The safety of chitosan as a pharmaceutical excipient
The safety of chitosan as a pharmaceutical excipient
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DOI：
10.1016/j.yrtph.2009.09.015
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发表时间：
2010-04-01
影响因子：
3.4
通讯作者：
Baldrick, Paul
中科院分区：
文献类型：
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作者：
Baldrick, Paul
对通过不同剂量途径和用于许多应用的多糖壳聚糖作为药物赋形剂的使用的兴趣不是新的，但它似乎仍然不存在于任何市售药物中，包括新药物制剂中的新型赋形剂，需要许多安全性考虑。肠胃外制剂先前的人类口服暴露是通过使用壳聚糖膳食补充剂和食品添加剂、医疗器械和化妆品应用而发生的。尽管母体壳聚糖的全身暴露可能有限（由于胃肠道消化）。任何被吸收的物质都可能经过酶降解成天然存在的葡糖胺和N-乙酰葡糖胺。它的共聚物，这是排泄或使用的氨基糖池。壳聚糖具有止血作用形式的局部生物学活性，以及其激活巨噬细胞和引起细胞因子刺激的能力（这引起了医疗器械和伤口愈合应用的兴趣），可能导致对其作为胃肠外赋形剂的安全性进行更仔细的评估（C）2009 Elsevier Inc.版权所有
Interest in use of the polysaccharide chitosan as a pharmaceutical excipient by different dose routes and for a number of applications is not new but it still does not appear to be present in any marketed drugs including a novel excipient in a new drug formulation requires a number of safety considerations Review of the published literature showed that chitosan has low oral toxicity and local tolerance potential supporting use in non-parenteral formulations Prior human oral exposure has occurred through use of chitosan dietary supplements and food additive, medical device and cosmetic applications. Although systemic exposure to parent chitosan may be limited (due to digestion in the gastrointestinal tract). any that is absorbed will likely undergo enzyme degradation to naturally occurring glucosamine, and N-acetylglucosamine. its copolymers, which are excreted or used in the amino sugar pool. Chitosan has local biological activity in the form of haemostatic action and, together with its ability to activate macrophages and cause cytokine stimulation (which has resulted in interest in medical device and wound healing applications), may result in a more careful assessment of its safety as a parenteral excipient (C) 2009 Elsevier Inc. All rights reserved