Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China.
Biomed Res Int. 2019 Mar 10;2019:1854323. doi: 10.1155/2019/1854323. eCollection 2019.
To evaluate the effect of Tanreqing injection on the pharmacokinetics of sirolimus in rats, a high performance liquid chromatography tandem mass spectrometry method was developed for sirolimus assay in whole blood. Calibration curve of sirolimus was acquired over a concentration ranging from 2.5 to 100 ng/mL with r= 0.9955. The matrix effects and extraction recoveries of sirolimus ranged from 144% to 152% and from 80% to 96%, respectively. The inter- and intraday relative standard deviations were both <10%. The stability investigation showed that the blood samples were stable for 30-day-storage at -20°C, for 8 h storage at room temperature, for 24 h storage in the auto-sampler at 4°C, and for three freeze-thaw cycle process. The pharmacokinetic results demonstrated that the , AUC, and AUMC of sirolimus in rats (7.5 mg/kg, i.g.) were increased after beincoadministration with Tanreqing Injection at 2.5, 5.0, and 7.5 mL/kg (i.v.), respectively, or at 5 min, 2 h, and 4 h (5.0 mL/kg, i.v.) after SRL dosing, respectively. For the first time, the results proved the herb-drug interaction between Tanreqing Injection and sirolimus and accordingly suggested avoiding concurrent reception of those two drugs for patients.
为评估痰热清注射液对大鼠体内西罗莫司药代动力学的影响，建立了一种测定全血中西罗莫司的高效液相色谱-串联质谱法。西罗莫司的校准曲线浓度范围为 2.5 至 100ng/mL，相关系数为 0.9955。西罗莫司的基质效应和提取回收率分别为 144%至 152%和 80%至 96%。日内和日间相对标准偏差均<10%。稳定性研究表明，血样在-20°C 下储存 30 天、室温下储存 8 小时、4°C 自动进样器中储存 24 小时以及经过三个冻融循环过程均稳定。药代动力学结果表明，大鼠（7.5mg/kg，灌胃）在分别静脉给予 2.5、5.0 和 7.5mL/kg 痰热清注射液后，或在静脉给予 5.0mL/kg 痰热清注射液后 5min、2h 和 4h，西罗莫司的 AUC 和 AUMC 增加。首次证明了痰热清注射液与西罗莫司之间的药物相互作用，并建议患者避免同时使用这两种药物。
