TABLE 1

Experimental groups for evaluating talinolol pharmacokinetics in rats

No. AnimalsTalinololP-Glycoprotein Inhibitor
DoseAdministration ModeFormulationaCompoundDoseAdministration Mode
mg/kgmg/kg
64i.v.A
62i.v.AVerapamil5p.o.
42i.v.ACyclosporine100p.o.
640p.o.B
540p.o.BVerapamil5p.o.
640p.o.BCyclosporine100p.o.
540Cecum infusion over 4 hB
540Cecum infusion over 4 hBCyclosporine100Cecum bolus
64p.o.C
54p.o.CVerapamil5p.o.
94p.o.CCyclosporine100p.o.
  • a Formulations of talinolol: A, 2 mg/ml solution in 40% sodium phosphate buffer 0.2 M, pH 7, 40% propylene glycol and 20% ethanol; B, 8 mg/ml solution in 25% polyethylene glycol 400, 15% ethanol, and 60% water; and C, 1 mg/ml solution in 25% polyethylene glycol 400, 15% ethanol, and 60% water.