Effects of Tongxinluo capsules on pharmacokinetics of rivaroxaban in rats
- VernacularTitle:通心络胶囊对利伐沙班在大鼠体内药代动力学的影响
- Author:
Guosheng FU
1
;
Jie SHEN
1
;
Jiekai HUA
2
;
Yupeng SHAO
3
;
Wenna MA
4
;
Wei LIU
2
;
Jianwei ZHANG
1
;
Xinnan CHANG
1
Author Information
1. Dept. of Pharmacy，Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine/Third Grade Laboratory of Traditional Chinese Medicine Preparations，National Administration of Traditional Chinese Medicine，Shanghai 201203，China
2. Dept. of Pharmacy，Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine/Third Grade Laboratory of Traditional Chinese Medicine Preparations，National Administration of Traditional Chinese Medicine，Shanghai 201203，China;School of Pharmacy，Hangzhou Normal University，Hangzhou 311121，China
3. College of Pharmacy，Shanghai University of Medicine and Health Sciences，Shanghai 200237，China
4. Hebei Chemical & Pharmaceutical Vocational Technology College，Shijiazhuang 050026，China
- Publication Type:Journal Article
- Keywords:
rivaroxaban;
Tongxinluo capsules;
pharmacokinetics;
drug interaction
- From:
China Pharmacy
2025;36(23):2930-2934
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To investigate the impact of Tongxinluo capsules on the pharmacokinetics of rivaroxaban in rats. METHODS Rats were randomly divided into rivaroxaban alone group （2.70 mg/kg）， low-dose Tongxinluo capsules combined with rivaroxaban group （Tongxinluo capsules 0.28 g/kg+rivaroxaban 2.70 mg/kg）， and high-dose Tongxinluo capsules combined with rivaroxaban group （Tongxinluo capsules 0.84 g/kg+rivaroxaban 2.70 mg/kg）， with five rats in each group. Following seven consecutive days of gavage with normal saline or the corresponding doses of Tongxinluo capsules， the rats were subjected to a final gavage administration of rivaroxaban. Blood samples were collected at 0 h prior to the final administration and at 0.16， 0.33， 0.50， 0.75， 1， 1.5， 2， 4， 8， 12 and 24 h post-final administration. The plasma concentration of rivaroxaban in rats was determined by high-performance liquid chromatography-tandem mass spectrometry. The pharmacokinetic parameters [peak concentration （cmax）， half-life （t1/2）， area under the drug concentration time curve （AUC）， mean residence time （MRT）， clearance （CL）， apparent volume of distribution （Vd） and peak time （tmax）] of each group were calculated using a non-compartmental model of MonolixSuite 2023R1 pharmacokinetic software. RESULTS Compared with rivaroxaban alone group， AUC₀₋ₜ and AUC0-∞ of rivaroxaban in rats were increased significantly in high-dose Tongxinluo capsules+rivaroxaban group （P＜0.05）， while CL was decreased significantly （P＜0.05）； t1/2 and MRT were shortened， tmax was extended， cmax was increased， while Vd was decreased， but there was no statistical significance （P＞0.05）. CONCLUSIONS Rivaroxaban combined with Tongxinluo capsules significantly increases the plasma exposure of rivaroxaban in rats. Potential drug-drug interactions should be considered in clinical practice based on the co-administration conditions.
