European Journal of Biomedical and Pharmaceutical Sciences

DISSOLUTION RATE ENHANCEMENT OF DOMPERIDONE MALEATE THROUGH FORMATION OF HYDROXYPROPYL ?-CYCLODEXTRIN - HYDROPHILIC POLYMER COMPLEXES

Varalakshmi Mummidi* and Ajay Babu Ch.

ABSTRACT

Complexation of domperidone maleate with hydroxypropyl β-cyclodextrin (HPβCD) in the presence and absence of 3 hydrophilic polymers—polyvinyl pyrrolidone (PVP), and hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) —was investigated with an objective of evaluating the effect of hydrophilic polymers on the complexation and solubilizing efficiencies of HPβCD and on the dissolution rate of domperidone maleate from the HPβCD complexes. The phase solubility studies indicated the formation of domperidone maleate-HPβCD inclusion complexes at a 1:1M ratio in solution in both the presence and the absence of hydrophilic polymers. The complexes formed were quite stable. Addition of hydrophilic polymers markedly improved the complexation and solubilizing efficiencies of HPβCD. Solid inclusion complexes of domperidone maleate-HPβCD were prepared in 1:1 and 1:2 ratios by the kneading method, with and without the addition of hydrophilic polymers. The solubility and dissolution rate of domperidone maleate were significantly improved by complexation with HPβCD. The domperidone maleate-HPβCD (1:2) inclusion complex yielded a 11.21-fold increase in the dissolution rate of domperidone maleate. The addition of hydrophilic polymers also markedly improved the dissolution rate of domperidone maleate from HPβCD complexes: a 31.39-, 25.41-, 19.72- and fold increase was observed with PVP, HPMC and PEG respectively. X-ray diffractometry and differential scanning calorimetry indicated stronger drug amorphization and entrapment in HPβCD because of the combined action of HPβCD and the hydrophilic polymers.

Keywords: Domperidone maleate, hydroxypropyl ?-cyclodextrin, hydrophilic polymers, complexation, dissolution rate.