摘要
目的建立快速、灵敏的液相色谱-串联质谱法(LC-MS/MS)测定人血浆中甘草次酸(治疗慢性肝病药物)的浓度,评价国产与进口复方甘草酸苷片在健康人体的生物等效性。方法 22名中国健康男性志愿者随机分为试验组和对照组,采用双交叉设计和单剂量口服方式,以LC-MS/MS法测定血浆中甘草次酸浓度,经DAS2.0统计软件计算主要药代动力学参数。结果线性范围0.50～800.00ng·mL-1,最低定量浓度为0.50ng·mL-1,日内精密度(RSD)<10.60%,日间精密度(RSD)<8.80%。受试制剂或参比制剂的主要药动学参数:t1/2分别为(13.1±8.5)和(10.3±5.6)h;tmax分别为(13.5±6.0)和(16.7±7.2)h;Cmax分别为(288.0±249.0)和(287.0±160.0)ng·mL-1。试验制剂相对生物利用度为(117.4±79.8)%。结论试验制剂与参比制剂具有人体生物等效性。
Objective To establish a rapid and sensitive LC -MS/MS method for the determination of glycyrrhetic acid in human plasma and to evaluate the bioequivalence of domestic and imported compound glyeyrrhizin tablets in healthy volunteers. Methods Twenty two Chinese healthy male volunteers were randomly divided into two groups （test and reference） , with double cross -over design and single -dose oral administration. The concentration of glycyrrhetic acid in plasma was determined by LC -MS/MS. The main pharmaeokinetic parameters were calculated and the bioequivalence was evaluated with DAS 2.0 practical pharmacokinetic program. Results The linear range of glycyrrhetic acid was 0. 50 -800. 00 ng · mL^-1. The lower limit of quantification was 0. 50 ng · mL^-1. The main pharmacokinetic parameters of test and reference were as follows： t1/2 were （13.1 ±8.5） and （10. 3 ±5.6） h; tmax were （13.5 ±6.0） and （16.7 ±7.2） h; Cmax were （288.0 ±249.0） and （287.0 ± 160.0） ng · mL^-1. The relative bioavailahility of the test preparation was （ 117.4 ± 79.8 ） %. Conclusion The test and reference preparations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2010年第7期513-517,共5页
The Chinese Journal of Clinical Pharmacology
基金
新疆维吾尔自治区科技攻关(含重大专项)
重点基金资助项目(200733146-4)
