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LC/MS/MS法测定中国健康志愿者血浆中瑞舒伐他汀浓度及药动学
引用本文:文爱东,毕琳琳,罗晓星,贾艳艳,陈笑艳,张逸凡. LC/MS/MS法测定中国健康志愿者血浆中瑞舒伐他汀浓度及药动学[J]. 解放军药学学报, 2007, 23(2): 110-113
作者姓名:文爱东  毕琳琳  罗晓星  贾艳艳  陈笑艳  张逸凡
作者单位:1. 第四军医大学西京医院,药剂科,陕西,西安,710032
2. 第四军医大学,药理教研室,陕西,西安,710032
3. 中国科学院上海药物研究所,上海,201203
摘    要:目的 建立人血浆中瑞舒伐他汀的液相色谱-质谱-质谱联用测定方法,研究中国健康人体药代动力学。方法 以氢氯噻嗪为内标物,采用液相色谱-质谱-质谱联用法,电喷雾电离源选择性正离子峰检测。测30名健康男性志愿者单剂量口服瑞舒伐他汀钙片的体内血药浓度,获得药动学参数。结果 口服瑞舒伐他汀钙片5、10、20mg后的主要药代学参数:达峰时间Tmax分别为(3.10±0.99)、(2.00±0.82)、(3.40±1.58)h;峰值血浆浓度Cmax分别为(8.32±2.44)、(14.8±3、97)、(20.1±5.0)ng·ml^-1;药时曲线下面积AUC0-∞分别为(77.0±22.6)、(153±38)、(270±61)ng·h·ml^-1;AUCo.1分别为(75.8±22.0)、(151±37)、(258±62)ng·h·ml^-1;T1/2分别为(13.0±3.9)、(12.5±3.5)、(18.5±4.9)h。结论 受试者口服瑞舒伐他汀钙片后,在人体内表现为线性药代学特征。

关 键 词:瑞舒伐他汀  药代动力学  LC/MS/MS
文章编号:1008-9926(2007)02-0110-04
收稿时间:2006-04-11
修稿时间:2006-12-30

Determination of Rosuvastatin in Human Plasma by LC/MS/MS and Study of Pharmacokinetics
WEN Ai-Dong,BI Lin-Lin,LUO Xiao-Xing,JIA Yan-Yan,CHEN Xiao-Yan,ZHANG Yi-Fan. Determination of Rosuvastatin in Human Plasma by LC/MS/MS and Study of Pharmacokinetics[J]. Pharmaceutical Journal of Chinese People's Liberation Army, 2007, 23(2): 110-113
Authors:WEN Ai-Dong  BI Lin-Lin  LUO Xiao-Xing  JIA Yan-Yan  CHEN Xiao-Yan  ZHANG Yi-Fan
Affiliation:WEN Ai-Dong ,BI Lin-Lin, LUO Xiao-Xing ,JIA Yan-Yan,CHEN Xiao-Yan ,ZHANG Yi-Fan(1.Department of Pharmacy,Xijing Hospital of Fourth Military Medical University,Xi'an 710032,Shaanxi China;2.Department of Pharmacology, Fourth Military Medical University, Xi'an 710032,Shaanxi China;3.Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203 China)
Abstract:Aim To determine rosuvastatin in Chinese human plasma by an LC/MS/MS method, and to study its pharmacokinetics. Methods Rosuvastatin concentrations in plasma were determined by LC/MS/MS. The test and reference formulations of rosuvastatin were given to 30 healthy male volunteers. Results The main pharmacokinetic parameters for rosuvastatin tablets : T max were ( 3. 10± 0.99), (2.00 ± 0.82) and ( 3.40± 1.58) h ; C max were ( 8. 32 ± 2.44), ( 14.8 ± 3.97) and (20.1 ± 5.0) ng·ml^-1 ; AUC0-∞ were (77.0 ± 22.6 ), ( 153 ± 38 ) and ( 270-± 61)ng·h·ml^-1 ;AUC0-1 were (75.8 ±22.0) ,(151±37) and (258 ±62)ng·h·ml^-1; T 1/2 were (13.0 ±3.9), ( 12.5 ±3.5) and ( 18.5 ±4.9) h. Conclusion Rosuvastatin showed linear pharmacokinetics in the dosing setting in bodies of healthy subjects.
Keywords:Rosuvastatin    Pharmacokinetics    LC/MS/MS
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