Ophthalmic compositions and methods for treating ophthalmic conditions

• US 20060009498A1
• Filed: 07/11/2005
• Published: 01/12/2006
• Est. Priority Date: 07/12/2004
• Status: Abandoned Application

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Whitcup, Scott M.
• Application Number:
  US11/180,752
• Publication Number:
  US 20060009498A1
• Time in Patent Office: Days
• US Class Current: 514/357
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0024 Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 33/02 Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component. The composition is in a fluid form before placement in the interior of an eye, and becomes less fluid after the composition is placed in the eye to form an extended or delayed release drug delivery element or system. The drug delivery element is formed by the dissipation of the solvent from the composition when the composition is placed in the interior of an eye. One example of a composition includes triamcinolone acetonide as a therapeutic agent. A method of treating an ophthalmic condition, or otherwise improving or enhancing vision of a patient, comprises placing the fluid composition in the interior of the eye. The method may be practiced by injecting the fluid composition into the interior of the eye.

Claims

1. An ophthalmic composition useful for intraocular placement in an eye of a human or animal comprising:

a corticosteroid component present in a therapeutically effective amount;

a biocompatible polymeric component in an amount effective to delay release of the corticosteroid component into the interior of the eye after the composition is intraocularly placed in the eye; and

an ophthalmically compatible solvent component in an amount effective to solubilize the polymeric component, the composition being effective, after being intraocularly placed into the interior of the eye, to form a delayed release composition effective to delay the release of the corticosteriod component in the eye relative to intraocular placement of a substantially identical composition without the polymeric component.

2. The composition of claim 1 wherein the solvent component is effective to dissipate after the composition is placed into the eye.

3. The composition of claim 1 wherein the corticosteroid component is soluble in the composition.

4. The composition of claim 1 wherein the corticosteroid component is insoluble in the composition.

5. The composition of claim 1 wherein the corticosteroid component is selected from the group consisting of alclometasone dipropionate, amcinonide, amcinafel, amcinafide, beclamethasone, betamethasone, betamethasone dipropionate, betamethasone valerate, clobetasone propionate, chloroprednisone, clocortelone, cortisol, cortisone, cortodoxone, difluorosone diacetate, descinolone, desonide, defluprednate, dihydroxycortisone, desoximetasone, dexamethasone, deflazacort, diflorasone, diflorasone diacetate, dichlorisone, esters of betamethasone, fluazacort, flucetonide, flucloronide, fludrotisone, fluorocortisone, flumethasone, flunisolide, fluocinonide, fluocinolone, fluocinolone acetonide, flucortolone, fluperolone, fluprednisolone, fluroandrenolone acetonide, fluocinolone acetonide, flurandrenolide, fluorametholone, fluticasone propionate, hydrocortisone, hydrocortisone butyrate, hydrocortisone valerate, hydrocortamate, loteprendol, medrysone, meprednisone, methylprednisone, methylprednisolone, mometasone furoate, paramethasone, paramethasone acetate, prednisone, prednisolone, prednidone, triamcinolone acetonide, triamcinolone hexacatonide, and triamcinolone, salts thereof, derivatives thereof, and mixtures thereof.

6. The composition of claim 1 wherein the corticosteroid component is triamcinolone acetonide.

7. The composition of claim 1 wherein the polymeric component is effective, after the composition is placed in the eye, to be included in a solid or gelatinous polymer matrix.

8. The composition of claim 7 wherein the polymer matrix is microporous.

9. The composition of claim 7 wherein the polymer matrix is biocompatible.

10. The composition of claim 1 wherein the polymeric component comprises a water coagulable polymer material.

11. The composition of claim 10 wherein the polymer material is a thermoplastic polymer material.

12. The composition of claim 1 wherein the polymeric component is selected from the group consisting of polylactides, polyglycolides, polycaprolactones, polyanhydrides, polyamides, polyurethanes, polyesteramides, polyorthoesters, polydioxanones, polyacetals, polyketals, polycarbonates, polyorthoesters, polyphosphazenes, polyhydroxybutyrates, polyhydroxyvalerates, polyalkylene oxalates, polyalkylene succinates, poly(malic acid), poly(amino acids), poly(methyl vinyl ether), poly(maleic anhydride), chitin, chitosan, copolymers thereof, combinations thereof and mixtures thereof.

13. The composition of claim 1 wherein the polymeric component is selected from the group consisting of poly lactic acid, poly glycolic acid, poly lactic acid/glycolic acid and mixtures thereof.

14. The composition of claim 1 wherein the solvent component is non-aqueous.

15. The composition of claim 1 wherein the solvent component is water-miscible.

16. The composition of claim 1 wherein the solvent component is organic.

17. The composition of claim 1 wherein the solvent is liquid.

18. The composition of claim 1 wherein the solvent component is selected from the group consisting of dimethyl sulfoxide, methyl-2-pyrrolidone, 2-pyrrolidone, C₂ to C₆ alkanols, propylene glycol, acetone, alkyl esters such as methyl acetate, ethyl acetate, ethyl lactate, alkyl ketones such as methyl ethyl ketone, dialkylamides such as dimethylformamide, dimethyl sulfoxide, dimethyl sulfone, tetrahydrofuran, cyclic alkyl amides such as caprolactam, decylmethylsulfoxide, oleic acid, propylene carbonate, aromatic amides such as N,N-diethyl-m-toluamide, 1-dodecylazacycloheptan-2-one, and the like. Preferred solvents according to the invention include N-methyl-2-pyrrolidone, 2-pyrrolidone, dimethyl sulfoxide, ethyllactate, propylene carbonate and mixtures thereof.

19. The composition of claim 18 wherein the solvent component comprises dimethyl sulfoxide.

20. The composition of claim 1 which includes no preservative component.

21. The composition of claim 1 which includes a preservative component.

22. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 1 into the interior of the eye of the human or animal.

23. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 2 into the interior of the eye of the human or animal.

24. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 5 into the interior of the eye of the human or animal.

25. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 6 into the interior of the eye of the human or animal.

26. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 7 into the interior of the eye of the human or animal.

27. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 10 into the interior of the eye of the human or animal.

28. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 11 into the interior of the eye of the human or animal.

29. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 13 into the interior of the eye of the human or animal.

30. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 14 into the interior of the eye of the human or animal.

31. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 18 into the interior of the eye of the human or animal.

32. A method of treating a condition of an eye of a human or animal comprising intraocularly placing the composition of claim 19 into the interior of the eye of the human or animal.