WO2010075611A1 - Composition comprenant de la proanthocyanidine, une enzyme protéolytique et une substance de l'espèce aloe vera/agave - Google Patents

Composition comprenant de la proanthocyanidine, une enzyme protéolytique et une substance de l'espèce aloe vera/agave Download PDF

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Publication number
WO2010075611A1
WO2010075611A1 PCT/AU2010/000005 AU2010000005W WO2010075611A1 WO 2010075611 A1 WO2010075611 A1 WO 2010075611A1 AU 2010000005 W AU2010000005 W AU 2010000005W WO 2010075611 A1 WO2010075611 A1 WO 2010075611A1
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WIPO (PCT)
Prior art keywords
composition
proanthocyanidin
aloe vera
proteolytic enzyme
plant
Prior art date
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PCT/AU2010/000005
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English (en)
Inventor
Victor Patrick Davidson
Original Assignee
Bio - Enhancements Pty Ltd
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Publication date
Priority claimed from AU2009900028A external-priority patent/AU2009900028A0/en
Application filed by Bio - Enhancements Pty Ltd filed Critical Bio - Enhancements Pty Ltd
Publication of WO2010075611A1 publication Critical patent/WO2010075611A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/13—Coniferophyta (gymnosperms)
    • A61K36/15—Pinaceae (Pine family), e.g. pine or cedar
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/886—Aloeaceae (Aloe family), e.g. aloe vera
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/4873—Cysteine endopeptidases (3.4.22), e.g. stem bromelain, papain, ficin, cathepsin H
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06—Anabolic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • the present invention relates to a composition containing proanthocyanidin and to uses of the composition.
  • Proanthocyanidin sometimes referred to as procyanidin, oligomeric proanthocyanidin (OPC), Pycnogenol®, leukocyanidin or leucoanthocyanin is an oligomeric or polymeric species derived from flavonoids such as catechins. It has been linked with health effects associated with its antioxidant and vasodilatory effects. There is however a need for an improved composition of proanthocyanidin which provides bettei bioavailability for the active ingredients. There is also a need for an improved understanding of the range of health benefits which may be addressed by means of such compositions.
  • composition comprising:
  • the proteolytic enzyme may have one or more, optionally all, of the following properties:
  • the proteolytic enzyme may comprise bromelain.
  • the composition should not contain papain.
  • composition comprising:
  • composition does not comprise papain.
  • the proanthocyanidin may be oligomeric. It may be obtained from a source selected from the group consisting of bark of a French Maritime Pine tree, grape seed and bark of a Pinus radiata tree. It may be, or may comprise, an extract from the bark of the French Maritime Pine tree.
  • the proteolytic enzyme may have any one or more, optionally all, of the properties listed above. It may be a digestive enzyme. It may be, or may comprise, bromelain. It may be such that it does not cause (or may be such that it is not capable of causing) hypersensitivity reaction. It may have anti-inflammatory activity.
  • the substance derived from Aloe Vera and/or from a plant of the Agave species may be, or may comprise, an extract of Aloe Vera or of a plant of the Agave species. It may be, or may comprise, a juice of Aloe Vera or of a plant of the Agave species, or a concentrate thereof. It may be, or may comprise, a powder obtained by drying a juice of Aloe Vera or of a plant of the Agave species. It may be, or may comprise, an Aloe Vera extract. It may be Aloe Vera juice. It may be Aloe Vera juice concentrate. It may be a powder obtained by drying Aloe Vera juice.
  • the plant of the Agave species may be Century Plant, American Aloe, False Aloe, Flowering Aloe, Spiked Aloe or Maguey.
  • the substance may be, or may comprise, a combination of substances from these different plants.
  • the ratio of the amount of proanthocyanidin to the amount of proteolytic enzyme in the composition maybe between about 1 and about 1.5 (i.e. about 1:1 to about 1.5:1) on a weight basis.
  • the proanthocyanidin and the proteolytic enzyme in combination may be present in an amount about 1 to about 1.5% on a weight/weight or a weight/volume basis relative to the substance derived from Aloe Vera and/or from a plant of the Agave species.
  • the composition may be acidic. It may be pH about neutral.
  • the composition may additionally comprise an organic acid, preferably a non-toxic organic acid such as a food acid.
  • the organic acid may comprise, or may be, acetic acid.
  • the composition may have a pH of about 2 to about 7, or about 3 to 7, 4 to 7, 5 to 7, 2 to 5 or 3 to 6, e.g. about 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5 or 7.
  • the composition may additionally comprise a saccharide.
  • the saccharide may be a fructan.
  • the saccharide may comprise sucrose, maltodextrin, inulin or a combination of any two or all of these.
  • a fructan for example inulin
  • the ratio of proanthocyanidin to bromelain is between about 1 and about 1.5 on a weight basis, the proanthocyanidin and bromelain in combination are present in an amount of about 1 to about 1.5% on a weight/volume basis relative to the Aloe Vera juice, the vinegar is present in a ratio of about 10 to about 15% relative to the Aloe Vera juice and the fructan is present in an amount about 1 to about 2 times that of the combined proanthocyanidin and bromelain by weight, and wherein said composition does not comprise papain.
  • an oligosaccharide for example maltodextrin
  • the ratio of proanthocyanidin to bromelain is between about 1 and about 1.5 on a weight basis, the proanthocyanidin and bromelain in combination are present in an amount of about 1 to about 1.5% on a weight/volume basis relative to the Aloe Vera juice, the vinegar is present in a ratio of about 10 to about 15% relative to the Aloe Vera juice and the oligosaccharide is present in an amount about 10 to about 50 times that of the combined proanthocyanidin and bromelain, and wherein said composition does not comprise papain.
  • the preparation may be suitable for ingestion, e.g. oral ingestion, by a patient.
  • a composition according to the first aspect for improving athletic performance or for improving health and wellbeing or as an isotonic drink.
  • the composition for the treatment of multiple sclerosis or cancer and/or for management of symptoms and/or signs therof.
  • the preparation should be administered internally, e.g. by mouth.
  • liver disease and kidney disease should be taken to encompass liver disfunction and kidney disfunction respectively.
  • a method for treating a condition selected from the group consisting of multiple sclerosis, cancer, diabetes, hypercholesterolemia, asthma, heart disease, liver disease and/or disfunction and kidney disease and/or disfunction comprising administering to a patient in need thereof a composition according to the first aspect.
  • the administering may comprise orally administering.
  • a method for management of symptoms and/or signs of said condition comprising administering to a patient in need thereof a composition according to the first aspect.
  • the proteolytic enzyme may have anti-inflammatory activity. It may not cause hypersensitivity reaction. It may be bromelain.
  • the combining may also comprise combining said components with a water soluble organic acid.
  • the organic acid may be acetic acid.
  • the acetic acid may be in the form of glacial acetic acid. It may be in the form of vinegar. The process may be such that no papain is added.
  • a proanthocyanidin a proteolytic enzyme and a substance derived from Aloe Vera and/or from a plant of the Agave species for the manufacture of a medicament for improving athletic performance or for improving health and wellbeing or for use as a sports isotonic drink or for the treatment of a condition selected from the group consisting of multiple sclerosis, cancer, diabetes, hypercholesterolemia, asthma, heart disease, liver disease and/or disfunction and kidney disease and/or disfunction, or for management of symptoms and/or signs of said condition, or for any two or more of these applications, wherein said enzyme is not papain.
  • the proteolytic enzyme may have anti-inflammatory activity. It may not cause hypersensitivity reaction. It may be bromelain.
  • a process for preparing a composition comprising combining a proanthocyanidin, a proteolytic enzyme and a substance derived from Aloe Vera and/or from a plant of the Agave species.
  • the combining may be such that it does not comprise addition of papain.
  • the invention also comprises a composition made by this process.
  • the composition of the present invention is a very strong antioxidant.
  • the particular combination of components used in the composition, particularly in the quantities described herein, causes a cascade of physiological events which increases the bioavailability of those components and thereby improves the potency of the composition. This thereby provides the beneficial effects that have been observed following ingestion of the composition.
  • the inventor considers that beneficial effects on blood cholesterol levels, diabetes, injury repair and further athletic parameters may arise from use of the present composition.
  • the compositions of this invention have been used in the treatment of multiple sclerosis and demyelination, several oncological conditions, fatigue syndromes and physiological recuperation.
  • treatment may refer to administration of the composition to a patient for the purpose of managing and/or alleviating and/or relieving symptoms and/or signs of the condition in said patient. It may refer to administration of the composition to the patient for the purpose of at least partially curing the condition. It may refer to administration of the composition to the patient for both of these purposes.
  • the treatment may not result in a change in the pathology of a condition, but rather may rely only on the potential to change the experience of symptoms of a condition and/or signs of that condition.
  • the composition may be made from natural ingredients, optionally only from natural ingredients.
  • the proanthocyanin, the proteolytic enzyme and the substance derived from Aloe Vera and/or from a plant of the Agave species may all be natural ingredients. As many people prefer to use products, particularly health and wellbeing promoting products, that are derived from natural sources, this feature may be a benefit of the present composition.
  • the composition may in some embodiments contain no synthetic ingredients.
  • the proteolytic enzyme serves to improve bioabsorption of the proanthocyanin and of one or more compounds present in the substance derived from Aloe Vera and/or from a plant of the Agave species.
  • the composition may be substantially non-toxic. In particular it may be substantially non-toxic to humans, or to the subject to whom it is administered. In this context, "non-toxic" indicates that at the normal dose at which the composition is administered in order to obtain the desired effect, it does not cause adverse effects (e.g. death) to the subject to whom it is administered.
  • the composition may be orally administrable. It may not cause a hypersensitivity reaction in said subject. It may contain no enzymes that cause a hypersensitivity reaction when administered to a subject. It will be recognised that certain individuals may have sensitivity to substances which do not cause hypersensitivity reactions in the vast majority of people and which are not generally regarded as sensitisers.
  • composition of the present invention comprises a proanthocyanidin, a proteolytic enzyme having anti-inflammatory activity and a substance derived from Aloe Vera and/or from a plant of the Agave species.
  • the proanthocyanidin may be obtained, e.g. extracted, from a plant source.
  • the plant may be for example a pine tree (the proanthocyanidin may be obtained from the bark thereof), grape (the proanthocyanidin may be obtained from the seeds and or the skins), bilberry, cranberry, black currant, chokeberry (particularly the berries, preferably of the black chokeberry), tea or some other plants.
  • the proanthocyanidin may be oligomeric. It may be obtained from a source selected from the group consisting of bark of a French Maritime Pine tree, grape seed and bark of a Pinus radiata tree. It may be an extract from the bark of the French Maritime Pine tree.
  • Proteolytic enzyme Proteolytic (or digestion) enzymes break down or hydrolyse proteins e.g. during digestion. They therefore occur naturally in the digestive tract of animals where they are partially responsible for the digestive process. They may also occur inside cells, especially in lysosomes.
  • the proteolytic enzyme may be, or comprise a protease or proteinase.
  • the proteolytic enzyme may for example be bromelain.
  • Bromelain is a mixture of proteases with other substances including peroxidase, acid phosphatase, protease inhibitors and calcium.
  • the proteases in bromelain include stem bromelain (EC 3.4.22.32) and fruit bromelain (EC 3.4.22.33 ).
  • the proteolytic enzyme is not papain.
  • the composition contains no papain.
  • the FDA US Food and Drug Administration
  • the FDA has warned companies to stop marketing topical drug products containing papain by 4 November, 2008.
  • the FDA has said "No topical drug product containing papain has been approved by the FDA.”
  • Topical drug ointments containing papain are used to remove dead or contaminated tissue in acute and chronic lesions, such as diabetic ulcers, pressure ulcers, varicose ulcers and traumatic infected wounds.
  • the FDA has received reports of serious adverse events in patients using products containing papain.
  • Glarative hypersensitivity reactions that lead to hypotension (low blood pressure) and tachycardia (rapid heart rate).
  • patients may be allergic to papaya, the source of papain. Therefore, patients with latex sensitivity may be at increased risk of suffering an adverse reaction.
  • Substance derived from Aloe Vera and/or from a plant of the Agave species Aloe Vera taken orally has been found to improve blood glucose levels in diabetics, and to lower blood lipids in hyperlipidaemic patients. It has also been found to be useful in reducing inflammation in patients with ulcerative colitis, and it may also find application as an immunostimulant for treatment (e.g. management of symptoms and/or signs) of cancers.
  • Extracts of Aloe Vera have been shown to exhibit antibacterial and antifungal activities. They have been shown to contain a variety of biologically active substances including acetylated mannans, polymannans, anthraquinone C-glycosides, anthrones, anthraquinones and lectins.
  • the substance derived from Aloe Vera may be a solid or it may be a liquid. It may be a dried extract or dried juice (e.g. a freeze dried extract). It may comprise Aloe Vera juice or Aloe Vera juice concentrate. It may comprise any one or more, optionally all, of the biologically active substances listed above. It may additionally or alternatively comprise a substance derived from a plant of the Agave species (e.g.
  • the substance may be combination of individual substances, each of which may be obtained from one or more of the above mentioned plants. It may comprise a substance (e.g. a plant extract or plant derived substance) having similar or equivalent biological activity to Aloe Vera juice.
  • the proanthocyanidin may be present in an amount approximately the same as the amount of proteolytic enzyme or greater than the amount of proteolytic enzyme.
  • the ratio of the amount of proanthocyanidin to the amount of proteolytic enzyme may be about 1 to about 1.5 on a weight basis, or about 1 to 1.2, 1.2 to 1.5 or 1.2 to 1.4, e.g. about 1, 1.1, 1.2, 1.3, 1.4 or 1.5.
  • the proanthocyanidin may represent about 0.2 to about 0.3 wt% of the composition, or about 0.2 to 0.25, 0.25 to 0.3 or 0.22 to 0.27 wt%, e.g.
  • the amount of proteolytic enzyme may be about 0.15 to about 0.25 wt% of the composition, or about 0.15, 0.16, 0.17, 0.18, 0.19, 0.2, 0.21, 0.22, 0.23, 0.25 or 0.25 wt% of the composition.
  • the proanthocyanidin and the proteolytic enzyme in combination may be present in an amount about 1 to about 1.5% on a weight/weight or a weight/volume basis relative to the substance derived from Aloe Vera and/or from a plant of the Agave species, or about 1 to 1.3, 1.2 to 1.5 or 1.2 to 1.4%, e.g. about 1 , 1.1 , 1.2, 1.3, 1.4 or 1.5%.
  • the substance derived from Aloe Vera and/or from a plant of the Agave species may be present in the composition between about 10 and about 50%, or about 10 to 40, 10 to 30, 20 to 50, 30 to 50 or 20 to 40%, e.g. about 10, 15, 20, 25, 30, 35, 40, 45 or 50 % on a w/v or v/v basis. It may be present in a smaller quantity, e.g. about 1 to about 5% (particularly in a composition that is diluted from a pre-prepared concentrate), or about 1 to 3, 3, to 5 or 2 to 4%, for example about 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5 or 5% (w/w or w/v).
  • the quantity will depend on whether a juice, extract, juice concentrate or powdered juice is used, as well as on which plant said substance is derived from. It may be present at about 5 to about 10%, or about 5 to 8 or 7 to 10%, e.g. about 5, 6, 7, 8, 9 or 10%.
  • the substance derived from Aloe Vera and/or from a plant of the Agave species is commonly an extract or a juice of a plant or a concentrate of such an extract. As such it commonly comprises significant amounts of water. It may comprise about 0.1 to about 20% solids, the remainder being essentially water. It may comprise about 0.1 to 10, 0.1 to 5, 0.1 to 2, 0.1 to 1, 1 to 20, 2 to 20, 5 to 20, 10 to 20, 1 to 10, 1 to 5, 0.5 to 5 or 0.5 to 2% solids, e.g.
  • the ratios defined herein may be adjusted to account for the loss of water from the original extract or juice.
  • the composition may additionally comprise an organic acid.
  • the organic acid may be, or may comprise, a water soluble organic acid. It may comprise acetic acid or propanoic acid or a mixture of these. It may be a non-toxic or low toxicity organic acid.
  • the organic acid may be present in a matrix.
  • acetic acid may be present as a component of vinegar, which may be used in making the composition. It may be added to the composition in the form of glacial acetic acid.
  • the organic acid may be present at up to about 0.25% w/v of the composition, or up to about 0.2, 0.15, 0.1, 0.05, 0.025 or 0.01%, e.g.
  • composition in the form of vinegar which is between about 0.4 and 0.6% acetic acid by volume.
  • organic acid may be added in the form of vinegar.
  • composition is to be made as a medication, it may be advantageous to add the organic acid as an appropriate amount of glacial acetic acid so as to meet requirements of the TGA (Therapeutic Goods Administration) for OTC (over the counter) medications manufactured in a GMP (good manufacturing practice) facility.
  • TGA Therapeutic Goods Administration
  • OTC over the counter
  • GMP Good manufacturing practice
  • Some of the embodiments of the inventions will be concentrates, which may be diluted before use.
  • the concentrations of the active components will be correspondingly higher in such concentrates.
  • the concentrates may be diluted between about 2-fold and about 50-fold before use.
  • Suitable dilution ratios are from about 2 to about 50, or about 2 to 20, 2 to 10, 2 to 5, 5 to 50, 10 to 50, 20 to 50, 5 to 20, 5 to 10, 10 to 20 or 5 to 15, e.g. about 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 20, 25, 30, 35, 40, 45 or 50.
  • the dilution ratio may be dependent on the desired application for the diluted composition as well as the nature of the concentrate and the concentration of individual components in the concentrate.
  • the stated concentrations of components may vary from the stated ranges depending on whether the composition is a concentrate or is a diluted version of the composition.
  • the composition may additionally comprise a saccharide or more than one saccharide, each of which may be a monosaccharide (e.g. glucose), a disaccharide (e.g. sucrose), an oligosaccharide or a polysaccharide (e.g. inulin, maltodextrin).
  • the saccharide may comprise sucrose, maltodextrin, inulin or a combination of any two or all of these.
  • the amount of saccharide may depend on the nature of the saccharide.
  • the (or each) saccharide may, if present, be present at up to about 10% w/v, or up to about 5, 2, 1, 0.5, 0.2 or 0.1%, e.g.
  • composition may additionally comprise any one or more, optionally all, of the following:
  • a sodium salt for example sodium chloride, equivalent to about 0.01 to about 0.5% sodium w/v, or about 0.01 to 0.2, 0.01 to 0.1, 0.01 to 0.05, 0.05 to 0.5, 0.1 to 0.5, 0.2 to 0.5, 0.05 to 0.2 or 0.1 to 0.2%, e.g.
  • a potassium salt for example potassium chloride, equivalent to about 0.01 to about 0.2% potassium w/v, or about 0.01 to 0.1, 0.01 to 0.05, 0.05 to 0.2 or 0.1 to 0.2%, e.g. about 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.15 or 0.2% potassium;
  • purified water may represent up to about 75% of the composition, or up to about 60% or up to about 50%, and may for example represent about 0, 5, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, 65, 70 or 75% of the composition;
  • flavourings for example a berry flavour (e.g. strawberry, raspberry, blueberry etc.) in a quantity sufficient to provide the composition with an acceptable or pleasing flavour;
  • a berry flavour e.g. strawberry, raspberry, blueberry etc.
  • one or more preservatives for example sodium benzoate and/or potassium sorbate (each, or in combination, suitably about 50 to about lOOmicrograms/ml, e.g. about 50, 60, 70, 80, 90 or 100 micrograms/ml).
  • composition A Suitable compositions according to the invention include: Composition A
  • composition Composition B Purified water to 1 litre total volume of composition Composition B
  • composition Composition C Purified water to 1 litre total volume of composition Composition C
  • the composition described may be used for improving athletic performance or for improving health and wellbeing or as a sports isotonic drink, or for the treatment (e.g. management of symptoms and/or signs) of multiple sclerosis or cancer.
  • the composition may be used to improve one or more (optionally all) of endurance, strength, power and speed in subjects engaged in sporting, athletic or other physical activity.
  • a suitable quantity of the composition should be ingested between about 1 and about 3 hours (e.g. about 1, 1.5, 2, 2.5 or 3 hours) prior to commencing the activity.
  • the resulting improvement in performance may be about 10 to about 50%, or about 10 to 25, 20 to 50, 15 to 30 or 15 to 25%, e.g. about 10, 15, 18, 20, 25, 30, 35, 40, 45 or 50%.
  • the amount ingested may be sufficient to achieve this improvement.
  • the composition may be used to improve general wellbeing in a subject.
  • a quantity of the composition of about 20 to about 100ml should be ingested daily, or about 20 to 50, 50 to 100, 30 to 70 or 40 to 60ml, e.g. 20, 30, 40, 50, 60, 70, 80, 90 or 100ml.
  • a smaller amount may be ingested more frequently (e.g. twice or 3 times daily) or a larger amount may be ingested less frequently (e.g. every 2, 3 or 4 days).
  • the subject may be a human subject.
  • the subject may be a non-human subject, for example a non-human mammal.
  • the non-human mammal may be a non-human primate (e.g. a monkey or an ape). It may be a non-human placental mammal. It may be a domesticated animal. It may be a wild animal.
  • the subject may be a bird.
  • the composition may be used for treatment (e.g. management of symptoms and/or signs) of a condition in the subject (said subject being any of the above). It may be used for a therapeutic purpose in any of the above (e.g. in a non-human subject). It may be used for a non-therapeutic purpose (e.g. improving athletic performance or for improving health and wellbeing or for use as a sports isotonic drink) in any of the above.
  • the composition may be used to improve, ameliorate or arrest the progress of a serious illness such as cancer and/or multiple sclerosis, hi order to achieve this, a quantity of the composition of about 100 to about 500ml should be ingested daily, or about 100 to 250, 200 to 500 or 150 to 300ml, e.g. about 100, 150, 200, 250, 300, 350, 400, 450 or 500ml daily. Once improvement in the condition is observed, this may be reduced to about 20 to about 100ml daily, or about 20 to 50, 50 to 100, 30 to 70 or 40 to 60ml, e.g. 20, 30, 40, 50, 60, 70, 80, 90 or 100ml daily for maintenance of the improvement. Alternatively a smaller amount may be ingested more frequently (e.g.
  • the reduced daily dose may be continued for an extended period.
  • the extended period may be at least about 3 months, or at least 4, 5, 6, 9 or 12 months (or about 3 months to 10 years, or about 6 months to 10 years, 1 to 10 years, 2 to 10 years, 5 to 10 years, 3 to 12 months, 3 to 6 months, 4 to 12 months or 4 to 8 months, e.g. about 3, 4, 5, 6, 7, 8, 9, 10 or 11 months, or about 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 years, or more than 10 years).
  • the reduced daily dose may be continued indefinitely.
  • the composition may be a solution. It may be a suspension. It may be an emulsion. It may be a microemulsion. It may be more than one of these. For example some components may be dissolved in the composition and others may be emulsified.
  • the particle/droplet size may be between about 0.1 and 100 microns in mean diameter or about 0.1 to 10, 0.1 to 1, 1 to 100, 10 to 100 or 1 to 10 microns, e.g. about 0.1, 0.2, 0.5, 1, 2, 5, 10, 20, 50 or 100 microns.
  • the emulsion/suspension may be a stable emulsion (i.e.
  • the composition may resist settling/separation) or it may be an unstable emulsion.
  • the composition may be clear, hazy, cloudy or opaque.
  • the composition may be a dark red/brown colour. It may be some other colour, depending on the details of the composition, for example on the nature and quantity of any flavouring components used.
  • the composition may be fully in solution. It is however preferable that the composition be shaken or otherwise agitated shortly prior to consumption in order to ensure that any undissolved matter is evenly distributed throughout the composition.
  • the composition may be stable at room temperature, or at a temperature below room temperature. It may be stable at about 5, 10, 15 or 2O 0 C.
  • stable indicates that the composition retains at least about 90% of its activity with respect to the desired application when stored, optionally stored in the dark, for a period of at least about 1 week, or at least about 1 month, or at least about 6 months, or at least about 1 year, or at least about 18 months or at least about 2 years.
  • the composition may be stable for the above periods when stored unopened. It may be stable for the above periods when stored in the dark. Once opened, it is advisable to refrigerate the composition so as to reduce degradation of one or more components therein.
  • the composition of the invention may be made by combining a proanthocyanidin, a proteolytic enzyme having anti-inflammatory activity and a substance derived from Aloe Vera. Other substances as described above may also be combined to form the composition. Suitable amounts and/or ratios of the components are described above.
  • the components in general do not react with each other. Consequently the order of addition of the different components is not critical, and any convenient order may be used.
  • One or more premixes of components may be prepared and combined in order to form the final composition.
  • the combining may be accompanied and/or followed by agitation.
  • the agitation may comprise any one or more of stirring, shaking, mixing, swirling, sonicating or ultrasonicating, either sequentially or simultaneously.
  • the combining may comprise dissolving and/or emulsifying one or more components of the composition.
  • the composition may be used to obtain a range of health benefits, for example for improving athletic performance or for improving health and wellbeing or for use as a sports isotonic drink or for the treatment (e.g. management of symptoms and/or signs) of multiple sclerosis or cancer or for any two or more of these applications. It may be used for making a medicament for obtaining those health benefits.
  • the composition or medicament may be administrated (or administrable) orally. It may be an orally acceptable composition or medicament. It may be in the form of a drink which the patient drinks in order to obtain the health benefits.
  • the invention also comprises a process for preparing the composition.
  • a proanthocyanidin, a proteolytic enzyme and a substance derived from Aloe Vera and/or from a plant of the Agave species are combined.
  • the combining is preferably such that it does not comprise addition of papain.
  • the components used in the method may be as described in the composition of the first aspect.
  • the combining may comprise dissolving and/or suspending and/or emulsifying. It may comprise agitating, for example mixing, stirring, swirling, sonicating etc.
  • the addition of components may be in any desired order.
  • the proanthocyanidin and the enzyme may be combined and then added to the substance derived from Aloe Vera and/or from a plant of the Agave species, or the enzyme may be combined with the substance and then the proanthocyanidin added to the resulting mixture.
  • Dilution with water if required, may be conducted following preparation of the initial composition or it may be conducted as the composition is prepared.
  • the substance derived from Aloe Vera and/or from a plant of the Agave species may be diluted in a desired quantity of water (or a portion thereof) and the proanthocyanidin and enzyme added to form a diluted form of the composition.
  • Other components of the composition e.g. salts, flavours, acid etc.
  • each addition is accompanied by agitation as described above.
  • the juice would be stirred while the enzyme is added.
  • the process may additionally comprise dissolving or suspending that component in a suitable solvent, e.g. water.
  • Example 1 a base concentrate
  • Oligomeric proanthocyanidin available from the following sources: a. Extract from the bark of the French Maritime Pine tree (corporate trade name Pycnogenol®) - this is a preferred option; or b. Grape seed extract; or c. Extract from the bark of the Pinus radiate tree (which is produced in NZ under a trade mark EnzogenolTM)
  • Proteolytic enzyme - suitable examples include bromelain, which may be for example extracted from pineapple; and/or
  • Aloe Vera extract e.g. as a pure juice or powder concentrate
  • the preferred proteolytic enzyme in this composition is Bromelain. This enzyme provides faster digestion and further anti-inflammatory properties. Papain is not used in the composition, and the inventor considers that compositions containing bromelain in the absence of papain are as effective as those containing papain in speeding up the digestion.
  • composition may be used for athletic performance, health and wellness applications. It may be used as a concentrate, for dilution prior to ingestion by a subject
  • Example 2
  • Aloe Vera juice 350ml or powdered Aloe Vera extract in sufficient quantity to provide a similar level of Aloe Vera derived solids
  • This composition may be used as a sports drink or as a general wellness drink. It may be used as a concentrate, for dilution prior to ingestion by a subject.
  • Example 3
  • a 600ml isotonic drink was prepared using:
  • Example 4 This formulation may be used as an isotonic drink for physical activities.
  • Example 4 This formulation may be used as an isotonic drink for physical activities.
  • Randomised control double blind ' trials were conducted on elite athletes using the composition of Example 1 and a placebo, which was a fruit juice with a similar taste to that of the test composition, but contained no bromelain.
  • the study used 12 athletes of whom 6 were controls and 6 were test subjects.
  • the athletes each consumed 150ml of the product or of the placebo 2 hours prior to the commencement of the physical tests.
  • the physical tests involved a repeat running sprint test over 20m. This test is known in the industry as the "Yoyo Test". In this test, athletes repeatedly sprint a 2x20m course in a specified time. A 5 second rest is allowed between each sprint, and the time allowed for each sprint reduces over time. The number of sprints completed until the athlete can no longer complete the sprint in the allowed time is taken as a measure of endurance.
  • Formulations according to the invention have been found to be highly beneficial in people with diagnosed multiple sclerosis, and some cancer sufferers have shown marked improvements in their condition associated with consumption of the composition of Example 1.
  • DV a 47 year old married male, attended his dentist for routine work in August 2001.
  • DV was a horse trainer by occupation and spent significant time with these animals. That night he felt unwell and on the following day awoke with numbness over the right side of his face and a dull right-sided headache. During the course of the day he became aware of unsteadiness on his feet and by the next morning complained of vertigo and vomiting.
  • a Magnetic Resonance Imaging (MRI) scan was performed to exclude posterior fossa stroke, sequelae of vertebral artery dissection or demyelination.
  • the MRI scan showed an extensive area of abnormal signal intensity from the right side of the medulla superiorly into the inferior cerebellar peduncle and right brachium pontus, with some mass effect.
  • the findings are reported to be consistent with demyelination.
  • Other studies showed that vertebral artery and cerebral vasculature were normal.
  • Visual evoked response testing was performed, showing abnormal delay of the central field response for the right eye, strongly suggestive of Multiple Sclerosis.
  • Fig. 1 An MRI of DV taken on 15 August 2001 is shown in Fig. 1.
  • the radiologist noted as follows: "Extensive area of abnormal signal intensity extending from the right side of the medulla, superiorly, into the inferior cerebellar peduncle and the right brachium Pontus. There is considerable associated mass effect. The appearances are felt most likely to represent a focus of demyelination.”
  • DV was not prescribed medications.
  • an herbal preparation that included pine bark and aloe.
  • the preparation was as described in the present specification, and comprised Pycnogenol®, an extract of aloe or some product of agave, a digestive enzyme and such additives as made the product palatable. After some six months of daily intake of this preparation he noticed some improvement in his instability. He returned to the neurologist to seek confirmation as to whether there was any objective evidence of change.
  • Example 6 Case History 2 Presentation MC is a 70 year old retired female medical practitioner. She first presented to her doctor prior to 1992 with symptoms of progressive weakness in all limbs and has subsequently developed severe dysarthria. She has had multiple sclerosis, permanent, for about 20 years. By early 2009 she was in assisted living, wheelchair bound, with almost no strength in her lower limbs and unable to hold a pencil with between her fingers. She remained with very severe dysarthria. Her symptoms do not fluctuate. Examination
  • Examples 5 and 6 are adapted from clinical reports authored by Dr Stan Goldstein MB 5 BS; MHA (Assoc. Prof., Conjoint, University of New South Wales, School of Community Medicine and Public Health).

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Abstract

L'invention porte sur une composition comprenant une proanthocyanidine, une enzyme protéolytique et une substance issue de l'aloe vera et/ou provenant d'une plante de l'espèce agave, la composition étant exempte de papaïne. L'utilisation de la composition permet d'améliorer les performances athlétiques, d'améliorer la santé et le bien-être, et est destinée à être utilisée en tant que boisson isotonique sportive ou pour le traitement d'un état choisi parmi la sclérose en plaques, le cancer, le diabète, l'hypercholestérolémie, l'asthme, une cardiopathie, une maladie hépatique et une maladie rénale.
PCT/AU2010/000005 2009-01-05 2010-01-04 Composition comprenant de la proanthocyanidine, une enzyme protéolytique et une substance de l'espèce aloe vera/agave WO2010075611A1 (fr)

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AU2009900028A AU2009900028A0 (en) 2009-01-05 Composition containing proanthocyanidin

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WO2012014165A1 (fr) * 2010-07-28 2012-02-02 Indus Biotech Private Limited Procédé de traitement d'une affection broncho-constrictrice
WO2013011458A1 (fr) * 2011-07-19 2013-01-24 Indus Biotech Private Limited Procédé de traitement de l'alopécie ou de la cachéxie induite par la chimiothérapie, ou des deux
CN104491215A (zh) * 2015-01-22 2015-04-08 潘剑崎 一种治疗痿症的中药
WO2016123659A1 (fr) * 2015-02-05 2016-08-11 Plasmaide Pty Ltd Composition et formulation d'extrait d'écorce de pin (pbe) bénéfiques pour la santé

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Cited By (9)

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Publication number Priority date Publication date Assignee Title
WO2012014165A1 (fr) * 2010-07-28 2012-02-02 Indus Biotech Private Limited Procédé de traitement d'une affection broncho-constrictrice
CN103025382A (zh) * 2010-07-28 2013-04-03 梧桐生物技术私人有限公司 处理支气管收缩病症的方法
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CN103025382B (zh) * 2010-07-28 2016-04-20 梧桐生物技术私人有限公司 组合物在制备用于处理支气管收缩病症的药物中的应用
WO2013011458A1 (fr) * 2011-07-19 2013-01-24 Indus Biotech Private Limited Procédé de traitement de l'alopécie ou de la cachéxie induite par la chimiothérapie, ou des deux
US9775825B2 (en) 2011-07-19 2017-10-03 Indus Biotech Private Limited Method of managing chemotherapy induced alopecia or cachexia or both
CN104491215A (zh) * 2015-01-22 2015-04-08 潘剑崎 一种治疗痿症的中药
WO2016123659A1 (fr) * 2015-02-05 2016-08-11 Plasmaide Pty Ltd Composition et formulation d'extrait d'écorce de pin (pbe) bénéfiques pour la santé

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