Ktoconazole Case Study

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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…show more content…
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…show more content…
Ethyl cellulose (2gm) was dissolved in 20 ml of methylene chloride and KTZ was added to this solution, in varying amounts, corresponding to theoretical initial loading range from 5 to 40%w/w (F1- F7), Table 2. The polymer phase was then added to 250 ml of 0.25% w/v methylcellulose aqueous solution (over night dispersion). Agitation was maintained at 350 rpm until complete evaporation of methylene chloride. Microspheres were then collected, washed three times with distilled water, filtered and stored under reduced pressure, overnight in a desiccator to ensure complete removal of residual solvent. At the end of 15 minutes residual ketoconazole microspheres were again subjected to 0.1N HCl and absorbance of filtered extract was determined. It was found to be negligible with negative absorbance to the tune of 0.001 and TLC of the sample did not show any spot corresponding to KTZ. EVALUATION OF KETOCONAZOLE MICROSPHERES Drug entrapment

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