LOW IMMUNOGENICITY CORTICOSTEROID COMPOSITIONS

• US 20070224278A1
• Filed: 04/27/2007
• Published: 09/27/2007
• Est. Priority Date: 11/12/2003
• Status: Abandoned Application

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Chang, James, Robinson, Michael, Whitcup, Scott, Lyons, Robert, Trogden, John, Lam, Sam
• Application Number:
  US11/741,366
• Publication Number:
  US 20070224278A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• 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 31/715 Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• CPC Class Codes: A61K 47/02 Inorganic compounds
• 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 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 47/40 Cyclodextrins; Derivatives thereof
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Triamcinolone compositions, and methods of using such compositions, useful for injection into the vitreous of human eyes or into a joint are provided. Such compositions can include triamcinolone particles present in a therapeutically effective amount, a viscosity inducing component, and an aqueous carrier component. The compositions have viscosities of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity is in the range of from about 80,000 cps to about 300,000 cps. In a most preferred embodiment, the viscosity is in the range of from about 140,000 cps to about 280,000 cps t a shear rate of 0.1/second at 25° C. The compositions advantageously suspend the triamcinolone particles for prolonged periods of time.

Claims

1. A pharmaceutical composition for treating a posterior ocular condition, the pharmaceutical composition comprising:

(a) a plurality of corticosteroid particles mixed with;

(b) a viscous polymer, wherein the pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C., and the pharmaceutical composition can be injected into the vitreous of a human eye through a 25 to 33 gauge needle.

2. The pharmaceutical composition of claim 1, wherein the corticosteroid particles have a substantially uniform diameter.

3. The pharmaceutical composition of claim 1, wherein substantially all the corticosteroid particles are embedded within the viscous polymer.

4. The pharmaceutical composition of claim 1, wherein the corticosteroid is a triamcinolone.

5. The pharmaceutical composition of claim 1, wherein the viscous polymer is a polymeric hyaluronate or a polymeric hyaluronic acid.

6. A pharmaceutical composition for treating a posterior ocular condition, the composition comprising:

(a) a plurality of triamcinolone particles with a substantially uniform diameter, and;

(b) a viscous polymeric hyaluronate or polymeric hyaluronic acid, wherein the pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C. and can be injected into the vitreous of a human eye through a 25 to 33 gauge needle, wherein the triamcinolone particles are mixed with the viscous polymer substantially all the corticosteroid particles are embedded within and coated by the viscous polymeric hyaluronate or a polymeric hyaluronic acid.

7. A method for treating a posterior ocular condition, the method comprising the step of injecting into the vitreous of a patient'"'"'s eye with a posterior ocular condition a viscous pharmaceutical composition comprising a plurality of corticosteroid particles mixed into a viscous polymeric matrix, wherein the pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C., such that about one hour after the intravitreal injection only about 10% or less of the corticosteroid particles are present in the vitreous free of the polymeric matrix.

8. The method of claim 7, wherein about one hour after the intravitreal injection only about 5% or less of the corticosteroid particles are present in the vitreous free of the is polymeric matrix.

9. The method of claim 7, wherein about one hour after the intravitreal injection only about 3% or less of the corticosteroid particles are present in the vitreous free of the polymeric matrix.

10. A process for making an intraocular pharmaceutical composition, the method comprising the step of mixing an aqueous suspension of a plurality of corticosteroid particles and an aqueous solution of a viscous polymeric matrix, so that the resulting pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C.

11. The process of claim 10, wherein the corticosteroid particles have a median particle size of between about 4 microns and about 5 microns.

12. The process of claim 10, wherein the corticosteroid particles have a stable diameter for at least three months after the pharmaceutical has been made and stored for three months in a syringe placed horizontally at about 25°

C. at about 60% relative humidity.

13. The pharmaceutical composition made by the method of claim 10.

14. A pharmaceutical composition for treating an articular pathology, the pharmaceutical composition comprising:

(a) a plurality of corticosteroid particles mixed with;

(b) a viscous polymer, wherein the pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C.,

15. A method for treating an articular pathology, the method comprising the step of is injecting into a joint of a patient with an articular pathology a viscous pharmaceutical composition comprising a plurality of corticosteroid particles mixed into a viscous polymeric matrix, wherein the pharmaceutical composition has a viscosity of between about 130,000 cps and about 300,000 cps at a shear rate of about 0.1/second at about 25°

C.