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建立了测定大鼠血浆中益母草碱(1)及其葡萄糖醛酸结合物(2)的LC-MS/MS方法。考察了大鼠单次和连续28 d灌胃给予低、中、高剂量1(200、600和2 000 mg/kg)后1和2在体内的暴露水平,绘制药-时曲线并计算毒代动力学参数。单剂量试验表明,低、中、高剂量组1的AUC分别为(1.946±0.908)、(7.002±2.759)和(26.408±11.491)mol.L-1.h,1在大鼠体内消除行为符合线性动力学模型。多剂量试验表明,低、中、高剂量组1的AUC分别为(2.987±1.089)、(9.083±3.140)和(20.178±7.484)mol.L-1.h。长期大剂量灌胃给予1,1和2均未见在大鼠体内明显蓄积,且试验过程中未见大鼠有明显的毒性反应。
A LC-MS / MS method for the determination of Leonurine (1) and its glucuronic acid conjugate (2) in rat plasma was established. The level of exposure to 1 and 2 in rats after single and continuous 28-day oral administration of low, medium and high doses of 1 (200, 600 and 2000 mg / kg) was investigated. The drug-time curve was plotted and the toxin generation Kinetic parameters. The single-dose test showed that the AUC of low, medium and high dose group 1 were (1.946 ± 0.908), (7.002 ± 2.759) and (26.408 ± 11.491) mol.L-1.h, 1, respectively, Linear dynamic model. Multiple dose experiments showed that the AUC of low, medium and high dose group 1 were (2.987 ± 1.089), (9.083 ± 3.140) and (20.178 ± 7.484) mol.L-1.h respectively. Long-term high-dose gavage given 1,1 and 2 were no significant accumulation in rats, and no obvious toxicity in rats during the test.