TABLE 3.
Comparison of mean drug levels in ocular tissues after single and multiple topical dosing (42 doses)
Drug levels were assessed at 1 h after the last dose. To assess drug accumulation, ratios of the drug levels between multiple and single dose regimens were calculated. Brinzolamide was not detected in the posterior vitreous after single dose administration.
Tissue | Dorzolamide |
Brinzolamide |
||||
---|---|---|---|---|---|---|
Single Dose | Multiple Dose | Multiple Dose/Single Dose Ratio | Single Dose | Multiple Dose | Multiple Dose/Single Dose Ratio | |
μg/g | μg/g | μg/g | μg/g | |||
Cornea | 10.31 | 21.4 | 2.08 | 7.99 | 14.1 | 1.76 |
Conjunctiva | 10.10 | 5.89 | 0.60 | 6.77 | 4.57 | 0.68 |
Aqueous humor | 1.49 | 2.35 | 1.58 | 0.530 | 1.48 | 2.80 |
Sclera (anterior) | 9.12 | 7.67 | 0.85 | 1.57 | 4.20 | 2.60 |
Sclera (posterior) | 0.460 | 0.56 | 1.21 | 0.140 | 0.57 | 4.07 |
Retina (anterior) | 1.02 | 3.00 | 2.94 | 0.821 | 2.30 | 2.80 |
Retina (posterior) | 0.023 | 2.10 | 90.13 | 0.015 | 1.30 | 86.7 |
Vitreous (anterior) | 0.07 | 0.17 | 2.43 | 0.034 | 0.05 | 1.47 |
Vitreous (posterior) | 0.0096 | 0.065 | 6.80 | – | 0.029 | – |
Optic nerve | 0.657 | 0.86 | 1.31 | 0.269 | 0.370 | 1.38 |
–, Pharmacokinetic parameters are not available due to undetected drug levels.