Details for Patent: 9,555,047

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)
Filing Date:	Aug 18, 2014
Application Number:	14/461,883
Claims:	1. A method of manufacturing 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 microparticle and wherein the PLGA has the following characteristics: (i) a molecular weight in the range or about 40 to 70 k Da; and (ii) a lactic acid: glycolic acid molar ratio of 80:20 to 60:40, the method comprising: (a) dispersing the TCA and the poly(laclic-co-glycolic) acid copolymer in an organic solution to produce a TCA-PLGA mixture, wherein the PLGA has a molecular weight in the range of about 40 to 70 kDa and a lactic acid: glycolic acid molar ratio of 80:20 to 60:40, and wherein the ratio of TCA to PLGA to organic solution in the TCA-PLGA mixture is 1:3:57; (b) atomizing the TCA-PLGA mixture into micro-droplets by adding the TCA-PLGA mixture to a spinning disk; and (c) treating the TCA-PLGA mixture to remove the solvent, thereby producing an injectable formulation comprising controlled- or sustained-release microparticle comprising TCA or a pharmaceutically-acceptable salt thereof and a 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 or about 40 to 70 k Da; and (ii) a lactic acid: glycolic acid molar ratio of 80:20 to 60:40. 2. The method of claim 1, wherein step (c) comprises a solvent evaporation process to remove the solvent. 3. The method of claim 2, wherein the solvent evaporation process utilizes a drying chamber. 4. The method of claim 1, wherein the solvent is dichloromethane. 5. The method of claim 1 further comprising step (d) collecting the controlled- or sustained-release microparticles using a cyclone separator. 6. The method of claim 5 further comprising step (e) using a secondary drying step to remove residual solvents. 7. The method of claim 6 further comprising step (f) sieving the collected controlled- or sustained-release microparticles. 8. The method of clam 7, wherein step (f) uses a 150 .mu.m sieve. 9. The method of claim 1, wherein the spinning disk rotates at a speed of approximately 3300 rpm inside temperature controlled chamber maintained at 38-45.degree. C.