pH对吲哚美辛理化性质和离体透皮参数的影响
x

请在关注微信后,向客服人员索取文件

篇名: pH对吲哚美辛理化性质和离体透皮参数的影响
TITLE:
摘要: 目的:研究不同pH对吲哚美辛理化性质和离体透皮参数的影响。方法:采用高效液相色谱法进行定量分析,测定pH分别为5.0、5.8、6.5、7.3、8.0下吲哚美辛的溶解度、表观油水分配系数(Kapp)和吲哚美辛凝胶的离体透皮参数[渗透速率(Js)和4、12、24 h累积渗透量(Q4 h、Q12 h、Q24 h)],通过复相关分析法与回归模型确定pH、溶解度、Kapp与离体透皮参数的相关性。结果:吲哚美辛凝胶离体透皮模型符合零级动力学模型,pH与溶解度、Kapp具有良好线性模型(r≥0.892 0),相关性良好(r≥0.968 0);pH、溶解度、Kapp与离体透皮参数之间基本呈指数模型,以pH 7.3为调节临界点的对应Kapp为3.34。结论:调节pH,可改善吲哚美辛的溶解度与Kapp;调节分子-离子存在形式,可提高吲哚美辛的Q和Js。
ABSTRACT: OBJECTIVE: To study effects of different pH values on physicochemical property and in vitro transdermal parameters of indomethacin. METHODS: HPLC method was used for quantitative analysis; solubility, apparent partition coefficient (Kapp) and in vitro transdermal parameters [permeation rate (Js) and 4, 12, 24 h accumulative premeation amount (Q4 h, Q12 h, Q24 h)] of Indomethacin gel were determined at pH 5.0, 5.8, 6.5, 7.3, 8.0. The multiple correlation analysis and regression model were used to determine the correlations of pH, solubility, Kapp and transdermal parameters. RESULTS: Indomethacin gel in vitro transdermal model fully complied with zero-order kinetic model; and pH was good linear relationship with solubility and Kapp (r≥0.892 0), showing good correlation (r≥0.968 0); the exponential model relationships were shown among pH, solubility, Kapp and in vitro transdermal parameters; using pH 7.3 as the critical point, corresponding Kapp was equal to 3.34. CONCLUSIONS: Adjusting pH can improve the solubility and Kapp of indomethacin; adjusting existing form of molecular ion can increase Q and Js of indomethacin.
期刊: 2016年27卷第34期
作者: 张永萍,徐剑,吴静澜,谢伟杰
AUTHORS: ZHANG Yongping,XU Jian,WU Jinglan,XIE Weijie
关键字: pH;吲哚美辛;理化性质;离体透皮参数;相关性
KEYWORDS: pH; Indomethacin; Physicochemical property; in vitro transdermal parameters; Correlation
总下载数: 1 次
本日下载数: 0次
本月下载数: 0次
文件大小: 619.60Kb

* 注:未经本站明确许可,任何网站不得非法盗链资源下载连接及抄袭本站原创内容资源!在此感谢您的支持与合作!