摘要
目的 :测定 125I -PEG -SOD和 125I -SOD肠溶胶囊分别单次灌胃后不同时间家兔全血中的放射性计数 ,分别计算其药动学参数。方法 :以SOD和PEG -SOD(PEG6000)进行 125I标记并制成肠溶胶囊 ,分别将平均放射性为566082cpm/30s的 125I -SOD肠溶胶囊和588942cpm/30s的125I -PEG -SOD肠溶胶囊灌入家兔胃中 ,于给药后15、45、60、90、120、180、240、270、360、450、540、600min和24h自家兔耳缘静脉分别取血样1ml ,分别测量全血中的放射性计数 ,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 -SOD和 125I -PEG -SOD肠溶胶囊的全血放射性计数 -时间曲线呈二项指数函数关系 ,符合开放型二房室动力学模型 ;125I -PEG -SOD和 125I -SOD肠溶胶囊的Tmax 分别为 (3.37±0.20)h、(1 10±0 07)h ,Cmax 分别为 (70379.16±6375.68)cpm、(91131 66±8201 85)cpm ,T1/2α 分别为 (1.08±0.14)h、(1 06±0 16)h ,T1/2β 分别为 (6.73±0.43)h、(2 62±0 39)h ;灌胃24h后 ,125I -SOD和125I -PEG -SOD肠溶胶囊在家兔体内的分布次序均为肾>肝>肠>胃>肺>脾>胆>心。结论 :PEG -SOD肠溶胶囊半衰期大大延长 ,可作为一种新型制剂进一步研究。
OBJECTIVE:To calculate the pharmacokinetic parameters by measuring the radioactivities in blood at different time periods after 125 I-PEG-SOD or 125 I-SOD enteric-coated capsuls were fed to different group of rabbits.METHODS:The enteric-coated capsules were prepared by labelling SOD and PEG-SOD(PEG6000)with 125 I. 125 I-SOD(566082cpm/30s)and 125 I-PEG-SOD(588942cpm/30s)enteric-coated capsules were intragestrically given to rabbits.15,45,60,90,120,180,240,270,360,450,540,600min and24h after administration,1ml venous blood was taken to detect the radiocountˉing.Radioactivity-time curves were processed with3p97program and calculated by using remnant-number method combinˉing non-linearity weighted least-square-method.RESULTS:The radioactivity-time curves conformed to two-compartm_ ent open model.The pharmacokinetic parameters were as follows: 125 I-PEG-SOD capsule:T max ,(3.37±0.20)h;C max ,(70379.16±6375.68)cpm;T 1/2 α,(1.08±0.14)h;T 1/2 β,(6.73±0.43)h; 125 I-SOD capsule:T max ,(1.10±0.07)h;C max ,(91131.66±8201.85)cpm;T 1/2 α,(1.06±0.16)h;T 1/2 β,(2.62±0.39)h.24h after administration,the distribution of 125 I-SOD and 125 I-PEG-SOD in organs was in sequence of kidney>liver>intestine>stomach>lung>spleen>gall bladder>heart.CONCLUSION:The half-life of PEG-SOD enteric coated capsules is much longer than that of SOD enteric coated capsule and is worth further studying as a new type preparation
出处
《中国药房》
CAS
CSCD
2003年第10期587-589,共3页
China Pharmacy
基金
国家自然科学基金资助项目 (29676017)
