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DOAC-Stop对直接口服抗凝药的清除作用
Scavenging effect of DOAC-Stop on zifaxaban
in vitro andin vivo - 第三军医大学学报 2021年43卷第13期 页码：1293-1298
- 作者机构：
1.300222 天津，天津市胸科医院药剂科
2.300070 天津，天津医科大学研究生院
3.300193 天津，天津医药集团研究院有限公司
- 作者简介：
[孙双勇，E-mail: sunshuangyong@163.comSUN Shuangyong, E-mail: sunshuangyong@163.com
- 基金信息：天津市第二批特支计划青年拔尖人才基金(TJTZJH-QNBJRC-2-7);利益冲突声明 本研究与天津医药集团研究院有限公司不存在利益冲突
DOI：10.16016/j.1000-5404.202101080
中图分类号： R965;R969.2;R973.2收稿：2021-01-08，
修回：2021-03-24，
纸质出版：2021-07-15
- 稿件说明：
移动端阅览
张思培, 章彦文, 孙双勇. DOAC-Stop对直接口服抗凝药的清除作用[J]. 第三军医大学学报, 2021,43(13):1293-1298.
Sipei ZHANG, Yanwen ZHANG, Shuangyong SUN. Scavenging effect of DOAC-Stop on zifaxaban
in vitro andin vivo [J]. Journal of Third Military Medical University, 2021, 43(13): 1293-1298.张思培, 章彦文, 孙双勇. DOAC-Stop对直接口服抗凝药的清除作用[J]. 第三军医大学学报, 2021,43(13):1293-1298. DOI： 10.16016/j.1000-5404.202101080.
Sipei ZHANG, Yanwen ZHANG, Shuangyong SUN. Scavenging effect of DOAC-Stop on zifaxaban
in vitro andin vivo [J]. Journal of Third Military Medical University, 2021, 43(13): 1293-1298. DOI： 10.16016/j.1000-5404.202101080.
摘要
目的
2
观察DOAC-Stop对血浆内知非沙班的清除作用。
方法
2
离体实验中，犬血浆内加入0.1 mg/mL的知非沙班致凝血酶原时间(prothrombin time
PT)、活化部分凝血酶时间(activated partial thrombopastin time
APTT)延长，凝血因子Xa(FXa)活性降低，然后加入梯度浓度(1/512~1 minitabs)的DOAC-Stop，观察血浆PT、APTT、FXa活性以及知非沙班浓度变化情况；在体实验中，大鼠灌胃给予30 mg/kg的知非沙班，1.5 h后取血分离血浆，使用DOAC-Stop处理后，观察血浆PT、APTT、FXa活性及知非沙班浓度变化情况。
结果
2
在加入0.1 mg/mL知非沙班的血浆内加入梯度浓度的DOAC-Stop后，PT、APTT显著缩短(
P
<
0.001)，FXa活性升高(
P
<
0.001)，知非沙班浓度显著降低(
P
<
0.001)，且具有一定的剂量依赖性。灌胃给予30 mg/kg知非沙班大鼠的血浆使用DOAC-Stop处理后，PT、APTT显著降低(
P
<
0.001)，FXa活性恢复(
P
<
0.001)，血浆内无知非沙班检出，各项指标已接近对照组。
结论
2
DOAC-Stop对血浆内知非沙班具有良好的清除作用。
Abstract
Objective
2
To determine the scavenging effect of DOAC-Stop on zifaxaban in plasma.
Methods
2
In
in vitro
experiment
0.1 mg/mL zifaxaban was added into the plasma derived from Beagle dogs
then
DOAC-Stop with gradient concentration (1/512~1 minitabs) was added to observe the changes of prothrombin time (PT)
activated partial thrombopastin time (APTT)
FXa activity and zifaxaban concentration. In
in vivo
experiment
Wistar rats of both sexes were given 30 mg/kg zifaxaban
by gavage
and in 1.5 h later
their blood samples were harvested to separate plasma. The plasma was treated with DOAC-Stop
and PT
APTT
FXa activity and zifaxaban concentration in the plasma were measured.
Results
2
The results of
in vitro
experiments showed that when the gradient concentrations of DOAC-Stop were added to the plasma containing 0.1 mg/mL zifaxaban
PT and APTT were significantly shortened (
P
<
0.001)
FXa activity was increased (
P
<
0.001)
and concentration of zifaxaban was significantly decreased (
P
<
0.001)
in a dose-dependent manner. After the plasma from zifaxaban gavaged rats was treated with DOAC-Stop
PT and APTT were significantly shortened (
P
<
0.001)
FXa activity was restored (
P
<
0.001)
and no zifaxaban was detected in the plasma
which indicated that all indexes in the DOAC-Stop group were close to those of the blank control group.
Conclusion
2
DOAC-Stop has a good scavenging effect on zifaxaban in plasma.
关键词
Keywords
references
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