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Table 2 Geometric means (68% inter-percentile range) of the main pharmacokinetic variables for roflumilast and roflumilast N-oxide at steady state

From: No relevant cardiac, pharmacokinetic or safety interactions between roflumilast and inhaled formoterol in healthy subjects: an open-label, randomised, actively controlled study

 

Regimen A

Regimen B

 

Day 11 (roflumilast alone)

(n = 12)

Day 18 (roflumilast plus formoterol)

(n = 12)

Day 18 (formoterol plus roflumilast)

(n = 12)

Roflumilast

   

C trough (μg/L)

0.53 (0.33-0.85)

0.50 (0.29-0.86)

0.37 (0.18-0.77)

Cmax (μg/L)

6.89 (4.94-9.62)

6.43 (4.79-8.63)

5.92 (4.27-8.22)

AUCτ (μg.h/L)

35.8 (27.8-46.1)

36.9 (28.1-48.4)

31.8 (21.2-47.7)

CL/F (L/h)

13.9 (10.8-17.9)

13.5 (10.3-17.7)

15.7 (10.4-23.5)

Roflumilast N-oxide

   

C trough (μg/L)

12.43 (8.24-18.76)

12.72 (8.18-19.79)

10.66 (6.29-18.06)

AUCτ (μg.h/L)

417 (299-582)

414 (293-584)

369 (254-537)

Cmax (μg/L)

23.3 (17.3-31.3)

23.7 (17.2-32.6)

22.04 (15.9-30.5)

  1. AUCÏ„, area under the plasma concentration versus time curve; Cmax, maximum plasma concentration; Ctrough, trough plasma concentration; CL/F, apparent clearance at steady state.