Formulation, development, and performance evaluation of metoclopramide HCl oro-dispersible sustained release tablet

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Metoclopramide hydrochloride (HCl) is a widely used antiemetic.
• Conventional dosage forms may not provide optimal therapeutic profiles.
• Sustained release formulations can improve drug efficacy and patient compliance.

Purpose of the Study:

• To develop and evaluate an oro-dispersible, sustained release tablet of metoclopramide HCl.
• To create a dosage form combining fast oral disintegration with prolonged drug release.
• To assess the stability and in vivo performance of the developed formulation.

Main Methods:

• Preparation of metoclopramide HCl sustained release microparticles using ethylcellulose via emulsification-solvent evaporation.
• Evaluation of microparticle characteristics including morphology, particle size, and entrapment efficiency.
• Compression of optimized microparticles into fast dispersible tablets using direct compression with selected excipients.
• Assessment of tablet properties (hardness, friability, disintegration time) and in vitro drug release.
• Stability studies according to ICH guidelines and in vivo pharmacokinetic studies in rats.

Main Results:

• Spherical metoclopramide HCl microparticles with a mean diameter of 81.27 ± 5.87 μm and 70.15 ± 3.06% encapsulation efficiency were successfully prepared.
• Formulation variables significantly influenced microparticle characteristics and drug release.
• The optimized tablets exhibited good mechanical properties (hardness 59 ± 3 N, friability 0.21%) and rapid disintegration (27 ± 3 sec).
• In vitro drug release studies indicated sustained release properties.
• The formulation was stable for 6 months under ICH conditions.
• In vivo studies in rats showed sustained plasma concentrations of metoclopramide HCl for up to 20 hours.

Conclusions:

• A novel oro-dispersible, sustained release tablet of metoclopramide HCl was successfully developed.
• The combination of sustained release microparticles and fast dispersible tablet technology offers a promising approach for improved antiemetic therapy.
• The developed formulation provides prolonged drug release and stability, with potential for enhanced patient compliance.