LC-MS/MS法测定大鼠血浆中芦荟苦素浓度及其药动学研究
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篇名: LC-MS/MS法测定大鼠血浆中芦荟苦素浓度及其药动学研究
TITLE: Determination of Aloesin in Rat Plasma by LC-MS/MS and Its Pharmacokinetic Study
摘要: 目的:建立测定大鼠血浆中芦荟苦素浓度的方法,并考察芦荟苦素的药动学特征。方法:血浆样品经甲醇沉淀蛋白后,以芦荟新苷D为内标,采用液相色谱-串联质谱法测定大鼠血浆中芦荟苦素的血药浓度。以SynergiHydro-RP为色谱柱,以0.1‰甲酸溶液-甲醇为流动相进行梯度洗脱,流速为0.50mL/min,柱温为30℃,进样量为5µL;采用电喷雾离子源,以多反应监测模式进行负离子检测,用于定量分析的离子对分别为m/z393.1→272.9(芦荟苦素)、m/z555.3→144.9(内标)。采用上述方法测定大鼠尾静脉注射(3.35mg/kg)和灌胃(16.75mg/kg)芦荟苦素后0.083、0.167、0.333、0.667、1、1.5、2.5、4、6、8、10h静脉血中芦荟苦素的质量浓度,采用DAS3.0软件计算药动学参数。结果:芦荟苦素检测质量浓度的线性范围为1~600ng/mL(r=0.9945),定量下限为1ng/mL,批内、批间RSD均小于15%,批内、批间准确度在±15%内,基质因子为(92.74±4.33)%~(94.84±2.57)%,提取回收率为(69.04±2.13)%~(75.03±2.84)%,稳定性试验的实测结果与理论值的偏差在±15%内。大鼠静脉注射和灌胃芦荟苦素后,主要药动学参数cmax分别为(10693.3±2745.3)、(223.3±36.2)ng/mL,t1/2分别为(2.45±1.45)、(3.33±1.91)h,AUC0-24h分别为(4190.6±883.6)、(1210.1±93.9)ng·h/mL(n=3),口服绝对生物利用度为11.13%。结论:本研究成功建立了一种快速、灵敏的芦荟苦素血药浓度测定方法,适用于其药动学研究。
ABSTRACT: OBJECTIVE:To establish a method for the determination of aloesin in plasma of rats ,and to investigate pharmacokinetic characteristics of aloesin. METHODS :The plasma samples were precipitated with methanol. Using aloeresin D as internal standard ,the plasma concentration of aloesin was determined by LC-MS/MS. The determination was performed on Synergi Hydro-RP column with mobile phase consisted of 0.1‰ formic acid-methanol (gradient elution )at the flow rate of 0.50 mL/min. The column temperature was 30 ℃,and sample size was 5 µL. The electrospray ionization source was applied to carry out negative ion detection with multiple reaction monitoring mode . The ion transitions for quantitative analysis were m/z 393.1→272.9(aloesin) and m/z 555.3→144.9(internal standard ),respectively. The concentration of aloesin in venous blood was determined by above method at 0.083,0.167,0.333,0.667,1,1.5,2.5,4,6,8,10 h after intravenous injection (3.35 mg/kg)and intragastric administration(16.75 mg/kg)of aloesin. DAS 3.0 software was used to calculate pharmacokinetic parameters. RESULTS :The linear range of aloesin were 1-600 ng/mL(r=0.994 5). The lower limit of quantification was 1 ng/mL,and RSDs of within and between batches were less than 15%;accuracies within and between batches were within ±15%. The matrix factors were (92.74± 4.33)%-(94.84±2.57)%,and extraction recoveries were (69.04±2.13)%-(75.03±2.84)%;the deviation between the measured results of the stability test and the theoretical values were within ±15%. After intravenous injection and intragastric administration of aloesin ,main pharmacokinetic parameters were as follows :cmax were(10 693.3±2 745.3)and(223.3±36.2)ng/mL;t1/2 were (2.45±1.45)and(3.33±1.91)h;AUC0-24h were(4 190.6±883.6)and(1 210.1±93.9)ng·h/mL(n=3). Absolute bioavailabi- lity was 11.13%. CONCLUSIONS :The established method is rapid and sensitive for plasma determination of aloesin ,and suitable for its pharmacokinetic study.
期刊: 2021年第32卷第22期
作者: 谭银丰,孙墨箫,张蕾,杨雯悦,李海龙,李友宾
AUTHORS: TAN Yinfeng ,SUN Moxiao ,ZHANG Lei,YANG Wenyue ,LI Hailong ,LI Youbin
关键字: 芦荟苦素;芦荟新苷D;血药浓度;药动学;液相色谱-串联质谱法;大鼠
KEYWORDS: Aloesin;Aloeresin D ;Plasma concentration ;
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