The effect of food on the pharmacokinetic properties and bioequivalence of two formulations of pitavastatin calcium in healthy Chinese male subjects. (2nd January 2016)

• Record Type: Journal Article
• Authors: Shang, Dewei; Deng, Shuhua; Yao, Zhenhong; Wang, Zhanzhang; Ni, Xiaojia; Zhang, Ming; Hu, Jinqing; Lu, Haoyang; Zhu, Xiuqing; Huang, Wencan; Qiu, Chang; Wen, Yuguan
• Is Part Of: Xenobiotica. Volume 46:Number 1(2016:Jan.)
• Page Start: 34
• Page End: 39
• Publication Date: 2016-01-02
• Subjects: Bioequivalent -- food effect -- pharmacokinetics -- pitavastatin; Metabolism -- Periodicals; Drugs -- Physiological effect -- Periodicals; Food additives -- Periodicals; Chemicals -- Physiological effect -- Periodicals; Biochemistry -- Periodicals; Pharmaceutical Preparations -- metabolism -- Periodicals; Metabolism -- Periodicals; 574.133
• DOI: 10.3109/00498254.2015.1046153
• Languages: English
• ISSNs: 0049-8254

Abstract

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 AUC0–48 h ratios were 92.2–102.4%, 93.1–104.5%, the ratios of ln(AUC0–∞ ) 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 AUC0–48 h, AUC0–∞ and C max decreased noticeably following a high-fat breakfast. Values for AUC0–48 h were 87.69% and 83.7%, values for AUC0–∞ 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.