Table 2.
Pharmacokinetic parameters of PEITC
| Route of admin istrati on |
Dose | Vehicl e |
Mo del |
Nu mb er of sa mp les (n) |
Org an |
AUC ±SD or (SE) |
Cmax ±SD or (SE) |
Tmax ±SD or (SE) |
T1/2a±S D or (SE) |
T1/2e ±SD or (SE) |
Vd ±SD or (SE) |
F %± SD or (SE) |
R ef |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Oral | 10μmol (50μmol/kg) (single) | Corn Oil | Male F344 rats | 3/time point | Blood | 328.1 nmol ml−1 h (106.93) | 18.77 pmol/μl (2.9) | 2.94h (0.78) | 1.34h (3.15) | α=2.41h (6.96) β=21.7h (25.77) | - | - | [182] |
| Liver | 1277.57 nmol ml−1 h (291.76) | 39.79 pmol/μl (3.29) | 2.5h (0.56) | 0.44h (0.14) | 20.45h (5.84) | - | - | ||||||
| Lungs | 346.321 nmol ml−1 h (6.51) | 9.73 pmol/μl (0.39) | 4.53h (0.4) | 0.97h (0.14) | 21.3h (2.99) | - | - | ||||||
| Kidneys | 987.941 nmol ml−1 h (114.88) | 46.29 pmol/μl (2.06) | 4.31h (0.39) | 1.18h (0.2) | 11.37h (1.99) | - | - | ||||||
| Nasal mucosa | 378.50 pmol mg−1h (341.42) | 20.4 pmol/mg (7.31) | 3.52 (0.66) | 0.93h (1.2) | 10.10 (12.16) | - | - | ||||||
| Esophagus | 140.19 pmol mg−1 h (111.69) | 8.2 pmol/bg (2.14) | 2.77h (1.78) | 0.67h (0.69) | 9.72h (9.89) | - | - | ||||||
| Stomach | 1409.7 pmol mg−1 h (457.62) | 211.19 pmol/mg (26.44) | 1.35h (0.45) | 0.37h (0.24) | 3.57h (1.93) | - | - | ||||||
| Small Intestine | 1691.21 pmol mg−1 h (292.94) | 130.58 pmol/mg (7.64) | 4.07h (0.41) | 1.69h (0.64) | 5.23h (2.22) | - | - | ||||||
| Cecum | 102422.29 pmol mg−1 h (44129.9) | 15.07 pmol/mg (1.78) | 19.09h (11.51) | 465.87h (2061.42) | 2.52h (1.07) | - | - | ||||||
| Colon | 361.39 pmol mg−1 h (47.32) | 16.43 pmol/g (1.22) | 8.08h (1.15) | 5.81h (37.92) | 5.4h (35.71) | - | - | ||||||
| Pancreas | 176.0 pmol mg−1 h (29.04) | 9.73 pmol/mg (0.39) | 4.53h (0.4) | 54.96h (11.78) | 0.97h (0.14) | - | - | ||||||
| Spleen | 57.71 pmol mg−1 h (30.55) | 9.64 pmol/mg (2.0) | 1.2h (0.71) | 3.2h (2.83) | 0.33h (0.37) | - | - | ||||||
| Heart | 94.35 pmol mg−1 h (22.99) | 5.71 pmol/mg (0.51) | 4.36h (0.74) | 7.75h (3.41) | 1.48h (0.61) | - | - | ||||||
| Brain | 53.71 pmol mg−1 h (5.4) | 2.07 pmol/mg (0.1) | 6.46h (0.57) | 12.58h (2.27) | 2.07h (0.41) | - | - | ||||||
| Oral (Gastric-intubation) | 0.5, mg/kg(single) | DMSO | Male Wistar albino rats | 4 | Blood | 1033±174 378 μg L− 1 h | 318±62 μg/L | 0.73±0.15h | 0.2h (Ka=3.52±1.58) | 2.62±1.37h | 1.53±0.81 L/kg | 77±13 | [37] |
| 1.0 mg/kg(single) | 4 | 1646±284 378 μg L− 1 h | 387±73 μg/L | 0.45±10h | 0.13h (Ka=5.19±2.14) | 2.78±0.36h | 1.75±0.29 L/kg | 61±11 | |||||
| 5.0 mg/kg(single) | 4 | 2438±462 μg L−1 h | 769±107 μg/L | 0.78±0.21h | 0.18h (Ka=3.88±0.40) | 3.19±0.37h | 2.15±0.40 | 23±5 | |||||
| 0.5 mg/kg/day (4 days) | 4 | 1117±282 378μg L−1 h | 404±80 μg/L | 0.7±0.24h | 0.16h (Ka=4.26±2.31) | 2.55±0.26h | 1.5±0.14 L/kg | 83±21 | |||||
| 1.0 mg/kg/day (4 days) | 4 | 2311±258 μg L− 1 h | 647±38 μg/L | 0.90±0.12h | 0.3h (Ka=2.26±0.48) | 1.86±0.2 h | 1.05±0.10 L/kg | 86±10 | |||||
| 5.0mg/kg/day (4 days) | 4 | 5796±1004 μg L−1 h | 2139±444 μg/L | 0.95±0.10h | 0.22h (Ka=3.02±2.03) | 1.62±0.44h | 0.88±0.28 L/kg | 43±7 | |||||
| Intravenous | 0.5mg/kg (single) | 15% hydroxypropyl-β-cyclodextrin | 4 | 1346±378 μg L− 1 h | - | - | - | 1.36±0.36h | 0.75±0.06 L/kg | 100 | |||
| Intravenous | 2μmol/kg | 15% hydroxypropyl-β-cyclodextrin | Male Sprague Dawley rats | 3–4 | Blood | 2.96±0.78 μM h | - | - | - | 3.52±0.35h | 1.94±0.42 L/kg | 100 | [36] |
| 10μmol/kg | 17.3±9.3 | - | - | - | 6.92±3.73h | 3.27±2.06 | 100 | ||||||
| 100μmol/kg | 322.1±149.6 | - | - | - | 9.19±0.83h | 2.66±1.22 | 100 | ||||||
| 400μmol/kg | 807.5±66.9 | - | - | - | 13.1±2.0 | 5.72±1.10 | 100 | ||||||
| Oral | 10μmol/kg | - | 19.89±3.27 | 9.2±0.6 μM | 0.44±0.1h | - | - | - | 115 | ||||
| 100μmol/kg | 298±139.4 | 42±11.4 | 2±1 | - | - | - | 93 |