Tables 4a and 4b.
Pharmacokinetic parameters derived from repeated dose inhalations (1000 µg twice daily) of budesonide via Turbuhaler and of fluticasone via pMDI and Diskus.
| a) | ||||||||
|---|---|---|---|---|---|---|---|---|
| Regimen | Subjects | n | AUC (nmol l−1 h) | MAT (h) | Cmax (nmol) | ΔC(%) | tmax (min) | Racc [ratio] |
| Budesonide | Healthy | 13 | 10.5 (8.5; 13.2) | 0.6 (0.3; 0.9) | 3.8 (3.1; 4.6) | 414 (342; 500) | 17 (10; 24) | 1.09 (1.07; 1.10) |
| Turbuhaler | With asthma | 8 | 12.9 (11.4; 14.5) | 1.0 (0.7; 1.3) | 4.3 (3.1; 5.9) | 379 (288; 499) | 15 (6; 24) | 1.14 (1.09; 1.20) |
| Total | 21 | 11.4 (9.9; 13.1) | 0.8 (0.6; 1.0) | 4.0 (3.4; 4.6) | 400 (346; 462) | 16 (11; 21) | 1.11 (1.09; 1.13) | |
| Fluticasone pMDI | Healthy | 13 | 5.5 (4.5; 6.9) | 7.1 (5.6; 8.5) | 0.7 (0.6; 0.9) | 104 (94; 14) | 113 (84; 143) | 1.63 (1.55; 1.70) |
| Fluticasone Diskus | Healthy | 13 | 3.5 (2.9; 4.3) | 5.3 (4.0; 6.6) | 0.5 (0.4; 0.6) | 112 (102; 124) | 100 (66; 135) | 1.66 (1.54; 1.78) |
| With asthma | 8 | 3.0 (2.2; 4.1) | 6.9 (4.5; 9.3) | 0.4 (0.3; 0.5) | 108 (86; 136) | 79 (14; 144) | 1.63 (1.48; 1.80) | |
| Total | 21 | 3.3 (2.9; 3.9) | 5.9 (4.8; 7.0) | 0.4 (0.4; 0.5) | 111 (101; 122) | 92 (63; 122) | 1.65 (1.56; 1.74) | |
| b) | ||||||||
| Regimen | Subjects | n | Dose-to-subject (%) (µg)* | Fnominal (%) | Flung, nominal (%) | Flung, DTS (%) | ||
| Budesonide | Healthy | 13 | 572 (77) | 36 (29; 46) | 32 (24; 43) | 59 (41; 82) | ||
| Turbuhaler | With asthma | 8 | 587 (64) | 45 (36; 55) | 42 (32; 53) | 82 (66; 102) | ||
| Total | 21 | 578 (72) | 39 (34; 46) | 36 (29; 43) | 68 (55; 83) | |||
| Fluticasone pMDI | Healthy | 13 | 668 (95) | 21 (17; 25) | 20 (16; 25) | 31 (25; 37) | ||
| Fluticasone Diskus | Healthy | 13 | 755 (102) | 13 (11; 16) | 12 (10; 15) | 17 (14; 21) | ||
| With asthma | 8 | 768 (109) | 13 (10; 17) | 12 (9; 16) | 19 (14; 26) | |||
| Total | 21 | 760 (105) | 13 (11; 15) | 12 (10; 14) | 18 (15; 21) | |||
Values are given as geometric means (95% CI).
*
Arithmetic mean (s.d.).
AUC=area under the curve of plasma concentration vs time; MAT=mean absorption time; Cmax=maximum concentration
C=plasma variability; tmax=time for Cmax; Racc=accumulation index; F=systemic availability; DTS=dose-to-subject.