Bioavailability in the Human Eye of a Fixed Combination of Latanoprost and Timolol Compared to Monotherapy

The ocular pharmacokinetics of a single topical administration of a fixed combination (FC) of latanoprost 0.005% and timolol 0.5% was compared to the monotherapies of latanoprost and timolol in cataract surgery patients. The absorption rate of latanoprost and timolol into the aqueous humor was similar after administration of the FC compared to the two drugs given separately. The aqueous humor concentration of the acid of latanoprost tended to be higher 1-4 hours after administration of FC compared to latanoprost monotherapy. This resulted in an increased AUC. The Tmax and elimination half-life of both latanoprost and timolol were similar after administration of either FC or the two drugs given as monotherapy. Latanoprost did not have any influence on the ocular pharmacokinetics of timolol. The bioavailability of latanoprost and timolol into human aqueous humor, after FC, was at least as good as for the two drugs administered separately.