使用混合等级的乌龙茶经皮给药甲氨蝶呤:物理化学,体外和体内评价

Ashok R. Chandak, P. Verma
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引用次数: 10

摘要

本研究旨在开发以乌拉吉为基础的基质系统,用于类风湿性关节炎免疫抑制剂甲氨蝶呤的经皮给药。药物释放动力学遵循零级而非一级或Higuchi型释放动力学。FT-IR, DSC和X-RD研究表明药物与聚合物无相互作用。采用双因素方差分析(two-way ANOVA)对体外溶出速率常数、溶出半衰期、药代动力学参数(Cmax、tmax、AUC(s)、t1/2、Kel、MRT)进行统计学评价。在测试产品之间观察到显著差异,但在测试产品内部没有观察到显著差异。统计上,贴片吸收的药物百分比与Cmax和AUC(s)之间存在良好的相关性。在给定时间内药物溶解的百分比与血清药物浓度有统计学相关性。本研究结果表明甲氨蝶呤聚合物基质膜具有透皮的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Transdermal Delivery of Methotrexate Using Mixed Grades of Eudragit: Physico-Chemical, In-Vitro, and In-Vivo Evaluations
The present study was aimed to develop Eudragit-based matrix system for transdermal delivery of methotrexate, an immunosuppressant drug for rheumatoid arthritis. Drug release followed zero order rather than first order or Higuchi type release kinetics. FT-IR, DSC and X-RD studies indicated no interaction between drug and polymer. The in-vitro dissolution rate constant, dissolution half life, and pharmacokinetic parameters (Cmax, tmax, AUC(s), t1/2, Kel, and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between test products but not within test products. Statistically, a good correlation was found between percent of drug absorbed from patches versus Cmax, and AUC(s). Percent of drug dissolved at a given time versus serum drug concentration was correlated statistically. The results of this study indicate that the polymeric matrix films of methotrexate hold potential for transdermal.
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