Biological Availability of Ophthalmic Preparations. I. Increased Penetrability of the
Active Ingredient Through the Cornea
MASTEIKOVÁ R., CHALUPOVÁ Z., SAVICKIENE N.
Ústav technologie léků Farmaceutické fakulty Veterinární a farmaceutické univerzity, Brno 1Katedra farmaceutické chemie a farmakognozie Farmaceutické fakulty Kaunasské univerzitymedicíny, Kaunas, Litevská republika |
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Summary:
Most eye diseases are treated by topical administration of ophthalmic preparations. Low ophthalmic
bioavailability is due to a number of physiological and physicochemical factors. The main obstacle
to the penetration of active ingredients to the eye is the layered character of the cornea. Formulation
of ophthalmic preparations enabling easier penetration of this biological barrier thus ranks among
the most effective ways of improving bioavailability. Penetrability of the cornea can be increased by
the following methods: a) adjustment of the actual acidity in such a way that pH of the preparation
makes it possible to produce the optimal portion of non-ionized particles; b) incorporation of
absorption enhancers (non-ionic tensides, salts of bile acids, some antimicrobial substances, EDTA,
cyclodextrins, etc.) into the composition of the preparation, and c) production of prodrugs or ionic
pairs.
Key words:
ophthalmic preparations – biological availability – actual acidity –
absorption enhancers – prodrugs – ion pairs
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