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局部用抗真菌双凝胶:制剂、表征及评价

Topical antifungal bigels: Formulation, characterization and evaluation.

作者信息

Mazurkeviciute Agne, Ramanauskiene Kristina, Ivaskiene Marija, Grigonis Aidas, Briedis Vitalis

机构信息

Department of Clinical Pharmacy Faculty of Pharmacy, Lithuanian University of Health Sciences, 50161 Kaunas, Lithuania.

Department of Non-infectious Diseases, Faculty of Veterinary Medicine, Veterinary Academy Lithuanian University of Health Science, 47181 Kaunas, Lithuania.

出版信息

Acta Pharm. 2018 Jun 1;68(2):223-233. doi: 10.2478/acph-2018-0014.

Abstract

Bigels with antifungal substances, ciclopirox olamine and terbinafine hydrochloride, were made of hydrogel (poloxamer 407 gel) and oleogel (polyethylene and liquid paraffin mixture). Prepared bigels were found physically stable at room temperature for six months and at least four months at 40 °C. Released amount of drug decreased when oleogel concentration in the formulation increased. Release test results depended on the insertion place of active substances. The amount of released substance was highest when ciclopirox olamine was incorporated in both phases in an equal quantity, and terbinafine hydrochloride in oleogel or in hydrogel. All formulations showed great inhibition of Microsporum canis. Thus, bigels with ciclopirox olamine and terbinafine hydrochloride are a promising dosage form for topical use.

摘要

含有抗真菌物质环吡酮胺和盐酸特比萘芬的双凝胶,由水凝胶(泊洛沙姆407凝胶)和油凝胶(聚乙烯与液体石蜡混合物)制成。所制备的双凝胶在室温下物理稳定六个月,在40℃下至少稳定四个月。制剂中油凝胶浓度增加时,药物释放量减少。释放试验结果取决于活性物质的加入位置。当环吡酮胺等量加入两相且盐酸特比萘芬加入油凝胶或水凝胶中时,释放物质的量最高。所有制剂对犬小孢子菌均有很强的抑制作用。因此,含环吡酮胺和盐酸特比萘芬的双凝胶是一种很有前景的局部用剂型。

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