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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 ； |
| 阅读数： | 264 次 |
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