Abstract

STUDIES ON PARTIAL AMORPHIZATION OF CARBAMAZEPINE USING MEDIA MILLING IN SYNERGISM WITH SPRAY DRYING

*Harita Desai, Komal Meshram, Juilee Parab, Akanksha Kolhe and Purnima Amin

ABSTRACT

The present study's goal was to investigate top-down size reduction methods like high-speed homogenization and media milling in synergism with spray drying in amorphization and improvement in solubility of BCS Class II Carbamazepine drug. Spray-dried micronized carbamazepine was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. The ratio of the drug to the stabiliser and the duration of homogenization and ball milling, were optimised. Spray drying was used to transform the obtained dispersion into solid powder. The obtained Spray-dried micronized Carbamazepine was evaluated using various techniques like visual morphology, infrared spectroscopy, differential scanning calorimetry, x-ray diffractometry, in vitro drug release, solubility, scanning electron microscopy, contact angle measurement and aqueous dispersibility, According to studies, Carbamazepine exhibited amorphization of the crystalline form of the drug. Spray-dried micronized carbamazepine demonstrated enhanced drug hydrophilicity and solubility as observed from the contact angle and increase in the solubility and ease of dispersibility. An increase in in vitro drug release was observed from 14% for plain drug to 51% for spray dried-micronized Carbamazepine. For the poorly soluble drug Carbamazepine, media milling in conjunction with spray-drying was found to amorphize Carbamazepine leading to increase in solubility and dissolution rate.

Keywords: Carbamazepine, Solubility, Media milling, Homogenization, Spray drying, Contact angle.