对乙酰氨基酚(AAP)为临床最为常用的退热药物。如果使用不当或错服、误服过量,则会引起严重肝中毒。

为此,本项目设计了温度触发释药式智能系统。项目思路为:以AAP与膨胀剂为核,以嵌接释药阀门的不溶性包衣为壳,制备壳核结构温控微丸。当体温正常时,释药阀门关闭,水分不能进入;当体温超过38.5℃时,释药阀门打开,水分进入丸核,接触膨胀剂,丸核迅速膨胀... 为此,本项目设计了温度触发释药式智能系统。项目思路为:以AAP与膨胀剂为核,以嵌接释药阀门的不溶性包衣为壳,制备壳核结构温控微丸。当体温正常时,释药阀门关闭,水分不能进入;当体温超过38.5℃时,释药阀门打开,水分进入丸核,接触膨胀剂,丸核迅速膨胀,撑破包衣,释放AAP。从而实现AAP根据体温高低“按需”释放,避免AAP超剂量使用导致的肝中毒。本项目关键在于合成释药阀门,其主要原理是利用温敏凝胶的“开关效应”。但由于温敏材料的天然缺陷,包括:安全性差、温度敏感性差和温敏专属性差。因此限制其广泛应用。本项目将重点解决上述3个难题,为温敏材料的实际应用提供实验和理论依据。同时将利用体外释放度、单向肠灌流模型、家兔发热模型等体内外一系列实验证明该系统的有效性和可靠性。对乙酰氨基酚:Acetaminophen退热:defervescence肝中毒:HEPATIC INJURY温度触发:temperature-triggered释药式智能系统:intelligent drug release system膨胀剂:expansive agent释药阀门:Release valve温敏凝胶:temperature-sensitive gel体外释放度:in-vitro release单向肠灌流模型:in situ single pass perfusion家兔发热模型:rabbit fever model体内外:in vivo and in vitro麻烦能不能帮忙翻译下下,不胜感激 展开
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For this,we design the temperature-triggered intelligent drug release system to prepare core-shell micropill ,In which APP and expansive agent are the core and the insoluble coat rabbeted with release valve is the shell.When the temperature is in normal,the release valve closes and the water can not get in;when the temperature is above 38.5℃,the release valve is open ,then the water get into the core and get in touch with the expansive agent,resulting in expansion of the core and bursting the coat and then APP releases.From which,AAP can release depending on temperature ,in other words "on demand",avoiding hepatotoxicity resulting from overdose of AAP.Synthesis of the release valve is the key procedure of the programe,the primary mechanism of which is to make use of the "open-close effect" of the temperature-sensitive gel .但由于温敏材料的天然缺陷,包括:安全性差、温度敏感性差和温敏专属性差。因此限制其广泛应用。本项目将重点解决上述3个难题,为温敏材料的实际应用提供实验和理论依据。同时将利用体外释放度、单向肠灌流模型、家兔发热模型等体内外一系列实验证明该系统的有效性和可靠性。Hower,temperature-sensitive gel has so much deficiency in nature including the poor safety ,bad temperature-sensitivity and error specificity of the temperature-sensitivity,making it can not be used extensively.The aim of the programe is to resulve the three questions and to provide experimental and theoretical basis for its practical use . At the same time,we utilize a series of experiments to identify the effectiveness and reliability of the system including in-vitro release , in situ single pass perfusion and the model of rabbit fever .

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