Table 2.
Estimated Pharmacokinetic Parameters of RBZ and 10×RBZ after Intravitreal Injection into New Zealand White Rabbits
| t 1/2 (h) | MRT (h) | Cmax (µg/mL) | Tmax (h) | AUC (h × µg/mL) | V/F (mL) | CL/F (mL/h) | |
|---|---|---|---|---|---|---|---|
| Anterior chamber | |||||||
| RBZ 0.3 mg/0.03 mL | 55.58 ± 7.72 | 171.04 ± 19.82 | 23.08 | 1 | 3431.81 | 7.01 | 0.087 |
| 10×RBZ 3.0 mg/0.03 mL | 53.36 ± 5.14 | 138.03 ± 15.19 | 181.48 | 1 | 23.020.1 | 10.03 | 0.130 |
| Vitreous | |||||||
| RBZ 0.3 mg/0.03 mL | 51.70 ± 6.03 | 81.59 ± 7.48 | 140.01 | 1 | 12,202.52 | 1.81 | 0.024 |
| 10×RBZ 3.0 mg/0.03 mL | 52.60 ± 4.86 | 131.28 ± 10.67 | 1637.54 | 1 | 198,715.6 | 1.15 | 0.015 |
| Retina | |||||||
| RBZ 0.3 mg/0.03 mL | 36.74 ± 3.79 | 107.19 ± 9.32 | 102.70 | 24 | 16,491.45 | 0.96 | 0.018 |
| 10×RBZ 3.0 mg/0.03 mL | 76.85 ± 6.63 | 140.51 ± 11.37 | 224.68 | 96 | 34,656.53 | 9.58 | 0.086 |
| Serum | |||||||
| RBZ 0.3 mg/0.03 mL | 91.93 ± 7.75 | 252.73 ± 18.46 | 7.35 × 10−3 | 24 | 1644.41 × 10−3 | 21.85 × 103 | 0.164 × 103 |
| 10×RBZ 3.0 mg/0.03 mL | 179.01 ± 15.09 | 479.98 ± 31.25 | 22.07 × 10−3 | 24 | 6885.24 × 10−3 | 103.73 × 103 | 0.401 × 103 |
AUC, area under concentration-time curve; CL/F, apparent clearance; Cmax, observed maximum concentration; MRT, mean residence time; 10×RBZ, 10-fold ranibizumab; RBZ, ranibizumab; t1/2, half-life; Tmax, time to Cmax; V/F, apparent volume of distribution.