Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Corticosteroids for the Treatment of Joint Pain

a technology of corticosteroids and joint pain, which is applied in the direction of drug compositions, immune disorders, nervous 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: 2014-08-28
FLEXION THERAPEUTICS
View PDF7 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a way to treat pain and inflammation using microparticle formulations of corticosteroids. These formulations provide effective treatment with minimal side effects of corticosteroid administration, including HPA suppression. The corticosteroid microparticle formulations are delivered through injection into the site of pain or inflammation. The formulations provide both an immediate and sustained release of the corticosteroid, with the levels of cortisol suppression negligible by day 14 post-injection. The combination of an immediate release and a sustained release form of corticosteroids can provide both immediate and long-term therapy. Overall, the corticosteroid microparticle formulations provide a safer and effective treatment for pain and inflammation.

Problems solved by technology

The administration of corticosteroids, particularly for extended periods of time, can have a number of unwanted side effects.
The HPA axis may be suppressed by the administration of corticosteroids, leading to a variety of unwanted side effects.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0224]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

[0225]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

[0226]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 (FIGS. 4A, 4C and 4E). The change (decrease) in HPA axis sensitivity vs. time is then determined on a day-by-day and final basis (FIGS. 4B, 4D and 4F), permitting determination of the correct steady-state intra-articular doses of cort...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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 of U.S. Ser. No. 13 / 368,580, filed Feb. 8, 2012, which is a continuation-in-part of U.S. Ser. No. 13 / 198,168, filed Aug. 4, 2011, which claims priority and the benefit of U.S. Ser. 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 ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/58
CPCA61K31/58A61K9/0019A61K9/1641A61K9/1647A61K9/1694A61K31/573A61K9/0024A61P19/00A61P19/02A61P19/06A61P25/00A61P25/04A61P29/00A61P37/06A61P43/00A61P5/44A61K47/34A61K47/50A61K9/00A61K9/14A61K9/16A61K9/1682
Inventor BODICK, NEILBLANKS, ROBERT C.KUMAR, ANJALICLAYMAN, MICHAEL D.MORAN, MARK
Owner FLEXION THERAPEUTICS
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com