Aspect on Corneal Permeability of Bupranolol

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Abstract
Because the cornea forms an important boundary tissue in the anterior eye portion, the corneal permeability of ophthalmic drugs is important in drugs administered topically. To evaluate the intraocular penetration of bupranolol [1-tert-butylamino-3-(2-chloro-5-methylphenoxy)-2-propanol hydrochloride], an antiglaucoma ophthalmic solution, its in vitro corneal permeability was examined using excised rabbit cornea mounted on the methacrylate chamber. Permeation time was carried out within 10-30 min at 35.degree. C. Permeability constants were calculated from measuring the initial amount of bupranolol (C0), the residual amount of bupranolol in the tear-side chamber (C1), the concentration in the aqueous-side chamber (C2), thickness of the cornea (.DELTA.x) and corneal permeation area (A) after each permeation time. In both tissue culture medium and ophthalmic solution, the constant of corneal permeable velocity (K) and permeability constant of the membrane (P) of bupranolol increased with permeation time, and the values did not depend on bupranolol concentration. The bupranolol compound at the precorneal pocket penetrates into the intraocular area through the cornea.

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