| PMC full text: | Published online 2018 Nov 14. doi: 10.1089/jop.2017.0106
|
Table 1.
Pharmacokinetic Parameters of Lifitegrast Calculated for Various Ocular Tissues and Plasma for Each Formulation
| Formulation No. 1 | Formulation No. 2 | |||||||
|---|---|---|---|---|---|---|---|---|
| Tissue | Cmax(ng/mL or ng/g) | tmax(h) | AUC0-8 (ng·h/mL or ng·h/g) | t1/2(h)a | Cmax(ng/mL or ng/g) | tmax(h) | AUC0-8 (ng·h/mL or ng·h/g) | t1/2(h)a |
| Conjunctiva (palpebral) | 11,900 | 0.250 | 30,800 | — | 9,620 | 0.250 | 36,600 | — |
| Cornea | 5,930 | 0.250 | 25,500 | — | 5,190 | 1.00 | 15,200 | — |
| Sclera (anterior) | 11,200 | 0.250 | 17,500 | 1.97 | 5,870 | 0.500 | 11,200 | 2.32 |
| Conjunctiva (bulbar) | 14,200 | 0.250 | 13,400 | 2.02 | 9,370 | 0.250 | 12,000 | — |
| Sclera (posterior) | 826 | 0.250 | 2,360 | — | 369 | 0.500 | 1,570 | — |
| Iris-ciliary body | 190 | 0.250 | 1,130 | — | 195 | 1.00 | 778 | — |
| Aqueous humor | 79.0 | 3.00 | 530 | — | 89.5 | 1.00 | 340 | — |
| Choroid-RPE | 119 | 0.250 | 492 | — | 45.9 | 3.00 | 231 | — |
| Plasma | 17.4 | 0.250 | 11.2 | 0.850 | 9.52 | 0.250 | 16.4 | — |
| Lens | 3.85 | 1.00 | 5.44 | — | 0.794 | 3.00 | NR | — |
| Optic nerve | 36.0 | 1.00 | NR | — | 10.8 | 0.250 | NR | — |
| Retina | 31.2 | 1.00 | NR | — | NR | NR | NR | — |
| Vitreous humor | 2.09 | 0.250 | NR | — | 0.372 | 0.250 | NR | — |
aCould not be calculated for most tissues due to the lack of a distinct elimination phase.
AUC0–8, area under the concentration-time curve from 0 to 8
h; choroid-RPE, choroid-retinal pigment epithelium; Cmax, maximum concentration; NR, not reported due to limited measurable data; tmax, time to maximum concentration.