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目的研究苦参碱在健康人体内的药动学特征。方法 9例健康男性受试者分别给予不同剂量的苦参碱胶丸(100、200或400 mg,服药间隔至少为7 d)后,采用液相色谱-串联质谱(LC-MS/MS)法测定血浆中苦参碱的浓度,经DAS 2.0软件计算药动学参数。结果健康受试者口服苦参碱胶丸100、200或400 mg后,血浆中苦参碱的ρmax、tmax、t1/2、AUC0-t和AUC0-∞分别为(603.84±131.80)、(1 207.27±331.95)和(2 384.44±720.67)μg.L-1,(1.33±0.61)、(1.61±0.78)和(1.67±0.71)h,(8.68±1.32)、(8.28±0.97)和(7.82±0.76)h,(6 203.25±131.80)、(12 816.34±4 665.77)和(20 077.59±6 841.86)μg.h.L-1,(6 375.38±2 253.17)、(13 047.49±4 780.74)和(20 316.03±6 939.34)μg.h.L-1。结论苦参碱在健康人体内的安全性和耐受性良好,血药浓度与药物剂量成正相关。
Objective To study the pharmacokinetics of matrine in healthy volunteers. Methods Nine healthy male subjects were given different doses of matrine capsules (100, 200 or 400 mg, at least for 7 days), and then analyzed by liquid chromatography-tandem mass spectrometry (LC-MS / MS) The concentration of matrine in plasma was measured and the pharmacokinetic parameters were calculated by DAS 2.0 software. Results After oral administration of matrine capsules at 100, 200 or 400 mg, the mean ρmax, tmax, t1 / 2, AUC0-t and AUC0-∞ of matrine were (603.84 ± 131.80) and 207.27 ± 331.95) and (2.384.44 ± 720.67) μg.L-1, (1.33 ± 0.61), (1.61 ± 0.78) and (1.67 ± 0.71) h, (8.68 ± 1.32), (8.28 ± 0.97) and ± 0.76) h, (6 203.25 ± 131.80), (12 816.34 ± 4 665.77) and (20 077.59 ± 6 841.86) μg.hL-1, (6 375.38 ± 2 253.17), (13 047.49 ± 4 780.74) and 20 316.03 ± 6 939.34) μg.hL-1. Conclusion Matrine is safe and well tolerated in healthy volunteers. The concentration of matrine is positively correlated with the dose of matrine.