The effect of food on the pharmacokinetic properties and bioequivalence of two formulations of pitavastatin calcium in healthy Chinese male subjects

Abstract

1. Pitavastatin is an effective treatment for primary hyperlipidemia and mixed dyslipidemia. The aim of the present study was to investigate the effect of food on the pharmacokinetic properties and bioequivalence of the original, branded, formulation of pitavastatin calcium and a new generic formulation in healthy Chinese male subjects under fasting and fed conditions.

2. Under fasting and fed conditions, 90% CIs of the geometric mean of generic/branded AUC_0–48 h ratios were 92.2–102.4%, 93.1–104.5%, the ratios of ln(AUC_0–∞) were 92.6–103.7%, 93.2–103.5%, and ln(C_max) ratios were 90.7–110.3%, 84.7–100.8%, respectively. The generic and branded formulations were bioequivalent in terms of rate and extent of absorption under both the conditions. The average values of AUC_0–48 h, AUC_0–∞ and C_max decreased noticeably following a high-fat breakfast. Values for AUC_0–48 h were 87.69% and 83.7%, values for AUC_0–∞ were 87.5% and 84.6%, and values for C_max were 45.0% and 50.4% in subjects given the generic and branded preparations, respectively. The absorption of pitavastatin calcium tablets was delayed following a high-fat meal, with T_max increasing by up to 2.43-fold.

3. Both formulations were generally well tolerated, with no serious adverse reactions reported. The newly developed generic formulation may provide a reliable alternative to the branded tablets for patients with primary hyperlipidemia or mixed dyslipidemia.

• Bioequivalent
• food effect
• pharmacokinetics
• pitavastatin

Declaration of interest

This research was sponsored by Hualon Pharmaceutical Co. Ltd. (Hannan, China), the manufacturer of pitavastatin calcium tablets. Z.Y. is an employee of Hualon Pharmaceutical Co. Ltd. The authors have indicated that they have no conflicts of interest with regard to the content of this article. This work was supported by grants from Guangdong Science and Technology Major Project (grant no. 2011A080300003) and Guangzhou municipal key discipline in medicine for Guangzhou Brain Hospital (grant no. GBH2014-ZD07).