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曲昔派特聚氧化乙烯和泊洛沙姆控释胃滞留给药系统的设计与评价

Design and evaluation of polyox and pluronic controlled gastroretentive delivery of troxipide.

作者信息

Jagdale Swati C, Kamble Shraddha B, Kuchekar Bhanudas S, Chabukswar Aniruddha R

机构信息

Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, MIT Campus, Kothrud, Pune 411038, India.

出版信息

J Drug Deliv. 2014;2014:804616. doi: 10.1155/2014/804616. Epub 2014 Nov 19.

Abstract

Objective. Objective of the present work was to develop site-specific gastroretentive drug delivery of Troxipide using polymers Pluronic F127 and Polyox 205 WSR. Troxipide is a novel gastroprotective agent with antiulcer, anti-inflammatory, and mucus secreting properties with elimination half-life of 7.4 hrs. Troxipide inhibits H. pylori-derived urease. It is mainly absorbed from stomach. Methods. 3(2) factorial design was applied to study the effect of independent variable. Effects of concentration of polymer on dependant variables as swelling index, hardness, and % drug release were studied. Pluronic F127 and Polyox 205 WSR were used as rate controlled polymer. Sodium bicarbonate and citric acid were used as effervescent-generating agent. Results. From the factorial batches, it was observed that formulation F5 (19% Pluronic F127 and 80% Polyox 205 WSR) showed optimum controlled drug release (98.60% ± 1.82) for 10 hrs with ability to float >12 hrs. Optimized formulation characterized by FTIR and DSC studies confirmed no chemical interactions between drug and polymer. Gastroretention for 6 hrs for optimized formulations was confirmed by in vivo X-ray placebo study. Conclusion. Results demonstrated feasibility of Troxipide in the development of gastroretentive site-specific drug delivery.

摘要

目的。本研究的目的是使用泊洛沙姆F127和聚氧乙烯205 WSR聚合物开发曲昔派特的胃滞留型药物递送系统。曲昔派特是一种新型胃保护剂,具有抗溃疡、抗炎和分泌黏液的特性,消除半衰期为7.4小时。曲昔派特可抑制幽门螺杆菌衍生的脲酶。它主要从胃中吸收。方法。采用3(2)析因设计研究自变量的影响。研究了聚合物浓度对诸如溶胀指数、硬度和药物释放百分比等因变量的影响。泊洛沙姆F127和聚氧乙烯205 WSR用作控释聚合物。碳酸氢钠和柠檬酸用作泡腾剂。结果。从析因批次中观察到,制剂F5(19%泊洛沙姆F127和80%聚氧乙烯205 WSR)在10小时内显示出最佳的控释效果(98.60%±1.82),漂浮能力超过12小时。通过傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)研究表征的优化制剂证实药物与聚合物之间没有化学相互作用。通过体内X射线安慰剂研究证实了优化制剂的胃滞留时间为6小时。结论。结果证明了曲昔派特在开发胃滞留型部位特异性药物递送系统方面的可行性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d8e9/4253710/c8278fdb544a/JDD2014-804616.001.jpg

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