Liquid antisolvent precipitation process for solubility modulation of bicalutamide

T. Meer,Kiran P. Sawant,P. Amin

Published 2011 in Acta Pharmaceutica

ABSTRACT

Liquid antisolvent precipitation process for solubility modulation of bicalutamide 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. Tekućinski antisolvent postupak taloženja za modifikaciju topljivosti bikalutamida Tekućinski antisolvent postupak upotrijebljen je za moduliranje topljivosti bikalutamida. Zbog vrlo slabe topljivosti u vodi i sporog oslobađanja, bioraspoloživost bikalutamida je mala i varijabilna. Cilj rada je poboljšati topljivost bikalutamida koristeći antisolvent precipitaciju. Kao hidrofilni polimer korišten je HPMC E5, a kao surfaktant Poloxamer 407. Variranjem količine polimera, surfaktanta i lijeka proces je optimiran. Nastali mikrokristali analizirani su uobičajenim instrumentalnim tehnikama za karakterizaciju materijala kao što su IR, DSC, SEM, XRD, veličina čestica, specifična površina i brzina oslobađanja.

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