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[Pharmacokinetics of epristeride in rats and beagle dogs]
Aim:
To study the pharmacokinetics of epristeride (EPR) in rats and Beagle dogs.
Methods:
The concentrations of EPR in biological samples were determined by an HPLC method with UV detection.
Results:
The concentration-time curves in rat serum showed two peak concentrations after i.g. doses of 10, 20 and 40 mg.kg-1. The Tpeak1 and Tpeak2 were attained within 0.5-1 h and 3-4 h, respectively. The elimination half-life(T1/2 beta) was 2.43-3.14 h. The Tpeak and T1/2 beta in Beagle dogs were 1 h and 5 h, respectively. EPR was shown to be widely distributed to various tissues after i.g. dose of 20 mg.kg-1. The concentrations in most tissues at 3 h were higher than those of 6 h. The excretion of parent drug in urine amounted to only 0.09% of the dosage and in feces to 42.9% within 24 h after dosing. The biliary excretion were mainly metabolites and only 0.14% of parent drug of the dosage within 12 h. Plasma protein binding ratio of EPR was 92.3% at the concentration range of 50-3,000 ng.mL-1.
Conclusion:
The absorption of EPR was shown to be of first order processes at doses of 10-40 mg.kg-1, both the Cmax and AUC increased proportionally with the dosages. EPR was shown to be widely distributed to the various tissues and mainly eliminated via the feces and bile.