Metoclopramide-oros dispersible tablets optimized formula bioavailability study

Abstract

BACKGROUND: Bioavailability and bioequivalence studies required by regulations to ensure therapeutic equivalence between a pharmaceutically equivalent test product and a reference product. AIM: This study aimed to evaluate the bioavailability performance between the optimum formula of OROS dispersible tablet-metoclopramide dosage forms (FCL-6) and the Primperan® as the reference product. METHODS: The FCL-6 formula was design by simplex lattice design model with a three components mixture of excipients: Solid tapai extract, corn starch, and Avicel. The optimum formula of OROS dispersible tablet (ODT)metoclopramide consists of solid tapai extract (27.038 mg), corn starch (27.407 mg), and Avicel (53.555 mg), metoclopramide hydrochloric acid (HCl) (10.00 mg), LH-11 (22.50 mg), aspartame (5.00 mg), talcum BP (3.00 mg), and Mg stearate (1.50 mg). The in vivo test was done by cross-over design method using six rabbits. The level of metoclopramide concentration from in vivo test was measured by high-performance liquid chromatography instrument. RESULTS: The study revealed that the tmax, Cmax, and area under curve (AUC) of ODT-metoclopramide FCL-6 were 60 min, 1.95 ± 0.13 µg/mL, and 1118.20 ± 150 µg/mL. min consecutively. The Cmax and the concentration of the drug absorbed in the blood (AUC) of ODT-metoclopramide were larger than Primperan® tablets. Statistical data of the optimized ODT-metoclopramide compared with Primperan® showed that the Cmax and AUC significance values were <0.05 (p < 0.05). CONCLUSION: The optimized formula of ODT-metoclopramide revealed a better characteristic of Cmax and AUC concentration compared with Primperan®. The optimized ODT-metoclopramide with tapai extract was found to be promising to improved bioavailability of metoclopramide.