Pharmacokinetics of resveratrol and three metabolites in the plasma of volunteers after a single oral dose
| Variable . | Dose level (g) . | . | . | . | ||||
|---|---|---|---|---|---|---|---|---|
| . | 0.5 . | 1.0 . | 2.5 . | 5.0 . | ||||
| Resveratrol | ||||||||
| AUCinf (ng h/mL) | 223.7* | 544.8 (57.2) | 786.5 (36.2) | 1,319 (59.1) | ||||
| Cmax (ng/mL) | 72.6 (48.9) | 117.0 (73.1) | 268.0 (55.3) | 538.8 (72.5) | ||||
| Tmax (h) | 0.833 (0.5-1.5) | 0.759 (0.5-4.0) | 1.375 (0.5-4.0) | 1.500 (0.67-5.0) | ||||
| Cav (ng/mL) | 8.36 (57.8) | 18.04 (51.6) | 32.25 (43.0) | 51.90 (80.7) | ||||
| Half-life (h) | 2.85* | 8.87 (91.1) | 4.22 (51.6) | 8.52 (95.8) | ||||
| CL/F (L/h) | 2,235* | 2,593 (65.1) | 3,471 (29.9) | 4,930 (50.0) | ||||
| CLR (L/h) | 1.177 (102.5) | 0.696 (71.5) | 0.656 (53.1) | 1.443 (139.2) | ||||
| V/F (liters) | 9,198* | 19,298 (54.3) | 22,226 (67.3) | 66,991 (112) | ||||
| Glucuronide 1 | ||||||||
| AUCinf (ng h/mL) | 1,919 (33.6) | 3,059 (60.9) | 5,664 (27.7) | 9,923 (40.9) | ||||
| Cmax (ng/mL) | 404.6 (35.3) | 473.6 (76.8) | 874.4 (37.5) | 1,285 (55.4) | ||||
| Tmax (h) | 2.00 (1.0-6.0) | 2.250 (1.0-6.0) | 2.375 (1.0-8.0) | 2.00 (1.5-5.0) | ||||
| Cav (ng/mL) | 76.9 (37.2) | 110.3 (56.1) | 215.5 (43.5) | 344.1 (51.5) | ||||
| Half-life (h) | 2.85 (48.6) | 7.27 (93.9) | 10.6 (92.9) | 7.90 (39.1) | ||||
| CL/F (L/h) | 282.7 (27.3) | 493.5 (74.7) | 469.5 (25.7) | 590.6 (45.2) | ||||
| Glucuronide 2 | ||||||||
| AUCinf (ng h/mL) | 1,287 (21.7) | 2,589 (66.4) | 4,320 (32.9) | 8,546 (62.3) | ||||
| Cmax (ng/mL) | 369.5 (39.6) | 672.6 (81.1) | 1,626 (71.5) | 1,735 (66.4) | ||||
| Tmax (h) | 1.500 (1.0-5.0) | 1.750 (1.0-5.1) | 2.000 (1.0-6.0) | 2.520 (1.5-8.0) | ||||
| Cav (ng/mL) | 51.0 (27.6) | 99.9 (66.2) | 193.8 (39.3) | 317.8 (65.6) | ||||
| Half-life (h) | 3.09 (69.8) | 6.64 (92.1) | 8.42 (88.9) | 5.83 (51.2) | ||||
| CL/F (L/h) | 408.8 (26.7) | 642.5 (83.0) | 636.9 (32.6) | 1,017 (94.6) | ||||
| 3-Sulfate | ||||||||
| AUCinf (ng h/mL) | 4,049 (26.6) | 10,053 (73.2) | 16,984 (41.7) | 30,898 (46.1) | ||||
| Cmax (ng/mL) | 1,135 (25.7) | 2,102 (81.3) | 2,786 (27.2) | 4,294 (48.0) | ||||
| Tmax (h) | 1.500 (1.0-5.0) | 2.000 (1.0-5.0) | 2.000 (1.0-5.2) | 2.050 (1.0-6.0) | ||||
| Cav (ng/mL) | 172.0 (23.2) | 402.6 (70.5) | 597.0 (27.0) | 1,089 (49.4) | ||||
| Half-life (h) | 3.21 (56.6) | 4.51 (82.8) | 11.5 (95.5) | 7.71 (42.3) | ||||
| CL/F (L/h) | 131.2 (25.8) | 151.8 (62.7) | 171.2 (40.0) | 207.8 (63.9) | ||||
| Variable . | Dose level (g) . | . | . | . | ||||
|---|---|---|---|---|---|---|---|---|
| . | 0.5 . | 1.0 . | 2.5 . | 5.0 . | ||||
| Resveratrol | ||||||||
| AUCinf (ng h/mL) | 223.7* | 544.8 (57.2) | 786.5 (36.2) | 1,319 (59.1) | ||||
| Cmax (ng/mL) | 72.6 (48.9) | 117.0 (73.1) | 268.0 (55.3) | 538.8 (72.5) | ||||
| Tmax (h) | 0.833 (0.5-1.5) | 0.759 (0.5-4.0) | 1.375 (0.5-4.0) | 1.500 (0.67-5.0) | ||||
| Cav (ng/mL) | 8.36 (57.8) | 18.04 (51.6) | 32.25 (43.0) | 51.90 (80.7) | ||||
| Half-life (h) | 2.85* | 8.87 (91.1) | 4.22 (51.6) | 8.52 (95.8) | ||||
| CL/F (L/h) | 2,235* | 2,593 (65.1) | 3,471 (29.9) | 4,930 (50.0) | ||||
| CLR (L/h) | 1.177 (102.5) | 0.696 (71.5) | 0.656 (53.1) | 1.443 (139.2) | ||||
| V/F (liters) | 9,198* | 19,298 (54.3) | 22,226 (67.3) | 66,991 (112) | ||||
| Glucuronide 1 | ||||||||
| AUCinf (ng h/mL) | 1,919 (33.6) | 3,059 (60.9) | 5,664 (27.7) | 9,923 (40.9) | ||||
| Cmax (ng/mL) | 404.6 (35.3) | 473.6 (76.8) | 874.4 (37.5) | 1,285 (55.4) | ||||
| Tmax (h) | 2.00 (1.0-6.0) | 2.250 (1.0-6.0) | 2.375 (1.0-8.0) | 2.00 (1.5-5.0) | ||||
| Cav (ng/mL) | 76.9 (37.2) | 110.3 (56.1) | 215.5 (43.5) | 344.1 (51.5) | ||||
| Half-life (h) | 2.85 (48.6) | 7.27 (93.9) | 10.6 (92.9) | 7.90 (39.1) | ||||
| CL/F (L/h) | 282.7 (27.3) | 493.5 (74.7) | 469.5 (25.7) | 590.6 (45.2) | ||||
| Glucuronide 2 | ||||||||
| AUCinf (ng h/mL) | 1,287 (21.7) | 2,589 (66.4) | 4,320 (32.9) | 8,546 (62.3) | ||||
| Cmax (ng/mL) | 369.5 (39.6) | 672.6 (81.1) | 1,626 (71.5) | 1,735 (66.4) | ||||
| Tmax (h) | 1.500 (1.0-5.0) | 1.750 (1.0-5.1) | 2.000 (1.0-6.0) | 2.520 (1.5-8.0) | ||||
| Cav (ng/mL) | 51.0 (27.6) | 99.9 (66.2) | 193.8 (39.3) | 317.8 (65.6) | ||||
| Half-life (h) | 3.09 (69.8) | 6.64 (92.1) | 8.42 (88.9) | 5.83 (51.2) | ||||
| CL/F (L/h) | 408.8 (26.7) | 642.5 (83.0) | 636.9 (32.6) | 1,017 (94.6) | ||||
| 3-Sulfate | ||||||||
| AUCinf (ng h/mL) | 4,049 (26.6) | 10,053 (73.2) | 16,984 (41.7) | 30,898 (46.1) | ||||
| Cmax (ng/mL) | 1,135 (25.7) | 2,102 (81.3) | 2,786 (27.2) | 4,294 (48.0) | ||||
| Tmax (h) | 1.500 (1.0-5.0) | 2.000 (1.0-5.0) | 2.000 (1.0-5.2) | 2.050 (1.0-6.0) | ||||
| Cav (ng/mL) | 172.0 (23.2) | 402.6 (70.5) | 597.0 (27.0) | 1,089 (49.4) | ||||
| Half-life (h) | 3.21 (56.6) | 4.51 (82.8) | 11.5 (95.5) | 7.71 (42.3) | ||||
| CL/F (L/h) | 131.2 (25.8) | 151.8 (62.7) | 171.2 (40.0) | 207.8 (63.9) | ||||
NOTE: Values are the mean of n = 10 with coefficient of variation (in percent) or range in brackets.
Abbreviations: AUCinf, area under the concentration versus time curve to time infinity; Cmax, maximal plasma concentration; Tmax, median time of maximal plasma concentration; Cav, average plasma concentration; CL/F, apparent total body clearance (calculated as dose/AUCinf); CLR, apparent renal clearance approximated by amount excreted with urine within 24 h over AUC0-24; V/F, apparent volume of distribution.
n = 1, value for AUCinf at the lowest dose could be established in only one participant.