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Design and Evaluation of Polyox and Pluronic Controlled Gastroretentive Delivery of Troxipide

DOI: 10.1155/2014/804616

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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. 32 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. 1. Introduction Oral controlled release dosage forms have been developed over the past three decades due to their considerable therapeutic advantages such as ease of administration, patient compliance, and flexibility in formulation. Gastroretentive dosage form can remain in the gastric region for several hours and hence significantly prolong the gastric residence time of drugs. Prolonged gastric retention improves bioavailability, reduces drug wastage, and improves solubility of drugs that are less soluble in a high pH environment. It is also suitable for local drug delivery to stomach and proximal small intestine. Several approaches have been attempted in the preparation of gastroretentive drug delivery system as floating, swellable and expandable, high density, bioadhesive, altered shape, gel forming solution or suspension system and sachet systems [1–3]. In case of certain drug candidate, greater therapeutic value is achieved by increasing the gastric retention time. Some examples include drugs absorbed from the proximal part of the gastrointestinal tract, for example, diltiazem; drugs that get degraded in intestinal alkaline pH, for example, bromocriptine; drugs that are absorbed primarily in the stomach, for example, albuterol; and drugs that degrade in the colon,


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