Acta Pharm. 61 (2011) 435-445
Short communication
Liquid antisolvent precipitation process for
solubility modulation of bicalutamide
TARIQUE
ALI MEER, KIRAN P. SAWANT and PURNIMA D. AMIN
purnima.amin@yahoo.co.in
Department
of Pharmaceutical Sciences and Technology, Institute of Chemical Technology,
Matunga, Mumbai-400019, India
Accepted October 12, 2011
Liquid antisolvent process was explored as a solubility modulating tool. Bicalutamide, a poorly water soluble drug, was used as a candidate. Low aqueous solubility and poor dissolution of bicalutamide results into poor and variable bioavailability. Therefore, the objective of the present work was to modify the solubility of bicalutamide using the liquid antisolvent precipitation process. HPMC E5 and Poloxamer 407 were shortlisted as a hydrophilic polymer and surfactant, respectively, for the process. Process optimization was done with respect to the hydrophilic polymer, surfactant and drug loading concentration. The resultant microcrystals were characterized with various instrumental techniques for material characterization such as IR, DSC, SEM, XRD, particle size, specific surface area and dissolution kinetics.
Keywords: words: bicalutamide, solubility enhancement, dissolution
rate, liquid antisolvent precipitation