High-molecular-weight fucans for treating fibrous adhesions and other diseases and conditions
Inventors
SPRINGATE, CHRISTOPHER MICHAEL KEVIN • MILLET, IAN • DASWANI, SAILESH HARESH • SUN, HESONG
Assignees
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Publication Number
US-11419891-B2
Publication Date
2022-08-23
Expiration Date
Abstract
High-molecular-weight fucan compositions comprising a therapeutically effective, medically acceptable fucan in a composition comprising wherein the fucan, for example, has a molecular weight distribution in which more than 60% w/w of the composition has a molecular weight above 100 kDa.
Core Innovation
The invention relates to a high-molecular-weight fucan, such as fucoidan, that consists essentially of a molecular weight distribution in which at least 60% w/w of the molecular weight distribution is greater than about 1600 kDa. The high-molecular-weight fucan is measured using aqueous gel permeation chromatography with specified hydroxylated polymethacrylate-based gel columns, a guard column, a refractive index detector, and a sodium nitrate mobile phase, and is quantified against dextran peak molecular weight standards.
The disclosure also characterizes the high-molecular-weight fucan by compositional and physical attributes, including sulfate content, carbohydrate/fucose/galactose/uronic acid and other sugar content, low acetyl content substantially 0%, and viscosity at a specified concentration. The high-molecular-weight fucan is described with appearance and clarity attributes, including a white solid and a clear-colorless solution.
The high-molecular-weight fucan is positioned as a medical composition with medically acceptable buffers and defined concentration and dosing ranges. It is described for administration to surgical sites for post-surgical adhesion management, and is also associated with anti-proliferative and anti-inflammatory use in inflammatory disorders, including dermal inflammatory disorders such as dermatitis and rosacea.
Claims Coverage
The consolidated claim coverage identifies one independent inventive feature directed to a high-molecular-weight fucan defined by a molecular weight distribution threshold measured using an aqueous gel permeation chromatography setup with specified columns, detection, mobile phase, and dextran standards. Dependent refinements add compositional and physical limitations, and a medical composition concentration range for treatment in an animal.
High-molecular-weight fucan defined by aqueous gel permeation chromatography distribution
A high-molecular-weight fucan that consists essentially of a molecular weight distribution wherein at least 60% w/w of the molecular weight distribution is greater than about 1600 kDa, when measured using an aqueous gel permeation chromatography setup consisting essentially of specified hydroxylated polymethacrylate-based gel columns, a guard column, a refractive index detector, a sodium nitrate mobile phase, and quantification against dextran-based peak molecular weight standards.
Acetyl-limited high-molecular-weight fucan
The high-molecular-weight fucan has less than 5% (w/w) acetyl content, or substantially 0% w/w acetyl content as measured by 2D 1H-13C heteronuclear multiple quantum coherence.
Sulfate-content high-molecular-weight fucan
The high-molecular-weight fucan has a sulfate content between about 20% w/w and about 60% w/w.
Viscosity-constrained high-molecular-weight fucan
When dissolved in water at 50 mg/mL, the high-molecular-weight fucan has a viscosity between about 4 cP and about 50 cP.
Medical composition concentration for animal disease or condition treatment
A medical composition containing about 0.02 mg/mL to 100 mg/mL of the high-molecular-weight fucan, formulated to treat a disease or condition in an animal.
Overall, the claims are directed to a high-molecular-weight fucan defined by a molecular weight distribution threshold measured by a specified aqueous gel permeation chromatography setup with dextran standards, with dependent refinements that further constrain acetyl content, sulfate content, viscosity at a specified concentration, and formulation concentration in a medical composition for treating a disease or condition in an animal.
Stated Advantages
Inhibiting and treating and/or preventing inflammatory disorders, including dermal inflammatory disorders such as dermatitis and rosacea.
Improved efficacy for inhibiting, preventing, and reducing fibrous adhesions and surgical adhesions, with molecular-weight-dependent outcomes.
Documented Applications
Treating fibrous adhesions and post-surgical adhesions by administering the high-molecular-weight fucan to a surgical site.
Treatment, prevention, and inhibition of dermal inflammatory disorders, including dermatitis (including atopic dermatitis and contact dermatitis) and rosacea (including facial erythema and ocular rosacea).
Medical composition use for treating a disease or condition in an animal.
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