Sustained release intraocular implants and related methods

• US 8,119,154 B2
• Filed: 04/30/2004
• Issued: 02/21/2012
• Est. Priority Date: 04/30/2004
• Status: Active Grant

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Huang, Glenn T., Nivaggioli, Thierry
• Primary Examiner(s): Azpuru, Carlos
• Application Number:
  US10/837,356
• Publication Number:
  US 20050244468A1
• Time in Patent Office: 2,853 Days
• Field of Search: None
• US Class Current: 424/428
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61K 9/0092 Hollow drug-filled fibres, tubes of the core-shell type, coated fibres, coated rods, microtubules or nanotubes
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics

Abstract

Biocompatible intraocular implants include a steroid and a polymer associated with each other to facilitate release of the steroid into an eye for a period of time greater than about two months. The steroid may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants may be placed in an eye to treat one or more ocular conditions. The steroid is released from the implant for more than about two months, and may be release for more than several years.

Claims

1. A biodegradable intraocular implant comprising a steroid associated with a biodegradable polymer matrix including a first biodegradable polymer comprising a poly(lactide-co-glycolide) co-polymer having terminal acid groups and a second biodegradable polymer comprising a polylactide polymer having terminal acid groups;

wherein the steroid is a fluocinolone, a triamcinolone, or a mixture thereof; and

wherein the steroid is released at a rate effective to sustain release of a therapeutically effective amount of the steroid from the implant for a time greater than about two months from a time in which the implant is placed in an ocular site or region of an eye.

2. The implant of claim 1, further comprising an ophthalmically acceptable therapeutic agent in addition to the steroid.

3. The implant of claim 1, wherein the steroid is dispersed within the biodegradable polymer matrix.

4. The implant of claim 1, wherein the polylactide polymer is a poly (D,L-lactide) polymer.

5. The implant of claim 1, wherein the steroid is released at a rate effective to sustain release of a therapeutically effective amount of the steroid from the implant for more than three months from the time the implant is placed in the vitreous of the eye.

6. The implant of claim 1, wherein the steroid is released at a rate effective to sustain release of a therapeutically effective amount of the steroid from the implant for more than four months from the time the implant is placed in the vitreous of the eye.

7. The implant of claim 1, wherein the steroid is fluocinolone, and wherein fluocinolone is released at a rate effective to sustain release of a therapeutically effective amount of fluocinolone for about three months.

8. The implant of claim 1, wherein the steroid is triamcinolone, and wherein triamcinolone is released at a rate effective to sustain release of a therapeutically effective amount of triamcinolone for more than three months.

9. The implant of claim 8, wherein triamcinolone is released at a rate effective to sustain release of a therapeutically effective amount of triamcinolone for about three months to about six months.

10. The implant of claim 1, wherein the poly(lactide-co-glycolide) co-polymer is a fast degrading co-polymer.

11. The implant of claim 1, wherein the polylactide polymer is a slow degrading polymer.

12. The implant of claim 1, wherein the polylactic acid polymer has a molecular weight of less than 40 kD.

13. The implant of claim 1, wherein each of the first and second biodegradable polymers has an inherent viscosity in a range of about 0.16 dl/g to about 0.24 dl/g.

14. The implant of claim 13, wherein each of the first and second biodegradable polymers has an inherent viscosity of about 0.2 dl/g.

15. The implant of claim 1 which is formed by an extrusion process.

16. The implant of claim 1, wherein the poly(lactide-co-glycolide) co-polymer is a poly(D,L-lactide-co-glycolide) co-polymer.

17. The implant of claim 1, wherein the percent of polylactide in the poly(lactide-co-glycolide) co-polymer is from about 15% to about 85%.

18. The implant of claim 1, wherein the biodegradable polymer matrix comprises a 1:

1 ratio of the first biodegradable polymer and the second biodegradable polymer.

19. A biodegradable intraocular implant comprising a steroid associated with a biodegradable polymer matrix including a first biodegradable polymer comprising a poly(lactide-co-glycolide) co-polymer having terminal free acid groups and a second biodegradable polymer comprising a polylactide polymer having terminal free acid groups;

wherein the steroid is a fluocinolone, a triamcinolone, or a mixture thereof; and

wherein the steroid is released at a rate effective to sustain release of a therapeutically effective amount of the steroid from the implant for a time greater than about two months from a time in which the implant is placed in an ocular site or region of an eye.