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)
  • A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
  • A61K36/734—Crataegus (hawthorn)
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23K—FODDER
  • A23K20/00—Accessory food factors for animal feeding-stuffs
  • A23K20/10—Organic substances
  • A23K20/111—Aromatic compounds
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23K—FODDER
  • A23K50/00—Feeding-stuffs specially adapted for particular animals
  • A23K50/40—Feeding-stuffs specially adapted for particular animals for carnivorous animals, e.g. cats or dogs
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
  • A23L2/52—Adding ingredients
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
  • A23L33/11—Plant sterols or derivatives thereof, e.g. phytosterols
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/40—Complete food formulations for specific consumer groups or specific purposes, e.g. infant formula
• • 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
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/06—Antihyperlipidemics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

• the present invention generally relates to the field of health and wellness.
• the present invention addresses hyperlipidemia, hypercholesterolemia and disorders associated therewith.
• the present invention describes a composition comprising phytosterols and hawthorn for use in the treatment, alleviation or prevention of disorders associated with hypercholesterolemia.
• Cardiovascular Diseases are the leading cause of death and disability globally. More people are severely affected annually by CVDs than from any other cause. From a WHO report, an estimated 17.3 million people died from CVDs in 2008, representing 30% of all global deaths. Of these deaths, an estimated 7.3 million were due to coronary heart disease and 6.2 million were due to stroke. By 2030, almost 23.6 million people will die from CVDs, mainly from heart disease and stroke. These are projected to remain the single leading causes of death.
• Hawthorn and phytosterols are well known to have beneficial health effects, however, both individual ingredients have their limitations.
• Hawthorn a flowering shrub of the rose family, has an extensive history of use in cardiovascular diseases, dating back to the 1 st century. Hawthorn has been shown to have a promising effect on blood cholesterol reduction. However, to achieve a biologically significant effect, daily consumption of hawthorn juice frequently causes stomach discomfort due to its acidic taste. In addition, hawthorn has limited reducing effect on blood triglycerides, which is an important risk factor for cardiovascular disease among blood lipids.
• Phytosterols are known to be able to reduce blood concentrations of total and LDL cholesterol by reducing cholesterol absorption in the gut.
• a daily intake of around 2.4 g of plant sterols (or its saturated form, stands) is associated with ci.n 8 "6 reduction of blood total cholesterol concentrations.
• phytosterols have unwanted side effects. For example, they inhibit alpha and beta carotene absorption.
• Beta carotene is an important source of Vitamin A. Vitamin A is essential for growth and development.
• the present inventors were surprised to see that the subject matter of the independent claim achieves the objective of the present invention.
• the subject matter of the dependant claims further develops the central idea of the present invention.
• the inventors have found in a hamster model that - when administered together - hawthorn and phytosterols act synergistically and allow reducing blood lipids and blood levels of LDL cholesterol statistically significantly, while keeping the individual dosages of phytosterols and hawthorn sufficiently low to avoid unwanted side effects and discomfort .
• the present invention relates in part to a composition comprising phytosterols and hawthorn for use in the treatment, alleviation or prevention of disorders associated with hyperlipidemia and/or hypercholesterolemia.
• the present invention also relates to the use of phytosterols and hawthorn in the preparation of a composition for treating, alleviating or preventing disorders associated with hyperlipidemia and/or hypercholesterolemia.
• disorders associated with hyperlipidemia and/or hypercholesterolemia are well known to those of skill in the art (see for example Bhatnagar D. et al . , BMJ 2008 ; 337 : a993, herewith incorporated by reference) .
• hypercholesterolemia is one of the major causes of atherosclerosis or coronary heart diseases.
• Hyperlipidemia is characterized by abnormally elevated levels of any or all lipids and/or lipoproteins in the blood.
• cardiovascular disorders are a group of disorders of the heart and blood vessels and include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, deep vein thrombosis and pulmonary embolism, etc.
• Cerdiovascular disorders generally refers to any disease that affects the cardiovascular system, and in particular refers to those disorders related to atherosclerosis (arterial disease) . These conditions usually have similar causes, mechanisms, and treatments.
• Atherosclerosis is the buildup of fatty deposits (such as cholesterol) called plaque on the inside walls of arteries. By the time that heart problems are detected, atherosclerosis is usually quite advanced, having progressed for decades.
• the main cause of atherosclerosis is yet unknown, it is a syndrome affecting arterial blood vessels, a chronic inflammatory response in the walls of arteries, caused largely by the accumulation of macrophages and promoted by low-density lipoproteins (LDL, plasma lipoproteins that carry cholesterol and triglycerides) without adequate removal of fats and cholesterol from the macrophages by functional high density lipoproteins (HDL) . It is commonly referred to as a hardening or furring of the arteries. This is caused by the formation of multiple plaques within the arteries.
• LDL low-density lipoproteins
• HDL functional high density lipoproteins
• Hype r 1 ip i demi a is the most important risk factor for atherosclerosis, which is the major cause of cardiovascular disease.
• Hyperlipidemias may also be classified directly into which types of lipids are elevated, that is hypercholesterolemia, hypertriglyceridemia or both in combined hyperlipidemia .
• Elevated levels of Lipoprotein (a) may also be classified as a form of hyperlipidemia.
• the present invention now provides a convenient dietary way to reduce cholesterol levels.
• composition of the present invention may be used for lowering the plasma total cholesterol level, in particular the plasma level of LDL cholesterol.
• a low LDL cholesterol concentration reduces the risk of cardiovascular disorders.
• composition of the present invention is administered in a caloric restriction regimen and/or to subject which exercise aerobically regularly.
• Typical cardio ascular disorders that can be prevented, ameliorated or treated with the composition of the present invention may be selected from the group consisting of artherosclerosis , myocardinal infarction, coronary heart disease, stroke, peripheral vascular diseases or combinations thereof .
• compositions of the present invention may also be for use in treating or preventing high blood triglyceride levels and/or disorders linked thereto.
• One major field of public concern is heart health.
• the compositions of the present invention may be for use in promoting heart health and/or in treating, alleviating or preventing an impaired heart health.
• compositions are administered in an amount sufficient to at least partially cure or arrest the symptoms of a disease and/or its complications. An amount adequate to accomplish this is defined as "a therapeutically effective dose”. Amounts effective for this purpose will depend on a number of factors known to those of skill in the art such as the severity of the disease and the weight and general state of the patient.
• compositions according to the invention are administered to a patient susceptible to or otherwise at risk of a particular disease in an amount that is sufficient to at least partially reduce the risk of developing a disease.
• a prophylactic effective dose Such an amount is defined to be "a prophylactic effective dose”.
• the compositions of the present invention are effective following a dose-response curve. They may be administered in a therapeutically effective dose or a prophylactic effective dose. Skilled artesians will be able to determine such dosages appropriately.
• composition of the present invention may be to be administered in a daily dose corresponding to at least 0.5 g, 1 g, or 3 g hawthorn and at least 15 mg, 50 mg, or lOOmg phytosterols per kg body weight per day.
• the composition of the present invention may comprise at least 0.5 g hawthorn and at least 15 mg phytosterols per kg body weight per day.
• composition of the present invention may comprise at least 1 g hawthorn and at least 50 mg phytosterols per kg body weight per day.
• composition of the present invention may comprise at least 3 g hawthorn and at least 100 mg phytosterols per kg body weight per day.
• the dosages should be kept at a reasonably low level.
• hawthorn may be provided in any form suitable for administration to humans or animals.
• hawthorn may be provided as fresh fruit, dried fruit, hawthorn leaf or as an extract thereof.
• Typical phytosterols that may be used for the purpose of the present invention may be selected from the group consisting of plant sterols, stands, or combinations thereof.
• Phytosterols may be provided as chemically pure compounds. As such they may be purified from plant sources or synthesized chemically. This allows a very precise dosing.
• phytosterols from natural sources or extracts thereof.
• the phytosterols may be dietary phytosterols. They may be provided as vegetable oils, nuts, cereal products, vegetables, fruit, berries or as extracts thereof.
• the composition may be any composition that is suitable for human or animal consumption.
• the composition may be selected from the group consisting of a food product, a drink, a functional food, a nutraceutical , a food additive, a nutritional formula, and a pet food product.
• composition of the present invention may be to be administered to adults or the elderly.
• a subject shall be considered as "elderly" if it has surpassed the first half of its average expected lifespan in its country of origin, preferably, if it has surpassed the first two thirds of the average expected lifespan in its country of origin, more preferably if it has surpassed the first three quarters of the average expected lifespan in its country of origin, most preferred if it has surpassed the first four fifths of the average expected lifespan in its country of origin.
• composition of the present invention may be to be administered to people above the age of 45, 50, 55, 60, 65, 70, 75 or 80 years.
• composition of the present invention may be to be administered to humans or animals, for example companion animals such as cats or dogs.
• NIH and NCEP for fasting HDL levels and risk for heart disease a level of less than 40 mg/dL HDL cholesterol for men and less than 50 mg/dL HDL cholesterol for women causes a heightened risk for heart disease.
• An HDL cholesterol level of 60-50 mg/dL for women and of 60-40 mg/dL for men is considered normal.
• composition of the present invention may be to be administered to people with a fasting HDL cholesterol level of below 60 mg/dL, of below 50 mg/dL or of below 40 mg/dL .
• the American Heart Association, NIH, and NCEP have also provided a set of guidelines for fasting LDL-Cholesterol levels and risk for heart disease.
• a fasting LDL-Cholesterol level of 100 to 129 mg/dL corresponds to a near optimal LDL level, corresponding to higher rates for developing symptomatic cardiovascular disease events .
• a fasting LDL-Cholesterol level of 130 to 159 mg/dL corresponds to a borderline high LDL level, corresponding to higher rates for developing symptomatic cardiovascular disease events .
• a fasting LDL-Cholesterol level of 160 to 199 mg/dL corresponds to a high LDL level, corresponding to much higher rates for developing symptomatic cardiovascular disease events .
• a fasting LDL-Cholesterol level of above 200 mg/dL corresponds to a very high LDL level, corresponding to highest increased rates of symptomatic cardiovascular disease events.
• composition of the present invention may be to be administered to people with a fasting LDL cholesterol level of above 100 mg/dL, of above 130 mg/dL, of above 160 mg/dL or of above 200 mg/dL.
• composition of the present invention may be consumed briefly before, with or briefly after the consumption of a high-fat or high LDL cholesterol meal.
• a meal shall be considered high in fat if it contains more than 60%, more than 80% or more than 100% of the daily recommended fat intake.
• a meal shall be considered high in LDL cholesterol if it contains more than 60%, more than 80% or more than 100% of the daily recommended LDL cholesterol intake.
• the composition may be to be administered in the time frame from 1 hour before to 1 hour after a high fat and/or high LDL cholesterol meal.
• PS plant sterol
• H hawthorn
• LDL Cholesterol After 6 weeks of treatment, a high fat diet (HFD) significantly elevated LDL cholesterol by 27mg/dL (Tablel.2, HFD-placebo vs. control). Simultaneously treatment with plant sterol or hawthorn had no significant alteration on high LDL cholesterol compared to HFD placebo (Figl, HFD-H, HFD-PS vs. control, *P ⁇ 0.05; HFD-H, HFD-PS vs. HFD-Placebo, P>0.05) .
• hypertriglyceridemia denotes high ⁇ hyper-) blood levels (-emia) of triglycerides, the most abundant fatty molecule in most organisms. It has been associated with atherosclerosis, even in the absence of hypercholesterolemia (high cholesterol levels) . It can also lead to pancreatitis in excessive concentrations (i.e. when the triglyceride concentration is greater, and often very much greater, than 1000 mg/dl or 12 mmol/1) .
• Blood Triglyceride After 6 weeks of treatment, high fat diet significantly elevated the blood triglyceride by 126mg/dL (Table2, HFD-Placebo vs. control) . Plant sterol alone showed robust reduction on blood triglyceride in HFD hamsters (Fig. 3, HFD-PS vs. control, P>0.05; HFD-PS vs. HFD-Placebo, ⁇ P ⁇ 0.05) . Although did not show the reduction effect alone, hawthorn has enhanced the blood triglyceride reduction effect of plant sterol by 8.8mg/dL.
• TG Blood Triglyceride
• H Hawthorn
• PS Plant Sterol

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• 2012
  • 2012-02-10 WO PCT/CN2012/071019 patent/WO2013117008A1/fr not_active Ceased
• 2013
  • 2013-02-08 WO PCT/EP2013/052604 patent/WO2013117732A1/fr not_active Ceased

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