Abstract: The invention disclosed is a composition and method for the slow sustained ocular delivery of a prophylactic agent contained in liposome vesicles. The liposome vesicles are composed of phospholipid and cholesterol in a molar ratio of phospholipid to cholesterol of 8:2 to 1:1. Preferably, stearylamine is included in the liposome composition.

Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.

Abstract: Compounds of Formula I ##STR1## the pharmaceutically acceptable salts, and the gamma-lactone form thereof are described. They are antagonists of leukotrienes and SRS-A.

Abstract: The present invention relates to an ophthalmological composition of matter comprising a suspension of eicosapentaenoic acid in an alkyl cellulose and/or hydroxyalkyl aqueous cellulose solution to be used in any case of ocular inflammation on men and/or on aminals.The invention also relates to the use of said eicosapentaenoic acid and to a method for the treatment of ocular inflammation by the same.

Abstract: There is provided a stable, ophthalmic aqueous composition for topical administration, comprising (a) acetazolamide and either (b) a pre-formed, pharmaceutically acceptable, aqueous gel or (c) an aqueous gel-forming liquid capable of forming a pharmaceutically acceptable gel in situ when applied topically to a patient; said composition having a pH of less than 5.0.

Abstract: Pharmaceutical compositions comprising tetrahydrocortisol and method of using same in the control of intraocular pressure are disclosed.

Abstract: A liposome composition designed for enhanced binding to mucosal tissue, The liposomes contain about 10-40 mole percent of an amine-derivatized lipid component in which a charged amine group is spaced from a lipid polar head region by a carbon-containing spacer arm at least 3 atoms in length. The liposomes preferably have a close packed lipid structure produced by inclusion of between 20-50 mole percent of cholesterol or an amine-derivatized cholesterol, and/or phospholipids with predominantly saturated acyl chain moieties. For ophthalmic use, the liposomes may be suspended in an aqueous medium containing a high-viscosity polymer, to enhance further the retention of liposomes on a corneal surface.

Abstract: The invention relates to the stabilization of mercury-containing preservatives in liquid or gel-form ophthalmic medicaments. This stabilization against chemical decomposition after the preservative has become deposited on the inner walls of the plastics containers is achieved by adding to the formulation 2-amino-2-hydroxymethyl-1,3-propanediol or a homologue thereof having up to 10 carbon atoms.

Abstract: The invention relates to an ophthalmic medicament containing diclofenac-sodium in aqueous solution. Owing to the addition of a specific stabilizer, the medicament has excellent stability against chemical decomposition of the active ingredient and outstanding preservation properties and is tolerated very well by the eye.

Abstract: A liposome composition with enhanced retention on ocular surfaces, for use in ophthalmic drug delivery and dry eye treatment. The liposomes contain about 10-40 mole percent of an amine-derivatized lipid component in which a charged amine group is spaced from a lipid polar head region by a carbon-containing spacer arm at least 3 atoms in length. The liposomes preferably have a close packed lipid structure produced by inclusion of between 20-50 mole percent of cholesterol or an amine-derivatized cholesterol, and/or phospholipids with predominantly saturated acyl chain moieties. The liposomes may be suspended in an aqueous medium containing a high-viscosity polymer, formulated in paste form, or embedded in a polymer matrix, to enhance further the retention of liposomes on a corneal surface.

Abstract: It is hereby described and claimed the new lysine salt of 4-diphenylacetic acid, having an antiinflammatory and analgesic activity, its preparation method and the pharmaceutical compositions containing it which are therapeutically useful both systemically and topically.

Abstract: The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.

Abstract: A target-entrapped drug comprising three chemically joined components(1) the active drug component;(2) a linking chain; and(3) an activatable group;the activatable group on exposure of the drug to activation liberating components (1) and (2) so that the drug component (1) is bound to a selected target site through the linking chain (2). The drug is administered and then activated by exposure to electromagnetic radiation or other energy such as thermal energy at the anatomic target site.

Abstract: Heavy metal salts of hyaluronic acid have been prepared. In particular, this invention is directed to silver, gold, cerium and tungsten salts of hyaluronic acid. These heavy metal salts of hyaluronic acid are useful as antimicrobial agents. Gold hyaluronate may also be used to treat arthritis. This invention also concerns methods of making the silver salt of hyaluronic acid as well as compositions containing silver hyaluronate or gold hyaluronate. The invention also concerns composition containing heavy metal salts having radioactively labelled hyaluronate moieties.

Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.

Abstract: Substituted 1-oxa-dethiacephalosporins are found to be effective elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: Anti-inflammatory compounds and a method of treating inflamed ocular tissue utilizing these compounds are described. The steroidal actives are advantageously characterized in that they do not cause any significant increase in intraocular pressure during chronic use.

Abstract: Disclosed are water based, viscoelastic compositions comprising a mixture of high molecular weights hyaluronic salts and water soluble poly(ethylene oxides). Also disclosed are cosmetic formulations including said compositions.

Abstract: Retinal edema, in particular cystoid macular edema, is prevented or treated by administering to the patient afflicted with retinal edema or in danger of experiencing retinal edema an amount of a dopaminergic antagonist effective to reduce the edema. A preferred dopaminergic antagonist is haloperidol. The activity of the dopaminergic antagonist may be potentiated by concurrent administration of ascorbic acid.

Abstract: Ointment compositions for the treatment of styes and related infectious conditions of the eyelid. The ointments contain an emollient base, including white petrolatum, mineral oil and microcrystalline wax, as well as boric acid, wheat germ oil and mercuric oxide, the concentration of boric acid in the ointment is about 2-10% by weight, as is the concentration of the wheat germ oil, while the mercuric oxide is present in a concentration of about 1-1.2% by weight. The wheat germ oil enhances the anti-bacterial potency of the mercuric oxide, and the boric acid stabilizes the mercuric oxide in the presence of the wheat germ oil to prevent discoloration of the ointment.

Abstract: An ophthalmic solution having anti-inflammatory action without side effects and irritativeness which comprises pranoprofen and boric acid.

Abstract: The compounds 9-(1,3-dihydroxy-2-propoxymethyl)guanine and the pharmaceutically acceptable salts thereof are useful as antiviral agents. The compound 1,3-dibenzyloxy-2-acetyloxy-methoxypropane is useful as an intermediate for the preparation of 9-(1,3-dihydroxy-2-propoxymethyl)guanine.

Abstract: Compounds of formula: ##STR1## (wherein R represents hydrogen or methyl, >A--B-- represents a >CH--CH.sub.2 -- or >C.dbd.CH-- group; >C--Z represents a >C.dbd.O or >CH--OH group; and n represents 1 or 2) and ophthalmically acceptable salts and esters thereof are useful as ophthalmic anti-inflammatory agents.

Abstract: Xanthine derivatives are described which decrease the stinging associated with the application of ophthalmic acidic anti-inflammatory agents.

Abstract: Novel carbonates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.