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Colon Specific Delivery of Indomethacin: Effect of Incorporating pH Sensitive Polymers in Xanthan Gum Matrix Bases

机译:吲哚美辛的结肠特异性递送:在黄原胶基质中掺入pH敏感聚合物的影响

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摘要

In the present study, an attempt has been made to design controlled release colon-specific formulations of indomethacin by employing pH responsive polymers Eudragit (L100 or S100) in matrix bases comprised of xanthan gum. The prepared tablets were found to be of acceptable quality with low-weight variation and uniform drug content. In vitro release studies indicated rapid swelling and release of significant percentage of drug in the initial period from matrix tablets composed of xanthan gum alone. Addition of pH responsive polymers Eudragit (L100 or S100) to xanthan gum matrix resulted in negligible to very low drug release in the initial period in acidic to weakly acidic medium. Furthermore, with increase in pH of the dissolution medium due to dissolution of Eudragit L100/Eudragit S100 that resulted in the formation of a porous matrix, faster but controlled drug release pattern was observed. Thus, a sigmoidal release pattern was observed from the designed formulations suitable for colonic delivery. Drug release mechanism in all cases was found to be of super case II type, indicating erosion to be the primary cause of drug release. Since the drug release from almost all the matrix bases in the initial phase was negligibly low and followed with controlled release for about 14–16 h, it was concluded that a matrix design of this composition could have potential applications as a colon-specific drug delivery device with additional advantage of easy scale-up and avoidance of all-or-none phenomenon associated with coated colon-specific systems.
机译:在本研究中,已经尝试通过在包含黄原胶的基质中使用pH响应聚合物Eudragit(L100或S100)来设计消炎痛的控释结肠特异性制剂。发现制备的片剂具有可接受的质量,具有低重量变化和均匀的药物含量。体外释放研究表明,在初期,仅由黄原胶组成的基质片剂会迅速膨胀并释放出显着百分比的药物。向黄原胶基质中添加pH响应性聚合物Eudragit(L100或S100)导致在酸性至弱酸性介质中的药物释放非常低。此外,随着由于Eudragit L100 / Eudragit S100的溶解而导致溶解介质的pH升高(导致形成多孔基质),观察到了更快但受控的药物释放模式。因此,从适合结肠递送的设计制剂中观察到了S形释放模式。在所有情况下,药物释放机制均为超级病例II型,表明侵蚀是药物释放的主要原因。由于在初始阶段几乎所有基质的药物释放量都很低,随后控制释放约14-16小时,因此得出的结论是,这种组合物的基质设计可以作为结肠特异性药物的潜在应用该设备具有易于放大和避免与包被的结肠特定系统相关的全有或全无现象的其他优点。

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