当前位置: X-MOL 学术J. Chromatogr. B › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Determination of quantitative retention-activity relationships between pharmacokinetic parameters and biological effectiveness fingerprints of Salvia miltiorrhiza constituents using biopartitioning and microemulsion high-performance liquid chromatography
Journal of Chromatography B ( IF 2.8 ) Pub Date : 2017-09-13 , DOI: 10.1016/j.jchromb.2017.09.018
Haoshi Gao 1 , Hongzhang Huang 2 , Aini Zheng 3 , Nuojun Yu 3 , Ning Li 3
Affiliation  

In this study, we analyzed danshen (Salvia miltiorrhiza) constituents using biopartitioning and microemulsion high-performance liquid chromatography (MELC). The quantitative retention-activity relationships (QRARs) of the constituents were established to model their pharmacokinetic (PK) parameters and chromatographic retention data, and generate their biological effectiveness fingerprints. A high-performance liquid chromatography (HPLC) method was established to determine the abundance of the extracted danshen constituents, such as sodium danshensu, rosmarinic acid, salvianolic acid B, protocatechuic aldehyde, cryptotanshinone, and tanshinone IIA. And another HPLC protocol was established to determine the abundance of those constituents in rat plasma samples. An experimental model was built in Sprague Dawley (SD) rats, and calculated the corresponding PK parameterst with 3P97 software package.

Thirty-five model drugs were selected to test the PK parameter prediction capacities of the various MELC systems and to optimize the chromatographic protocols. QRARs and generated PK fingerprints were established. The test included water/oil-soluble danshen constituents and the prediction capacity of the regression model was validated. The results showed that the model had good predictability.



中文翻译:


采用生物分配和微乳高效液相色谱法测定丹参成分药代动力学参数与生物有效性指纹图谱之间的定量保留活性关系



在本研究中,我们使用生物分配和微乳液高效液相色谱 (MELC) 分析了丹参 ( Salvia miltiorriza ) 成分。建立成分的定量保留活性关系(QRAR)来模拟其药代动力学(PK)参数和色谱保留数据,并生成其生物有效性指纹。建立了高效液相色谱(HPLC)方法测定提取的丹参素钠、迷迭香酸、丹酚酸B、原儿茶醛、隐丹参酮和丹参酮IIA等成分的丰度。并建立了另一个 HPLC 方案来测定大鼠血浆样品中这些成分的丰度。建立Sprague Dawley (SD)大鼠实验模型,并利用3P97软件包计算相应的PK参数。


选择 35 种模型药物来测试各种 MELC 系统的 PK 参数预测能力并优化色谱方案。建立了 QRAR 和生成的 PK 指纹。该测试包括水溶性/油溶性丹参成分,并且验证了回归模型的预测能力。结果表明,该模型具有良好的预测能力。

更新日期:2017-09-13
down
wechat
bug