PMID: 8951683Jan 1, 1996Paper

Pharmacokinetics and intraocular pressure lowering effect of timolol preparations in rabbit eyes

Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics
C H ChiangJ L Chen

Abstract

Two timolol preparations, a gel and an eyedrop with a thickening agent, and one commercial eyedrop without a thickening agent, were studied in rabbits. After topical administration of these three preparations in rabbits, aqueous humor was withdrawn and the proteins removed from the samples by precipitation with acetonitrile. Timolol concentrations were determined directly by an HPLC method. The HPLC mobile phase was composed of methanol and 5 mM d-camphorsulfonic acid (in 1% acetic acid) with a ratio of 49:51 (v/v). A reversed phase C18 column was used to separate samples with a flow rate of 0.8 mL/min and a UV detector set at 284 nm. A two-compartment pharmacokinetic model was used to fit the aqueous humor level for determining the drainage (kd) and absorption rate constants (ka) in the precorneal area as well as the elimination rate constant (ke) of timolol in aqueous humor. For ka +kd, the eyedrop without a thickening agent had the highest value (0.160 min-1), followed by the eyedrop with a thickening agent (0.030 min-1), and the gel had the lowest value (0.009 min-1). It suggests that the gel has a longer retention time in eyes to improve ocular bioavailability and decrease side effects. The AUC0 approximately infinity for ...Continue Reading

References

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Aug 1, 1994·Journal of Clinical Pharmacology·W H FrishmanM Tannenbaum

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Citations

Jan 3, 2006·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Sheng-Fu HuangChiao-Hsi Chiang
Feb 11, 2012·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Gustavo de Oliveira FulgêncioArmando da Silva Cunha-Júnior
Apr 17, 2016·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Sonia T HassibRawda M Sayed
Nov 12, 2016·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Erin LavikYoung H Kwon
Jun 29, 2000·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·F LacheretzG Le Fur
May 3, 2008·Biological & Pharmaceutical Bulletin·Koji SakanakaShun Higuchi

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