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首页> 外文期刊>Journal of Pharmaceutics >Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery
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Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery

机译：设计，开发和优化的壳聚糖/ Eudragit RLPO混合共混聚合物包衣的基于口香糖的片剂可能用于结肠药物的递送

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The purpose of this study is to explore the possible applicability ofSterculia urensgum as a novel carrier for colonic delivery system of a sparingly soluble drug, azathioprine. The study involves designing a microflora triggered colon-targeted drug delivery system (MCDDS) which consists of a central polysaccharide core and is coated to different film thicknesses with blends of chitosan/Eudragit RLPO, and is overcoated with Eudragit L00 to provide acid and intestinal resistance. The microflora degradation property of gum was investigated in rat caecal medium. Drug release study in simulated colonic fluid revealed that swelling force of the gum could concurrently drive the drug out of the polysaccharide core due to the rupture of the chitosan/Eudargit coating in microflora-activated environment. Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon. Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics.In vivostudy in rabbits shows delayedTmax, prolonged absorption time, decreasedCmax, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.
机译：这项研究的目的是探索尿小球藻作为微溶性药物硫唑嘌呤结肠递送系统的新型载体的可能应用。该研究涉及设计一种由菌群触发的靶向结肠的药物递送系统（MCDDS），该系统由中央多糖核心组成，并以壳聚糖/ Eudragit RLPO的混合物包被至不同的膜厚，并以Eudragit L00包被以提供耐酸和肠道抵抗。在大鼠盲肠培养基中研究了牙龈的微生物降解特性。在模拟结肠液中的药物释放研究表明，由于在菌群激活的环境中壳聚糖/ Eudargit涂层的破裂，口香糖的膨胀力可同时将药物驱出多糖核心。发现混合膜涂层中的壳聚糖通过结肠中菌群的酶促作用而降解。释放动力学数据表明，优化的MCDDS很好地适合一阶模型，表观滞后时间为6小时，随后是Higuchi释放动力学。家兔体内研究显示Tmax延迟，吸收时间延长，Cmax降低和吸收率常数（Ka），表明与其他剂型相比药物的全身毒性降低。

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