盐酸倍他洛尔蒙脱石微球的制备及其体外释放性能的研究

目的制备可满足缓释要求的镶嵌蒙脱石的离子交换缓释微球。方法采用S/O1/O2/O3复乳-溶剂挥发法制备微球,考察处方因素包括复乳相体积比例、药物质量浓度、膜材用量和乳化剂质量分数对微球制备的影响。以微球体外释放为考察指标,优化微球处方。结果研究所得到的微球最佳处方为大豆油∶药物=6∶1,药物∶膜材=1∶5,乳化剂质量分数为0.5%²%。除乳化剂外,其他因素对微球体外释放均有较大影响。所制备微球的体外释放可以达到10h,基本无突释现象。进行形态观察发现,微球较为圆整,粒径比较均匀。结论采用优化处方以复乳-溶剂挥发法所制备盐酸倍他洛尔蒙脱石微球体外具有缓释性能。

Study on the preparation and in vitro release behavior of the ion exchange drug de- livery system microspheres with a novel carrier of montmorillonite loaded with bet- axolol hydrochloride

Obj ective Betaxolol hydrochloride microspheres loaded by montmorillonite with appropriate release rate were prepared in this study.Methods Formulation and preparation parameters of the ion exchange drug delivery system microspheres with a novel carrier of montmorillonite loaded with betaxolol hydrochloride were prepared by S/O1/O2/O3 emulsion solvent evaporation meth-od.Release behaviors invitro were demonstrated for the controlled release of water-soluble drug betaxolol hydrochloride（BH）.To optimize the formulations,influence factors of polymer concentration of Eudragit RS,volume ratio of dispersed phase visus oil, drug concentration,and surfactant concentration were studied.Results The spherical and smooth microspheres were achieved with a mono dispersibility,and could release invitro as long as 10 h without burst release.Polymer concentration,volume ratio of dis-persed phase had significant influence on the release behavior.The optimized formulation was oil∶ drug=6∶1 ,drug∶polymer=1∶5,and composed with 0.5%-2% surfactants.Conclusion Betaxolol hydrochloride microspheres with appropriate release rate were achieved by S/O1/O2/O3 emulsion solvent evaporation preparation in this study.