Pharmacokinetics and tolerability of cinitapride in healthy Chinese volunteers: a randomized, open-label, single- and multiple-dose study. (4th March 2019)

• Record Type: Journal Article
• Authors: Zhang, Xiong; Wang, Ying; Cheng, Junlin; Hu, Yunfang; Liu, Jianghui; Chen, Jing; Yang, Xingye; Fan, Hongwei
• Is Part Of: Xenobiotica. Volume 49:Number 3(2019:Mar.)
• Page Start: 313
• Page End: 321
• Publication Date: 2019-03-04
• Subjects: Cinitapride -- pharmacokinetics -- tolerability -- single- and multiple-dose study -- gender differences; Metabolism -- Periodicals; Drugs -- Physiological effect -- Periodicals; Food additives -- Periodicals; Chemicals -- Physiological effect -- Periodicals; Biochemistry -- Periodicals; Pharmaceutical Preparations -- metabolism -- Periodicals; Metabolism -- Periodicals; 574.133
• DOI: 10.1080/00498254.2018.1447710
• Languages: English
• ISSNs: 0049-8254

Abstract

Abstract: Cinitapride (CIN) is a drug for functional dyspepsia. The purpose of the study was to investigate the pharmacokinetics and tolerability of CIN in healthy Chinese volunteers. A randomized, open-label, single- and multiple-dose study was conducted in 12 healthy volunteers. Three different doses of CIN (1, 2, 4 tablets) were given to six groups in the single-dose study, and one tablet (1 mg) of CIN was administered three times a day in the multiple-dose study. Blood samples were collected at predetermined time intervals after CIN dosing and analyzed by LC-MS/MS. Eleven volunteers completed the study. After single dose, the C max and AUC of plasma increased approximately linearly with dosage; no statistically significant differences were found in pharmacokinetic parameters between three dose groups. After multiple doses, there was no significant change in T max and t 1/2 compared with the results from the single dose. After repeated doses, AUC0-t and AUC0-∞ were increased, while CLz/F slightly decreased. And no differences between male and female. The pharmacokinetic parameters of this study were consistent with study results of non-Chinese subjects. Good tolerability was demonstrated in both single- and multiple-dose studies with dosage range from 1 to 4 mg in healthy Chinese subjects.