Pharmaceutical compositions suitable for articular delivery and use thereof in treatment of joint pain
Inventors
TSENG, Yun-Long • Shih, Sheue-Fang • Chang, Po-Chun • CHANG, Lo
Assignees
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Publication Number
US-12208104-B2
Publication Date
2025-01-28
Expiration Date
Abstract
The present disclosure relates to pharmaceutical composition for the treatment of joint pain. The composition contains a lipid mixture comprising one or more phospholipids; and an effective amount of a therapeutic agent or a pharmaceutically acceptable salt thereof, where the total amount of phospholipids in said composition is about 20 mM to about 150 mM, optionally 70 mM to 110 mM. Also provided is the use of the pharmaceutical composition in the treatment of joint pain by articular injection.
Core Innovation
The invention relates to an articular-injection pharmaceutical composition for treating joint pain. The composition comprises a lipid mixture containing one or more phospholipids and an effective amount of a steroid or a pharmaceutically acceptable salt thereof. The total amount of the one or more phospholipids is about 60 μmol to about 150 μmol per 1 mL of the pharmaceutical composition.
The core parameter of the invention is constraining the phospholipid amount per 1 mL to about 60 μmol to about 150 μmol, with an optionally discussed range of about 70 μmol to about 110 μmol, to enhance efficacy and sustain release while minimizing side effects compared with compositions having more than 150 μmol. The composition is presented as providing sustained therapeutic efficacy and as being associated with reduced adverse effects, including minimized cartilage/chondrotoxicity and an improved cortisol profile.
The disclosure further supports the claimed approach with representative formulation options for the lipid mixture, including liposomes, optional cholesterol or sterol, and excipients. Supporting data are described as showing phospholipid dose-dependent release control of dexamethasone sodium phosphate, with sustained improvements reported for knee osteoarthritis assessments, and a linkage described in an animal model between lipid/phospholipid content and prolonged anti-arthritic effectiveness.
Claims Coverage
The independent claim provides a pharmaceutical composition for treating joint pain with two key inventive elements: a lipid mixture of one or more phospholipids and an effective amount of a steroid or a pharmaceutically acceptable salt, with the phospholipid amount constrained per mL. Dependent claims refine the steroid type, lipid composition, phospholipid range, steroid concentration, and the enumerated arthritic, inflammatory, and autoimmune indications.
Phospholipid-constrained lipid mixture with steroid for joint pain treatment
A pharmaceutical composition comprising a lipid mixture comprising one or more phospholipids and an effective amount of a steroid or a pharmaceutically acceptable salt thereof, wherein the total amount of the one or more phospholipids is about 60 μmol to about 150 μmol per 1 mL.
Intra-articular corticosteroid for joint pain
The pharmaceutical composition is characterized in that the steroid is an intra-articular corticosteroid.
DOPC and DOPG phospholipid mixture
The lipid mixture contains DOPC and DOPG.
Tighter phospholipid range per mL
The pharmaceutical composition comprises one or more phospholipids at an amount ranging from about 70 μmol to about 120 μmol per mL.
Dexamethasone sodium phosphate concentration range per mL
Dexamethasone sodium phosphate is present at about 8 mg to about 18 mg per mL.
Enumerated arthritic and inflammatory/autoimmune indications
The pharmaceutical composition is specified for treating osteoarthritis, rheumatoid arthritis, infectious arthritis, psoriatic arthritis, acute gouty arthritis, reactive arthritis, arthritis caused by Ehlers-Danlos Syndrome, haemochromatosis, hepatitis, Lyme disease, Sjogren's disease, Hashimoto's thyroiditis, celiac disease, non-celiac gluten sensitivity, inflammatory bowel disease, Henoch-Schönlein purpura, Hyperimmunoglobulinemia D with recurrent fever, sarcoidosis, Whipple's disease, TNF receptor associated periodic syndrome, Granulomatosis with polyangiitis, familial Mediterranean fever, and systemic lupus erythematosus.
Overall claim coverage centers on a joint-pain pharmaceutical composition combining a steroid with a phospholipid-containing lipid mixture while constraining total phospholipid amount per 1 mL to the claimed range, with further refinements specifying intra-articular corticosteroids, particular phospholipids, tighter phospholipid and dexamethasone sodium phosphate concentration ranges, and an enumerated set of arthritic, inflammatory, and autoimmune indications.
Stated Advantages
Enhance efficacy and sustain release.
Minimize side effects compared with compositions with more than 150 μmol phospholipids.
Reduced adverse effects, including minimized cartilage/chondrotoxicity.
Improved cortisol profile.
Sustained therapeutic efficacy reported up to about 3–6 months.
Documented Applications
Treatment of joint pain, including knee osteoarthritis, with sustained improvements in VAS pain score and WOMAC through weeks 12–24, with monitored safety including cortisol reduction.
Use in an animal model of collagen-induced arthritis rat, described as relating lipid/phospholipid content to prolonged anti-arthritic effectiveness.
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