Hydrophilics International, Inc.

Forest Laboratories, Inc.

Izhak Blank

Joseph Fertig

A mixture of nitroglycerin and a water-insoluble vinylpyrrolidone polymer provides a polymeric matrix which gradually releases nitroglycerin upon application to the skin of a patient in the form of a film, gel or ointment. The water-insoluble vinylpyrrolidone polymer may be an uncrosslinked copolymer or a crosslinked homopolymer or copolymer. The polymer provides increased stability and reduced volatility of the nitroglycerin while permitting slow and sustained release of the drug upon topical application to the skin.

Nitroglycerin-containing polymeric matrix for sustained release on

Nitroglycerin preparations

A salt of a polymer, containing acid groups, soluble or dispersible in water or organic solvents, is combined with a salt-forming pharmaceutically effective compound for application, orally, topically, or systemically. A sustained release of the pharmaceutical compound is thus obtained.

Pharmaceutical base salts

A composition comprising a copolymer of from 20 to 60 parts of at least one member selected from the class consisting of acrylic and methacrylic acids, from 20 to 70 parts of one member selected from the class of lower alkyl acrylates and lower alkyl methacrylates, and from 5 to 20 parts of a plasticizing monomer, in which at least some of the acid groups have been neutralized by multivalent cations, where a chemical, exclusive of water and plasticizer, releasable from a film of the referenced copolymer, is formed by casting and drying an aqueous solution of the copolymer containing the chemical.

Sustained release polymers

A copolymer derived from a monomeric mixture comprising from 20 to 60 parts of acrylic or methacrylic acid, from 20 to 70 parts of a lower alkyl acrylate or methacrylate, and from 5 to 20 parts of a plasticizing monomer is at least partially neutralized by multivalent cations.

Copolymers comprising acrylic or methacrylic acid and methyl methacrylate are neutralized by the addition of cyclic alkylene imines, preferably ethylene imine, to form a product which is capable of absorbing large amounts of material soluble in water, and slowly releasing those materials. The fundamental copolymer may be modified by the addition of cross-linking agents, chain terminators, plasticizers, etc., prior to treatment with the alkylene imine. The treated copolymers are particularly useful in the formation of contact lenses for the application of medicinals to the eye, and for other depot materials.

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Haifa, Israel

Izhak Blank