摘要
目的：研究重组葡激酶在大鼠体内的药物动力学。方法：采用氯胺Ｔ法标计１２５Ｉ重组葡激酶（放化纯度＞９８％），给大鼠静注三种不同剂量后进行药物动力学试验，数据采用 ３ｐ８７程序按二室模型计算药动学参数。结果：ｔ１／２α约为０．９１３～１，３３６ｍｉｎ，ｔ１／２β约为２２．５１～２３．８９ｍｉｎ。５ｍｉｎ后各组织有较高放射量，以肾、脾、肝为最高。到１２０ｍｉｎ各组织只有很少的放射量。尿、胆汁在３ｈ内可明显测到放射性，２４ｈ内从尿中排出给药量的４２．８％放射量，从粪中排出 ７ ５％，在３３ｈ内从胆汁中排出给药量的 ９．４％放射量。 ＳｐｅＰＡＧＥ电泳结果表明，尿和胆汁中原形葡激酶甚微，排出物主要是分解产物。结论：１２５Ｉ－ｒ－Ｓａｋ静注，在大鼠体内分布快，分布广，消除快。
OBJECTIVE: To study the pharmacokinetic char- acteristics of r-SAK. in rats. METHODS: Our study employed Chloramine-T to label recombined glucokinases by 125I, the radiochemical purity was more than 98%. After the rats were administrated intraveously by three different doses of the labeled glucokinases. All data were calculated by 3g87 program on computer according to the two-compartment medel to detemine the phamarcokinetic parameters. RESULTS: We found that its distributing and clearance from the rats were quick. The T1/2β was 0. 913-1. 336 min and T1/2β was 22. 51-23. 89 min. 5 min after the administrations, high radiant has been detected in tis- sues, especially in kidney, liver and spleen. 120 min after the administrations left there negligible radiant in rats. Finally, compared to the total das administrated, 42. 8% of the radi- ant glucokinases excreted into urea and 7. 5% into faeces in 24 h, and 9.4% into bile in 33h after the administrations. CON- CLUSION: The results of SDS-PAGE indicate that there are trace prototypes glucokineases excreted into urea and bile, most of such excreted were decomposed glucokinases.
出处
《华西药学杂志》
CAS
CSCD
2001年第3期175-177,180,共4页
West China Journal of Pharmaceutical Sciences
关键词
重组葡激酶
药物代谢动力学
组织分布
Recomdined glucokinase
Parameters of pharmacokinetics
Tissues distribution
