目的:考察乌药总生物碱提取物中的主要活性成分去甲异波尔定及其代谢物去甲异波尔定-9-O-α-葡萄糖醛酸苷在大鼠体内的药代动力学特征。方法:18只SD大鼠随机分为3组,分别口服79.4,158.7和238.1 mg.kg-1的乌药总生物碱,以超高效液相色谱质谱法测定血浆中去甲异波尔定及其葡萄糖醛酸苷的血药浓度。采用PK-solution软件,以非房室模型计算药代动力学参数。结果:大鼠口服不同剂量乌药总碱,去甲异波尔定及其葡萄糖醛酸苷的血浆Cmax分别为(0.10±0.06),(0.10±0.05),(0.15±0.11)μg.mL-1和(9.23±3.33),(11.88±3.87),(12.42±2.52)μg.mL-1;Tmax分别为(10.83±9.70),(7.50±2.74),(9.17±5.85)min和(40.83±10.21),(50.83±35.41),(52.50±8.22)min;AUC0-∞分别为(5.38±1.24),(8.06±5.63),(8.22±2.77)mg.min.mL-1和(3 071.99±1 036.37),(6 469.75±3 068.94),(6 947.36±2922.44)mg.min.mL-1。结论:大鼠口服79.4～238.1 mg.kg-1乌药总碱提取物,去甲异波尔定在体内吸收和代谢非常迅速,其原型药物和葡萄糖醛酸结合物在体内呈线性动力学特征。 OBJECTIVE: To investigate the pharmacokinetics of norvalipidine and its metabolite norvalipine-9-O-α-glucuronide in the rat’s body, the main active component of total alkaloid extract Learn characteristics. Methods: Eighteen Sprague-Dawley rats were randomly divided into three groups. The total alkaloids of Radix Aconiti Lateralis were administered orally by 79.4, 158.7 and 238.1 mg.kg-1, respectively. The plasma concentrations of nor- Its glucuronide plasma concentration. PK-solution software was used to calculate pharmacokinetic parameters in a non-compartmental model. Results: The plasma Cmax of total alkaloids and desferrioxamine and glucuronide in different dosage groups were (0.10 ± 0.06), (0.10 ± 0.05) and (0.15 ± 0.11) μg.mL- Tmax were (10.83 ± 9.70), (7.50 ± 2.74), (9.17 ± 5.85) min and (40.83 ± 1), respectively, and (9.23 ± 3.33), (11.88 ± 3.87) and (12.42 ± 2.52) μg.mL- (50.83 ± 35.41) and (52.50 ± 8.22) min, respectively; AUC0-∞ were (5.38 ± 1.24), (8.06 ± 5.63), (8.22 ± 2.77) mg.min.mL-1 and (3 071.99 ± 1 036.37), (6 469.75 ± 3 068.94), (6 947.36 ± 2922.44) mg.min.mL-1. CONCLUSION: The total alkaloids extract of Radix Aconiti Lateralis Preparata from 79.4 to 238.1 mg · kg-1 is orally administered to rats, norfopidine is rapidly absorbed and metabolized in vivo, and its pharmacokinetics and glucuronic acid conjugate exhibit linear kinetic characteristics in vivo .