瑞舒伐他汀口崩片的人体生物等效性研究与药代动力学个体差异分析

Bioequivalence of Rosuvastatin Calcium Disintegrating、 Tablets and Individual Differences in Pharmacokinetics

目的研究瑞舒伐他汀钙口崩片(供试制剂)与瑞舒伐他汀钙片(参比制剂)的生物等效性。方法 20名健康受试者自身交叉单剂量口服20mg瑞舒伐他汀钙口崩片与瑞舒伐他汀钙片,采用液相色谱-质谱法测定血浆药物浓度,计算药代动力学参数,以方差分析与单向t检验进行统计分析。结果供试制剂和参比制剂的t1/2分别为(10.20±3.65)、(9.90±3.61)h,tmax分别为(2.90±0.97)、(2.90±1.25)h,Cmax分别为(26.96±10.69)、(26.37±11.64)ng.mL-1,药物-时间曲线下面积(AUC)0-72分别为(251.25±106.78)、(239.27±94.09)ng.h-1.mL-1。瑞舒伐他汀钙口崩片相对于片剂的生物利用度为(106.0±13.8)%。结论瑞舒伐他汀口崩片和瑞舒伐他汀钙片2种制剂具有生物等效性,药代参数个体差异大。

Objective To study the bioequivalence of rosuvastatin calcium disintegrating tablets and Rosuvastatin calcium tablets. Methods Twenty healthy volunteers were selected to receive a single dose of Rosuvastatin calcium disintegrating tablets(test tablets) and Rosuvastatin calcium tablets(reference tablets) at concentrations of 20 mg in a two-way cross-over design.Plasma concentrations of Rosuvastatin were determined by LC-MS method and pharmacokinetic parameters were calculated.Data were analyzed with one side t-test and variance analysis. Results The t1/2,tmax,Cmax and AUC0-72 were respectively,(10.20±3.65)h,(2.90±0.97)h,(26.96±10.69)ng·mL-1 and(251.25±106.78)ng·h-1·mL-1 for test tablets,and(9.90±3.61)h,(2.90±1.25)h,(26.37±11.64)ng·mL-1 and(239.27±94.09)ng·h·mL-1 for reference tablets.The bioavailability of the two preparations was(106.0±13.8)%.Conclusion Rosuvastatin calcium disintegrating tablets and Rosuvastatin calcium tablets were bioequivalent,but show individual differences in pharmacokinetics.