Compositions for treating joint or connective tissue disease comprising dextran or poloxamer

Inventors

Park, Yoo Sin • Lee, Il Hoon

Assignees

Medicine Park Co Ltd

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Publication Number

US-11801260-B2

Patent

Publication Date

2023-10-31

Expiration Date


Abstract

Disclosed is a composition for treating a joint disease or a connective tissue disease, a composition for cartilage regeneration, or a composition for treating an inflammatory disease, each of the compositions containing dextran, poloxamer or a mixture thereof. The composition stays in the joint or connective tissue for a long time due to the shock-absorbing effect, coating effect or anti-inflammation effect, relieves the shock, covers a damaged portion in a specific manner thereto, or reduces inflammation of an adhered portion. Thus, the composition may be useful for the treatment of the joint disease, the connective tissue disease, or for the cartilage regeneration.

Core Innovation

The patent discloses pharmaceutical compositions for joint or connective tissue diseases and for cartilage regeneration using dextran and/or poloxamer 188. The compositions are described as persisting at a lesion due to shock-absorbing and cushioning, coating, and anti-inflammation effects. The dextran is described as including low–intermediate molecular weight fractions, including “dextran 1” and “dextran 5,” together with poloxamer 188.

Dextran and poloxamer 188 compositions are described in relation to anti-inflammatory effects and cartilage breakdown inhibition, with endpoints including IL-10/IL-6 ratio changes and MMP-3 and MMP-13 expression changes. The document further describes cartilage regeneration endpoints involving type II collagen and aggrecan production. The patent presents that dextran generally supports chondrocyte proliferation, while poloxamer 188 alone may be cytotoxic at higher concentrations.

The disclosed compositions emphasize that appropriate dextran/poloxamer 188 mixtures improve anti-inflammatory and cartilage-regenerative outcomes. Mixture ratios are described, including combinations of dextran 1 + dextran 5 and mixtures of dextran with poloxamer 188. The patent frames the approach as administering compositions to a subject in need to regenerate or protect cartilage.

Claims Coverage

The independent claim is directed to a method for regenerating or protecting cartilage by administering a composition containing dextran with a defined average molecular weight range. The independent claim is refined by inventive features that further specify dextran molecular-weight sub-ranges, dextran concentration ranges, and additional components and functions including poloxamer 188 and inflammation inhibition.

Dextran average molecular weight range for cartilage regeneration or protection

A method of regenerating or protecting of a cartilage by administering to a subject a composition comprising dextran having an average molecular weight in a range of 3,000 Da to 8,000 Da.

Dextran concentration range

The method uses a composition where the dextran concentration is within 2 to 40 (w/v)%.

Dextran sub-range of 4,500 Da to 5,500 Da

The method uses dextran having an average molecular weight between 4,500 Da and 5,500 Da.

Two dextran molecular-weight fractions with specified concentrations

A composition containing dextran at specified concentrations for two average molecular-weight ranges (3,000–8,000 Da and 800–1,200 Da).

Poloxamer included in the composition

The method includes a composition that also includes poloxamer.

Inflammation inhibition of joints, cartilages, or connective tissues

The method further inhibits inflammation of joints, cartilages, or connective tissues.

Across the independent claim and its refinements, the core claimed concept is administering to a subject a cartilage-regenerating or cartilage-protecting composition containing dextran with a specified average molecular weight range, optionally refined by dextran concentration and molecular-weight sub-ranges, and further characterized by including poloxamer and inhibiting inflammation in joints, cartilages, or connective tissues.

Stated Advantages

The compositions are described as persisting at the lesion due to shock-absorbing/cushioning and coating effects.

The compositions are described as having anti-inflammation effects.

Dextran is described as supporting chondrocyte proliferation.

The compositions are described as inhibiting cartilage breakdown via MMP-3 and MMP-13 expression changes.

The compositions are described as promoting cartilage regeneration via type II collagen and aggrecan production.

Mixtures with dextran and poloxamer 188 are described as improving anti-inflammatory and cartilage-regenerative outcomes.

Documented Applications

Regenerating or protecting cartilage in a subject in need thereof, including in the context of joint and connective tissue diseases.

Cartilage regeneration and protection evaluated using rat chondrocyte studies, with reported endpoints involving IL-10/IL-6 ratio, MMP-3 and MMP-13 expression, and type II collagen and aggrecan production.

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