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目的:建立人血浆中瑞舒伐他汀钙的高效液相色谱-质谱(LC-MS/MS)测定方法,并评价瑞舒伐他汀钙片剂的药动学和人体生物等效性。方法:20名男性健康志愿者随机交叉口服瑞舒伐他汀钙片受试制剂和参比制剂各10mg,采用HPLC-MS/MS测定血药浓度,以BAPP2.0软件计算其药动学参数,考察其生物等效性。结果:受试制剂与参比制剂瑞舒伐他汀钙t1/2分别为(7.6±1.0)h和(7.8±1.1)h,tmax分别为(4.0±2.1)h和(4.2±1.6)h,Cmax分别为(15.7±7.8)ng·mL-1和(16.7±9.4)ng·mL-1,用梯形法计算所得的AUC0-72分别为(145±83)ng·mL-1·h-1和(142±67)ng·mL-1·h-1,AUC0-分别为(147±84)ng·mL-1·h-1和(144±70)ng·mL-1·h-1,以AUC0-72计受试制剂相对参比制剂生物利用度为(102±40)%。结论:该方法重复性好,灵敏度高,瑞舒伐他汀钙片受试制剂和参比制剂具有生物等效性。
Objective: To establish a method for the determination of rosuvastatin calcium in human plasma by LC-MS / MS and to evaluate the pharmacokinetics and bioequivalence of rosuvastatin calcium tablets. Methods: Twenty healthy male volunteers were randomized to receive 10 mg of rosuvastatin calcium tablets and reference preparations respectively. The plasma concentrations were determined by HPLC-MS / MS. The pharmacokinetic parameters were calculated by BAPP2.0 software. Examine its bioequivalence. Results: The t1 / 2 of rosuvastatin in the test preparation and the reference preparation were (7.6 ± 1.0) h and (7.8 ± 1.1) h, respectively, and the tmax were (4.0 ± 2.1) h and (4.2 ± 1.6) Cmax were (15.7 ± 7.8) ng · mL-1 and (16.7 ± 9.4) ng · mL-1, respectively. The AUC0-72 values calculated by trapezoidal method were (145 ± 83) ng · mL-1 · h- (142 ± 67) ng · mL-1 · h-1 and (147 ± 84) ng · mL-1 · h-1 and (144 ± 70) ng · mL-1 · h- The bioavailability of the relative reference formulation with AUC0-72 was (102 ± 40)%. Conclusion: This method has good repeatability and high sensitivity, bioequivalence of rosuvastatin calcium tablets and reference preparations.