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M. Diestelhorst, S. Fauser, K. Gruner, R. Sueverkruep; The Ocular Bioavailability of Latanoprost Lyophilizate 0.75 µg Compared With Xalatan® 1.5 µg. Invest. Ophthalmol. Vis. Sci. 2010;51(13):5307.
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Ophthalmic lyophilizate carrier systems (OLCS) are preservative free, chemically stable and physiologically inert drug delivery systems with potentially superior topical bioavailability(1). Production methods, content uniformity and physico-chemical characteristics of latanoprost OLCS (Lyo-Lat) were described earlier(2). We studied latanoprost free acid (Lat-FA) concentrations in rabbit aqueous humor after administration of Xalatan® eye drops containing 0.005% latanoprost ester and single-dose lyophilizates containing 0.75 µg of the active ingredient.
Preservative-free lyophilizates with 3000 µg mannitol and 30 µg Pluronic F68® were prepared by freeze-drying. Latanoprost was applied at random to 24 eyes of 12 chinchilla pigmented rabbits as one drop of Xalatan® (1.5µg) or one Lyo-Lat (0.75µg). Aqueous humor samples were taken +100 minutes after application. Samples were immediately frozen in dry ice/ethanol and shipped over night under dry ice to the bioanalytical laboratory (Cayman Chemical, USA-Ann Arbor, MI). The Lat-FA content of each sample was determined by enzyme immuno assay.
Absolute concentrations of Lat-FA in aqueous humor of Lyo-Lat 0.75 µg (16.7±8.7 ng/ml, n=12) were equivalent to those of Xalatan® (32.6±10.9 ng/ml, n=12). There were no statistically significant differences (p=0.89; t-test) of mean and variance of the concentration-dose-ratios for OLCS and Xalatan®.
For the first time the Lyo-Lat demonstrate clinically relevant concentrations of Lat-FA in the living eye. OLCS containing latanoprost show equivalent concentration-dose-ratios compared to Xalatan®. In terms of stability, ocular tolerability and handling OLCS are superior to conventional eye drops and shall improve the treatment of glaucoma.(1) Abduljalil K. et al.: Modelling ocular pharmacokinetics of fluorescein administered as lyophilisate or conventional eye drops, Eur J Clin Pharmacol 2008 64: 521-529(2) Gruner K, Suverkrup R, Diestelhorst M: Latanoprost Ophthalmic Lyophilizate Carrier Systems (OLCS), IOVS 2009 50: E-abstract 5555
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