首页|甘草查尔酮A在比格犬体内的药代动力学研究

甘草查尔酮A在比格犬体内的药代动力学研究

扫码查看
目的 建立测定比格犬血浆中甘草查尔酮A含量的UPLC-MS/MS分析方法,并研究甘草查尔酮A单剂量静脉注射和灌胃给药后在比格犬体内药代动力学模式.方法 比格犬以3 mg·kg-1的剂量分别进行静脉注射和灌胃给药甘草查尔酮A,采集不同时间点的血浆样品,采用UPLC-MS/MS方法测定血浆中甘草查尔酮A的浓度,采用DAS 2.1.1版软件对血药浓度-时间曲线进行统计矩拟合,计算甘草查尔酮A的药代动力学参数.结果 血浆中甘草查尔酮A的线性回归方程为:Y=0.039X+0.1959,R2=0.9997,线性范围为2~2000 μg·L-1.静脉注射甘草查尔酮A在血浆中的半衰期t1/2为6.57 h,药时曲线下面积(AUC0~t)为1665 h·mg·L-1,平均驻留时间(MRT0~t)为5.68h,清除率(CL)为2106L·h-1·kg-1.灌胃给药甘草查尔酮A在血浆中的t1/2为8.23 h,AUC0~,为397 h·mg·L-1,MRT0~t为9.35 h,口服生物利用度为23.8%.结论 甘草查尔酮A在血浆的UPLC-MS/MS方法具有良好的专属性与灵敏度.灌胃给药甘草查尔酮A具有良好的血浆暴露量及口服生物利用度.
Pharmacokinetics of licochalcone A in Beagle dogs
Objective To develop an UPLC-MS/MS to determine the concentration of licochalcone A in the plasma of Beagle dogs and the pharmacokinetics after a single dose intravenous and oral administration of licochalcone A,respectively.Methods Beagle dogs were intravenously and orally administered licochalcone A(3 mg·kg-1).The plasma samples were collected at different time spots.UPLC-MS/MS was used to determine the concentration of licochalcone A in the plasma.The plasma concentration-time curves were fit by DAS 2.1.1 software to determine the pharmacokinetic parameters of licochalcone A.Results The linear regression of licochalcone A in the plasma was:Y=0.039X+0.1959,R2=0.9997,and the linear range was 2~2000 μg·L-1.In the intravenous administration model,the half-life(t1/2)of licochalcone A in the plasma was 6.57 h,the area under the drug-time curve(AUC0~t)was 1665 h·mg·L-1,the mean residence time(MRT0~t)was 5.68 h,and the clearance rate(CL)was 2106 L·h-1·kg 1.While in the oral administration model,the t1/2 of licochalcone A in the plasma was 8.23 h,AUC0~t was 397 h·mg·L-1,the MRT0~t was 9.35 h,and the oral bioavailability was 23.8%.Conclusion The UPLC-MS/MS method is accurate and applicable for the pharmacokinetic study of licochalcone A in the plasma of Beagle dogs.Licochalcone A shows moderate oral bioavailability.

licochalcone ApharmacokineticsUPLC-MS/MSoral bioavailability

杨文娜、翟亚楠、邵寒冰、卢伟

展开 >

沧州市疾病预防控制中心,河北 沧州 061000

甘草查尔酮A 药代动力学 UPLC-MS/MS 口服生物利用度

沧州市科技计划自筹经费项目

222106158

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(7)
  • 14