FORMULATION AND EVALUATION OF BUCCAL TABLETS OF METOCLOPRAMIDE HYDROCHLORIDE

Abstract

The present study aimed to develop and evaluate mucoadhesive buccal tablets of Metoclopramide Hydrochloride for prolonged drug release, enhanced bioavailability, and avoidance of hepatic first-pass metabolism. A 3² full factorial design was employed to investigate the influence of Carbopol 940 (CP) and Guar Gum (GG) on drug release and mucoadhesive performance. Buccal tablets were prepared by direct compression and evaluated for physicochemical characteristics, including hardness, friability, weight variation, drug content, surface pH, swelling index, mucoadhesive strength, and in vitro drug release. FTIR studies confirmed compatibility between the drug and excipients. The cumulative drug release from different formulations ranged between 74.83% and 100.41%, with formulation F9 exhibiting the most desirable balance of sustained drug release and mucoadhesive properties. Drug release kinetics were best described by the Korsmeyer–Peppas model, indicating a non-Fickian diffusion mechanism. Stability studies conducted under accelerated conditions demonstrated the stability of the optimized formulation.The optimized formulation (F9) was further subjected to in vivo evaluation in New Zealand White rabbits. The formulation exhibited prolonged buccal residence time (6.42 ± 0.58 h), excellent mucosal tolerability, and sustained plasma drug concentrations up to 24 h. Pharmacokinetic studies revealed a significantly delayed Tmax (8.0 ± 0.6 h) and higher AUC₀–₂₄ (2946 ± 185 ng·h/mL) compared with the marketed oral tablet, indicating enhanced systemic exposure and improved bioavailability through buccal administration. The findings demonstrate that the optimized mucoadhesive buccal tablet effectively prolongs drug release, enhances bioavailability, and provides sustained therapeutic plasma concentrations. Therefore, the developed buccal delivery system represents a promising alternative to conventional oral administration of Metoclopramide Hydrochloride.