Formulation and evaluation of mucoadhesive fluconazole vaginal tablets

A. Raza, Taiba Waheed, Usama Ikhlaq, Rimsha Farooq, Qasim Raza, Z. Javed, T. Hussain
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Abstract

Objective: Fluconazole is a triazole antifungal agent, and is used to treat fungal infections but because of frequent dosing and undesirable side effects it affects patient compliance. There came the need for a delivery system that can skip first pass metabolism and adhere long enough to treat the infection effectively, that was the aim for this study. Mucoadhesive drug delivery system adheres to mucous membrane and provide prolonged and sustained drug release. Method: Five formulations were formed by granulation method. The granules were then compressed and tablets were formed each of 250mg. Different evaluation parameters were determined like hardness, friability, weight variation, content uniformity, mucoadhesive strength, swelling index, dissolution and compatibility analysis. Results: The hardness (7.2-8.9kg), friability (0.02-0.05%), weight variation (0.1-0.4%), content uniformity (96.9-103%), were all in the pharmacopeial range. Dissolution was determined using rotating paddle apparatus with a phosphate buffer of 6.8 pH. Release kinetics showed that F1, F2, F3 showed Fickian release while F4 showed both Fickian and non Fickian release and F5 showed non Fickian release. Mucoadhesive strength was found to be the highest (46g) in formulation F5. The highest swelling index (70.34%) was shown by formulation F3 at 12h. Differential scanning calorimeter and Fourier transform infrared spectroscopy showed that there is no interaction between excipients. Conclusion: Hence, results showed that fluconazole vaginal tablets can be formed by using these ingredients and formulation F5 was the most optimum formulation.
黏附型氟康唑阴道片的研制及评价
目的:氟康唑是一种三唑类抗真菌药物,用于治疗真菌感染,但由于给药频繁和不良副作用影响了患者的依从性。因此,需要一种能够跳过第一次代谢并坚持足够长的时间来有效治疗感染的递送系统,这就是本研究的目的。黏附给药系统粘附在粘膜上,提供持久的药物释放。方法:采用造粒法制备5种配方。然后压缩颗粒,制成每片250毫克的片剂。测定了不同的评价参数,如硬度、脆性、重量变化、含量均匀性、粘接强度、溶胀指数、溶解度和相容性分析。结果:硬度(7.2 ~ 8.9kg)、脆度(0.02 ~ 0.05%)、重量变异(0.1 ~ 0.4%)、含量均匀度(96.9 ~ 103%)均在药典范围内。释放动力学结果表明,F1、F2、F3为Fickian释放,F4为Fickian和非Fickian释放,F5为非Fickian释放。粘接强度在配方F5中最高(46g)。F3在12h时溶胀指数最高,为70.34%。差示扫描量热仪和傅里叶变换红外光谱分析表明,辅料之间没有相互作用。结论:由此可见,氟康唑阴道片可由这些成分组成,F5为最佳处方。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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