Pharmacokinetics and Bioequivalence Studies of Galantamine Hydrobromide Dispersible Tablet in Healthy Male Chinese Volunteers

Abstract

ABSTRACTA randomized, two-way, crossover study was conducted in 18 healthy male Chinese volunteers to compare pharmacokinetics profiles of galantamine hydrobromide dispersible tablet with that of conventional tablet. A single oral dose of 10 mg galantamine was administrated to each volunteer. Plasma concentrations of galantamine were determined by a validated high-performance liquid chromatography (HPLC) method with fluorescence detection, which allowed 1 ng/mL to be assayed as the lowest quantifiable concentration. From plasma concentrations, AUC0→t (the area under the plasma concentration-time curve from time 0 to the last sampling time, 32 hr), AUC0→∞ (the area under the plasma concentration-time curve from time 0 to infinity), t½ (elimination of half-life of the terminal log linear phase), Cmax (maximum plasma drug concentration) and Tmax (time to reach Cmax) were evaluated through noncompartmental pharmacokinetic analysis. AUC0→t and AUC0→∞ were calculated by the linear-log trapezoidal rule method. Cmax and Tmax were obtained directly from the plasma concentration-time curve. Analysis of variance was carried out using logarithmically transformed AUC0→t, AUC0→∞ and Cmax. As far as AUC0→t, AUC0→∞ and Cmax were concerned, there was no statistically significant difference between the test and reference formulations. Ninety percent confidence intervals (90% CI) for the ratio of AUC0→t, AUC0→∞ and Cmax values for the test and reference formulations were 100.4–107.8%, 99.0–107.2% and 87.5–111.3%, respectively. As the 90% CIs of AUC0→t, AUC0→∞ and Cmax were entirely within 80–125%, two formulations were considered bioequivalent.