外用抗真菌药物水凝胶的制备及评价

T. Kumar, M. C. Eswaraiah
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引用次数: 4

摘要

盐酸特比萘芬是一种抗真菌药物,用于治疗真菌感染。不建议口服盐酸特比萘芬,因为它有许多潜在的副作用,并经历肝脏第一次代谢。本研究旨在研制盐酸特比萘芬外用水凝胶治疗皮肤真菌感染。用三种不同浓度的胶凝剂HPMC、CMC钠和聚丙烯酸甲酯配制凝胶。对制备的水凝胶配方进行物理化学参数评价,如物理外观、pH值、皮肤刺激、药物释放、药物含量和流变性参数,如伸展性和挤压性。以念珠菌为模型菌,对制备的凝胶进行抑菌活性评价。采用含玻璃纸膜的Franz扩散池,以pH为5.8的磷酸盐缓冲液为受体培养基,评价了凝胶的体外释药效果。采用DSC和FT-IR分析进行药物赋形剂配伍性研究。所有凝胶制剂均显示出可接受的物理化学和流变性能,结果均在规定范围内。药物释放随聚合物浓度的增加而降低。在所有凝胶制剂中,Polaxomer的释药效果最好,其次是HPMC和CMC钠。配方F4抗真菌活性最高。药物-赋形剂相容性研究表明,药物与所选赋形剂之间没有相互作用。
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Formulation and evaluation of topical hydrogel containing antifungal drug
Terbinafine hydrochloride is an antifungal drug used in the treatment of fungal infections. The oral use of Terbinafine hydrochloride is not recommended as it has many potential side effects and undergoes hepatic first pass metabolism. This study was conducted to formulate and evaluate Terbinafine hydrochloride topical hydrogel for treatment of fungal infection of skin. The gel was formulated by using different gelling agents like HPMC, Sodium CMC and Polaxomer in three different concentrations. The prepared hydrogel formulations were evaluated for physico chemical parameters like physical appearance, pH, skin irritation, drug release, drug content and rheological parameters like spredability and extrudability. Antifungal activity of the prepared gels was evaluated using Candida as model fungus. The in vitro drug release from gels was evaluated using Franz diffusion cell containing cellophane membrane with phosphate buffer pH 5.8 as the receptor medium. Drug-excipients compatibility studies were performed by DSC and FT-IR analysis. All gel formulations showed acceptable physico chemical and rheological properties and results were found to be within the limits. The drug release was found to decrease with increase in polymer concentration. Among all the gel formulations Polaxomer showed superior drug release than followed by HPMC and sodium CMC. Formulation F4 shows the highest antifungal activity. Drug-excipients compatibility studies showed that there no interaction between the drug ad selected excipients.
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