January 1991
Volume 32, Issue 1
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Articles  |   January 1991
Penetration and binding of aldose-reductase inhibitors in the lens.
Author Affiliations
  • A Ohtori
    Itami Research Laboratories, Senju Pharmaceutical Co., Osaka, Japan.
  • Y Yamamoto
    Itami Research Laboratories, Senju Pharmaceutical Co., Osaka, Japan.
  • K J Tojo
    Itami Research Laboratories, Senju Pharmaceutical Co., Osaka, Japan.
Investigative Ophthalmology & Visual Science January 1991, Vol.32, 189-193. doi:
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      A Ohtori, Y Yamamoto, K J Tojo; Penetration and binding of aldose-reductase inhibitors in the lens.. Invest. Ophthalmol. Vis. Sci. 1991;32(1):189-193.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Diffusion, partitioning, and binding of two aldose-reductase inhibitors (ARI) in the rat lens were investigated under in vitro conditions. A lipophilic ARI (CT-112) and a hydrophilic ARI (AD-5467) were used as model drugs. Under lens-uptake conditions, the drug concentration in the lens increased rapidly during the initial 10 hr and reached steady state (equilibrium) after 24 hr. Despite the equilibrium concentration of CT-112 in the lens which is approximately three times of that of AD-5467, the inhibition rate of CT-112 against the accumulation of sugar alcohols was appreciably lower than that for AD-5467. The equilibrium concentration in the lens after the penetration/binding experiment also suggested that AD-5467 may interact with the target sites of enzymes more than that for CT-112. The time course of the lens concentration during the uptake and desorption experiments was well described by a diffusion/binding model assuming a Langmuir binding. The diffusion coefficient, the partition coefficient, and binding parameters in the rat lens were determined for the two ARIs.

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