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痰热清注射液对大鼠体内西罗莫司药代动力学的影响。

The Effect of Tanreqing Injection on the Pharmacokinetics of Sirolimus in Rats.

机构信息

Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China.

出版信息

Biomed Res Int. 2019 Mar 10;2019:1854323. doi: 10.1155/2019/1854323. eCollection 2019.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f557/6431440/21290691bd93/BMRI2019-1854323.001.jpg

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