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.