制剂的体外释放行为遵循零级动力学方程（r ＝0．9887），由 Ritger －Peppas 方程拟合的 n 值为0．7533。结论盐酸川芎嗪眼用温敏凝胶体外释药是由药物扩散和凝胶溶蚀双重机制控制。

Preparation and drug release in vitro of the thermosensitive in-situ gel system containing ligustrazine hydrochloride for ocular use

Objective To prepare the thermosensitive in -situ gel system containing ligustrazine hydrochloride for ocular use and to study the drug release in vitro.Methods The thermosensitive in-situ gel system containing ligustrazine hydrochloride was prepared by Poloxamer 407(P407)and Poloxamer 188 (P188)as thermosensitive materials.The membraneless model was applied to investigate the drug release and gel erosion,and the data were analyzed with fitted equations.Results The release behavior in vitro could be de-scribed by the zero-order kinetics equation(r =0.988 7).The release parameter n obtained from Ritger-Peppas equation was 0.753 3. Conclusions The release mechanism of this thermosensitive in-situ gel system containing ligustrazine hydrochloride for ocular use was fiffusion as well as matrix erosion.