Essay On Ketoconazole

Keywords: Ketoconazole, Antifungal agents, Optimization, Baker Lonsdale model, Peppas model, Higuchi plot

INTRODUCTION The main objective was to design diffusion controlled microsphere drug delivery system of ketoconazole in order to sustain the delivery of the drug and thereby reduce the gastrointestinal disturbances and dose related adverse effects like hepatic dysfunction and allergic reactions as observed with conventional oral dosage form of ketoconazole (tablet). Ketoconazole microspheres prepared using dichloromethane, one of the class II solvents proposed in ICH guidelines (Q3C) to be used in the pharmaceutical industry because of their low toxic potential, as the coacervating agent to reduce residual solvent. MATERIALS AND METHODS
Materials
Ketoconazole was obtained as gift sample from Torrent pharmaceuticals ltd (Indrad)

The optimized ratios of the polymers were calculated by using 22 factorial design. (Table 1). Ethyl cellulose (2gm) was dissolved in 20 ml of methylene chloride2. The polymer phase of ethyl cellulose was then added to 250 ml of 0.25% w/v methylcellulose aqueous solution (over night dispersion). Agitation speed was maintained at 350 rpm which helps in complete removal of methylene chloride. Microspheres were then collected, filtered, washed three times with distilled water and stored under reduced pressure, overnight in a desiccator. Additionally, optimization of the process was done by selecting suitable stirring device element i.e. magnetic stirrer vs mechanical stirrer in order to improve the shape and yield of microspheres. A paired t- test was applied for final selection of the stirring element based on 95% confidence