Mrhar A, Kopitar Z, Kozjek F, Krusic L, Lenardic A
Eur J Drug Metab Pharmacokinet. 1983;8(1):17-20. doi: 10.1007/BF03189576.
Wistar rats received an intravenous dose of 20 micrograms/kg and an oral does of 40 micrograms/kg 3H-Dihydroergosine. Concentrations of radioactivity were measured in plasma, bile, urine, and faeces, and pharmacokinetical parameters of an open two compartment model were calculated. After intravenous injection and oral administration 3H-Dihydroergosine is rapidly lost from the central compartment with distribution rate constants alpha = 0.889 h-1 and beta = 0.722 h-1, respectively. Biological half life in the elimination phase after both application is nearly the same t 1/2 = 13.6 h. The volume of central compartment is Vc = 3.075 l/kg and the volume of distribution Vd beta = 30.75 l/kg. The fraction of 3H-Dihydroergosine absorbed after oral administration, calculated from areas under the curves upon oral and intravenous administration, is 31%. The percentage of 3H-radioactivity eliminated with bile was 98.3% of the dose within 72 hours after intravenous and 29.3% after oral administration. The main portion of the administered 3H-radioactivity was recovered in faeces -66.1% after intravenous and 81.3% after oral administration, while only 17.4% and 4.9% of the administered dose was eliminated in the urine within 120 hours, respectively.
将20微克/千克的剂量静脉注射给Wistar大鼠，并口服40微克/千克的3H - 二氢麦角隐亭。测量血浆、胆汁、尿液和粪便中的放射性浓度，并计算开放二室模型的药代动力学参数。静脉注射和口服给药后，3H - 二氢麦角隐亭从中央室迅速消除，分布速率常数α分别为0.889小时-1和β为0.722小时-1。两种给药方式后消除相的生物半衰期几乎相同，t1/2 = 13.6小时。中央室的容积为Vc = 3.075升/千克，分布容积Vdβ = 30.75升/千克。根据口服和静脉给药后的曲线下面积计算，口服给药后3H - 二氢麦角隐亭的吸收分数为31%。静脉注射后72小时内，经胆汁消除的3H放射性占剂量的98.3%，口服给药后为29.3%。给药的3H放射性主要在粪便中回收——静脉注射后为66.1%，口服给药后为81.3%，而在120小时内，经尿液消除的给药剂量分别仅为17.4%和4.9%。
