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

Journal of drug delivery Pub Date : 2014-01-01 Epub Date: 2014-11-19 DOI:10.1155/2014/804616
Swati C Jagdale, Shraddha B Kamble, Bhanudas S Kuchekar, Aniruddha R Chabukswar
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引用次数: 8

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.

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多氧和pluronic控制胃保留给药的设计和评价。
目标。本研究的目的是利用Pluronic F127和Polyox 205 WSR聚合物开发特洛昔肽的胃保留药物递送位点。Troxipide是一种新型的胃保护剂,具有抗溃疡、抗炎和粘液分泌的特性,消除半衰期为7.4小时。Troxipide抑制幽门螺杆菌衍生的脲酶。它主要由胃吸收。方法:采用3(2)因子设计研究自变量的影响。考察了聚合物浓度对溶胀指数、硬度、药物释放率等因变量的影响。采用Pluronic F127和Polyox 205 WSR作为速率控制聚合物。以碳酸氢钠和柠檬酸为起泡剂。结果。从析因批次中观察到,配方F5 (19% Pluronic F127和80% Polyox 205 WSR)的控释效果最佳(98.60%±1.82),控释时间为10小时,漂浮能力>12小时。优化后的配方经FTIR和DSC表征,证实药物与聚合物无化学相互作用。经体内x线安慰剂研究证实,优化配方可维持胃潴留6小时。结论。结果证明了托昔必特在胃保留部位特异性药物递送方面的可行性。
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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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