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

Abstract

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.

Keywords

• doac-stop
• zifaxaban
• plasma
• scavenging effect