眼用盐酸倍他洛尔脂质体-原位凝胶的研制及体外释药的研究

目的制备盐酸倍他洛尔(BH)眼用脂质体-原位凝胶(ISG),并对其体外释药特性进行考察。方法采用逆向蒸发法制备BH脂质体(BHL);以泊洛沙姆407和188(P407,P188)为温敏性ISG基质,以胶凝温度为指标,筛选P407与P188的最佳配比;采用无膜溶出模型对BHL的体外释放行为进行考察。结果 BHL的平均包封率为(88.24±5.46)%(n=3);当P407与P188的处方用量分别为21%及6%时,胶凝温度最接近人眼表温度(34℃);BHL-ISG体外药物释放和凝胶溶蚀均呈现零级释放特征,两者相关性良好。结论 BHL-ISG结合脂质体和原位凝胶的特点,延缓药物释放,为其角膜滞留性研究奠定了基础。

Preparation and the drug release in vitro of ocular betaxolol hydrochloride liposome-in-situ gels

Objective To prepare ocular betaxolol hydrochloride（BH） liposome-in-situ gels（ISG） and to investigate the drug release pro- file in vitro. Method BH liposomes（BHL） were prepared by a reverse phase evaporation method. Temperature-sensitive poloxamer 407 and 188 （P407 and P188）were selected as the base for the ISG,and the formula amount was screened according to the gelation tempera- ture. A rnembraneless model was used to study the drug release in vitro. Results The average entrapment efficiency of BHL was （88.24 -＋ 5.46） % （ n = 3 ）. The optimal amount of P407 and P188 in the formula was 20% and 6% , respectively, and the gelation temperature was nearly 34~C. Both the drug release in vitro and the gel dissolution of BHL-ISG exhibited the characteristics of zero order kinetics with promising correlation. Conclusion BHL-ISG shows the advantages of liposomes and ISG with the property of sustained drug release in vitro,which provides the basis for the further study on the cornea residence time in vivo.