颈舒颗粒中三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1在脊髓型颈椎病模型大鼠中的药代动力学研究
Pharmacokinetic Study on Notoginsenoside R1,Ginsenoside Rg1 and Ginsenoside Rb1 of Jingshu Keli in Rat with Cervical Spondylotic Myelopathy Model
周传铭 1陈瑞 1许杉 2律立红 1徐智儒1
作者信息
- 1. 中国医药工业研究总院有限公司,上海医药工业研究院创新药物与制药工艺国家重点实验室,上海 200437;上海市生物物质成药性评价专业技术服务中心,上海 200437
- 2. 河南省肿瘤医院,郑州大学附属肿瘤医院,河南郑州 450008
- 折叠
摘要
颈舒颗粒在临床上己被证明对脊髓型颈椎病(CSM)有较好的治疗效果,其主要活性成分为三七皂苷R1(1)、人参皂苷Rg1(2)和人参皂苷Rb1(3).该研究建立了超高效液相色谱-质谱联用(UPLC-MS)法检测CSM模型大鼠血浆中的1、2和3浓度,用于研究颈舒颗粒在大鼠体内的药代动力学特征.结果显示,大鼠灌胃给予颈舒颗粒后,1的血浆浓度较低(＜8.892 ng/mL),2 和 3 的 cmax、AUC0→t和t1/2分别为(27.75±4.13)和(123.60±8.56)ng/mL、(255.41±38.59)和(1 344.32± 122.52)h·ng·mL-1,以及(11.97±3.75)和(14.54±2.71)h.该检测方法灵敏、可靠,可用于1、2和3在CSM模型大鼠体内的药代动力学研究.
Abstract
The therapeutic effects of Jingshu Keli(or Jingshu granules)on cervical spondylotic myelopathy(CSM)have been substantiated in clinical practice.Its main active constituents are notoginsenoside R1(1),ginsenoside Rg1(2),and ginsenoside Rb1(3).This study established an ultra-performance liquid chromatography-mass spectrometry(UPLC-MS)method for determination of the concentrations of 1,2,and 3 in plasma of rats with CSM,then the pharmacokinetic characteristics of 1,2,and 3 in the rats were investigated.The results showed that after oral gavage administration of Jingshu Keli to the rat,the plasma concentration of 1 was low(＜8.892 ng/mL);the cmax,AUC0→t and t1/2 for 2 and 3 were(27.75±4.13)and(123.60±8.56)ng/mL,(255.41±38.59)and(1 344.32±122.52)h·ng·mL-1,(11.97±3.75)and(14.54±2.71)h,respectively.This detection method was sensitive and reliable,and was suitable for the pharmacokinetic study of 1,2,and 3 in the rat model of CSM.
关键词
颈舒颗粒/脊髓型颈椎病/药代动力学/LC-MS/MSKey words
Jingshu Keli/cervical spondylotic myelopathy/pharmacokinetics/LC-MS/MS引用本文复制引用
出版年
2023
NETL
NSTL
万方数据