摘要
目的:以抗结核药物利福平(RFP)为模型药物,制备利福平缓释微球,并对其进行体外释药评价。方法:以乳酸-羟基乙酸共聚物(PLGA)为载体材料,采用乳化-溶剂挥发法制备利福平缓释微球;通过单因素试验,考察影响微球质量的因素,采用正交试验的方法进行优化,选出较佳的处方和工艺参数;采用透析释药法进行体外释放特性研究。结果:最佳处方为利福平∶PLGA=1∶5(W/W),PLGA∶二氯甲烷=1∶20(W/V);水相为2%(W/V)PVA水溶液,油相/水相比例为1∶10(V/V),搅拌速度为900 r·min-1。利福平微球的平均粒径为42.42μm,载药量为17.73%,包封率为76.55%,体外释放试验,538 h释放了27.50%,释放动力学模型拟合,较符合Higuchi模型。结论:以PLGA为载体材料,采用乳化-溶剂挥发法可以制备包封率较高的利福平微球,体外释放实验也表明该微球具有明显的缓释作用。
OBJECTIVE A kind of treatment of tuberculosis were selected as model drug to prepare rifampicin microspheres,and to evaluate its property in vitro. METHODS Emulsification-solvent evaporation method was developed to prepare RFP-MS with PLGA as carries; The influence of formulation and manufacture was studied by the single factor experiments,the optimal formulation was verified by orthogonal design; Dialysis method was selected to examine the drug release in vitro. RESULTS The optimum prescription was RFP∶ PLGA = 1∶ 5（ W / W）,PLGA∶ DCM = 1∶ 20（ W / V）; 2%（ W / V） PVA water solution,oil and water phase ratio is 1∶ 10（ V /V）,mixing speed is 900 r·min- 1. The photos showed that RFP-MS had good appearance,with middle diameter of 42. 42 μm,drug loading percent of 17. 73%. and entrapment efficiency of 76. 55%. By the study of drug realease in vitro,RFP-MS release 27. 50% after 538 hours. Release kinetics conform to the higuchi model. CONCLUSION Emulsification-solvent evaporation method was developed to prepare PLGA- RFP-MS with higher entrapment efficiency,the results showed that preparations could induce sustained release of RFP.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2014年第24期2111-2116,共6页
Chinese Journal of Hospital Pharmacy
关键词
利福平
PLGA
微球
体外释药
rifampicin
PLGA
microspheres
drug release in vitro
