TABLE 1

Single-dose pharmacokinetic parameters of bosentan in rats


Oral

AUC0-inf

Cmax

Tmax

F
ng · h/ml ng/ml h %
Bosentan alone 3228 ± 693 744 ± 168 1.7 ± 0.5 42 ± 8
+ cyclosporin A 53,500 ± 12,100** 3310 ± 523*** 4.3 ± 0.8 69 ± 15
+ verapamil
4,453 ± 292
541 ± 63
2.5 ± 0.3
36 ± 2
Intravenous
AUC0-inf.
CL
Vss
T1/2
ng · h/ml ml/min · kg l/kg h
Bosentan alone 765 ± 93 23 ± 3 2.5 ± 0.5 1.9 ± 0.1
+ cyclosporin A 7762 ± 1093*** 2.2 ± 0.3** 1.1 ± 0.2 7.2 ± 0.4***
+ verapamil
1275 ± 62
13 ± 1
1.4 ± 0.3
1.7 ± 0.1
  • **P < 0.01; ***P < 0.001.