Bioequivalence Study of 2 Orodispersible Formulations of Zolmitriptan 5 mg in Healthy Volunteers

Abstract

A bioequivalence study of 2 zolmitriptan (CAS 139264-17-8) orodispersible tablet formulations was carried out in 26 healthy volunteers according to an open label, randomized, 2-period, 2-sequence, crossover, single dose and fasting conditions design. The test and reference formulations were administered in 2 treatment days, separated by a washout period of 7 days. Plasma concentrations of zolmitriptan and its active metabolite (N-desmethyl-zolmitriptan) were obtained by LC/MS/MS method. Log-transformed AUCs and Cmax values were tested for bioequivalence based on the ratios of the geometric means (test/reference). Tmax was analysed nonparametrically. The 90% confidence intervals of the geometric mean values for the test/reference ratios for AUC0-t and Cmax were within the bioequivalence acceptance range of 80-125%. According to the European Guideline 1 it may be therefore concluded that test formulation of zolmitriptan 5 mg orodispersible tablet is bioequivalent to the reference formulation.

Intranasal Pharmacokinetic Data for Triptans Such as Sumatriptan and Zolmitriptan Can Render Area Under the Curve (AUC) Predictions for the Oral Route: Strategy Development and Application

“…Using mean concentration vs. time profiles from the pharmacokinetic studies for sumatriptan [23][24][25][26]28,30,31,[33][34][35] and zolmitriptan, [40][41][42][43][44][45]47 the AUC predictions were made using the concentration data at the select time point for the two triptans that would likely coincide with the T max value for the respective drug. Accordingly, the concentrations observed at 1 and 3 hours from the mean concentration vs. time plots for sumatriptan and zolmitriptan, respectively, were considered appropriate for this analysis.…”