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. 2011 Sep;39(9):1529–1537. doi: 10.1124/dmd.111.040055

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.