Volume 9, Issue 6 p. 671-676
Original Manuscript

Pharmacokinetics, Bioequivalence, and Safety Studies of Prucalopride in Healthy Chinese Subjects

Ziye Zhou,

Ziye Zhou

Department of Pharmacy, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

Ziye Zhou and Chenxiang Wang contributed equally to this work.

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Chenxiang Wang,

Chenxiang Wang

Department of Pharmacy, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

Ziye Zhou and Chenxiang Wang contributed equally to this work.

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Xuyong Zheng,

Xuyong Zheng

Department of Pharmacy, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

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Xuben Yu,

Xuben Yu

Department of Pharmacy, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

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Chao Yu,

Chao Yu

Department of Pharmacy, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

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Dongchuan Zhang,

Dongchuan Zhang

Dikang Pharmaceutical Co, Ltd, Sichuan, China

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Yan Xia,

Yan Xia

Leeway Biological Technology Co, Ltd, Jiangsu, China

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Huafang Chen,

Huafang Chen

Office of Drug Clinical Trial Institution, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

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Xiaoxiao Huang,

Xiaoxiao Huang

Office of Drug Clinical Trial Institution, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

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Xiuhua Zhang,

Corresponding Author

Xiuhua Zhang

Office of Drug Clinical Trial Institution, First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China

Corresponding Author:

Xiuhua Zhang, First Affiliated Hospital of Wenzhou Medical University, Nanbaixiang Street, Ouhai District, Wenzhou, Zhejiang 325000, China

(e-mail: wzzhangxiuhua@126.com)

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First published: 03 December 2019

Abstract

The objectives of the present study were to evaluate the bioequivalence of 2 tablet formulations of prucalopride, generic and branded, and to investigate relevant pharmacokinetic and safety profiles. This study was designed as a randomized, open-label, fasting, single-dose, crossover, and dual-period trial. After overnight fasting, 12 subjects were given prucalopride tablets via oral administration, and blood specimens were obtained up to 96 hours after dosing. Prucalopride concentrations in plasma were measured using ultraprecision liquid chromatography–tandem mass spectrometry followed by calculation of pharmacokinetic parameters. The safety of prucalopride was assessed throughout the study. The pharmacokinetics of prucalopride can be defined as a 2-compartment model with a long elimination phase. No significant differences were observed between the pharmacokinetic profiles of the generic and branded prucalopride tablets. Bioequivalence was evaluated using 90%CIs for the ratio test/reference of log area under the concentration-time curve over 96 hours, log area under the concentration-time curve to infinity, and log peak concentration from generic and branded tablets, which were 100.06–109.94%, 100.63–110.32%, and 95.84–113.08%, respectively. During administration of the medication, there were 18 adverse events in 6 subjects in the test formulation group and 19 cases of adverse events in 6 subjects in the reference formulation group (P > .05). No severe adverse effects were detected. These results suggest that generic and branded prucalopride tablets are bioequivalent and show similar safety profiles.