Abstract
Chemical degradation of drugs may result in altered therapeutic efficacy and even toxic effects. Therefore, understanding the factors that change the stability of pharmaceuticals and identifying ways to guarantee their stability are important. In this work stability-indicating Liquid Chromatographic (LC) and bioassay methods were validated and employed in the fluconazole stability studies. The correlation of sample results from both methods was evaluated. Fluconazole raw material stability was investigated in aqueous, acid (0.1 M HCl), alkaline (0.1 M NaOH) and oxidative (3% v/v H2O2) reflux for 6 hours, by LC method. Fluconazole capsules were exposed to UVC (254 nm, 66 and 180 days), climatic chamber (40°C, 75% RH, 90 days) and oven (60°C, 60 days), these samples were analyzed by LC and bioassay methods It was found that the drug is degraded (10% decrease) with arising of a possible degradation product in an oxidative medium and UVC exposure, in all the others conditions fluconazole remained chemically stable (higher than 98%) when analyzed by LC. However when the capsules stressed samples were evaluated through bioassay very low antifungal activity was found (about 30%). Fluconazole showed to be an unstable drug and it indicates that special care must be taken during the handling, storage and quality control using appropriated methods to analyze this therapeutic agent. This work suggests monitoring the fluconazole stability by bioassay and the stability-indicating LC methods.
Highlights
Stability is defined as the capacity of a drug substance or product to remain within established specifications and to maintain its identity, strength, quality, and purity throughout expiration dating period
Liquid Chromatographic (LC) is a separation method widely used in stability studies
The results indicate that the most adverse conditions to fluconazole stability are an oxidative medium, UVC-254 radiation and elevated temperature
Summary
Stability is defined as the capacity of a drug substance or product to remain within established specifications and to maintain its identity, strength, quality, and purity throughout expiration dating period. Pharmaceuticals are especially sensitive to environmental factors. Strict storage conditions are necessary for the maintenance of integrity and product activity [1]. Stability test of an active substance or drug product can provides evidence on the drug quality and if it can be influenced by a variety of environmental factors such as temperature, humidity and light [1]. Chemical and physical degradation of drugs may result in altered therapeutic efficacy and even toxic effects. Understanding the factors that change the stability of pharmaceuticals and identifying ways to guarantee their stability are important [2]
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