TABLE 2.

Pharmacokinetic parameters estimated for dorzolamide and brinzolamide after single topical ocular administration of Trusopt (dorzolamide hydrochloride solution, 2%) and Azopt (brinzolamide suspension, 1%) to pigmented rabbit

Parameters were estimated using noncompartmental analysis (WinNonlin, version 1.5; Pharsight, Inc.). For brinzolamide, no drug levels were detected in the posterior vitreous.

Tissue	Dorzolamide				Brinzolamide
	Cmax	Tmax	T1/2	AUC0–24	Cmax	Tmax	T1/2	AUC0–24
	μg/g	h	h	μg h/ml or g	μg/g	h	h	μg h/ml or g
Cornea	36.61	0.25	1.08	51.21	19.27	0.50	1.71	50.88
Conjunctiva	68.74	0.25	0.720	49.55	28.80	0.25	1.01	37.94
Aqueous humor	1.92	0.50	7.06	6.159	0.97	0.75	6.16	3.14
Sclera (anterior)	47.18	0.50	0.559	36.13	8.17	0.25	0.929	5.22
Sclera (posterior)	4.92	0.25	1.09	3.46	2.70	0.25	0.134	1.34
Retina (anterior)	3.68	0.50	0.87	3.46	0.82	1.0	3.94	2.42
Retina (posterior)	0.091	0.50	1.23	0.095	0.059	0.50	0.812	0.051
Vitreous (anterior)	0.07	0.75	1.99	0.208	0.034	1.0	8.07	0.185
Vitreous (posterior)	0.0096	1.0	1.23	0.018	–	–	–	–
Optic nerve	1.08	0.50	2.77	6.16	0.28	0.75	3.52	0.66

C_max, the maximum observed drug concentration in a particular tissue; T_max, the time at which C_max occurs; T_1/2, the half-life of the drug in tissue; AUC_0–24, the area under the curve obtained by plotting the concentration-time data, where t is the last time point at which drug concentration was measured.

–, Pharmacokinetic parameters are not available due to undetected drug levels.