期刊论文

Preparation and in vitro Transdermal Permeation of Fluorofenidone Gels

中文

中国医药工业杂志

1001-8255

2020

51

02

220-225

10.16522/j.cnki.cjph.2020.02.012

湖南省卫生计生委2018年度科研计划课题项目（B20180636、C20180628）；

本校为其他机构

采用HPLC法测定了25 ℃、100 r/min条件下平衡48 h时氟非尼酮在水性溶剂和非水溶剂中的溶解度。结果表明,氟非尼酮在水及其他水性溶剂中微溶,溶解度约为2.5 mg/ml,溶剂的pH值对溶解度影响小;氟非尼酮易溶于乙醇,可溶于聚乙二醇400、1,2-丙二醇和异丙醇,微溶于甘油。摇瓶法测得氟非尼酮的油水分配系数(logP)值为1.182,略有亲脂性。以乳猪皮肤为模型,采用改良的Franz扩散池法评价不同载药量(0.5%和1% )凝胶及溶液的经皮渗透特性。结果表明,2种载药量的氟非尼酮凝胶的经皮渗透行为均符合零级模型,1%凝胶的24 h单位面积累积渗透量(Q_(24 h))和单位面积皮肤滞留量(Q_(skin))均比0.5%凝胶增加约1倍;同...

The equilibrium solubilities of fluorofenidone in various aqueous and non-aqueous solvents after shaking at 25 ℃ and 100 r/min for 48 h were determined by HPLC method. The results showed that fluorofenidone was slightly soluble in water and other aqueous solvents with the solubility about 2.5 mg/ml, and pH value of the aqueous solvents had little effect on its solubility. While in non-aqueous solvents, fluorofenidone was easily soluble in ethanol, soluble in polyethylene glycol(PEG) 400, 1,2-propylene glycol and isopropanol, and slightly solub...