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首页> 外文期刊>World Journal of Gastroenterology >Colon-specific drug delivery systems based on cyclodextrin prodrugs: in vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates.
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Colon-specific drug delivery systems based on cyclodextrin prodrugs: in vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates.

机译：基于环糊精前药的结肠特异性药物递送系统：体内评估5-氨基水杨酸的环糊精结合物。

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AIM: To investigate the release of cyclodextrin-5-aminosalicylic acid (CyD-5-ASA) in cecum and colon. METHODS: An anti-inflammatory drug 5-ASA was conjugated onto the hydroxyl groups of alpha-, beta- and gamma-cyclodextrins (CyDs) through an ester linkage, and the in vivo drug release behavior of these prodrugs in rat's gastrointestinal tract after the oral administration was investigated. RESULTS: The 5-ASA concentration in the rat's stomach and small intestine after the oral administration of CyD-5-ASA conjugate was much lower than that after the oral administration of 5-ASA alone. The lower concentration was attributable to the passage of the conjugate through the stomach and small intestine without significant degradation or absorption, followed by the degradation of the conjugate site-specific in the cecum and colon. The oral administration of CyD-5-ASA resulted in lower plasma and urine concentration of 5-ASA than that of 5-ASA alone. CONCLUSION: CyD-5-ASA conjugates may be used as prodrugs for colon-specific drug delivery system.
机译：目的：研究环糊精-5-氨基水杨酸（CyD-5-ASA）在盲肠和结肠中的释放。方法：通过酯键将抗炎药5-ASA偶联至α-，β-和γ-环糊精（CyDs）的羟基上，并且在麻醉后，这些前药在大鼠胃肠道中的体内药物释放行为口服给药进行了调查。结果：口服CyD-5-ASA结合物后，大鼠胃和小肠中5-ASA的浓度远低于单独口服5-ASA后的浓度。较低的浓度归因于缀合物通过胃和小肠而没有明显的降解或吸收，随后在盲肠和结肠中特异性降解缀合物。口服CyD-5-ASA可使5-ASA的血浆和尿液浓度低于单独的5-ASA。结论：CyD-5-ASA结合物可用作结肠特异性药物递送系统的前药。

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