Table 1.
Mean (±SD) pharmacokinetic parameters of diclofenac in plasma (total concentrations) and microdialysates from skeletal muscle (MD i.m.) and subcutaneous adipose tissue (MD s.c.) (free, non-protein bound concentrations)
| DCF100C1 (1%) | DCF100C2 (1%) | DCF100C1 (2.5%) | DCF100C2 (2.5%) | Voltaren® Emulgel® | |
|---|---|---|---|---|---|
| Plasma | |||||
| AUC(0,10 h) (pg ml−1 h) | 23 771.6 ± 11 308.1 | 19 733.7 ± 8 202.7 | 42 103.6 ± 19 474.4 | 35 704.7 ± 15 872.0 | 7306.2 ± 4790.7 |
| Cmax (pg ml−1) | 4 210.2 ± 2 110.6 | 3484.7 ± 1 612.8 | 8 222.6 ± 4 750.7 | 6 578.5 ± 3 877.9 | 1102.9 ± 852.9 |
| tmax (h) | 5.67 ± 2.19 | 6.42 ± 1.93 | 4.50 ± 2.32 | 4.50 ± 2.15 | 1.25 ± 1.96 |
| MD i.m. | |||||
| AUC(0,10 h) (pg ml−1 h) | 1 089.2 ± 1 443.6 | 2 089.5 ± 1 045.1 | 1 477.7 ± 1 732.4 | 12 031.0 ± 34 572.3 | 2004.5 ± 3257.4 |
| Cmax (pg ml−1) | 368.5 ± 449.9 | 1 071.2 ± 832.7 | 746.2 ± 673.3 | 6 277.4 ± 18 339.8 | 448.2 ± 435.3 |
| tmax (h) | 4.13 ± 2.90* | 4.92 ± 3.58 | 4.36 ± 3.17† | 4.64 ± 3.80† | 4.00 ± 3.43‡ |
| MD s.c. | |||||
| AUC(0,10 h) (pg ml−1 h) | 1 408.6 ± 1 234.8 | 2 429.8 ± 2 507.2 | 1 957.6 ± 2 138.8 | 3 709.4 ± 3 794.0 | 2925.5 ± 3501.2 |
| Cmax (pg ml−1) | 545.3 ± 366.7 | 1065.9 ± 1261.4 | 811.1 ± 970.0 | 1235.2 ± 1456.6 | 611.4 ± 498.9 |
| tmax (h) | 3.10 ± 2.77‡ | 5.64 ± 3.72† | 2.55 ± 1.63† | 2.00 ± 1.61† | 3.55 ± 3.64† |
*
n = 8
†
n = 11
‡
n = 10. n = 12; unless otherwise specified. DCF100C1 (1%) and DCF100C1 (2.5%) contained menthol and eucalyptus oil as sensory signals.