Pharmacokinetics and tolerability of cinitapride in healthy Chinese volunteers: a randomized, open-label, single- and multiple-dose study

Abstract

1. 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.

2. 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.

3. 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, AUC_0-t and AUC_0-∞ were increased, while CLz/F slightly decreased. And no differences between male and female.

4. 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.

Keywords:

• Cinitapride
• pharmacokinetics
• tolerability
• single- and multiple-dose study
• gender differences

Disclosure statement

We have no declarations or conflicts of interest.

Additional information

Funding

This work was supported by ALMIRALL Prodesfarma, S.A. (Drug clinical trial approval number 2008L10331; Nanjing First Hospital Ethics Committee approval number YW2010020).