Pharmacokinetics and relative bioavailability of a generic amisulpride tablet in healthy Chinese volunteers

摘要

Objective: To assess and compare the pharmacokinetic properties and bioavailability of a newly developed formulation of amisulpride with those of a conventional formulation in healthy Chinese volunteers under fasting state. Materials and methods: A single-dose, two-sequence crossover study was designed. 20 healthy subjects (14 males and 6 females) were randomized into two groups. A single oral dose of amisulpride (200 mg) was given after an overnight fast of 12 hours. Blood samples were taken at scheduled time spots and separated by a washout period of 14 days. Plasma concentration of amisulpride was measured by high-performance liquid chromatographyfluorescence detector (HPLC-FLD) method. Results: The pharmacokinetic parameters of AUC(0-tlast), AUC(0-infinity), and Cmax for the 20 subjects after a single oral dose of the trial preparation or the reference preparation were 4,767.2 and 4,856.3 ngxhxmL(-1); 4,891.7 and 5,043.2 ngxhxmL(-1); 584.7 and 586.3 ngxmL(-1), respectively. The relative bioavailability was 98.9 +/- 14.5%. No significant difference was found among the main pharmacokinetic parameters in the two preparations by ANOVA. The 90% confidence intervals for the geometric mean ratios (test/ reference) of C-max and AUC(0-tlast) were 90.7 - 109.1% and 92.5 - 103.6%, respectively, meeting the predetermined criteria (80 - 125%) for bioequivalence. No serious adverse events were reported. Conclusion: The study demonstrated that the two preparations met the regulatory criteria for bioequivalence and both formulations were well tolerated.