Topical ocular pharmacokinetics and bioavailability for a cocktail of atenolol, timolol and betaxolol in rabbits.
Atenolol
Betaxolol
Eye drop
Ocular bioavailability
Ocular pharmacokinetics
Rabbit
Timolol
Journal
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
ISSN: 1879-0720
Titre abrégé: Eur J Pharm Sci
Pays: Netherlands
ID NLM: 9317982
Informations de publication
Date de publication:
01 Dec 2020
01 Dec 2020
Historique:
received:
24
06
2020
revised:
02
09
2020
accepted:
07
09
2020
pubmed:
19
9
2020
medline:
22
6
2021
entrez:
18
9
2020
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 32946960
pii: S0928-0987(20)30341-9
doi: 10.1016/j.ejps.2020.105553
pii:
doi:
Substances chimiques
Adrenergic beta-Antagonists
0
Ophthalmic Solutions
0
Atenolol
50VV3VW0TI
Timolol
817W3C6175
Betaxolol
O0ZR1R6RZ2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
105553Informations de copyright
Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.