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Pharmacokinetic Study of Delavinone in Mice after Intravenous and Oral Administration by UPLC-MS/MS.
BioMed Research International ( IF 2.6 ) Pub Date : 2019-03-21 , DOI: 10.1155/2019/3163218
Shuanghu Wang 1 , Zhiguang Zhang 2 , Zheng Yu 2 , Cheng Han 2 , Xianqin Wang 2
Affiliation  

Thirty-one compounds, including delavinone, were isolated from the methanol extract of F. cirrhosa by modern chromatographic techniques. The pharmacological action of Fritillaria is widely used in clinical practice. However, the pharmacokinetic studies on delavinone have not been reported. Therefore, the chemical constituents of this species were investigated. Therefore, it is necessary to establish an analytical method to monitor the concentration of delavinone. An UPLC-MS/MS method was established to determine delavinone in the mouse blood, and the pharmacokinetics of delavinone after intravenous (1.0 mg/kg) and intragastric (2.5, 10.0 mg/kg) administration were studied. The lower limit of quantification was 1.0 ng/mL. The intraday and interday precision RSD were less than 13%, the accuracy ranged from 96.8% to 104.9%, the average recovery was better than 80.6%, and the matrix effect was between 88.8% and 103.4%. The UPLC-MS/MS method has been successfully applied to the pharmacokinetics of delavinone in mice. The noncompartment model was used to fit the main pharmacokinetic parameters. It was found that AUC in mice was higher than that in mice given orally, and the bioavailability of delavinone was 12.4%.

中文翻译:

UPLC-MS/MS 静脉和口服给药后地拉维酮在小鼠体内的药代动力学研究。

通过现代色谱技术从F. cirrhosa的甲醇提取物中分离出包括地草酮在内的 31 种化合物。贝母的药理作用在临床上广泛应用。但地拉维酮的药代动力学研究尚未见报道。因此,对该物种的化学成分进行了研究。因此,有必要建立一种分析方法来监测地拉维酮的浓度。建立了小鼠血液中地氢维酮的UPLC-MS/MS测定方法,并研究了地氢维酮静脉注射(1.0 mg/kg)和灌胃(2.5、10.0 mg/kg)后的药代动力学。定量下限为1.0 ng/mL。日内、日间精密度RSD均小于13%,准确度为96.8%~104.9%,平均回收率优于80.6%,基质效应在88.8%~103.4%之间。UPLC-MS/MS方法已成功应用于地拉维酮在小鼠体内的药代动力学研究。使用非房室模型来拟合主要药代动力学参数。结果发现,小鼠体内AUC高于口服小鼠,地拉维酮的生物利用度为12.4%。
更新日期:2019-03-21
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