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机构地区:[1]浙江大学医学院附属第一医院药剂科,杭州310003
出 处:《同济大学学报(医学版)》2011年第1期35-39,共5页Journal of Tongji University(Medical Science)
摘 要:目的阐明不同含量和聚合度PEG修饰对SLN在胃肠道转运和体内消除的影响。方法溶剂扩散法合成荧光标记不同含量和聚合度PEG修饰SLN,建立血样中PEG-SLN检测方法学,对大鼠灌胃后对PEG-SLN体内浓度经时变化进行考察。结果口服后1~2 h,PEG含量和聚合度越高,体内浓度越低;至8 h后,PEG含量和聚合度越高,体内浓度越高。结论 PEG含量和聚合度提高减慢SLN在胃肠道内吸收,延长SLN体循环时间,在设计PEG-SLN制备处方时须综合考虑吸收、药物释放以及体内消除等多方面因素。Objective To clarify the influence of SLN modified by PEG with different contents and polydispersity on biotransport in gastrointestinal tract and elimination in vivo.Methods Different contents and polydispersity of PEG-modified fluorescent SLN were synthesized by solvent diffusion method,and the blood sample detection methodology was established.The concentration-time inspection changes of PEG-SLN in vivo in rats after oral administration were investigated.Results The higher the PEG content and polydispersity 1~2 hrs after oral administration,the lower the concentration in vivo.For 8 hrs,the higher the PEG content and polydispersity,the higher the concentration in vivo.Conclusion The increase of content and polydispersity of PEG slows down the SLN absorption in the gastrointestinal tract and extends the time of SLN in vivo.It is necessary to take into account absorption,release and elimination in vivo when PEG-SLN prescription was designed.
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