TABLE 1

Pharmacokinetic parameters in humans for fluticasone furoate, GW694301X, and 14C radioactivity in plasma

Mean pharmacokinetic parameters of fluticasone furoate, a carboxylic acid metabolite GW694301X, and 14C radioactivity in plasma of healthy male subjects following a single p.o. (2 mg) or a single i.v. (0.25 mg) administration of [14C]fluticasone furoate are shown. Mean ± S.D., n = 5.


Treatment

Parameter

Fluticasone Furoate

GW694301X

Radioactivitya
2 mg p.o. AUC(0-t) (pg · h/ml) 511 ± 358 102 ± 61 26,400 ± 14,400
AUC(0-∞) (pg · h/ml) 1080b 120 ± 59 39,300 ± 11,700c
Cmax (pg/ml) 213 ± 177 71 ± 42 1380 ± 239
Tmax (h)d 0.50 0.75 0.75
t½ (h) 4.05b 1.04 ± 0.39 20.8 ± 5.30c
0.25 mg i.v. AUC(0-t) (pg · h/ml) 4000 ± 846 N.D. 11,300 ± 5150
AUC(0-∞) (pg · h/ml) 4410 ± 834 N.D. 21,400 ± 15,200e
Cmax (pg/ml) 2980 ± 1140 N.D. 5060 ± 1330
Tmax (h)d 0.50 N.D. 0.50
t½ (h) 15.3 ± 2.74 N.D. 35.6 ± 33.3e
Cl (l/h) 58.3 ± 10.9 N.D. N.A.

Vss (liter)
642 ± 215
N.D.
N.A.
  • N.D., not determined, all the concentrations below lower limit of quantification (10 pg/ml); N.A., not applicable.

  • a Radioactivity concentrations are expressed in terms of picogram equivalents of fluticasone furoate.

  • b n = 2, because of inadequate definition of the terminal elimination phase these pharmacokinetic parameters could not be defined in all the subjects.

  • c n = 3, because of inadequate definition of the terminal elimination phase these pharmacokinetic parameters could not be defined in all the subjects.

  • d Tmax quoted as median.

  • e n = 4, because of inadequate definition of the terminal elimination phase these pharmacokinetic parameters could not be defined in all the subjects.