Preparation and Evaluation of Sustained Release Matrix Formulations of Voriconazole

Abstract

Voriconazole is a triazole antifungal with a half-life of 1.7 hours and 96% oral bioavailability. The oral route is the most popular of drug delivery routes. However, there are a few limitations to the traditional dosage form, for instance, fluctuations in plasma drug level. Sustained drug delivery system overcomes these limitations; it helps to maintain stable plasma drug concentrations by decreasing drug r elease and extending the duration of the effect. The main purpose of this study was to formulate voriconazole sustained release dosage form to enhance efficacy, decrease dose frequency, decrease its side effects, and improve patient compliance. The study explored various formulations for producing the sustained-release (S.R) dosage form, as well as assessed the drug's release kinetics and its stability.Methodology: Fourier-transform Infrared Spectroscopy was used to investigate drugpolymer compatibility. The micromeritics of voriconazole powder and its blends were evaluated. Different sustained release tablets were formulated utilizing a wet granulation process and acrylic polymers (Eudragit) i.e., Eudragit RL100 and RS100 alone and as mixtures with different ratios, in different concentrations. In-vitro drug release of formulae was performed for 24 hours. The formula with desired control of drug release and complied with dissolution specifications for SR dosage forms was further evaluated for its stability by storage for 3 months at 30 o C and 40 o C and 75% relative humidity.Results: no interaction was observed between voriconazole and polymers using FTIR. The powder blends micromeritics were found to be in accordance with the specification. Tablets showed release from 37.29 to 76 % up to 24 hr using USP type I technique. It was found that as polymer concentration increased, the drug release from tablet decreased. The selected formulation F13 which containing 5% of Eudragit RL100:RS100 at a ratio of (10:1) was found to be stable. Conclusion:The obtained data concluded that the F13 formula gave more prominent S.R effect than using Eudragit RL100 or RS 100 alone.