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Original Article

J App Pharm Sci. 2016; 6(10): 037-044


Physical stabilization of amorphous itraconazole in solid dispersions for improved dissolution profile

Yogesh Vilas Pore, Vikram Ramchandra Shinde, J. Venkateswara Rao.


Abstract

The main objective of the present investigation was to improve dissolution efficiency and stabilize amorphous form of itraconazole (ITR) through formulation of ternary solid dispersion system (SDs) with polyvinylpyrrolidone K30 (PVP K30) and sylysia®350 using spray drying technique. The prepared ternary SD system was characterized for solid state properties, in vitro dissolution efficiency and accelerated stability study at 40 °C/75% RH for the period of 3 months to explore extent of stabilization of amorphous itraconazole (AITR). Surprisingly, AITR was found to have no significant improvement in its dissolution characteristics compared to pure drug. The formation of cohesive supercooled liquid state might be the reason for poor solubility. Hence a combined approach of SD system with an antiplasticizing agent and surface adsorption technique was employed to prevail over functional inabilities of AITR. The binary and ternary SDs of AITR were prepared employing PVP K30 as antiplasticizer and/or sylysia®350 as adsorbent in the ratio 1:1:1 w/w using spray drying technique. The prepared systems have shown significant improvement in dissolution characteristics when compared to pure drug. Accelerated stability studies confirmed the absence of crystallization events over a period of 3 months endorsing excellent stabilization of AITR.

Key words: Itraconazole; amorphous; solid dispersion; physical stability; dissolution






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