Abstract

FORMULATION AND EVALUATION OF SUSTAINED-RELEASE FLOATING TABLET OF DOMPERIDONE

Vijay Yadav*, Sharad Pudasaini, Prashann Jha, Prabin Kumar Marbaita, Anji Maharjan, Sandhya Pandit, Rabindra Kumar Rokaya, Kedar Prasad Shah, Navin Thapa Magar and Lalit Mohan Pant

ABSTRACT

Background: Domperidone is a synthetic benzimidazole compound that blocks d2 and d3 dopamine receptors, found in the chemoreceptor trigger zone, located just outside the blood-brain barrier. Being a weak base with good solubility in acidic pH but significantly reduced solubility in alkaline medium, domperidone shows better absorption characteristics in acidic medium. Aim: This study was designed to prepare a floating tablet of domperidone using methocel (HPMC K4M polymer) to complement the pharmaceutical activity of the medicament to achieve better selectivity as it gets retained in stomach pH for a longer period. Method: A total of nine formulations of floating tablets of domperidone with varying compositions of excipients were formulated by the wet granulation method and were subsequently evaluated for floating potency, weight variation, thickness, hardness, friability and in-vitro dissolution to detect the drug release mechanism. Formulations were designed by using central composite design two-level full factorial design. Result: Assay of formulations was found to be between 72-98.27%, the average weight was 180.4 mg, friability was <1%, average hardness 2 kg/cm², average diameter was 0.8 cm and minimum floating lag time was 9sec (0.15 minute) and maximum floating lag time was >44 hrs for different formulations. Formulations followed the Hixson Crowell model and first-order release kinetics. Conclusion: F6 formulation was found to be the best formulation of a sustained-release floating tablet of domperidone as it showed the maximum amount of drug released for a sustained period of 5 hours. Also, the study showed an increase in the concentration of HPMC K4M increases the time required to release the drug and an increase in the concentration of sodium bicarbonate decreases the time required to release the drug. An increase in the concentration of sodium bicarbonate increased floating lag time.

Keywords: Domperidone, Floating tablet, Methylcellulose, Sodium bicarbonate.