Topical ocular pharmacokinetics and bioavailability for a cocktail of atenolol, timolol and betaxolol in rabbits.

Ocular bioavailability after eye drops administration is an important, but rarely determined, pharmacokinetic parameter. In this study, we measured the pharmacokinetics of a cocktail of three beta blockers after their topical administration into the albino rabbit eye. Samples from aqueous humour were analysed with LC-MS/MS. The pharmacokinetic parameters were estimated using compartmental and non-compartmental analyses. The ocular bioavailability was covering broad range of values: atenolol (0.07 %), timolol (1.22%, 1.51%) and betaxolol (3.82%, 4.31%). Absolute ocular bioavailability presented a positive trend with lipophilicity and the values showed approximately 60-fold range. The generated data enhances our understanding for ocular pharmacokinetics of drugs and may be utilized in pharmacokinetic model building in ophthalmic drug development. Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.

Citation

Anam Fayyaz, Veli-Pekka Ranta, Elisa Toropainen, Kati-Sisko Vellonen, Annika Valtari, Jooseppi Puranen, Marika Ruponen, Iain Gardner, Arto Urtti, Masoud Jamei, Eva M Del Amo. Topical ocular pharmacokinetics and bioavailability for a cocktail of atenolol, timolol and betaxolol in rabbits. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2020 Dec 01;155:105553

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PMID: 32946960

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