Claims for Patent: 9,555,048

Summary for Patent: 9,555,048

Title:	Corticosteroids for the treatment of joint pain
Abstract:	Corticosteroid microparticle formulations are provided for use for treating pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and for slowing, arresting or reversing structural damage to tissues caused by an inflammatory disease, for example damage to articular and/or peri-articular tissues caused by osteoarthritis or rheumatoid arthritis. Corticosteroid microparticle formulations are administered locally as a sustained release dosage form (with or without an immediate release component) that results in efficacy accompanied by clinically insignificant or no measurable effect on endogenous cortisol production.
Inventor(s):	Bodick; Neil (Boston, MA), Blanks; Robert C. (Auburndale, MA), Kumar; Anjali (Belmont, MA), Clayman; Michael D. (Gloucester, MA), Moran; Mark (Orinda, CA)
Assignee:	FLEXION THERAPEUTICS, INC. (Burlington, MA)
Application Number:	14/461,884
Patent Claims:	1. A method of treating pain or inflammation in a patient comprising administering to said patient a therapeutically effective amount of an injectable formulation comprising controlled- or sustained-release microparticles comprising triamcinolone acetonide (TCA) or a pharmaceutically-acceptable salt thereof and a poly(lactic-co-glycolic) acid copolymer (PLGA) matrix, wherein the TCA comprises between 22% to 28% of the microparticles and wherein the PLGA has the following characteristics: (i) a molecular weight in the range of about 40 to 70 kDa; and (ii) a lactic acid:glycolic acid molar ratio of 80:20 to 60:40. 2. The method of claim 1, wherein the PLGA copolymer has a molar ratio of lactic acid:glycolic acid of 75:25. 3. The method of claim 1, wherein the injectable formulation further comprises a pharmaceutically acceptable excipient. 4. The method of claim 1, wherein the injectable formulation is administered as one or more intra-articular injections. 5. The method of claim 3, wherein the injectable formulation is administered as one or more intra-articular injections. 6. The method of claim 1, wherein the TCA is released for between at least 14 days and 90 days upon administration to a joint. 7. The method of claim 6, wherein the formulation releases the corticosteroid for at least 14 days at a rate that does not adversely suppress the hypothalamic-pituitary-adrenal axis (HPA axis). 8. The method of claim 1, wherein the 22% to 28% of TCA in the microparticles comprises a total TCA load dose between 10 to 50 mg. 9. The method of claim 1, wherein the lactic acid-glycolic acid copolymer has an inherent viscosity in the range of 0.3 to 0.5 dL/g. 10. The method of claim 1, wherein the microparticles have a mean diameter of between 10 .mu.m to 100 .mu.m. 11. The method of claim 1, wherein the microparticles further comprise a polyethylene glycol (PEG) moiety, wherein the PEG moiety comprises between 25% to 0% weight percent of the microparticle. 12. The method of claim 1, wherein the subject is human. 13. The method of claim 1, wherein the subject has osteoarthritis, rheumatoid arthritis, gouty arthritis, juvenile arthritis, psoriatic arthritis, ankylosing spondylitis, or synovitis. 14. The method of claim 1, wherein the subject has a joint disorder of a joint tissue. 15. The method of claim 14, wherein the subject has acute bursitis, sub-acute bursitis, acute nonspecific tenosynovitis, epicondylitis, or Morton's neuroma. 16. The method of claim 1, wherein the subject has radicular pain, neurogenic claudication secondary to lumbar spinal stenosis, or back pain. 17. The method of claim 16, wherein the radicular pain is selected from sciatica, radicular pain of the arm, radicular pain of neck, radicular pain of lumbar, and radicular pain of thorax. 18. The method of claim 1, where in the subject has a disorder of the dermal tissue. 19. The method of claim 18, wherein the subject has alopecia areata, discoid lupus, erythematosus, keloids, localized hypertrophic, infiltrated inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus (neurodermatitis), psoriasis, psoriatic plaques, or necrobiosis lipoidica diabeticorum. 20. The method of claim 1, wherein the subject has asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, seasonal or perennial allergic rhinitis, serum sickness, transfusion reactions, bullous dermatitis herpetiformis, exfoliative dermatitis, mycosis fungoides, pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), primary or secondary adrenocortical insufficiency in conjunction with mineralocorticoids, congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsupportive thyroiditis, exacerbations of regional enteritis and ulcerative colitis, acquired (autoimmune) hemolytic anemia, congenital (erythroid), hypoplastic anemia (Diamond blackfan anemia), pure red cell aplasia, secondary thrombocytopenia, trichinosis with neurologic or myocardial involvement, tuberculosis meningitis with subarachnoid block or impending block, palliative management of leukemias and lymphomas, acute exacerbations of multiple sclerosis, cerebral edema associated with primary or metastatic brain tumor or craniotomy, proteinuria in idiopathic nephrotic syndrome, proteinuria in lupus erythematosus, berylliosis, symptomatic sarcoidosis, fulminating or disseminated pulmonary tuberculosis, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis, dermatomyositis, polymyositis, systemic lupus erythematosus, or postoperative pain and swelling.