Pharmacokinetics of dihydroergosine in rats after intravenous and oral administration

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Abstract
Wistar rats received an intravenous dose of 20 μg/kg and an oral dose of 40 μg/kg3H-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 administration3H-Dihydroergosine is rapidly lost from the central compartment with distribution rate constants α=0.889 h−1 and β=0.722 h−1, respectively. Biological half life in the elimination phase after both application is nearly the same t1/2=13.6 h. The volume of central compartment is Vc=3.075 1/kg and the volume of distribution Vdβ=30.75 1/kg. The fraction of3H-Dihydroergosine absorbed after oral administration, calculated from areas under the curves upon oral and intravenous administration, is 31%. The percentage of3H-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 administered3H-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.