生物学的同等性とバイオアベイラビリティのジャーナル

概要

Bioequivalence Study of Rosuvastatin 20 mg Tablets in Healthy Thai Volunteers under Fasting Conditions

Jaturavit Vattanarongkup, Charinthon Seeduang, Sumate Kunsa-ngiem, Vipada Khaowroongrueng, Lalinthip Saeaue, Busarat Karachot, Piengthong Narakorn, Porranee Puranajoti, Isariya Techatanawat

Rosuvastatin is a member of high-potency statins. It is indicated for the treatment of homozygous familial hypercholesterolemia, hyperlipidemia, mixed dyslipidemia, primary dysbetalipoproteinemia, and hypertriglyceridemia. The study aimed to compare the rate and extent of absorption as well as safety of two rosuvastatin 20 mg tablet formulations; the test product ROZACOR^® manufactured by the Government Pharmaceutical Organization, Thailand and the reference product CRESTOR^® manufactured by IPR Pharmaceuticals Inc., Puerto Rico. An open label, randomized, two-treatment, two-sequence, two-period, single oral dose, crossover bioequivalence study was conducted in healthy Thai adult volunteers under fasting conditions. The concentrations of rosuvastatin in plasma samples were determined using a validated liquid chromatography-tandem mass spectroscopy method. The pharmacokinetic parameters were computed from the plasma concentration-time data using a non-compartmental model. The 90% confidence intervals of the geometric least squares mean ratios (test/reference) were 91.81%- 104.50%, 93.26%-105.29% and 89.88%-105.96% for ln-transformed AUC_0-tlast, AUC_0-∞ and C_max, respectively which were within the bioequivalence limits of 80.00%-125.00%. Both test and reference products were well tolerated by the study subjects. There were total 5 incidents of mild adverse events reported in this study. In conclusion, ROZACOR^® and CRESTOR^® were bioequivalent in terms of rate and extent of absorption and can be used interchangeably.