Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo

Objective To determine the scavenging effect of DOAC-Stop on zifaxaban in plasma. Methods 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 tim...

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Main Authors: ZHANG Sipei, ZHANG Yanwen, SUN Shuangyong
Format: Article
Language:zho
Published: Editorial Office of Journal of Third Military Medical University 2021-07-01
Series:Di-san junyi daxue xuebao
Subjects:
Online Access:http://aammt.tmmu.edu.cn/Upload/rhtml/202101080.htm
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spelling doaj-31fc157b62f54595bfddb3369b89322c2021-07-16T01:25:14ZzhoEditorial Office of Journal of Third Military Medical UniversityDi-san junyi daxue xuebao1000-54042021-07-0143131293129810.16016/j.1000-5404.202101080Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivoZHANG Sipei0 ZHANG Yanwen1ZHANG Yanwen2SUN Shuangyong3 Department of Pharmacy, Tianjin Chest Hospital, Tianjin, 300222Graduate School of Tianjin Medical University, Tianjin, 300070Tianjin Pharmaceutical Group Research Institute Co., Ltd, Tianjin, 300193, ChinaTianjin Pharmaceutical Group Research Institute Co., Ltd, Tianjin, 300193, ChinaObjective To determine the scavenging effect of DOAC-Stop on zifaxaban in plasma. Methods 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 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 DOAC-Stop has a good scavenging effect on zifaxaban in plasma.http://aammt.tmmu.edu.cn/Upload/rhtml/202101080.htmdoac-stopzifaxabanplasmascavenging effect
collection DOAJ
language zho
format Article
sources DOAJ
author ZHANG Sipei
ZHANG Yanwen
ZHANG Yanwen
SUN Shuangyong
spellingShingle ZHANG Sipei
ZHANG Yanwen
ZHANG Yanwen
SUN Shuangyong
Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
Di-san junyi daxue xuebao
doac-stop
zifaxaban
plasma
scavenging effect
author_facet ZHANG Sipei
ZHANG Yanwen
ZHANG Yanwen
SUN Shuangyong
author_sort ZHANG Sipei
title Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
title_short Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
title_full Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
title_fullStr Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
title_full_unstemmed Scavenging effect of DOAC-Stop on zifaxaban in vitro and in vivo
title_sort scavenging effect of doac-stop on zifaxaban in vitro and in vivo
publisher Editorial Office of Journal of Third Military Medical University
series Di-san junyi daxue xuebao
issn 1000-5404
publishDate 2021-07-01
description Objective To determine the scavenging effect of DOAC-Stop on zifaxaban in plasma. Methods 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 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 DOAC-Stop has a good scavenging effect on zifaxaban in plasma.
topic doac-stop
zifaxaban
plasma
scavenging effect
url http://aammt.tmmu.edu.cn/Upload/rhtml/202101080.htm
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AT zhangyanwen scavengingeffectofdoacstoponzifaxabaninvitroandinvivo
AT sunshuangyong scavengingeffectofdoacstoponzifaxabaninvitroandinvivo
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