Ocular inserts

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert

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424428, 528271, A61F 200

Patent

active

056608519

ABSTRACT:
Absorbable ocular inserts fabricated of materials that are biologically inert, biodegradable, non-allergenic, and insoluble in tear liquid, and a method for delivering substances to the eye using the ocular insert, are disclosed. In embodiment A of the invention, the insert and method include the covalent attachment of a carboxylic acid-containing substance to be delivered to a polymer that contains pendent carboxylic acid groups, through anhydride linkages. The drug is released over time by hydrolysis of the anhydride bonds. In embodiment B of the invention, a substance to be delivered (whether or not it contains a carboxylic acid group) is dispersed within an anhydride polymer or copolymer matrix and the mixture is formed into an appropriately shaped article for ocular delivery. In embodiment C of the invention, the insert and method include the covalent attachment of a carboxylic acid-containing substance to be delivered to a polymer that contains pendent carboxylic acid groups through methylene diester bonds which degrade in vivo over time.

REFERENCES:
patent: 3618604 (1971-11-01), Ness
patent: 3625214 (1971-12-01), Higuchi
patent: 3626940 (1971-12-01), Zaffarone
patent: 3630200 (1971-12-01), Higuchi
patent: 3811444 (1974-05-01), Heller et al.
patent: 3914402 (1975-10-01), Shell
patent: 3960150 (1976-06-01), Hussain et al.
patent: 3981303 (1976-09-01), Higuchi et al.
patent: 3986510 (1976-10-01), Higuschi et al.
patent: 3991759 (1976-11-01), Urquhart
patent: 3993071 (1976-11-01), Higuchi et al.
patent: 3995635 (1976-12-01), Higuchi et al.
patent: 4014987 (1977-03-01), Heller et al.
patent: 4093709 (1978-06-01), Choi et al.
patent: 4180064 (1979-12-01), Heller et al.
patent: 4180646 (1979-12-01), Choi et al.
patent: 4190642 (1980-02-01), Gale et al.
patent: 4248855 (1981-02-01), Blank et al.
patent: 4249531 (1981-02-01), Heller et al.
patent: 4271143 (1981-06-01), Schoenwald et al.
patent: 4281654 (1981-08-01), Shell et al.
patent: 4303637 (1981-12-01), Shell et al.
patent: 4304765 (1981-12-01), Shell et al.
patent: 4327725 (1982-05-01), Cortese et al.
patent: 4346709 (1982-08-01), Schmitt
patent: 4407792 (1983-10-01), Schoenwald et al.
patent: 4415551 (1983-11-01), Fang
patent: 4432964 (1984-02-01), Shell et al.
patent: 4449983 (1984-05-01), Cortese et al.
patent: 4472427 (1984-09-01), Baldwin et al.
patent: 4478818 (1984-10-01), Shell et al.
patent: 4519801 (1985-05-01), Edgren
patent: 4522829 (1985-06-01), Harting et al.
patent: 4553973 (1985-11-01), Edgren
patent: 4730013 (1988-03-01), Bondi et al.
patent: 4765977 (1988-08-01), Baron
patent: 4789724 (1988-12-01), Domb et al.
patent: 4857311 (1989-08-01), Domb et al.
patent: 4863457 (1989-09-01), Lee
patent: 4888176 (1989-12-01), Langer et al.
patent: 4911920 (1990-03-01), Jani et al.
patent: 4940588 (1990-07-01), Sparks et al.
patent: 4952402 (1990-08-01), Sparks et al.
patent: 4966773 (1990-10-01), Gressel et al.
patent: 5075104 (1991-12-01), Gressel et al.
patent: 5137728 (1992-08-01), Bawa
patent: 5147647 (1992-09-01), Darougar
patent: 5171812 (1992-12-01), Domb
patent: 5173298 (1992-12-01), Meadows
patent: 5175235 (1992-12-01), Domb et al.
patent: 5182102 (1993-01-01), DeSantis, Jr. et al.
patent: 5192535 (1993-03-01), Davis et al.
patent: 5206341 (1993-04-01), Ibay et al.
patent: 5209927 (1993-05-01), Gressel et al.
patent: 5212162 (1993-05-01), Missel et al.
patent: 5225196 (1993-07-01), Robinson
patent: 5240963 (1993-08-01), Domb et al.
patent: 5270419 (1993-12-01), Domb
patent: 5340572 (1994-08-01), Patel et al.
patent: 5354556 (1994-10-01), Sparks et al.
patent: 5384333 (1995-01-01), Davis et al.
Atherton, E., et al., "Peptide Synthesis. Part 12. 3,4-Dihydro-4-oxo-1,2,enzotriazin-3-yl Esters of Fluorenylmethoxycarbonyl Amino Acids as Self-Indicating Reagents for Solid Phase Peptide Synthesis," J. Chem. Soc., Perkin Trans., 1:2887-2894 (1988).
Brewer, J.H., et al., "Sterilization," Remington's Pharmaceutical Sciences, vol. XIV, pp. 1501-1518 (1970).
Ertain, M., et al., "Synthesis and Antipseudomonal Activities of Some Ofloxacin Esters as Prodrugs," Arzneimittel-Forschung/Drug Research, 42(I), Nr. 1, pp. 70-72 (1992).
Guerin, P., et al., "Drug Carriers," Polymer Bulletin, 14:187-192 (1985).
Guerin, Ph., et al., "Benzyl Esters of Optically Active Malic Acid Stereocopolymers as Obtained by Ring-Opening Polymerization of (R)-(+) and (S)-(-)-Benzyl Malolatonates," Makromol. Chem. Macromol. Symp., 6:305-314 (1986).
Jampel, Henry D., et al., "Glaucoma Filtration Surgery in Nonhuman primates Using Taxol and Etoposide in Polyanhydride Carriers," Investigative Ophthalmology & Visual Science, 34(11):3076-3083 (1993).
Knorr, R., et al., "New Coupling Reagents in Peptide Chemistry", Tetrahedron Lett., 30(15):1927-1930 (1989).
Larock, "Comprehensive Organic Transformation," VCH Publishers, New York (1989) (Table of Contents only).
Maeda, Y., et al., "Effects of Aluminium-Containing Antacid on Bioavailability of Ofloxacin Following Oral Administration of Pivaloyloxymethyl Ester of Ofloxacin as Prodrug," Biol. Pharm. Bull., 16(6):594-599 (1993).
The Merck Index, 14th edition, Merck & Co., Inc., New Jersey (1989), examples of carboxylic acid-containing bioactive compounds.
Patai, S., ed. The Chemistry of Acid Derivatives, part 1, Wiley, New York (1979) (book).
Reid, G.E. and Simpson, R.J., "Automated Solid-Phase Peptide Synthesis: Use of 2-(1H-Benzotriazol-1-yl)-1,1,3,3,-tetramethyluronium Tetrafluoroborate for Coupling of tert-Butyloxycarbonyl Amino Acids," Ann. Biochem., 200:301-309 (1992).
Rivaille, P., et al., "Synthesis of LH-RH Using a New Phenolic Polymer as Solid Support and Bop Reagent for Fragment Coupling," Tetrahedron Lett., 36:3413-3419 (1980).
Rasmussen, M. and Leonard, N.J., "The Synthesis of 3-(2'-Deoxy-D-Ribofuranosyl) Adenine. Application of a New Protecting Group, Pivaloyloxymethyl (Pom).sup.1 ", J. Amer. Chem. Soc., 89(21):5439-5445 (1967).
Roberts, J.D. and Caserio, M.C., editors in the Basic Principles of Organic Chemistry, California Institute of Technology, W.A. Benjamin, Inc., publishers, New York (1965) (Table of Contents only).
Schon, I. and Kisfaludy, L., "9 Fluorenylmethyl Pentafluorophenyl Carbonate as a Useful Reagent for the Preparation of N-9-Fluorenylmethyloxycarbonylamino Acids and Their Pentafluorophenyl Esters," Synthesis, pp. 303-305 (1986).
Tamargo, Rafael J., et al., "Growth Inhibition of the 9L Glioma Using Polymers to Release Heparin and Cortisone Acetate," Journal of Neuro-Oncology, 9:131-138 (1990).

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