Fluconazole

To develop and validate simple, rapid, linear, accurate, precise and economical UV Spectroscopic method for estimation of Fluconazole in tablet dosage form. The drug is freely soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide. The drug was identified in terms of solubility studies and on the basis of melting point done on Melting Point Apparatus of Equiptronics. It showed absorption maxima were determined in Ethanol. The drug obeyed the Beer’s law and showed good correlation of concentration with absorption which reflect in linearity. The UV spectroscopic method was developed for estimation of Fluconazole in tablet dosage form and also validated as per ICH guidelines. The drug is freely soluble in organic solvents such as Ethanol, DMSO, and Dimethyl Formamide. So, the Analytical Grade Ethanol is used as a diluent in method. The melting point of Fluconazole was found to be 139-140?C (uncorrected). It showed absorption maxima 252 nm in Ethanol. On the basis of absorption spectrum the working concentration was set on 60µg/ml (PPM). The linearity was observed between 20-100 μg/ml (PPM). The results of analysis were validated by recovery studies. The recovery was found to be 98.75, 101.00 and 100.83% for three levels respectively. The % RSD for precision was found to be 0.78%. A simple, rapid, linear, accurate, precise and economical UV Spectroscopic method has been developed for estimation of Fluconazole in tablet dosage form. The method could be considered for the determination of Fluconazole in quality control laboratories.

A fluconazole o/w microemulsion was developed for topical application using isopropyl myristate as the oil phase. Pseudo-ternary phase diagrams were constructed for the determination of existence region of micro emulsion region using the surfactant (tween 80 & Cremophor RH-40) and co-surfactant (ethanol). Different formulations were prepared for the evaluation of oil content, surfactant/co-surfactant concentration on in-vitro permeation rates. In-vitro transdermal permeability of flucanazole from the micro emulsions was evaluated using Keshary Chien diffusion cells mounted with 0.45µ with cellulose acetate membrane. The amount of drug (Fluconazole) permeated was analyzed by HPLC.

The present investigation focuses on the Optimization and formulation of medicated nail lacquer containing Fluconazole for transungual drug delivery system using ethyl cellulose as polymer and two different penetration enhancers. Fluconazole is a tri azole antifungal drug having broad spectrum activity. It acts by inhibiting 14 – α demethylase, a cytochrome P450 enzyme which converts lanosterol to ergosterol. Ergosterol inhibition causes increase in permeability of cellular membrane of fungi and hence leakage of cellular components. In present study Formulations were designed according by the design expert software 8.0.7.1 and the central composite design was selected for designing of experiments. The prepared formulations were evaluated for the different parameters such as drying time, smoothness of flow, gloss, water resistance, non – volatile content, drug content, in – vitro diffusion studies, in – vitro permeation studies, drug release kinetic studies. By applying the available information from the evaluation of nail lacquer 35 optimized formulations were obtained and out of which three were selected for further studies. Three optimized products were subjected to different evaluation parameters, drug release kinetics, anti – fungal testing and stability studies. Key words: transungual drug delivery, Fluconazole, optimization, penetration enhancers, in – vitro permeation studies, ethyl cellulose.