EP0251680A2
Expired / Lapsed
EP
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Controlled release bioerodible drug delivery system
Assignee: Novartis AG
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Filing: 1987-06-24
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Granted: —
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Expires: 2007-06-24
Abstract
Abstract A dosage composition for controlled release of a pharmaceutical compound to body fluids such as the tears of the eye, or surgical site fluids, has an external matrix rapidly soluble in said fluids, and bioerodible microparticles dispersed in the external matrix, the microparticles containing the pharmaceutical compound and being capable of releasing it gradually and in controlled fashion to the body fluids, and being of a size to be retained for a period of time long enough to provide an effective dose of the pharmaceutical compound to the site of placement for an extended period of time. The microparticles ultimately dissolve in the body fluids.
Inventors
- 👤 John Weldon Shell
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 23:23
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0048; A61K9/0051; A61F; A61F9/00; A61F9/0008; A61F9/0017; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/1658; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5031
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
50 words
A composition for controlled release of a drug contained therein to a body fluid, said composition comprising an external matrix rapidly soluble in said body fluid, and bioerodible microparticles dispersed in said external matrix, said microparticles containing said drug and being capable of releasing it gradually to said body fluid.
Claim 2
Dependent Claim
50 words
A composition for controlled release of a drug contained therein to a body fluid, said composition comprising an external matrix rapidly soluble in said body fluid, and bioerodible microparticles dispersed in said external matrix, said microparticles containing said drug and being capable of releasing it gradually to said body fluid.
Claim 3
Dependent Claim
88 words
The composition of claim 1, which comprises an ocular dosage form for controlled release of the drug to the tear fluid of a mammalian eye, wherein said external matrix is rapidly soluble in said tear fluid of the eye, said microparticles are capable of releasing the drug gradually to said tear fluid, and said microparticles are of a size to be retained in the eye for a period of time long enough to provide an effective dose of the drug over an extended time period to the eye.
Claim 4
Dependent Claim
22 words
The composition of claim 2 wherein said microparticles have a dimension ranging from about 50 microns to about 2 mm in diameter.
Claim 5
Dependent Claim
24 words
The composition of any one of claims 1 to 3 wherein said microparticles comprise a drug dispersed within a bioerodible release rate controlling matrix.
Claim 6
Dependent Claim
29 words
The composition of claim 3 wherein said release rate controlling matrix is selected from the group consisting of poly(lactic acid), poly(beta-hydroxybutyrate), cross-linked alginate, cross-linked gelatin, and a bioerodible carbohydrate.
Claim 7
Dependent Claim
15 words
The composition of claim 3, wherein said release rate controlling matrix is a poly(ortho ester).
Claim 8
Dependent Claim
28 words
The composition of claim 6, wherein said poly(ortho ester) is of the following formula: wherein n is the degree of polymerization and is from about 10 to 1000.
Claim 9
Dependent Claim
75 words
The composition of any one of claims 1 to 7 wherein said drug is selected from the group consisting of anti-inflammatory agents; carbonic anhydrase inhibitors; beta-adrenergic blocking agents; antiglaucoma agents, and combinations of any of the foregoing; antibiotics; or combinations of anti-inflammatory and antibiotic agents; antiviral agents; combinations of anti-glaucoma and alpha-adrenergic blocking agents; diuretics; aldoseredutase inhibitors; mast cell stabilizers; agents to enhance wound healing; immunosuppressive agents; non-steriodal anti-inflammatory agents; alpha andrenergic agonists; and mydriatics.
Claim 10
Dependent Claim
34 words
The composition of claim 8 wherein said pharmaceutical compound is fluorometholone, acetazolamide, metipranolol, pilocarpine, epinephrine, vancomycin, penicillin, chloromphenicol, thymoxamine, triamterene, sorbinil, sodium cromoglycate, fibronectin, epidermal growth factor, cyclosporin A, indomethacin, ketorolac, clonidine, or atropine.
Claim 11
Dependent Claim
43 words
A process for the production of a composition of any one of claims 1 to 9 comprising incorporating said drug into microparticles of a controlled release composition and suspending said microparticles in a solid matrix which is readily soluble in said body fluid.
References Cited (Backward Citations)
No citation records indexed.
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