Chitosan as a pore former in coated beads for colon specific drug delivery of 5-ASA.
Chitosan as a pore former in coated beads for colon specific drug delivery of 5-ASA.
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DOI：
10.1016/j.ijpharm.2012.11.022
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发表时间：
2013-01-30
影响因子：
5.8
通讯作者：
Neau, Steven H.
中科院分区：
文献类型：
--
作者：
Omwancha, Wycliffe S.;Mallipeddi, Rama;Valle, Brenda L.;Neau, Steven H.
关键词：
已经开发并表征了用于小分子药物的结肠特异性递送的多颗粒产品。根据析因设计，用壳聚糖和Aquacoat® ECD混合物涂覆通过挤出-滚圆制备的含有5-氨基水杨酸的微晶纤维素芯珠。包衣珠的特征在于药物释放，形状和脆碎度。最佳制剂为肠溶包衣，并暴露于模拟胃、小肠和结肠条件的介质中。在模拟肠液中的释放研究表明，药物从包衣珠，这是球形和凹凸不平的释放速率依赖于壳聚糖在涂层和涂层厚度的水平。与仅暴露于模拟胃液和肠液的对照相比，在暴露于含有大鼠盲肠和结肠酶的介质的包衣珠表面上观察到的扩大的孔被认为引起了药物释放速率的显著增强。在模拟肠液和模拟结肠液中的释放机制分别涉及聚合物弛豫和溶解药物扩散。从促进药物在结肠环境中的释放和胃和肠道条件下的药物释放的抑制，可以得出结论，这种多颗粒系统展示了结肠特异性药物递送的潜力。
A multiparticulate product for colon-specific delivery of a small molecule drug has been developed and characterized. Microcrystalline cellulose core beads containing 5-aminosalicylic acid produced by extrusion-spheronization were coated with chitosan and Aquacoat® ECD mixtures according to a factorial design. Coated beads were characterized in terms of drug release, shape, and friability. The optimum formulation was enteric coated and exposed to media simulating conditions in the stomach, small intestine, and colon. Release studies in simulated intestinal fluid revealed that the drug release rate from the coated beads, which were spherical and rugged, depended on the level of chitosan in the coat and the coat thickness. Enlarged pores observed on the surface of the coated beads exposed to the medium containing rat cecal and colonic enzymes are believed to have caused a significant enhancement of the drug release rate compared to the control exposed only to simulated gastric and intestinal fluids. The release mechanisms involved polymer relaxation and dissolved drug diffusion for simulated intestinal fluid and simulated colonic fluid, respectively. From the facilitated drug release in a colonic environment and the inhibition of drug release under gastric and intestinal conditions, it can be concluded that this multiparticulate system demonstrates the potential for colon-specific drug delivery.
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影响因子：
3.3
作者：
HARDY, JG;WILSON, CG;WOOD, E
通讯作者：
WOOD, E
影响因子：
3.3
作者：
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通讯作者：
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影响因子：
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作者：
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通讯作者：
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影响因子：
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作者：
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通讯作者：
SAKR, A
DOI：
10.1016/s0939-6411(02)00121-2
发表时间：
2002-11-01
影响因子：
4.9
作者：
Leong, CW;Newton, JM;Ring, SG
通讯作者：
Ring, SG