Effect of drug vehicle on human ocular retention of topically applied tetracycline. 1976

J Y Massey, and C Hanna, and R Goodart, and T Wallace

Tetracycline hydrochloride--as a 1% suspension in oil, 1 and 2% suspension in ointment, and 1 and 2% solution in water or balanced salt solution USP--was applied once to the conjunctival cul-de-sacs of volunteers and patients before cataract extraction. The tear film concentrations of drug were maintained above a bacteriostatic level in excess of six hours for 1 and 2% tetracycline in ointment, less than two hours for 1% tetracycline in oil, and less than 30 minutes for 1 and 2% tetracycline in water or balanced salt solution. The 2% tetracycline in ointment produced the highest tear film levels of drug. The 1% tetracycline in oil induced excessive lacrimation and much of the drug was washed from the conjunctival surface. The tear film levels of the drug were mirrored by the maintenance of bacteriostatic levels of tetracycline in the aqueous humor for 1 1/2 hours with 2% tetracycline in ointment. Whereas 1% tetracycline in ointment produced drug levels approaching bacteriostasis in the aqueous humor, 1% tetracycline in oil produced only trace levels of the drug within the anterior chamber. The ointment acted as a depot for the suspended drug and most of the drug in the absence of excessive tearing was lost from the conjunctiva via the lacrimal system.

UI MeSH Term Description Entries
D009823 Ointment Bases Various mixtures of fats, waxes, animal and plant oils and solid and liquid hydrocarbons; vehicles for medicinal substances intended for external application; there are four classes: hydrocarbon base, absorption base, water-removable base and water-soluble base; several are also emollients. Bases, Ointment
D005128 Eye Diseases Diseases affecting the eye. Eye Disorders,Eye Disease,Eye Disorder
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000287 Administration, Topical The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example. Drug Administration, Topical,Administration, Topical Drug,Topical Administration,Topical Drug Administration,Administrations, Topical,Administrations, Topical Drug,Drug Administrations, Topical,Topical Administrations,Topical Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001082 Aqueous Humor The clear, watery fluid which fills the anterior and posterior chambers of the eye. It has a refractive index lower than the crystalline lens, which it surrounds, and is involved in the metabolism of the cornea and the crystalline lens. (Cline et al., Dictionary of Visual Science, 4th ed, p319) Aqueous Flare,Intraocular Fluid,Aqueous Flares,Aqueous Humors,Flare, Aqueous,Fluid, Intraocular,Fluids, Intraocular,Humor, Aqueous,Humors, Aqueous,Intraocular Fluids
D013666 Tears The fluid secreted by the lacrimal glands. This fluid moistens the CONJUNCTIVA and CORNEA. Meibomian Lipids,Meibum,Lipid, Meibomian,Meibomian Lipid,Tear
D013752 Tetracycline A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis. 4-Epitetracycline,Achromycin,Achromycin V,Hostacyclin,Sustamycin,Tetrabid,Tetracycline Hydrochloride,Tetracycline Monohydrochloride,Topicycline,4 Epitetracycline
D014677 Pharmaceutical Vehicles A carrier or inert medium used as a solvent (or diluent) in which the medicinally active agent is formulated and or administered. (Dictionary of Pharmacy, 1986) Pharmaceutical Vehicle,Vehicle, Pharmaceutical,Vehicles, Pharmaceutical
D014867 Water A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Hydrogen Oxide

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