TABLE 11.
Pharmacokinetic parameters of bentysrepinine, M8 and M9 in a multiple doses study (Study 02).
| Analyte | Dose (mg) | Day | Cmax (ng/ml) | Cmin (ng/ml) | Tmax (h) | t1/2 (h) | AUC0-t (ng·h/ml) | CL/F (l/h) | V/F (L) | R1 | R2 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Bentysrepinine | 300 | 1 | 521.2 (162.7) | — | 0.88 (0.50–5.00) | 1.6 (0.4) | 1,314.6 (209.5) | 229.4 (34.0) | 535.3 (185.7) | — | — |
| 300 | 9 | 607.3 (120.8) | 5.0 (1.5) | 1.00 (0.50–2.00) | 3.6 (5.9) | 1,436.3 (211.2) | 212.0 (31.1) | 535.3 (185.7) | 1.10 (0.20) | 1.10 (0.20) | |
| 600 | 1 | 1,368.7 (431.4) | — | 1.50 (0.50–2.50) | 3.7 (2.4) | 3,507.8 (765.5) | 175.5 (32.2) | 883.5 (577.3) | — | — | |
| 600 | 9 | 1769.4 (636.1) | 5.9 (2.4) | 1.25 (0.50–2.50) | 2.8 (1.4) | 3,793.4 (1,218.5) | 169.6 (45.2) | 722.2 (494.7) | 1.33 (0.37) | 1.09 (0.26) | |
| M8 | 300 | 1 | 1,687.5 (364.2) | — | 4.00 (2.00–6.00) | 6.2 (3.9) | 11,515.0 (2,156.9) | 26.6 (4.7) | 239.9 (166.4) | — | — |
| 300 | 9 | 1866.1 (259.1) | 33.9 (11.4) | 3.00 (2.50–6.00) | 10.3 (4.4) | 12,762.0 (2,336.0) | 25.2 (4.4) | 379.0 (194.8) | 1.13 (0.19) | 1.10 (0.14) | |
| 600 | 1 | 3,290.8 (776.2) | — | 3.50 (2.50–4.00) | 8.2 (2.5) | 23,158.8 (4,050.4) | 26.4 (4.4) | 312.0 (110.9) | — | — | |
| 600 | 9 | 3,763.3 (938.8) | 85.6 (23.6) | 3.00 (2.00–4.00) | 8.6 (4.8) | 25,475.0 (5,021.0) | 25.5 (5.1) | 308.3 (149.3) | 1.15 (0.17) | 1.10 (0.10) | |
| M9 | 300 | 1 | 186.9 (47.6) | — | 5.50 (4.00–6.00) | 4.3 (1.2) | 1,639.5 (345.3) | 192.2 (57.5) | 1,161.4 (368.1) | — | — |
| 300 | 9 | 230.6 (60.4) | 4.9 (1.6) | 4.00 (4.00–6.00) | 7.1 (4.8) | 1908.3 (417.0) | 172.3 (47.5) | 1826.4 (1,368.1) | 1.25 (0.21) | 1.15 (0.12) | |
| 600 | 1 | 485.6 (215.6) | — | 4.00 (4.00–6.00) | 5.9 (1.9) | 3,919.6 (1,282.2) | 169.6 (60.3) | 1,430.3 (626.5) | — | — | |
| 600 | 9 | 595.3 (290.2) | 14.0 (3.9) | 4.00 (3.00–5.00) | 6.2 (2.3) | 4,745.6 (1894.3) | 148.4 (52.5) | 1,329.4 (546.4) | 1.24 (0.22) | 1.22 (0.21) |
The data are expressed as mean (SD). R1 = Cmax ss/Cmax; R2 = AUC 0-τ ss/AUC 0-τ.