Corticosteroids for the treatment of joint pain

a technology of corticosteroids and joint pain, which is applied in the direction of anti-inflammatory agents, drug compositions, immunological disorders, etc., can solve the problems of affecting the treatment effect of pain and/or inflammation, affecting the treatment effect, so as to reduce pain and/or inflammation, reduce the effect of long-term side effects and minimal side effects

Inactive Publication Date: 2012-11-08
FLEXION THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]Described herein are compositions and methods for the treatment of pain and inflammation using corticosteroids. The compositions and methods provided herein use one or more corticosteroids in a microparticle formulation. The corticosteroid microparticle formulations provided herein are effective at treating pain and/or inflammation with minimal long-term side effects of corticosteroid administration, including for example, prolonged suppression of the HPA axis. The corticosteroid microparticle formulations are suitable for administration, for example, local administration by injection into a site at or near the site of a patient's pain and/or inflammation. The corticosteroid microparticle formulations provided herein are effective in slowing, arresting, reversing or otherwise inhibiting structural damage to tissues associated with progressive disease with minimal long-term side effects of corticosteroid administration, including for example, prolonged suppression of the HPA axis. The corticosteroid microparticle formulations are suitable for administration, for example, local administration by injection into a site at or near the site of structural tissue damage. As used herein, “prolonged” suppression of the HPA axis refers to levels of cortisol suppression greater than 35% by day 14 post-administration

Problems solved by technology

The administration of corticosteroids, particularly for extended periods of time, can have a number of unwanted side effec

Method used

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  • Corticosteroids for the treatment of joint pain
  • Corticosteroids for the treatment of joint pain
  • Corticosteroids for the treatment of joint pain

Examples

Experimental program
Comparison scheme
Effect test

example 1

Sustained-Release Betamethasone or Triamcinolone Acetonide Microparticles

[0225]In one embodiment, the microparticle formulation contains a copolymer of DL-lactide (or L-lactide) and glycolide in a 45:55 molar ratio (up to 75:25 molar ratio) with an inherent viscosity ranging from 0.15 to 0.60 dL / g with either an ester or acid end group plus either the corticosteroid betamethasone or triamcinolone acetonide. If betamethasone is used, then the betamethasone is in the form of either betamethasone acetate, betamethasone diproprionate or a combination thereof. The total amount of betamethasone or triamcinolone acetonide incorporated into the microparticle ranges from 10% to 30% (w / w). The microparticles are formulated to mean mass range in size from 10 to 100 microns. The population of microparticles is formulated to be delivered through a 19 gauge or higher needle. Additional excipients may be added such as, but not limited to, carboxymethylcellulose sodium, mannitol, polysorbate-80, so...

example 2

Sustained-Release Betamethasone or Triamcinolone Acetonide Microparticles with an Immediate Release Form

[0226]In another embodiment, the microparticle formulation of Example 1 is further admixed with an immediate release betamethasone or triamcinolone acetonide component, such as a betamethasone or triamcinolone acetonide containing solution. If betamethasone is used, then the betamethasone in the immediate release component is in the form of either betamethasone acetate, betamethasone diproprionate or a combination thereof. If betamethasone is used, then the immediate release component provides an initial release of a total of about 5 to 20 mg of betamethasone over the first 1-10 days, while the sustained release component releases betamethasone at a rate of about 0.1 to 1.0 mg / day over the first 14 to 90 days following administration. If triamcinolone acetonide is used, then the immediate release component provides an initial release of a total of 10 to 40 mg of drug over the firs...

example 3

Determination of Time-Variance in HPA Axis Sensitivity

[0227]Adult volunteers (N=4 to 9 per group) give appropriate informed consent. Each individual in each group receives a single intra-articular administration of an exogenous corticosteroid (triamcinolone acetonide 40 mg; triamcinolone hexacetonide 20; betamethasone 7 mg (disodium phosphate 4 mg / acetate 3 mg). Blood samples for measurement of corticosteroid concentrations and / or cortisol concentrations are drawn at 8 AM at baseline and on days 1, 7, 9, 10, 12, 14, 18, and 21. The extent of suppression of endogenous cortisol was measured in each subject in each group. The extent of cortisol suppression predicted by previously published models (Meibohm, 1999) was determined and compared to observations (FIG. 4 Column 1). The change (decrease) in HPA axis sensitivity vs. time is then determined on a day-by-day and final basis (FIG. 4, Column 2), permitting determination of the correct steady-state intra-articular doses of corticoster...

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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.

Description

RELATED APPLICATIONS[0001]This application is a continuation-in-part of U.S. patent application Ser. No. 13 / 198,168, filed Aug. 4, 2011, which claims the benefit of U.S. Provisional Application No. 61 / 370,666, filed Aug. 4, 2010. The contents of each application are hereby incorporated by reference in their entirety.FIELD OF THE INVENTION[0002]This invention relates to the use of corticosteroids to treat pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and to slow, arrest or reverse 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. More specifically, a corticosteroid is 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.BACKGROUND OF ...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P25/00A61P29/00A61K9/14
CPCA61K9/0019A61K9/0024A61K9/1641A61K9/1647A61K9/14A61K31/573A61K31/58A61K47/34A61K9/1694A61P19/00A61P19/02A61P19/06A61P25/00A61P25/04A61P29/00A61P37/06A61P43/00A61P5/44A61K47/50A61K9/00A61K9/16A61K9/1682
Inventor BODICK, NEILBLANKS, ROBERT C.KUMAR, ANJALICLAYMAN, MICHAEL D.MORAN, MARK
Owner FLEXION THERAPEUTICS
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