Bioadhesive compositions and methods of treatment therewith

• US 4,983,392 A
• Filed: 12/20/1988
• Issued: 01/08/1991
• Est. Priority Date: 11/14/1983
• Status: Expired due to Term

• Current Assignee: Columbia Laboratories, Inc. (Catalent, Inc.)
• Original Assignee: Bio-Mimetics, Inc., Columbia Laboratories, Inc. (Catalent, Inc.)
• Inventors: Robinson, Joseph R.
• Primary Examiner(s): Cashion, Jr., Merrell C.
• Assistant Examiner(s): Horne, Leon R.
• Application Number:
  US07/287,464
• Time in Patent Office: 749 Days
• Field of Search: 424/427, 424/428, 424/434, 514/177
• US Class Current: 424/427
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/0065 Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/7007 Drug-containing films, membranes or sheets A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence

Abstract

A controlled release treatment composition and method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.

Claims

1. A controlled release ophthalmic treatment composition including a bioadhesive and an effective amount of an ophthalmic treating agent, said bioadhesive comprising a water-swellable, but water-insoluble, particular cross-linked carboxyl-functional polymer having particles sized so that visual impairment is substantially minimized when said composition is contacted with a mucous membrane of the eye, said polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least the carboxyl functionally, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkylenyl polyether, said percentages being based upon the weights of the unpolymerized repeating unit cross-linking agent, respectively.

2. A controller release ophthalmic treatment composition as recited in claim 1 wherein said bioadhesive and said treating agent are intimately admixed substantially uniformly.

3. A controlled release ophthalmic treatment composition as recited in claim 1 wherein at least about 90 percent of said polymer repeating units contain at least one carboxyl functionality.

4. A controlled release ophthalmic treatment composition as recited in claim 1 wherein at least about 95 percent of said polymer repeating units contain at least one carboxyl functionality.

5. A controlled release ophthalmic treatment composition as recited in claim 1 wherein said polymer contains about 0.1 to about 1 percent by weight of polymerized cross-linking agent.

6. A controlled release ophthalmic treatment composition as recited in claim 1 wherein said carboxyl functionality is provided by polymerized acrylic acid.

7. A controlled release ophthalmic treatment composition as recited in claim 1 wherein at least about 95 percent of said polymer repeating units contain at least one carboxyl functionality provided by acrylic acid, and said polymer contains about 0.1 to about 1 percent by weight of polymerized cross-linking agent.

8. A controlled release ophthalmic treatment composition as recited in claim 7 wherein said cross-linking agent is 3,4-dihydroxy-1,5-hexadiene.

9. A controlled release ophthalmic treatment composition as recited in claim 7 wherein said cross-linking agent is divinyl benzene.

10. A controlled release ophthalmic treatment composition as recited in claim 7 wherein said cross-linking agent is 2,5-dimethyl-1,5-hexadiene.

11. A controlled release ophthalmic treatment composition as recited in any one of claims 1-10, inclusive, wherein said ophthalmic treating agent constitutes an anti-inflammatory agent.

12. A controlled release opthahalmic treatment composition as recited in claim 11 wherein said anti-inflammatory agent is fluorometholone.