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通心络胶囊对利伐沙班在大鼠体内药代动力学的影响
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| 篇名： | 通心络胶囊对利伐沙班在大鼠体内药代动力学的影响 |
| TITLE： | Effects of Tongxinluo capsules on pharmacokinetics of rivaroxaban in rats |
| 摘要： | 目的 研究通心络胶囊对利伐沙班在大鼠体内药代动力学的影响。方法将大鼠随机分为利伐沙班单用组（2.70mg/kg）、低剂量通心络胶囊+利伐沙班组（通心络胶囊0.28g/kg+利伐沙班2.70mg/kg）、高剂量通心络胶囊+利伐沙班组（通心络胶囊0.84g/kg+利伐沙班2.70mg/kg），每组5只。各组大鼠连续灌胃生理盐水或相应剂量通心络胶囊7d后，再灌胃相应剂量利伐沙班。于末次给药（利伐沙班）前（即0h）和给药后0.16、0.33、0.50、0.75、1、1.5、2、4、8、12、24h采集血样，采用高效液相色谱-串联质谱法检测大鼠血浆中利伐沙班的质量浓度，并采用MonolixSuite2023R1药代动力学软件的非房室模型计算主要的药代动力学参数[包括峰浓度（cmax）、半衰期（t1/2）、药时曲线下面积（AUC）、平均滞留时间（MRT）、清除率（CL）、表观分布容积（Vd）、达峰时间（tmax）]。结果与利伐沙班单用组比较，高剂量通心络胶囊+利伐沙班组大鼠血浆中利伐沙班的AUC0-t、AUC0-∞均显著升高（P＜0.05），CL均显著降低（P＜0.05）；t1/2和MRT缩短，tmax延长，cmax升高，Vd减小，但其差异均无统计学意义（P＞0.05）。结论利伐沙班与通心络胶囊联用后，可增加利伐沙班在大鼠体内的血浆暴露量；两者临床联用时应考虑潜在的药物相互作用。 |
| 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. |
| 期刊： | 2025年第36卷第23期 |
| 作者： | 付国胜；沈杰；华杰凯；邵宇鹏；马文娜；刘伟；张建伟；常昕楠 |
| AUTHORS： | FU Guosheng，SHEN Jie，HUA Jiekai，SHAO Yupeng，MA Wenna，LIU Wei，ZHANG Jianwei，CHANG Xinnan |
| 关键字： | 利伐沙班；通心络胶囊；药代动力学；药物相互作用 |
| KEYWORDS： | rivaroxaban； Tongxinluo capsules； pharmacokinetics； drug interaction |
| 阅读数： | 1 次 |
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