Pharmacokinetics and Bioequivalence Study of a Fixed Dose Combination of Rabeprazole and Itopride in Healthy Indian Volunteers

Abstract

The aim of the present study was to compare the pharmacokinetics of rabeprazole (CAS 117976-89-3) and itopride (CAS 122898-67-3) after oral administration of a rabeprazole (20 mg)-itopride (150 mg) fixed dose combination (FDC) in healthy human volunteers. The bioequivalence of two formulations (test and reference) was determined in 12 healthy Indian male volunteers (age: 25.25 ± 4.69 years; weight: 60.50 ± 5.04 kg) in a randomized, single-dose, two-period, two-treatment crossover study. Both formulations were administered orally as a single dose, with the treatments separated by a washout period of 1 week. Rabeprazole and itopride plasma levels were determined by a validated HPLC method using UV detection. The formulations were compared using the pharmacokinetic parameters area under the plasma concentrationtime curve (AUC_0–t), area under the plasma concentration-time curve from zero to infinity (AUC_0–∞) and peak plasma concentration (C_max). General linear model (GLM) procedures were used in which sources of variation were subject, treatment and period. The results indicated that there were no statistically significant differences (P > 0.05) between the logarithmically transformed AUC_0–∞ and C_max values between test and reference formulation. The 90% confidence interval for the ratio of the logarithmically transformed AUC_0–t, AUC_0–∞ and C_max were within the bioequivalence limits of 0.8–1.25 and the relative bioavailability of rabeprazole and itopride test and reference formulations was 98.24 and 93.65%, respectively.

Key words

CAS 117976-89-3 - CAS 122898-67-3 - Itopride, bioequivalence, fixed dose combination, pharmacokinetics - Proton pump inhibitors - Rabeprazole, bioequivalence, fixed dose combination, pharmacokinetics

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