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灯盏花素是从干燥的灯盏细辛中提取的黄酮类混合物,其主要活性成分是灯盏乙素,而缬沙坦是抗高血压药,两药在临床上常联合应用治疗糖尿病肾病,联合用药增强了对糖尿病肾病的保护作用。本研究旨在探讨灯盏乙素和缬沙坦在大鼠体内的药动学相互作用。18只雄性SD大鼠分别单独或联合给予灯盏花素注射液(20 mg.kg1,iv)和缬沙坦(15 mg.kg1,ig),采用高效液相色谱法(HPLC)测定灯盏乙素和缬沙坦的浓度,通过非隔室模型计算药动学参数。研究发现与缬沙坦联合用药后灯盏乙素的药动学参数发生明显改变,血浆清除率和胆汁清除率显著降低,而单独给药及联合给药后缬沙坦的药动学参数没有显著性变化。实验结果表明联合使用缬沙坦减少了灯盏乙素的胆汁排泄,其原因可能是缬沙坦抑制由Mrp2(多药耐药相关蛋白2)介导的灯盏乙素的胆汁排泄。
Breviscapine is a mixture of flavonoids extracted from dried Erigeron breviscapus, the main active ingredient is scutellarin, and valsartan is an antihypertensive drug, two drugs are often clinically combined treatment of diabetic nephropathy, combination therapy Enhance the protection of diabetic nephropathy. This study aimed to investigate the pharmacokinetic interaction of Scutellarin and Valsartan in rats. Eighteen male Sprague Dawley rats were injected with breviscapine injection (20 mg.kg1, iv) and valsartan (15 mg.kg1, ig), respectively, either alone or in combination. High performance liquid chromatography (HPLC) And valsartan concentrations, pharmacokinetic parameters were calculated by a non-compartmental model. The study found that the pharmacokinetics parameters of scutellarin in combination with valsartan significantly changed, the plasma clearance rate and bile clearance rate decreased significantly, while the pharmacokinetic parameters of valsartan alone and in combination were not significantly Sexual change. The experimental results show that the combination of valsartan decreased the biliary excretion of scutellarin. The reason may be that valsartan inhibits the biliary excretion of scutellarin mediated by Mrp2 (multidrug resistance-associated protein 2).