Table 1:
Pharmacokinetics of raloxifene and raloxifene-6-glucuronide in the absence and presence of orally administered test articles (n=5 per time point)
| Vehicle | Green tea extract | EGCG | |
|---|---|---|---|
| Raloxifene | |||
| Cmax (nM) | 140 (22) | 79 (20)** | 168 (30) |
| AUC0-4h (nM•h) | 341 (16) | 200 (19) | 322 (80) |
| AUCR0-4h | NA | 0.59 (0.46 – 0.74) | 0.94 (0.44 – 2.01) |
| AUC0-24h (nM•h) | 867 (31) | 669 (14) | 867 (18) |
| AUCR | NA | 0.77 (0.6 – 1) | 1.01 (0.65 – 1.55) |
| tmax (h) | 2 (0.25 - 4) | 4 (1 - 6) | 0.5 (0.25 - 2) |
| Raloxifene-6-glucuronide | |||
| Cmax (nM) | 700 (44) | 288 (33)** | 820 (35) |
| AUC0-4h (nM•h) | 935 (33) | 624 (31) | 1200 (53) |
| AUCR0-4h | NA | 0.67 (0.40 – 1.12) | 1.29 (0.8 – 2.07) |
| AUC0-24h (nM•h) | 1930 (24) | 1560 (32) | 2150 (52) |
| AUCR0-24h | NA | 0.81 (0.50 - 1.30) | 1.11 (0.65 – 1.91) |
| tmax (h) | 0.25 (0.25 - 0.5) | 0.25 (0.25 - 0.5) | 0.5 (0.25 - 4) |
| Metabolite-to-parent | 2.74 (30) | 3.12 (34) | 3.74 (25) |
| AUC0-4h ratio | |||
| Metabolite-to-parent | 2.23 (36) | 2.33 (24) | 2.48 (38) |
| AUC0-24h ratio | |||
Values are geometric mean (CV%). AUCR values are geometric means (90% confidence interval), and tmax are median (range). CV, coefficient of variation; Cmax, maximum plasma concentration; AUC0-4h, area under the plasma concentration-time curve from 0 to 4 h; AUC0-12h, AUC from 0 to 12 h; tmax, time to Cmax; NA, not applicable. ** p < 0.01 compared to vehicle by 1-way ANOVA with Dunnett’s post-test.