目的 评价瑞舒伐他汀钙胶囊在健康人体中相对生物利用度及生物等效性。方法 随机、自身双交叉、单剂量口服试验制剂或参比制剂10 mg，采用液相色谱-串联质谱（LC-MS/MS）法测定血浆中药物浓度，药动学参数采用DAS软件处理获得。结果 两种制剂峰浓度（C_max ）分别为（7.32±4.21）ng/ml和（7.37±3.23）ng/ml，达峰时间（T_max）分别为（4.3±1.3）h和（3.4±1.6）h，半衰期（t_1/2）分别为（11.57±8.18）h和（10.70±5.26）h，0～t药时曲线下面积（AUC_0–t）分别为（64.8±28.0）ng/（ml.h）和（71.0±28.0）ng/（ml.h），0～∞药时曲线下面积（AUC_0–∞）分别为（66.1±28.3）ng/（ml.h）和（72.2±28.8）ng/（ml.h）；相对于参比制剂，试验制剂的生物利用度为（93.2±18.5）%（以AUC_0-t计）、（93.6±17.6）%（以AUC_0-∞计）。试验制剂和参比制剂的C_max、AUC_0–t和AUC_0–∞经对数转换后进行方差分析,两制剂间差异无统计学意义。结论 试验制剂瑞舒伐他汀钙胶囊和参比制剂瑞舒伐他汀钙片具有生物等效性。

Objective To study the bioavailability and bioequivalence of the tested and reference rosuvastatin calcium capsules in healthy male volunteers. Methods According to the crossover design,each volunteer was orally given 10 mg rosuvastatin capsules or tablets. The plasma concentrations were determined by LC/MS/MS. Pharmacokinetic parameters were obtained using DAS program. Results C_max were（7.32±4.21）ng/ml and （7.37±3.23）ng/ml，T_max were（4.3±1.3）h and （3.4 ± 1.6）h，T_1/2 were (11.57 ± 8.18）h and （10.70 ± 5.26）h，AUC_0-t were （64.8±28.0）ng/（ml·h） and（71.0±28.0）ng/（ml·h） ，AUC_0-∞ were （66.1±28.3） and （72.2±28.8）ng/（ml·h），respectively. The relative bioavailability was （93.2±18.5）% in AUC0-t and （93.6±17.6）% in AUC_0-∞.The data of the reference and tested drugs were not different as shown by F test. Conclusion The rosuvastatin calcium capsules and rosuvastatin calcium tablets are bioequivalent.