Improvement of the ocular bioavailability of timolol by sorbic acid

In Vitro Transport and Partitioning of AL-4940, Active Metabolite of Angiostatic Agent Anecortave Acetate, in Ocular Tissues of the Posterior Segment

“…This general fact can be advantageous for optimizing delivery of topically applied compounds, without requiring detailed measurements of partitioning into selected tissues. 37 Physiologically based pharmacokinetic (PBPK) modeling attempts to make more quantitative predictions of chemical species distribution, and have undertaken the systematic direct measurement of partition coeffi cients in each of the tissues of interest. 38 , 39 Rather than attempting to deduce the tissue partition coeffi cient from a lag-time coeffi cient, as has been done in other ocular PBPK studies, 8 , 9 , 40 we undertook the direct measurement of partitioning in the separate tissues of the posterior segment.…”

Ciprofloxacin surf-plexes in sub-micron emulsions: A novel approach to improve payload efficiency and antimicrobial efficacy

“…Many authors have reported use of ion pairs for enhanced or improved bioavailability of drug (Abdulrazik et al, 2001). Timolol bioavailability enhanced, when it was ion paired with sorbic acid (Higashiyama et al, 2004). Further, many studies have shown advantages of imparting cationic surface to SE which not only improves drug retention at infection site but also results in enhanced permeability of drug (Rabinovich-guilatt et al, 2004).…”

Evaluation of Aqueous Humor Concentrations of Istalol® and Betimol® Following a Single Ocular Instillation in Rabbit Eyes

“…There have been various studies addressing these alternatives, such as use of a prodrug, 6 use of ophthalmic inserts, 7 and a gel-forming solution, 8,9 which prolongs precorneal retention, but also causes blurred vision because of the increased viscosity of the preparation. 10, 11 Higashiyama and associates 12 have demonstrated that pairing timolol with sorbic acid greatly increases the lipophilicity, octanol and water partition coefficient, and penetration across the corneal barrier. The timolol maleate with potassium sorbate (TLA) formulation was developed to use this phenomenon in a topical solution for ophthalmic use.…”