肠溶胶囊;_____PEG-SOD;肠溶胶囊;药动学

125I-PEG-SOD(PEG6000)肠溶胶囊在家兔体内的药动学

http://www.100md.com 《广东药学院学报》 2002年第4期

肠溶胶囊;,,PEG-SOD;肠溶胶囊;药动学,1材料和方法,2结果,3讨论,参考文献

     摘要目的：测定125I-PEG-SOD肠溶胶囊单次灌胃后不同时间家兔全血中的放射性计数，计算其药动学参数。方法：以本实验室制成的PEG-SOD进行125I标记并制成肠溶胶囊。取8只新西兰纯种大白兔分为四组，各组于灌胃后0.25、0.75、1.0、1.5、2.0、3.0、4.5、6.0、7.5、9.0、10.0、24.0 h自耳缘静脉分别取血样1 mL，分别测量全血的放射性计数，血样放射性-时间数据用3P97程序处理，用残数法结合非线性加权最小二乘法计算药动学参数。结果：125I-PEG-SOD肠溶胶囊在家兔体内过程符合二室开放型特征，Tmax(3.37±0.20) h、Cmax(70379.16±6375.68)cpm(cpm为放射性计数)、T1/2α(1.08±0.14) h、T1/2β(6.73±0.43) h，灌胃24 h后，PEG-SOD在家兔体内的分布次序为肾>肝>肠>胃>肺>脾>胆>心。结论：经聚乙二醇(PEG6000)修饰得到PEG-SOD并制成肠溶胶囊后半衰期大大延长，可作为一种新制剂进一步研究。

    关键词 PEG-SOD;肠溶胶囊;药动学

    The pharmacokinetics of 125I-PEG-SOD (PEG6000) entericcoated capsuls in rabbits

    Abstract Objective:To calculate the pharmacokinetic parameters by measuring the radiation in blood at different time after the 125I-PEG-SOD entericcoated capsuls were fed on different group of rabbits. Methods:125I-PEG-SOD was prepared by chloineT method. After the 125I-PEG-SOD entericcoated capsuls were fed on different group of rabbits, blood were taken at different time to measure the radiocounting and the pharmacokineties parameters were calculated by using 3p97 pharmacokinetic program,combining remnantnumber method with nonlinearity weighted leastsquaremethod. Results:Tmax(3.37±0.20)h,Cmax(70379.16±6375.68)cpm,T1/2α(1.08±0.14)h, T1/2β(6.73±0.43)h. The concentrationtime curves was fitted as twocompartment open model. Conclusions: After the modification of SOD with polyethylene glycol (PEG, molecular weight 6 000),the halflife time of 125I-PEG-SOD entericcoated capsuls was largerly extended. ......

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