开发和评估酮康唑药盒的抗真菌功效

Srivastava Sk
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引用次数: 0

摘要

药体是一种中性胶体、脂质囊状给药系统,同时带有负电荷和正电荷,通过提高药物在水相和非水相中的溶解度来提高药物的生物利用度,同时降低药物的胃肠道毒性。酮康唑是一种咪唑类衍生物,可用于治疗局部或全身真菌感染,对皮癣菌、酵母菌和其他致病真菌具有静态活性。酮康唑是生物制药分类系统(BCS)第二类药物,其溶解和吸收与 pH 值有关。本研究采用传统的溶剂蒸发法,以不同比例的酮康唑-PC 复合物(1:1、1:1.5 和 1:2)制备了酮康唑的药膜。利用相衬显微镜(PCM)和扫描电子显微镜(SEM)对囊泡的形状和形态进行了研究,并对体外渗透研究和抗真菌活性进行了适当的检测。发现制剂(1:1)(1:1.5)和(1:2)中的药物含量分别为 92.5%、94.3% 和 89.7%。傅立叶变换红外光谱(FT-IR)显示药物-药球复合物形成正常。粒度分布规则,呈球形。体外渗透研究显示,KTP1、KTP2 和 KTP3 配方的药物释放率分别为 78.03%、89.05% 和 55.27%。与酮康唑(纯药)相比,酮康唑药体的抗真菌活性有所提高。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Antifungal Efficacy of Ketoconazole Pharmacosome
Pharmacosomes are neutral colloidal, lipid vesicular drug delivery system having both negative & positive charge that enhance the bioavailability of drugs by enhacing their solubility both in aqueous as well as non-aqueous phase, additionally reduce gastrointestinal toxicity of drug. Ketoconazole is an imidazole derivative agent which is used both in the treatment of topical or systematic fungal infections with fungi static activity against dermatophytes, yeasts and other pathogenic fungi. Ketoconazole is Biopharmaceutical classification system (BCS) class II drugs that display pH dependent dissolution and absorption. In this present research work Pharmacosome of Ketoconazole was prepared in different ratios of Ketoconazole-PC complex (1:1, 1:1.5 and1:2) using conventional solvent evaporation method. FT-IR spectra showed no significant untoward interaction, Vesicles shape and morphology was carried out with Phase contrast microscopy (PCM) and Scanning electron microscopy (SEM), In-vitro permeation study and anti-fungal activity were duly examined. Drug content in the formulations (1:1) (1:1.5) and (1:2) were found 92.5%, 94.3% and 89.7% respectively. FT-IR conformed proper formation of drug- Pharmaosome complex. Particle size distribution were found to be regular and of spherical shape. In-vitro permeation study showed 78.03%, 89.05% and 55.27% drug release as per respectively formulations (KTP1, KTP2 and KTP3). Pharmacosomes of ketoconazole show improvement in antifungal activity than ketoconazole (Pure).
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