中国临床药学杂志

目的考察2种市售咪唑斯汀缓释片在4种pH条件下不同时间点的体外释放度,并比较它们的差异。方法采用转篮法测定释放度,计算2种制剂在不同pH条件下的累积释放百分率,并绘制累积释放曲线。用威布尔(Weibull)方程进行拟合,并对释放参数t50、td、m采用方差分析及t检验进行统计分析。同时绘制时间-释放度-pH三维释放曲线,用相似因子法考察2种制剂的体外释放差异。结果在4种pH值不同的释放介质中,制剂A的t50、td均<制剂B,差异具有显著性意义(P<0.01)。在pH 1.0、4.0、6.8和蒸馏水中两者的相似因子分别为54.36、51.84、50.77和49.17。结论制剂A和制剂B的体外释放度随pH不同而不同,在4种pH条件下,制剂A的体外释放2 h前均快于制剂B,可供临床用药参考。

AIM To investigate release characteristics in vitro under 4 different pH conditions of 2 commercial mizolastine sustained release tablets and to compare their difference.METHODS The release tests were carried out with rotating basket method.The accumulative release percent under different pH conditions of 2 formulas was calculated,the accumulative release curves were made and the Weibull's equation was used to fit the data.The release parameters such as t₅₀,t_d and m were statistically analyzed by variance analysis and t test.Meanwhile time-release-pH three dimensional release curves were made and the difference of release in vitro between the 2 formulas was compared by f₂ fit factors method.RESULTS In 4 medium with different pH values,t₅₀ and t_d of formula A are smaller than those of formula B and the difference has significant meaning(P<0.01).The f₂ value is 54.36,51.84,50.77 and 49.17 in the medium with pH 1.0,4.0,6.8 and distilled water,respectively.CONCLUSION The release characteristics of the 2 formulas in vitro vary with different pH values.Under 4 different pH conditions,the release rates of formula A are more rapid than those of formula B before 2 h,which could be the basis for clinical use.