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136 ESOMEPRAZOLE PACKET (SACHET) FORMULATION FOR SUSPENSION IS BIOEQUIVALENT TO ESOMEPRAZOLE TABLET AND CAPSULE FORMULATIONS M Niazi, A Backlund, M Fjellman, C Lundin AIMS: A packet (sachet) formulation of esomeprazole for suspension has recently been developed for patients who have difficulty swallowing solid dosage forms. This randomized, open-label, 3-way crossover study aimed to establish whether the packet formulation is bioequivalent to the corresponding dose of an intact tablet or capsule.
AstraZeneca R&D, Mölndal, Sweden
METHODS: Healthy volunteers aged 20-50 years were enrolled. On each of the 3 study days (separated by washout periods of =>6 days), subjects received esomeprazole 40 mg either as the packet formulation or the corresponding commercially available tablet or capsule. Blood samples for the determination of esomeprazole in plasma were collected for up to 10 hours after drug administration. Total area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) were analyzed using a mixed model analysis of variance. In accordance with standard regulatory requirements, bioequivalence was established if the 90% confidence intervals (CIs) for ratios (packet:capsule and packet:tablet) of geometric means for AUC and Cmax were between 0.80 and 1.25.
RESULTS: In total, 96 volunteers (56 women, mean age 24.9 years) were randomized. The estimated ratios of geometric means for the packet:capsule and packet:tablet formulations were for AUC, 0.98 (90% CI: 0.93, 1.03) and 0.99 (90% CI: 0.94, 1.04), respectively and for Cmax, 0.90 (90% CI: 0.84, 0.96) and 0.95 (90% CI: 0.89, 1.01), respectively. Mean elimination half-life and time to Cmax were approximately 1.1 hours and 2 hours, respectively, for all 3 formulations. All formulations were well tolerated.
CONCLUSIONS: The packet (sachet) formulation of esomeprazole has pharmacokinetic bioequivalence to existing solid dosage forms and therefore provides an alternative dosing option for patients who are unable or unwilling to swallow solid dosage forms.
Supported by AstraZeneca. All authors are employees of AstraZeneca