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October 1974

Topically Applied Steroids in Corneal Disease: VI. Kinetics of Prednisolone Sodium Phosphate

Author Affiliations

From the Department of Ophthalmology and the Massachusetts Lions Eye Research Laboratory (Drs. Leibowitz and Kupferman), and the Department of Pharmacology (Dr. Kupferman), Boston University School of Medicine, Boston.

Arch Ophthalmol. 1974;92(4):331-334. doi:10.1001/archopht.1974.01010010341017

The corneal and aqueous humor steroid concentrations produced by topical application of a standard dose of tritiated 0.125% and 1.0% ophthalmic solutions of prednisolone sodium phosphate were determined. In the absence of the corneal epithelium, the 1.0% formulation achieved the highest total corneal and aqueous humor concentrations of any steroid measured in our laboratory to date. Despite its virtual insolubility in lipid media, the drug was also able to cross the lipophilic epithelial barrier in significant amounts. Increasing drug concentration (0.125% to 1.0%) produced at least a commensurate increase in corneal and aqueous humor bioavailability. The steroid concentration in the anterior segment of the eye, following administration of the commercially available preparation, was almost twice that produced by the same drug delivered in buffered normal saline, indicating the influence of the vehicle on corneal absorption and penetration.

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