罗红霉素片的制备及溶出度考察

摘要

目的 制备罗红霉素片并考察其体外溶出度.方法 以罗红霉素原料药平均粒径(X1,μm),低取代羟丙基纤维素用量(X2,％)和泊洛沙姆188用量(X3,％)作为考察对象,以罗红霉素在30min的溶出度(y,％)作为评价指标,采用Box-Behnken效应面法优化罗红霉素片处方;并通过f2相似因子法比较自研制剂和参比制剂的体外溶出相似性.结果 经优化得到的罗红霉素片的处方为:罗红霉素原料药平均粒径为80μm,低取代羟丙基纤维素用量为7.5％,泊洛沙姆188用量为4.0％,在4种溶出介质中自制的罗红霉素片与参比制剂体外溶出具有较好的相似性.结论 通过Box-Behnken效应面法优化得到的罗红霉素片处方与参比制剂体外溶出一致性良好,有望工业化生产.%Objective To prepare roxithromycin tablets and evaluate the in vitro drug dissolution.Methods The formulation of roxithromycin tablets was optimized by the Box-Behnken design response surface methodology.The roxithromycin particle size distribution (X1,μm),the amount of L-HPC (X2,％) and the amount of poloxamer 188 (X3,％) were selected as independent variables,and the roxithromycin dissolution at 30min(Y,％) was the dependent variable.The drug relcase rates of the roxithromycin tablets and the reference preparations were compared using the f2 similarity factor.Results The optimum formulation of roxithromycin tablets was as follows:The roxithromycin particle size distribution of 80μm,7.5％ L-HPC,and 4.0％ poloxamer 188.The dissolution behavior of roxithromycin tablets and the reference preparations were similar in four types of dissolution mediums.Conclusion The formulation of roxithromycin tablets was successfully optimized by the Box-Behnken design response surface methodology.The in vitro dissolution of roxithromycin tablets has good in vitro consistency with the reference preparations.Thus it could be used in the industrial production.