Table 3.
Summary of Pharmacokinetic Parameters for Single Ascending Dose (SAD) of Benfotiamine
| Analytes | Parameters | SAD | ||||
|---|---|---|---|---|---|---|
| 150 mg (n=10) | 300 mg (n=10) | 600 mg (n=10) | 900 mg (n=10) | 1200 mg (n=10) | ||
| TM | AUC0-t, ng·h/mL | 1983.4 (503.0) | 4823.6 (1400.6) | 14,399.1 (2395.1) | 25,841.3 (4177.2) | 39,155.3 (8194.7) |
| Cmax, ng/mL | 344 (83) | 674 (123) | 1601 (253) | 2607 (383) | 3730 (742) | |
| Tmax, h | 1.0 (0.5–2.5) | 1.3 (0.5–2.0) | 1.5 (0.5–2.0) | 1.5 (1.0–3.5) | 2.0 (1.0–3.0) | |
| t1/2, h | 13.9 (5.3) | 10.0 (2.3) | 6.6 (0.7) | 6.3 (0.4) | 6.3 (0.7) | |
| CL/F, L/h | 78.0 (19.0) | 67.4 (23.7) | 42.4 (6.4) | 35.4 (5.5) | 31.5 (5.9) | |
| Vd/F, L | 1489 (525) | 1039 (673) | 403 (80) | 324 (58) | 285 (38) | |
| TMP | AUC0-t, ng·h/mL | 164.6 (30.0) | 214.4 (43.9) | 271.5 (60.2) | 311.1 (77.4) | 380.0 (84.7) |
| Cmax, ng/mL | 7.99 (1.18) | 8.51 (1.84) | 9.24 (2.08) | 12.0 (2.65) | 12.6 (2.19) | |
| Tmax, h | 3.5 (2.0–8.0) | 5.0 (2.5–12.0) | 3.8 (2.5–12.0) | 5.0 (2.0–12.0) | 8.0 (2.5–12.0) | |
| t1/2, h | 35.3 (17.4) | 31.8 (12.2) | 36.0 (12.7) | 74.8 (157.0) | 44.9 (19.4) | |
| CL/F, L/h | 609.7 (146.9) | 974.4 (243.2) | 1453.6 (283.8) | 2200.2 (1294.2) | 1856.3 (506.2) | |
| Vd/F, L | 28,800 (9616) | 42,721 (14,554) | 73,258 (21,145) | 88,366 (35,343) | 110,122 (30,060) | |
| TDP | AUC0-t, ng·h/mL | 2002.9 (575.9) | 2785.2 (988.4) | 3130.5 (978.0) | 3804.3 (626.6) | 4601.3 (1135.2) |
| Cmax, ng/mL | 79.7 (19.5) | 99.3 (48.1) | 89.1 (31.8) | 101 (19.0) | 120 (30) | |
| Tmax, h | 8.0 (6.0–12.0) | 8.0 (4.0–24.0) | 24.0 (12.0–24.0) | 24.0 (8.0–24.0) | 24.0 (12.0–36.0) | |
| t1/2, h | 46.4 (45.8) | 18.6 (4.2) | 24.5 (6.3) | 42.5 (26.2) | 48.2 (23.1) | |
| CL/F, L/h | 47.6 (19.3) | 94.4 (27.0) | 141.9 (39.8) | 135.0 (51.4) | 127.9 (48.3) | |
| Vd/F, L | 2342 (1138) | 2535 (921) | 5111 (2200) | 6887 (1604) | 7891 (2060) | |