党参补血汤（DBD）是一种传统的中药方剂，其通过增加吉西他滨的活性代谢物，有潜力增强对非小细胞肺癌（NSCLC）治疗中的抗肿瘤作用。然而，吉西他滨是否会影响DBD的主要组分的药代动力学仍不清楚。本研究评估DBD的主要成分与吉西他滨之间的草药-药物相互作用，并验证其潜在的药代动力学机制。 在Sprague-Dawley大鼠中，研究了3.6克/千克DBD与50毫克/千克吉西他滨单次给药后的药代动力学。采用免疫印迹分析法确定了吉西他滨对大鼠组织中肠道渗透性和肝微粒体酶以及CYP3A过表达HepG2细胞的影响。 吉西他滨的联合应用显著改变了大鼠中DBD的主要成分的药代动力学特性。通过促进钠葡萄糖转运蛋白1（SGLT-1）的表达，大青蛰芥苷的Cmax和AUC显著增加。肉桂内酯和阿魏酸的AUC也显著增加，其消除半衰期（t1/2）分别延长了2.4倍和7.8倍，通过下调肝CYP3A和紧密连接蛋白zonula occludens-1（ZO-1）和occludin的表达。 吉西他滨通过增加肠道渗透性，增强转运蛋白表达，以及下调CYP3A调节了DBD的主要成分的药代动力学。这些结果为DBD作为NSCLC与吉西他滨的辅助剂剂量调整提供了关键信息，并有助于更科学、更合理地进行潜在的剂量调整的临床研究。

Danggui Buxue Decoction (DBD), a traditional Chinese medicine formula, has the potential to enhance the antitumor effect of gemcitabine in non-small cell lung cancer (NSCLC) treatment by increasing gemcitabine's active metabolites. However, whether gemcitabine affects the pharmacokinetics of DBD's major components remains unclear.This study evaluates the herb-drug interaction between DBD's major components and gemcitabine and validates the underlying pharmacokinetic mechanism.The pharmacokinetics of 3.6 g/kg DBD with and without a single-dose administration of 50 mg/kg gemcitabine was investigated in Sprague-Dawley rats. The effects of gemcitabine on intestinal permeability, hepatic microsomal enzymes in rat tissues, and CYP3A overexpressing HepG2 cells were determined using western blot analysis.The combination of gemcitabine significantly altered the pharmacokinetic profiles of DBD's major components in rats. The Cmax and AUC of calycosin-7-O-β-d-glucoside notably increased through sodium-glucose transporter 1 (SGLT-1) expression promotion. The AUC of ligustilide and ferulic acid was also significantly elevated with the elimination half-life (t1/2) prolonged by 2.4-fold and 7.8-fold, respectively, by down-regulating hepatic CYP3A, tight junction proteins zonula occludens-1 (ZO-1) and occludin expression.Gemcitabine could modulate the pharmacokinetics of DBD's major components by increasing intestinal permeability, enhancing transporter expression, and down-regulating CYP3A. These findings provide critical information for clinical research on DBD as an adjuvant for NSCLC with gemcitabine and help make potential dosage adjustments more scientifically and rationally.