乳化溶剂扩散法制备罗红霉素肠溶微球及影响因素考察  

Preparation of the enteric microspheres of roxithromycin by the emulsion solvent diffusion method and investigation of the influencing factors

作　　者：贺颖[1] 冯丽莉[1] 陶安进[1] 崔福德[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2005年第2期81-85,128,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的罗红霉素肠溶微球的制备及影响因素考察。方法应用肠溶高分子材料 ,采用乳化溶剂扩散法一步制备罗红霉素肠溶微球。对影响微球形态、粒度分布、收率及其在 0 . 1mol·L-1盐酸溶液和 pH 6 8磷酸盐缓冲溶液中累积释放度的处方因素、制备条件和溶剂系统进行了考察。应用X 射线粉末衍射实验考察了药物在微球中的分散状态。结果制备的微球外观圆整。微球粒径随着搅拌转速的增加而减小。微球收率随架桥剂用量减少 ,良溶剂用量增加而增加 ;并且受到不良溶剂中乳化剂种类的影响。药物在 0 . 1mol·L-1盐酸溶液中的释放速率随肠溶材料HP- 5 5用量增加显著降低。当HP- 5 5与药物质量比大于 5时 ,药物在 0 . 1mol·L-1盐酸溶液中释放小于 5 % (w) ,同时在pH 6 . 8磷酸盐缓冲溶液中可迅速释放。X- 射线粉末衍射结果显示 ,微球中药物已被高度分散 ,形成固体分散体。结论乳化溶剂扩散法适用于制备具有固体分散体结构的肠溶微球。Objective To prepare the enteric-release microspheres of roxithromycin and investigate the influencing factors.Methods The enteric dissolving roxithromycin microspheres were prepared with an enteric polymer in one step by the quasi-emulsion solvent diffusion method.The formulation of the micros- pheres,producing conditions and solvent system were investigated as the influencing factors on the preparation.The resultant microspheres were examined on their shape,size distribution,recovery and the release profiles in the 0.1 mol·L~ -1 HCl and pH 6.8 phosphate buffer.The x-ray diffraction method was used to check the drug's crystalline form in the microspheres.Results The microspheres are of a very round form,the mean size of the microspheres is decreased with increasing the stirring rate.The recovery of the microspheres is increased with decreasing the bridging liquid and increasing the good solvent and poor solvent.The release rate of the drug in the 0.1 mol·L~ -1 HCl is dramatically decreased with increasing the enteric polymer(HP-55).When the HP-55-to- drug ratio(w)is larger than 5,the drug release in the 0.1 mol·L~ -1 HCl over 2 h is less than 5%(w),and advance rapidly released in the pH 6.8 phosphate buffer.The drug in the microspheres exists in a solid dispersion form.Conclusions The emulsion solvent diffusion method is an efficient method to produce enteric microspheres having solid dispersion structure.

关 键 词：罗红霉素 HP-55 肠溶微球 乳化溶剂扩散法 

分 类 号：R944.9[医药卫生—药剂学]