Two-way Crossover Bioequivalence Study of Rosuvastatin Tablets 5 Mg in Healthy, Adult, Asian-indian Male Volunteers under Fasting Condition

Objective: To compare the bioavailability and characterize the pharmacokinetic profile of the test and reference formulations of rosuvastatin tablets 5 mg in healthy, adult, Asian-Indian male volunteers under fasting condition. Methods: An open label, randomized, two-treatment, two-period, two-sequence, single dose, two-way crossover study was conducted in forty healthy adult volunteers. All the subjects were randomly allocated to receive either of the treatment arms separated by a washout period of 9 days. In each period 20 blood samples including 0.00 to till 48.0 h post dose were collected and were analyzed by a validated LC-MS/MS method. Pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞, Tmax, Kel and T1/2 of rosuvastatin were characterized using non-compartmental analysis, and 90% confidence interval were estimated for ln-transformed parameters Cmax and AUC0-t. Results: Pharmacokinetic and statistical analysis was estimated in 37 completed subjects. The estimated mean (±SD) values of Cmax (ng/mL) for test and reference were 6.348 (±2.656) and 6.204 (±2.825), respectively; and the mean (±SD) values of AUC0-t (ng.h/mL) for test and reference were 55.084 (±23.745) and 54.041 (±23.949), respectively. Conclusions: The 90% CI for Cmax (93.40-116.4) and AUC0-t (93.61-112.10) were within the regulatory acceptance limit 80.00-125.00%, hence bioequivalence was concluded between test (rosuvastatin tablets 5 mg) and reference (Crestor® tablets 5 mg) formulations. The reported adverse events i.e. high SGPT and diarrhea in 2 subjects were followed up until resolution, however both the formulations appeared to be well tolerated.