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环吡酮胺凝胶的建模与生物药剂学评价

MODELLING AND BIOPHARMACEUTICAL EVALUATION OF CICLOPIROX OLAMINE GELS.

作者信息

Mazurkeviciute Agne, Ramanauskiene Kristina, Askiene Marija Iv, Grigonis Aidas, Briedis Vitalis

出版信息

Acta Pol Pharm. 2017 Mar;74(2):543-549.

Abstract

The ciclopirox olamine (CPO) has a broad antimicrobial profile including dermatophytes, yeasts and is used in various pharmaceutical forms. The aim of this study is to evaluate the quality of the CPO gels according to biopharmaceutial tests in vitro and antifungal activity assay. Hydroxypropyl cellulose, chitosan and poloxamer 407 were selected as agents gelificants. The effects of gelling agent properties and concentration on the consistency and flow characteristics have been studied by rheometer. CPO release rates from gel were measured with Franz type diffusion cells. The antifungal activity of gels was tested using agar well diffusion technique. The results of the experimental study have shown that the rheological properties of the medications depend on the selected gelling agent and the amount of it. The higher amounts of CPO were released from the poloxamer 407 gels. Though all tested CPO gels showed great inhibition of Microsporn canis.

摘要

环吡酮胺(CPO)具有广泛的抗菌谱,包括皮肤癣菌、酵母菌,并且有多种药物剂型。本研究的目的是根据体外生物药剂学试验和抗真菌活性测定来评估CPO凝胶的质量。选择羟丙基纤维素、壳聚糖和泊洛沙姆407作为凝胶剂。通过流变仪研究了凝胶剂性质和浓度对稠度和流动特性的影响。使用Franz型扩散池测量凝胶中CPO的释放速率。采用琼脂孔扩散技术测试凝胶的抗真菌活性。实验研究结果表明,药物的流变学性质取决于所选凝胶剂及其用量。泊洛沙姆407凝胶释放出的CPO量更高。尽管所有测试的CPO凝胶对犬小孢子菌均表现出很强的抑制作用。

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