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目的:研究蝙蝠葛苏林碱(DS)在兔体内的药代动力学和组织分布特征。方法:兔耳缘静脉注射给予DS后,采用高效液相色谱法测定各时间点血浆和组织器官药物浓度,并用3p97程序计算药代动力学参数。结果:兔DS2.5、5、10mg·kg-1静脉注射给药后,体内动力学行为符合二房室开放模型。T12β分别为3.0±0.6、3.4±0.9和6.9±0.6h;Cls分别为3.1±0.6、3.6±0.4和4.4±0.3L·h·kg-1;Vd分别为13.1±2.7、18.0±6.2和43.6±4.4L·kg-1;AUC0～t分别为0.84±0.13、1.41±0.17和2.30±0.18mg·h·L-1。在DS2.5～5mg·kg-1范围内主要药动学参数无显著性差异(P>0.05),但DS10mg·kg-1静脉注射后,C0超比例增加(P<0.01),T12β明显延长(P<0.01)。结论:在2.5～5mg·kg-1范围内DS的消除为线性动力学,而10mg·kg-1静脉注射后,本品在兔体内的消除未呈线性动力学。组织分布以肺脏含量最高,其次为肾、脾和肝脏。各组织器官中药量均显著高于血浆药物浓度。
Objective: To study the pharmacokinetics and tissue distribution characteristics of batuarine (DS) in rabbits. METHODS: Rabbits were injected intravenously with DS in the ear vein, and plasma and tissue concentrations at each time point were determined by high performance liquid chromatography. The pharmacokinetic parameters were calculated using the 3p97 program. RESULTS: After intravenous administration of DS2.5, 5, and 10 mg kg-1 in rabbits, the in vivo kinetics was consistent with a two-compartment open model. T12β was 3.0±0.6, 3.4±0.9, and 6.9±0.6h; Cls were 3.1±0.6, 3.6±0.4, and 4.4±0.3L·h·kg-1, respectively; Vd was 13.1±2.7, 18.0±6.2, and 43.6, respectively. ±4.4 L·kg-1; AUC0 to t were 0.84±0.13, 1.41±0.17 and 2.30±0.18 mg·h·L-1, respectively. There was no significant difference in the main pharmacokinetic parameters in the range of 2.5-5 mg·kg-1 (P>0.05), but after DS 10 mg·kg-1, the C0 overweight increased (P<0.01), and T12β was significantly prolonged. (P<0.01). Conclusion: In the range of 2.5-5 mg·kg-1, the linearity of DS was eliminated. However, after 10 mg·kg-1 intravenous injection, the linearity of the product was not eliminated in rabbits. The tissue distribution was highest in the lungs, followed by the kidneys, spleen, and liver. The amount of herbs in each tissue and organ was significantly higher than the plasma concentration.