FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF METOCLOPRAMIDE HYDROCHLORIDE USING NATURAL AND SYNTHETIC SUPERDISINTEGRANTS

Sumit, Munish, Lovekesh Nagpal*

ABSTRACT

Background: Fast dissolving tablets (FDTs) of metoclopramide hydrochloride, a dopamine antagonist used for nausea, vomiting and gastroparesis, can serve patients who cannot swallow conventional tablets or have no access to water. Objective: To develop and evaluate directly compressed FDTs of metoclopramide hydrochloride using two synthetic superdisintegrants (crospovidone and croscarmellose sodium) and one natural superdisintegrant (ispaghula husk). Methods: Swelling indices of the disintegrants were determined in water, 0.1 N HCl and phosphate buffer (pH 6.8). Twelve 200 mg tablets (F1–F12), each containing 10 mg of drug and 5, 10, 15 or 20 mg of a superdisintegrant, were compressed with microcrystalline cellulose as diluent. Blends and tablets were evaluated for flow, hardness, friability, weight and content uniformity, disintegration, dispersion and wetting time, and in vitro dissolution against a marketed tablet (Reglan). Drug–excipient compatibility was examined by FTIR. Results: Ispaghula husk showed the highest swelling index (86.70 ± 0.95% in water), followed by croscarmellose sodium (76.26 ± 0.65%) and crospovidone (57.23 ± 1.29%). All blends flowed well (angle of repose 25.96–30.49°; Hausner ratio 1.08–1.16). Disintegration time ranged from 9.33 s (F8, croscarmellose sodium) to 93.66 s (F4, crospovidone); the best ispaghula batch (F12) disintegrated in 15.53 s. After 4 min, F8 and F12 released 99.75% and 99.01% of drug, against 27.76% for the marketed tablet. FTIR revealed no drug–excipient interaction. Conclusion: Croscarmellose sodium and ispaghula husk, at 20 mg per tablet, gave rapidly disintegrating, mechanically acceptable metoclopramide FDTs, and ispaghula husk is a credible natural alternative to synthetic superdisintegrants.

Keywords: metoclopramide hydrochloride; fast dissolving tablets; superdisintegrants; croscarmellose sodium; crospovidone; ispaghula husk; direct compression.