Table 2.
Reported nutraceutical RSV pharmacokinetics parameters in humans
| 99% pure nutraceutical RSV | ||||||||
|---|---|---|---|---|---|---|---|---|
| Single dosing | ||||||||
| Dose | Cmax of total or [parent] RSV | Cmax of dominant conj. | tmaxof total or parent | Half-life of total, parent or [dominant conj.] | AUC of total, parent or [dominant conj.] (ng ml−1 h) | Tissue uptake of parent, or [dominant conj.] | CV for Cmax and AUC | Reference |
| 25 mg labelled RSV/70 kg BW | 2 µm[<0.02 µm] | 0.9–14 µm (C2, C3) | 60 min; 2nd peak at 360 min | 7.2 to 11.8 h | 6240 | [41] | ||
| 500 to 5000 mg | [0.3 to 2.4 µm] | 5 to 18.8 µm (C1) | 50 to 90 min | 2.8 to 8.9 h [3.2 to 11.5 h] | 224 to 1319 [4049 to 30 898] | Up to 80% | [44] | |
| 400 mg Fed | 0.18 µm | Not measured | 2 h | – | – | 128% | [39] | |
| 400 mg Fasting | 0.2 µm | 30 min | ||||||
| 85.5 mg piceid form equivalent to 50 mg RSV | n.d. | 0.94 µm (C3) | 360 to 480 min | – | – | [26] | ||
| 250 mg | [0.024 µm] | 1.3 µm | 90 min | Not reported | Not reported | [84] | ||
| 500 mg | [0.062 µm] | 3.1 µm (sulphates, unspecified) | ||||||
| Multiple dosing | ||||||||
| 25 mg | Dose ratio: 50 mg:25 mg = 6 | Not measured | 50 to 90 min | 1–3 h at dose | AUC ratio:150 mg/25 mg = 39 | [43] | ||
| 50 mg | 1 | |||||||
| 100 mg | Cmaxratio: 150 mg:25 mg = 25 | 2–5 h at dose | ||||||
| 150 mg | 13 | |||||||
| 13 doses over 48 h | ||||||||
| 200 mg × 3/day for 3 days | 0.15 µm | Not measured | 1 to 1.5 h | 2.9 to 4.7 h | 77 to 116 | 40% | [99] | |
| 2000 mg ×2/day | [33] | |||||||
| D7 SDBF | 5.6 µm | Not measured | 3 h | 2.4 h | 3558 | |||
| D8 HFBF | 3 µm | 5 h | 2.4 h | 1966 | ||||
| D15 SDQ | 5.6 µm | 4 h | 2.2 h | 4025 | ||||
| D16 SDQetoh | 5.7 µm | 3 h | 2.1 h | 3800 | ||||
| 500 mg – 8 days | ND | 13.4 µm (C6) | Not reported | Not reported | Not reported | 18.6 [86 C4] nmol g−1 | 200% | [45] |
| 1000 mg – 8 days | ND | 22.3 µm (C6) | 674 [67.2 C1] nmol g−1 | 200% | ||||
| 500 mg 29 days | [0.19 to 4.24 µm] | 2.5 to 18.3 µm (C1) | 60 to 70 min (0.25 to 5 h inter-subject variability) | 4.8 to 9.7 h [3.09 to 8.14 h] non dose-dependent | 175 to 4097 [3558 to 38 900] non dose-dependent | 35 to 107% | [31] | |
| 1000 mg 29 days | ||||||||
| 2500 mg 29 days | ||||||||
| 5000 mg 29 days | ||||||||
| 1000 mg 28 days | [0.3 µm] | 10.4 µm (C1) | Not reported | Not reported | Not reported | 400% | [34] | |
ND not detected; BW body weight; Cmax, maximal concentration; tmax, time of maximal concentration; AUC, area under the concentration vs. time curve; Total RSV, parent and conjugated RSV; CV, coefficient of variability; Conj. conjugates; C1, resverarol-3-O-sulphate; C2, resveratrol- 4′-O-sulphate; C3, resveratrol disulfate, C4; resveratrol 3-O-glucuronide; C5, resveratrol 4′-O- glucuronide; C6, resveratrol sulphate glucuronide; SDBF, standard breakfast; HFBF, high fat breakfast; SDQ, standard breakfast and quercetin; SDQetoh, standard breakfast and quercetin and ethanol.