摘要
目的旨在观察重组葡激酶（ｒＳａＫ）对兔肺栓塞的溶栓作用。用体外制备１２５Ｉ人纤维蛋白血块，颈静脉注入。０５ｈ内静滴２和０５万ＡＵ·ｋｇ－１ｒＳａＫ，与ＮＳ和２万Ｕ·ｋｇ－１链激酶（ＳＫ）比较。另设２５ｈ滴注组，速度与低剂量同而总剂量与高剂量同。结果表明，各组肺动脉内残留血栓分别为６２％±１１％，７８％±７％，９２％±７％，６０％±１３％和６４％±１６％，给药组与对照比较有显著差异。体外实验ｒＳａＫ与血凝块作用０５ｈ和２５ｈ的溶解率相近。ｒＳａＫ和ＳＫ的最大溶解速率分别为３４和１０ｋＢｑ·ｍｉｎ－１，Ｋｍ值均为１７ｋＢｑ·ｍｌ－１。
Thrombolysis effect of recombinant staphylokinase (rSaK) developed in China was evaluated in rabbits with experimental pulmonary embolus model. 125 I labeled human fibrin blood clot was prepared in vitro and was injected through jugular vein resulting in a pulmonary embolus. Twenty thousands AU·kg -1 (rSaK H) or 5000 AU·kg -1 (rSaK L) of rSaK was infused in 0 5 h at constant rate by a peristaltic 20000 U·kg -1 . Another 20000 AU·kg -1 of rSaK was infused within 2 5 h(rSaK 2 5 h). The residual labeled blood clot in lungs were found to be 62%±11%(rSaK H), 78%±7%(rSaK L), 92%±7%(NS), 60%±13%(SK), and 64%±16%(rSaK 2 5 h). 125 I labeled degradation products in blood and urine were also statistically higher in thrombolytic agents treated group than those in NS controls. The results suggest that the thrombolytic effect of rSaK was determined by total dose and not determined by infusion time. Two of seven rabbits in the rSaK 2 5 h infusion group, the bleeding time was prolonged to more than 10 minutes while no prolongation was seen in rSaK high dose group. The clot lysis curves were very similar in 0 5 h or 2 5 h treatment of rSAK in vitro . Michaelis Menten kinetics studies in vitro revealed that the Kms of rSaK and SK were almost the same, while a higher maximal velocity(34 kBq·min -1 ) was observed in rSaK than that in SK (10 kBq·min -1 ).
出处
《药学学报》
CAS
CSCD
北大核心
1998年第11期801-806,共6页
Acta Pharmaceutica Sinica
关键词
葡激酶
链激酶
溶栓
肺栓塞
Staphylokinase
Streptokinase
Thrombolysis
Pulmonary embolus
