Table 1.
Pharmacokinetic parameters of rosiglitazone and N-desmethylrosiglitazone after a single dose of 4 mg rosiglitazone in 10 healthy volunteers, following 6 days pretreatment with placebo or 10 mg montelukast once daily
| Placebo phase | Montelukast phase | Ratio (90% CI) | P value | |
|---|---|---|---|---|
| Rosiglitazone | ||||
| Cmax (ng ml−1) | 271.6 ± 57.4 | 264.2 ± 55.3 | 0.98 (0.92, 1.03) | 0.37 |
| tmax (h) | 1.2 ± 0.6 | 1.2 ± 0.7 | 1.24 (0.70, 1.78) | 1.00 |
| t1/2 (h) | 5.7 ± 3.3 | 5.5 ± 2.2 | 1.03 (0.89, 1.16) | 0.62 |
| AUC(0,24) (ng ml−1 h) | 1830.1 ± 454.0 | 1864.1 ± 452.2 | 1.02 (0.98, 1.07) | 0.42 |
| AUC(0, ∞) (ng ml−1 h) | 2004.4 ± 639.9 | 2027.4 ± 602.5 | 1.02 (0.97, 1.07) | 0.59 |
| CL/F (l h−1) | 4.5 ± 2.0 | 4.4 ± 1.6 | 1.00 (0.94, 1.05) | 0.50 |
| N-desmethylrosiglitazone | ||||
| Cmax (arbitrary U ml−1) | 53.7 ± 16.0 | 56.1 ± 16.0 | 1.05 (0.98, 1.13) | 0.25 |
| tmax (h) | 8.1 ± 3.0 | 6.5 ± 1.7 | 0.88 (0.73, 1.02) | 0.12 |
| t1/2 (h) | 27.3 ± 14.8 | 28.0 ± 18.8 | 1.00 (0.86, 1.15) | 0.73 |
| AUC(0,24) (arbitrary U ml−1 h) | 959.7 ± 357.7 | 931.5 ± 309.8 | 0.99 (0.94, 1.03) | 0.23 |
| AUC(0, ∞) (arbitrary U ml−1 h) | 2002.3 ± 1188.0 | 1971.1 ± 1163.3 | 0.98 (0.92, 1.04) | 0.50 |
| AUC ratio of N-desmethylrosiglitazone : rosiglitazone | 0.54 ± 0.20 | 0.52 ± 0.18 | 0.97 (0.90, 1.03) | 0.14 |
Cmax, peak plasma concentration; tmax, time to peak plasma concentration; AUC(0,24), area under the plasma concentration–time curve, from 0 to 24 hours; AUC(0, ∞), area under the plasma concentration–time curve from time 0 to infinity; CL/F, oral clearance. Data are expressed as mean ± SD.