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首页> 外文期刊>RSC Advances >An integrated pharmacokinetic study of Dengzhanxixin injection in rats by combination of multicomponent pharmacokinetics and anti-myocardial ischemic assay
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An integrated pharmacokinetic study of Dengzhanxixin injection in rats by combination of multicomponent pharmacokinetics and anti-myocardial ischemic assay

机译：多组分药代动力学与抗心肌缺血试验相结合的灯盏细辛注射液在大鼠体内的综合药代动力学研究

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This study aimed to investigate the integrated pharmacokinetics (PK) of Dengzhanxixin injection (EBI) in rats by combination of multicomponent PK and pharmacological assays. First, the protective effects of 13 main components (30 mg kg ~(?1) per day, i.v. for 7 days) on isoprenaline-induced myocardial infarction (MI) in mice were evaluated by measuring electrocardiogram and serum creatine kinase (CK) activity, and observing cardiac pathological changes. Second, the quantitative analysis method of the main components in rat plasma was established and applied to pharmacokinetic study of EBI in rats (0.72 mL kg ~(?1) and 3.2 mL kg ~(?1) of 10 times concentrated EBI, single i.v.). Third, based on the multicomponent PK and anti-MI effects, PK markers were selected, and the integrated PK of EBI in rats were investigated using “plasma drug concentration sum method” and “AUC weighting integrated method”. In the in vivo anti-MI study, the ST segment elevation seldom occurred and the serum CK significantly decreased ( P < 0.05 vs. model group); additionally tissue sections showed mild edema and inflammatory infiltration, and there was a little loss of striations in heart tissue in scutellarin, 3-caffeoylquinic acid (3-CQA), apigenin-7- O -glucuronide (A-7- O -G) and 4,5-dicaffeoylquinic acid (4,5-diCQA) treated groups, suggesting that scutellarin, 3-CQA, A-7- O -G and 4,5-diCQA were the main anti-MI effective substances. In the PK study, the systematic exposure level of scutellarin, erigoster B, 3,4-diCDOA (or 4,9-diCDOA), A-7- O -G, and 4,5-diCQA is relatively high. Considering the contents in EBI, anti-MI efficacy and PK properties of each component, scutellarin, 3-CQA, A-7- O -G, erigoster B, 3,4-diCDOA (or 4,9-diCDOA) and 4,5-diCQA were selected as pharmacokinetic markers to characterize the integrated pharmacokinetic behavior of EBI in vivo . The integrated pharmacokinetic study of EBI in rats could reveal the overall in vivo process and improve the safety and rationality of the clinical use of EBI.
机译：本研究旨在通过多组分PK和药理学检测相结合的方法研究灯盏细辛注射液（EBI）在大鼠中的综合药代动力学（PK）。首先，通过测量心电图和血清肌酸激酶（CK）活性来评估13种主要成分（每天30 mg kg〜（？1），静脉内连续7天）对异丙肾上腺素诱导的心肌梗塞（MI）的保护作用。 ，并观察心脏病理变化。其次，建立了大鼠血浆主要成分的定量分析方法，并将其用于大鼠EBI的药代动力学研究（0.72 mL kg〜（？1）和3.2 mL kg〜（？1）的10倍浓缩EBI，单次iv ）。第三，基于多组分PK和抗MI作用，选择PK标记，并采用“血浆药物浓度和法”和“ AUC加权积分法”研究了大鼠EBI的综合PK。在体内抗MI研究中，很少发生ST段抬高，血清CK显着降低（与模型组相比，P <0.05）;此外，组织切片显示轻度水肿和炎性浸润，并且黄cut苷，3-咖啡酰奎尼酸（3-CQA），芹菜素-7-O-葡萄糖醛酸苷（A-7-O-G）在心脏组织中有少量条纹消失和4,5-二咖啡酰奎尼酸（4,5-diCQA）处理的组，表明scutellarin，3-CQA，A-7-O -G和4,5-diCQA是主要的抗MI有效物质。在PK研究中，黄cut素，赤霉素B，3,4-diCDOA（或4,9-diCDOA），A-7-O-G和4,5-diCQA的系统暴露水平相对较高。考虑到EBI的含量，每种成分，黄cut素，3-CQA，A-7-O-G，赤霉素B，3,4-diCDOA（或4,9-diCDOA）和4的抗MI功效和PK特性选择5-diCQA作为药代动力学标记以表征EBI在体内的综合药代动力学行为。 EBI在大鼠中的综合药代动力学研究可以揭示整个体内过程，并提高EBI临床使用的安全性和合理性。

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