Pharmacokinetics and Bioequivalence of Rosuvastatin Calcium Capsules and Tablets in Healthy Volunteers / 中国药师

ABSTRACT

Objective:To develop an HPLC-MS/MS method for the determination of rosuvastatin in plasma and study the relative bioavailability and bioequivalence of the capsules and tablets in Chinese healthy volunteers. Methods: A single oral dose (20 mg of the test or reference preparation) was given to 24 male healthy volunteers in a randomized crossover study. The plasma concentration of rosuvastatin was determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated and the bioavailability and bioequiva-lence of the two preparations were evaluated by DAS 3. 0 software. Results:After a single dose, the pharmacokinetic parameters of ro-suvastatin capsules and tablets were as followsTmax was (3. 56 ± 1. 68) h and (3. 63 ± 1. 56) h, Cmax was (21. 17 ± 13. 74) ng· ml-1 and (26.33 ±23.22) ng·ml-1, t1/2 was (10.68 ±5.50) h and (9.04 ±6.00) h, AUC0-t was (219.31 ±146.09) ng·h· ml-1 and (252. 43 ± 194. 96) ng·h·ml-1 , AUC0-∞ was (225. 32 ± 146. 76) ng·h·ml-1 and (257. 24 ± 194. 61) ng·h·ml-1 , respectively. The 90% confidential interval of AUC0-t, AUC0-∞ and Cmax was 81. 1%-106% , 81. 8%-105. 4% and 77. 9%-104. 5%, respectively. The mean relative bioavailability of the test preparation(the capsules) to the reference preparation(the tablets) was (100. 7 ± 54. 1)%. Conclusion:The test and reference preparations are bioequivalent.