苦参碱胶丸在健康人体内的药动学
Pharmacokinetics of matrine capsules in healthy volunteers
张瑞雯 1徐红蓉 2胡朝英 3陈莉 3申渊钢 4刘罡一 3李雪宁 2李勤1
作者信息
- 1. 上海市生物医药科技产业促进中心,上海 201203
- 2. 复旦大学附属中山医院,上海 200032
- 3. 上海市徐汇区中心医院,上海 200031
- 4. 双鹤同德堂连锁大药房有限责任公司,江苏昆山 215300
- 折叠
摘要
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7d)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pmax、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.
Abstract
AIM To study the pharmacokinetics of matrine capsules in healthy volunteers. METHODS Nine healthy male volunteers were administered with a single dose of 100, 200 and 400 mg of matrine capsules, and the interval between administration was at least 7 days. The matrine concentration in plasma was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) method, and the relative bioavailability and bioequivalence of the tablets were analyzed by DAS 2.0 software. RESULTS The pharmacokinetic parameters of matrine in plasma of healthy volunteers administered with 100, 200 and 400 mg were as follows; pmax were (603.84 ± 131.80), (1 207.27 ± 331.95) and (2 384.44 ± 720.67) μg·L-1; tmax were (1.33 ±0.61), (1.61 ± 0.78) and (1.67 ± 0.71) h; tl/2 were (8.68 ± 1.32) , (8.28 ± 0.97) and (7.82 ± 0.76) h; AUC0_ were (6 203.25 ± 131.80), (12 816.34 ± 4 665.77) and (20 077.59 ± 6 841.86) μg·h·L-1; AUC0-∞ were (6 375.38 ± 2 253.17), (13 047.49 ± 4 780.74) and (20 316.03 ± 6 939.34) μg·h·L-1. CONCLUSION Matrine has good safety and tolerance in healthy male volunteers. Plasma concentration of matrine is positively correlated with dose level.
关键词
苦参碱/色谱法,高压液相/串联质谱法/药动学Key words
matrine/chromatography, high pressure liquid/tandem mass spectrometry/pharmaco-kinetics引用本文复制引用
基金项目
上海市科委科研计划(08411966700)
上海市徐汇区医学科研项目(SHXH201140)
出版年
2012
NETL
NSTL
维普
万方数据