木犀草素和木犀草苷在大鼠体内的药动学研究
x

请在关注微信后,向客服人员索取文件

篇名: 木犀草素和木犀草苷在大鼠体内的药动学研究
TITLE:
摘要: 目的:建立测定木犀草素和木犀草苷在大鼠体内的药动学方法并测定其药动学参数。方法: 16只SD大鼠随机分为木犀草素组(舌下iv,1.34 mg/kg)和木犀草苷组(舌下iv,0.64 mg/kg),并于给药前和给药后0、15、30 min及1、2、3、4、 6、8、12、24、48 h经尾静脉取血0.5 ml制备血浆,采用超高效液相色谱串联三重四级杆质谱法测定血药浓度,并计算药动学参数。色谱柱为CORTECSTM UPLC® C18(100 mm×2.1 mm,1.6 μm),流动相为乙腈-水(含0.1%甲酸),流速为0.4 ml/min,柱温为40 ℃,内标为槲皮苷。结果:木犀草素、木犀草苷的线性范围分别为2.5~500 ng/ml (r=0.998 2)、10~2 500 ng/ml (r=0.993 5),定量下限分别为1、2.5 ng/ml,提取回收率分别为70.75%~87.72%、75.40%~91.18%(n=6),日内、日间RSD均小于10%(n=3)。药动学参数t1/2分别为(1.88±0.32)、 (1.57±0.08) h,CL分别为(0.77±0.18)、(0.06±0.01) L/(h·kg),AUC0-6 h分别为(189.60±40.04)、(1 093.14±187.36) ng·h/ml,AUC0-∞分别为(195.18±38.37)、(1 097.11±188.07) ng·h/ml。结论:本研究建立的方法可用于木犀草素和木犀草苷在大鼠体内的药动学研究,两者在大鼠体内的药动学符合二室模型。
ABSTRACT: OBJECTIVE: To establish the method for pharmacokinetic study of luteolin and cynaroside in rats and to determine pharmacokinetic parameters. METHODS: 16 SD rats were randomly divided into luteolin group (sublingual iv, 1.34 mg/kg) and cynaroside group (sublingual iv, 0.64 mg/kg). 0.5 ml blood were collected before administration and 0,15,30 min and 1,2,3,4,6, 8,12, 24, 48 h after administration respectively to prepare plasma. UPLC-TQ-MS was adopted to determine plasma concentration, and pharmacokinetic parameters were calculated. A CORTECSTM UPLC® C18 (100 mm×2.1 mm, 1.6 μm) column was used with mobile phase consisted of acetonitrile-water (containing 0.1% formic acid) at a flow rate of 0.4 ml/min, the column temperature was set at 40 ℃, and quercetin was used as internal standard. RESULTS: The linear range of luteolin and cynaroside were 2.5-500 ng/ml (r=0.998 2) and 10-2 500 ng/ml (r=0.993 5). The lowest quantitation limits were 1 and 2.5 ng/ml, and extraction were 70.75%-87.72% and 75.40%-91.18% (n=6); RSD of inter-day and intra-day were all lower than 10% (n=3). Pharmacokinetic parameters as t1/2 were (1.88±0.32) and (1.57±0.08) h; CL were (0.77±0.18) and (0.06±0.01) L/(h·kg); AUC0-6 h were (189.60±40.04) and (1 093.14±187.36) ng·h/ml;AUC0-∞ were (195.18±38.37) and (1 097.11±188.07) ng·h/ml. CONCLUSIONS: The method can be used for pharmacokinetic study of luteolin and cynaroside in rats, and the pharmacokinetics of them in rats are in line with two-compartment model.
期刊: 2016年第27卷第22期
作者: 邹晓华,王双虎,周云芳
AUTHORS: ZOU Xiaohua,WANG Shuanghu,ZHOU Yunfang
关键字: 木犀草素;木犀草苷;血药浓度;药动学;超高效液相串联质谱法
KEYWORDS: Luteolin; Cynaroside; Plasma concentration; Pharmacokinetics; UPLC-ESI-MS/MS
阅读数: 246 次
本月下载数: 4 次

* 注:未经本站明确许可,任何网站不得非法盗链资源下载连接及抄袭本站原创内容资源!在此感谢您的支持与合作!