盐酸倍他洛尔/蒙脱石微球滴眼剂的制备及初步刺激性考察  

Studies on the preparation and irritation of betaxolol hydrochloride microspheres loaded by montmorillonite

作　　者：黄燚[1] 侯冬枝[1] 潘育方[1] 刘莉[1] 桂茹艺 胡晟[1] 田双艳[1] 平其能[2] 陈燕忠[1] 

机构地区：[1]广东药学院药科学院,广州510006 [2]中国药科大学药学院,南京210009

出　　处：《西北药学杂志》2016年第5期493-496,共4页Northwest Pharmaceutical Journal

基　　金：国家自然科学基金项目(编号:51102052);广东省医学科学技术研究基金(立项编号:A2016275)

摘　　要：目的制备新型盐酸倍他洛尔/蒙脱石微球滴眼剂并研究其初步刺激性。方法以蒙脱石为离子交换载体材料,用2种处方以O_1/O_2溶剂挥发法制备盐酸倍他洛尔缓释微球;对比微球的载药量和包封率等物化性能以得到最优处方,并将最优处方制备的微球制成滴眼剂以研究其初步刺激性。结果最优处方为丙烯酸树脂300mg(RS∶RL=1∶3),柠檬酸三乙酯60mg,甘油30mg,乳化剂400mg(吐温-80∶司盘-80=1∶2),盐酸倍他洛尔30mg,蒙脱石50mg,内外相体积比为1∶6。最优处方制得的微球载药量和包封率分别为14.31%和94.35%,初步刺激性实验显示微球滴眼剂对眼部组织无明显刺激性。结论微球制备方法简便易行,重复性好;制备的微球滴眼剂无明显刺激性,具有广阔的应用前景。Objective To prepare the eyedrops of betaxolol hydrochloride microspheres loaded by montmorillonite and to study its irritation.Methods Montmorillonites were used as ion exchange carrier material for hydrochloride microspheres in this study.The betaxolol hydrochloride microspheres were prepared with O1/O2 solvent evaporation method using two different formulations.To obtain the optimal formulations,the preparation parameters were investigated,such as drug-loading rate,and the encapsulation efficiency,etc.The optimal formulation was adopted to prepare the the eyedrops of betaxolol hydrochloride microspheres loaded by montmorillonite.The irritation of the prepared eyedrops was researched.Results The optimal fomulation was described as follows：300mg of acrylic resin（RS∶RL=1∶3）,60 mg of triethyl citrate,30 mg of glycerin,400 mg of emulgator（Tween-80∶Span-80=1∶2）,30 mg of betaxolol hydrochloride and 50 mg of montmorillonite.In addition,the volume ratio of internal phase to external phase was 1∶6.The drug-loading rate,and the encapsulation efficiency of microspheres prepared by the optimal formulation were 14.31%and 94.35%,respectively.The irritation tests showed that the eyedrops had no obvious irritation for eye tissues.Conclutions The preparation of microspheres is simple and reproducible and the eyedrops has no obvious irritation.

关 键 词：蒙脱石 盐酸倍他洛尔 微球 刺激性 

分 类 号：R944[医药卫生—药剂学]