WO2020160619A1 - Composition de réduction de glycation et procédé d'utilisation correspondant - Google Patents
Composition de réduction de glycation et procédé d'utilisation correspondant Download PDFInfo
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- WO2020160619A1 WO2020160619A1 PCT/AU2020/050094 AU2020050094W WO2020160619A1 WO 2020160619 A1 WO2020160619 A1 WO 2020160619A1 AU 2020050094 W AU2020050094 W AU 2020050094W WO 2020160619 A1 WO2020160619 A1 WO 2020160619A1
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- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
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- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
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Definitions
- the present disclosure relates to a glycation reducing composition and a method of use thereof.
- advanced glycation endproducts include reactive products that lead to cell damage, which is thought to be associated with age-related dysfunction of tissues and/or organs. Additionally, advanced glycation endproducts are also potentially associated with the development of morbidities within the ageing populations world-wide.
- compositions that will reduce the concentration of advanced glycation endproducts in a cell when administered in a therapeutically effective dose to a subject in need thereof and a method of using such a composition.
- Advanced glycation endproducts accumulate in multicellular organisms, such as humans, with the passage of time. Accumulation of advanced glycation endproducts is associated with deleterious effects that are typically termed“ageing”. These deleterious effects, including a deterioration of cell function, lead to an increase of ageing-related pathologies and inevitably accelerate mortality. A reduction in the concentration of advanced glycation endproducts may delay onset of ageing-related negative effects on the health of an individual and contribute to economic benefits insofar as the costs associated with an increase in the ageing populations world-wide may be diminished.
- the present disclosure in one aspect sets forth a composition including a therapeutically effective dose of each of b-alanine, aminoguanidine, carcinine, carnosine, pyridoxamine, quercetin, and vitamin E, the composition formulated to reduce the concentration of an advanced glycation endproduct in a cell of a subject.
- the present disclosure in another aspect sets forth a method of reducing the concentration of an advanced glycation endproduct in a cell of a subject, the method including administering to a subject in need thereof a therapeutically effective dose of each of b-alanine, aminoguanidine, carcinine, carnosine, pyridoxamine, quercetin, and vitamin E.
- the present disclosure is directed to a composition that reduces the concentration of advanced glycation endproducts in one or more cell of a multicellular organism, such as humans, that may arise with the passage of time.
- the present disclosure also relates to a method of use of the composition.
- the term“advanced glycation endproducts” should be understood for the purposes herein to define that those compounds that are formed when a protein or a lipid combine with a carbohydrate in one or more cell of an organism.
- composition formulated to reduce the concentration of an advanced glycation endproduct in a cell of a subject.
- the composition including a therapeutically effective dose of each of b-alanine, aminoguanidine, carcinine, carnosine, pyridoxamine, quercetin, and vitamin E.
- a therapeutically effective dose refers to an amount of a composition administered to a subject, either as a single dose or as part of a series of doses, which is effective to produce a desired therapeutic effect.
- each of b-alanine, aminoguanidine, carcinine, carnosine, pyridoxamine, quercetin, and vitamin E is present in an amount of 20 - 150 mg.
- b-alanine is present in an amount of 40 mg.
- aminoguanidine is present in an amount of 10 mg.
- carcinine is present in an amount of 50 mg.
- carnosine is present in an amount of 50 mg.
- pyridoxamine is present in an amount of 50 mg.
- quercetin is present in an amount of 50 mg.
- vitamin E is present in an amount of 40 mg.
- the vitamin E is a-tocopherol. In another preferred embodiment, the vitamin E is b-tocopherol. In another preferred embodiment, the vitamin E is g-tocopherol. In another preferred embodiment, the vitamin E is d-tocopherol. In another preferred embodiment, the vitamin E is a- tocotrienol. In another preferred embodiment, the vitamin E is b- tocotrienol. In another preferred embodiment, the vitamin E is y- tocotrienol. In another preferred embodiment, the vitamin E is d- tocotrienol.
- composition herein disclosed may be delivered to a subject in need thereof by any one of several routes.
- the composition may be delivered via buccal, infusion (e.g., a bolus infusion), inhalation, intracranial injection, enteral, intradermal, intramuscular, intranasal, intraocular, intraperitoneally, intravenously, orally, rectal, rectal, subcutaneously, sublingual, topically, transdermal, vaginal, or any combination thereof.
- the composition may be formulated for enteral administration.
- composition herein disclosed may be formulated for delayed release (also termed sustained or slow release, timed release, delayed release, or controlled release).
- delayed release also termed sustained or slow release, timed release, delayed release, or controlled release.
- Such compositions may generally be prepared using well known technology and administered by, for example, oral, rectal, intradermal, or subcutaneous implantation, or by implantation at the desired target site in a delayed release manner.
- Delayed-release formulations may contain the compound dispersed in a carrier matrix and/or contained within a reservoir surrounded by a rate controlling barrier.
- a particularly preferred embodiment of the composition may be formulated in an enteric coating layer.
- the enteric coating layer may include one or more of cellulose acetate phthalate, cellulose acetate trimellitate, hydroxypropyl methylcellulose acetate succinate, hydroxypropyl methylcellulose phthalate, polyvinyl acetate phthalate, and water-based polymer solutions or dispersions of acrylates.
- the composition disclosed herein may be formulated with a buffering agent to protect the compound from low pH of the gastric environment and/or an enteric coating.
- composition when administer orally, buccally, or sublingually, may be formulated with a flavouring agent, e.g., in a liquid, solid or semi-solid formulation.
- a flavouring agent e.g., in a liquid, solid or semi-solid formulation.
- Preferred embodiments may include one or more pharmaceutically acceptable dispersant, excipient, pH-buffering compound, and pigment.
- Preferred embodiments will include at least one excipient that is biocompatible and may also be biodegradable; preferably the formulation provides a relatively constant level of active component release.
- the excipient facilitates absorption. In yet a further particularly preferred embodiment, the excipient enhances solubility.
- the composition may be a tablet formulation.
- the composition may be a powder formulation.
- the powder formulation may be in a capsule.
- the composition may be a liquid formulation.
- the composition may be formulated for parenteral administration.
- the composition may be formulated for subcutaneous administration.
- the composition may be formulated for intramuscular administration.
- the composition may be formulated for intravenous administration.
- the composition may be formulated for intradermal administration.
- the composition may be formulated for transdermal administration.
- composition disclosed herein will be administered for a sufficient amount of time to selectively purge senescent cells from one or more tissue in a subject, wherein the purging of such cells does not lead to a cancer.
- purging of senescent cells may ameliorate at least one symptom associated with a number of pathologies.
- Such pathologies may include age-related loss of pulmonary function, Alzheimer's disease, angina, aortic aneurysm, arrhythmia, arteriosclerosis, asthma, atherosclerosis, atopic dermatitis, brain aneurysm, bronchiectasis, cardiac diastolic dysfunction, a cancer, cardiac fibrosis, cardiac stress resistance, cardiomyopathy, carotid artery disease, cataracts, chronic obstructive pulmonary disease, chronic renal failure, congestive heart failure, coronary artery disease, coronary thrombosis, cutaneous lupus, cutaneous lymphomas, cystic fibrosis, dementia, diabetes, diabetic ulcer, diseases and disorders related to photosensitivity or photoaging, dysesthesia, eczema, eczematous eruptions, emphysema, endocarditis, eosinophilic dermatosis, fibrohistocytic proliferations of skin, frailty, glaucoma,
- a method of reducing the concentration of an advanced glycation endproduct in a cell of a subject including administering to a subject in need thereof a therapeutically effective dose of each of b-alanine, aminoguanidine, carcinine, carnosine, pyridoxamine, quercetin, and vitamin E.
- the method may include a treatment course no longer than (a) one month, or (b) no longer than two months, or (c) no longer than three months.
- each treatment course is no longer than (a) five days, (b) seven days, (c) ten days, (d) fourteen days, or (e) twenty-one days.
- the composition is administered every second day or every third day of each treatment course.
- the composition is administered once daily during each treatment course.
- the composition is administered twice daily during each treatment course. Suitable interval periods between treatments will be known to a person skilled in the art.
- the subject may be a multicellular animal.
- the multicellular animal is a human.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Psychology (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
L'invention est motivée par le fait qu'un certain nombre de réactions complexes, comprenant des réactions d'Amadori, des réactions de Maillard et des réactions de base de Schiff, conduisent à une augmentation de la concentration en produits terminaux de glycation avancée dans les cellules au fur et à mesure du vieillissement des animaux, y compris les êtres humains. De tels produits terminaux de glycation avancée comprennent des produits réactifs qui conduisent à un dommage cellulaire, dont on pense qu'il est associé à un dysfonctionnement lié à l'âge de tissus et/ou d'organes. De plus, les produits terminaux de glycation avancée sont également potentiellement associés au développement de morbidités dans les populations vieillissantes partout dans le monde. Compte tenu du dysfonctionnement et des morbidités mentionnés ci-dessus dans les populations vieillissantes partout dans le monde, il existe un besoin d'une composition qui réduira la concentration en produits terminaux de glycation avancée dans une cellule lorsqu'elle est administrée dans en dose thérapeutiquement efficace à un sujet qui en a besoin et d'un procédé d'utilisation d'une telle composition. La présente invention concerne une composition de réduction de la glycation et un procédé de préparation associé.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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AU2019900346A AU2019900346A0 (en) | 2019-02-05 | A glycation reducing composition and method of use thereof | |
AU2019900346 | 2019-02-05 |
Publications (1)
Publication Number | Publication Date |
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WO2020160619A1 true WO2020160619A1 (fr) | 2020-08-13 |
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PCT/AU2020/050094 WO2020160619A1 (fr) | 2019-02-05 | 2020-02-05 | Composition de réduction de glycation et procédé d'utilisation correspondant |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2022039190A1 (fr) * | 2020-08-18 | 2022-02-24 | 有機合成薬品工業株式会社 | Activateur des sirtuines et procédé d'activation des sirtuines |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
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US20060045896A1 (en) * | 2004-08-31 | 2006-03-02 | Tracie Martyn International, Llc | Topical compositions comprising benfotiamine and pyridoxamine |
US20060216251A1 (en) * | 2005-03-24 | 2006-09-28 | Tracie Martyn International, Llc | Topical formulations and methods of use |
US20070065396A1 (en) * | 2005-09-21 | 2007-03-22 | Tracie Martyn International, Llc | Topical macqui berry formulation |
EP2939657A1 (fr) * | 2012-12-27 | 2015-11-04 | Hayashibara Co., Ltd. | Composition antivieillissement pour l'extérieur de la peau et procédé de production associé |
-
2020
- 2020-02-05 WO PCT/AU2020/050094 patent/WO2020160619A1/fr unknown
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060045896A1 (en) * | 2004-08-31 | 2006-03-02 | Tracie Martyn International, Llc | Topical compositions comprising benfotiamine and pyridoxamine |
US20060216251A1 (en) * | 2005-03-24 | 2006-09-28 | Tracie Martyn International, Llc | Topical formulations and methods of use |
US20070065396A1 (en) * | 2005-09-21 | 2007-03-22 | Tracie Martyn International, Llc | Topical macqui berry formulation |
EP2939657A1 (fr) * | 2012-12-27 | 2015-11-04 | Hayashibara Co., Ltd. | Composition antivieillissement pour l'extérieur de la peau et procédé de production associé |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2022039190A1 (fr) * | 2020-08-18 | 2022-02-24 | 有機合成薬品工業株式会社 | Activateur des sirtuines et procédé d'activation des sirtuines |
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