Stiekema J C, Wijnand H P, ten Cate H, ten Cate J W, Harenberg J, Egberts J F, van Dinther T G
Organon International B.V., Scientific Development Group, Oss, The Netherlands.
Thromb Res. 1991 Jul 1;63(1):157-67. doi: 10.1016/0049-3848(91)90278-5.
In a cross-over study increasing doses of protamine hydrochloride (20-100 mg) or placebo were administered to six groups of four healthy male volunteers each, following a single intravenous dose of 3200 anti-Xa units of Org 10172. No neutralising effects were observed on the Org 10172 induced changes in the bleeding time, prothrombin time and thrombin time. A small and statistically not significant temporary decrease in anti-Xa activity was observed after doses of 80 and 100 mg protamine chloride. The anti-thrombin activity was dose-dependently and partly irreversibly neutralised by protamine chloride to a maximum of approximately 60%. This neutralisation correlated with the observed shorter prolongation of the thrombin time. The thrombin-generation inhibition activity was for approximately 35% neutralised by protamine chloride doses of 60-100 mg.
在一项交叉研究中，对六组每组四名健康男性志愿者先静脉注射单次剂量3200抗Xa单位的Org 10172，随后分别给予递增剂量的盐酸鱼精蛋白（20 - 100毫克）或安慰剂。未观察到对Org 10172诱导的出血时间、凝血酶原时间和凝血酶时间变化有中和作用。在给予80毫克和100毫克氯化鱼精蛋白后，观察到抗Xa活性有轻微且无统计学意义的暂时下降。抗凝血酶活性被氯化鱼精蛋白以剂量依赖性方式部分不可逆地中和，最高可达约60%。这种中和作用与观察到的凝血酶时间延长缩短相关。60 - 100毫克氯化鱼精蛋白剂量可使凝血酶生成抑制活性约35%被中和。
