Classifications

• • 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
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/25—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
• • 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
  • A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
  • A23L29/10—Foods or foodstuffs containing additives; Preparation or treatment thereof containing emulsifiers
• • 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
  • A23L33/20—Reducing nutritive value; Dietetic products with reduced nutritive value
• • 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
  • A23L33/30—Dietetic or nutritional methods, e.g. for losing weight
• • 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
  • A61P3/04—Anorexiants; Antiobesity agents
• • 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
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
  • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

• the underlying reason for fatness is decreased physical activity together with an increased or unchanged amount of energy in the nutrition.
• fat contains the most energy, and with evolution, man 15 increasingly values fat not only as a source of energy, but also because of its palatability.
• the fat content in nutrition exceeds the recommendations.
• Continuous excessive intake of fat causes not only cosmetic harm associated with fatness, but also serious health problems and complications related to diseases, such as cardiovascular diseases, respi- 20 ratory diseases and diabetes. Significant costs are also associated with said national diseases.
• the most preferable way to prevent the drawbacks of excessive fat is increased exercise and adjustment of the energy obtained from food. Energy intake can be reduced for instance by observing a strict diet, by using low fat 25 preparations or by preventing full-scale utilization of the energy in the food.
• solutions based on this idea include for instance methods based on plant sterols and plant stanols, such as are described for instance in international patent publication WO 03/026672.
• American patent publication US 5,453,282 discloses chitosan-containing nutrients for preventing the absorption of the main component in fat, triacylglycerol (TAG), but, for the time being, the most effective prevention succeeds only by means of pharmacotherapy.
• TAG triacylglycerol
• the prescription medicine, orlistat tetrahydrolipstatin
• European patent EP 129748 can be used to reduce the absorption of triacylglycerols by 30% (Zhi et al., 1994).
• the invention relates to the use of an emulgator for the preparation of a product intended for the prevention of fat absorption.
• the use of a food- approved emulgator in the preparation of such a product fulfils the security requirements set by the authorities, thus enabling the preparation of a functional food fulfilling the regulations.
• Such a preparation is the first functional food that shows almost complete prevention of fat absorption in humans.
• the invention also relates to a food composition for preventing fat absorption, the emulgator being selected from the group consisting of sorbitan derivatives, polyoxyethylene sorbitan derivatives, saccharose esters of fatty acids and other fatty acid derivatives.
• the invention also relates to a functional food characterized in that it comprises an effective amount of a food-approved emulgator.
• the invention further relates to a pharmaceutical composition comprising an effective amount of an emulgator selected from the group consisting of sorbitan derivatives, polyoxyethylene sorbitan derivatives, saccharose es- ters of fatty acids and other fatty acid derivatives.
• the invention also relates to the use of an emulgator for the preparation of a pharmaceutical product intended for the prevention of fat absorption.
• the invention further relates to a method for the prophylaxis, treatment or alleviation of obesity and for reducing the risks associated with fatness, the method being characterized by administering, to a human or animal suffering from obesity, a preparation containing an effective amount of a pharmaceutically acceptable emulgator for preventing fat absorption, and optionally other, pharmaceutically acceptable additives and carriers.
• a pharmaceutically acceptable emulgator for preventing fat absorption and optionally other, pharmaceutically acceptable additives and carriers.
• FIG. 1 shows TAG concentrations measured from the plasma of subjects during 0 to 6 hours after intake of test product A
• Figure 2 shows TAG concentrations measured from the plasma of subjects during 0 to 6 hours after intake of test product B
• Figure 3 graphically shows the amount of fat absorbed by subjects as an iAUC value
• Figure 4 graphically shows the amount of fat absorbed expressed as percentages per tested product.
• the present invention is based on the surprising observation that a food-approved emulgator almost completely prevents fat absorption from the digestive tract. Said observation was made in a clinical trial whose aim was to find out how different treatments and formulations affect the absorption of valuable fats.
• the invention thus relates to the use of a food-approved emulgator as an additive or ingredient in a food product, as a nutriment additive or a pharmaceutical preparation for achieving a health-enhancing effect, i.e. partial or complete prevention of the absorption of fat.
• 'a food-approved emulgator' refers to a compound, detergent, emulgator or stabilizing agent accepted as a food additive.
• preferable food-approved emulgators include sorbitan derivatives of Formula I
• sorbitan derivatives such as sorbitan monostearate (E 491 ), sorbitan tristearate (E 492), sorbitan monolaurate (E 493), sorbitan monooleate (E 494) and sorbitan monopalmitate (E 495), or different polyoxyethylene sorbitan derivatives, such as -monolaurate (E 432), -monooleate (E 433), -monopalmitate (E 434), -monostearate (E 435) and -tristearate (E 436).
• sorbitan derivatives such as sorbitan monostearate (E 491 ), sorbitan tristearate (E 492), sorbitan monolaurate (E 493), sorbitan monooleate (E 494) and sorbitan monopalmitate (E 495), or different polyoxyethylene sorbitan derivatives, such as -monolaurate (E 432), -monooleate (
• a particularly preferable emulgator according to the inven- tion is sorbitan monooleate (E 494).
• Other preferable food-approved emulgators include saccharose esters (E 473) of fatty acids and other fatty acid derivatives, such as sodium salts, potassium salts and calcium salts (E 470a), magnesium salts (E 471), mono- and diglycerides (E 471 ), acetic acid esters (E 472a) of mono- and di- glycerides, lactic acid esters (E 472b) of mono- and diglycerides, citric acid (E 472c) esters of mono- and diglycerides, tartaric acid esters (E 472d) of mono- and diglycerides, mono- and diacetyl tartaric acid esters (E 472e) of mono- and diglycerides and mixtures of (E 472f) acetic acid and tartaric acid esters of mono- and diglycerides.
• Particularly preferable fatty acid derivative emulgators according to the invention include saccharose esters of fatty acids.
• the nutrient composition of the invention is the first functional food that has been proved to show an almost complete prevention of fat absorption in humans or animals.
• 'a functional food' refers to a nutrient/food product that has been shown to have, not only the conventional nutritional characteristics, but also a positive effect on one or more functions of the organ- ism in a manner enhancing health or reducing the risk of disease.
• the functional food according to the invention may be any food product, to which an emulgator according to the invention has been added, but preferable food products include beverages and other liquid food products, such as juices, milk beverages, gruel, soups and sauces.
• fat- containing food products or ingredients of food products whereto the food- approved emulgator of the invention can be added, include fat emulsions for baking or other use, cream-imitation preparations, ice creams, emulsified sauces, such as hamburger sauces, salad sauces and dip sauces, thermally processed meat preparations, such as a cooked hamburger and different chocolates.
• the functional foods of the invention also include fatty food products, such as pastry, cookies, potato chips, hamburgers and chocolates, in whose preparation the above fatty emulsions are used.
• Other preferred forms of use are evident to a person skilled in the art, and the intention is not for the above examples to restrict other applications outside the scope of the present invention.
• an amount of a food-approved emulgator is added that the desired effect is achieved.
• the effective amount may vary significantly depending on the composition of said food product and depending on the size of the dose of said food product to be ingested at a time.
• An effective amount of emulgator may also vary in accordance with the emulgator used, the food product and the amount of food product ingested.
• An effective amount of emulgator is 0.1 to 100 g/kg food product, preferably 1 to 25 g/kg, and most preferably 5 to 10 g/kg.
• a preferable form of use according to the invention are separately consumed functional foods ingested in addition to normal nutrition, for example as a snack bar or an 'energy drink'.
• the supple- ment of the invention may be for instance a capsule containing an effective amount of the emulgator of the invention.
• the capsule may be a soft or hard capsule, and the encapsulation material may be selected from the group consisting of gelatine, agar, starch, modified starch, modified starch power, carrageen, sugar, particularly sucrose, lactose or fructose.
• a preferable amount of emulgator per dose to be ingested is more than 1 mg, preferably 1 to 10,000 mg, more preferably 100 to 5,000 mg, still more preferably 500 to 5,000 mg, and most preferably 2,000 mg.
• Such preferable amounts correspond to 0 to 65 mg/person's weight-kg, most preferably about 25 to 60 mg/kg.
• the invention also relates to a pharmaceutical composition that can be a tablet, capsule, solution or emulsion depending on the emulgator used.
• the pharmaceutical composition of the invention can be prepared by using conventional methods.
• the pharmaceutical dosage form of the invention can be for instance a capsule containing an effective amount of the emulgator of the invention.
• the capsule may be a soft or hard capsule, the encapsulation material being selected from the group consisting of gelatine, starch, modified starch, modified starch powder, carrageen, sugar, particularly sucrose, lactose or fructose.
• the emulgator-containing pharmaceutical preparation of the invention can be prepared by using conventional methods (see for example Reming- ton's Pharmaceutical Sciences, 16. volume, 1990).
• the therapeutically effective amount of emulgator per unit can be, according to the desired effect, 1 to 10,000 mg, preferably 100 to 5,000 mg, more preferably 500 to 5,000 mg, and most preferably 2,000 mg.
• the pharmaceutical preparation of the invention may also contain other additives and carriers gen- erally used in the field, for instance pharmaceutically acceptable vegetable oils, such as paraffin oil, arrack oil, sesame oil, olive oil, soy oil and amygdale oil.
• the present invention also relates to a method of preventing partial absorption or complete absorption of fat from the digestive tract in an animal or human in need thereof, by administering an effective dose of the nutrient com- position or pharmaceutical composition of the invention, containing a food- approved emulgator.
• the method of the invention achieves cosmetic or therapeutic weight control and thus prophylaxis of health hazards or diseases associated with excessive use of fat or a decrease in the risk of contracting a disease.
• the treatment according to the invention can be administered either by ingestion of the functional food of the invention to replace part of normal nutrition, by ingestion of the functional food, for instance a beverage dose, in addi- tion to normal fatty nutrition, or by ingestion of a separate supplement, for instance in capsule form, as a supplement to normal nutrition.
• An effective single dose in connection with each meal, i.e. three times daily, is 500 mg/dose, which achieves the desired prevention of fat absorption.
• Ingredients 1 to 5 were mixed in accordance with a normal industrial preparation process. Ingredients 6, 7, 8 and 9 were added to the product under vigorous mixing.
• Ingredients 1 to 3 are mixed and acidified in accordance with a normal industrial preparation process.
• Ingredients 4 and 5 are mixed into the acidified prod- uct.
• Ingredients 6, 7, 8 and 9 are added to the product under vigorous mixing.
• the average single dose of the test product was thus 490 ml.
• the subjects in the control group ingested a corresponding oil-containing product (product A0), which did not contain emulgator.
• product A0 oil-containing product
• the next six hours the subjects spent under surveillance at the experimental laboratory, and altogether seven blood samples were taken from each them.
• the blood samples were collected before the test product was ingested and 30, 60, 180, 270 and 360 minutes thereafter.
• the subjects were contacted in order to find out any acute side effects.
• Experimental day 2 was carried out after 2 to 4 weeks, the arrangements being similar ex- cept for the test product ingested.
• the samples collected were either analyzed immediately or frac- tioned and frozen to wait for analyses to be performed later.
• the composition of cylomicrons was studied, since the lipids contained therein di- rectly reflect the fats and liposoluble compounds absorbed from a meal.
• the cylomicrons were separated from the plasma by ultracentrifugation and further fractioned into fatty acid and phospholipid fractions by means of micro silica columns.
• the fatty acids in the fractions were analyzed by gas chromatogra- phy.
• the results were subjected to statistical observation using the SPSS soft- ware.
• the enzymatically measured triacyl glycerol content in the plasma suggested non-absorption of emulsified oil. The result was highly unexpected, since it seemed as if absorption was completely prevented.
• test product A which contained emulsified oil
• Vitamin E and vitamin A as retinyl palmitate, which is soluble in the same way as fat, were added to the test products. It allows fat absorption, and, to some degree, the number of cylomicrons in the blood circulation, i.e. the discharge of fat from the blood circulation, to be monitored. No vitamin E and A could be measured from the samples of the subjects who were given the emulgator-containing product.
• the test products contained no cholesterol. However, a clear differ- ence between products A and A0 was observed in the cholesterol values. This result further supports the observations about the non-absorbability of emulsified oil, since fat absorption affects the organism's own cholesterol metabolism.
• EFFECT OF EMULGATOR DOSE ON FAT ABSORPTION the subjects ingested different amounts of emulgator-containing products.
• the test products were products A and B, prepared in Example 1 , wherein the amount of E494 was 0.1% (A1 and B1), 0.4% (A2 and B2), 0.98% (A3 and B3) or 0% (A0 and B0).
• the experiment and the sam- pling were arranged as was described in Example 2.
• the amount of test product ingested was proportional to the weights of the subjects such that the emulgator dose was according to Table 1. Thus, the average single dose was 490 ml.
• Figure 1 shows blood fat values during 0 to 6 hours for subjects that ingested test product A, and Figure 2 for subjects that ingested test product B.
• Figure 3 is a bar diagram showing the area (iAUC) remaining under the curves of Figures 1 and 2, which is an indicator of the amount of fat absorbed by a person and generally employed in the field.
• the dosage levels used in this example have a linear effect regarding product A.
• product B the effect is visible at all dosage levels, but on levels B1 and B2, the effect is equal. This refers to a possible plateau on the dose-response curve.
• the effect of the test products on the prevention of fat absorption was already clearly shown at lower dosage levels.
• the lower total level is likely to be due to the product being more complex (contains proteins and complex carbohydrates, for example), whereby the effect on fat absorption is not as strong as for product A.
• the effect manifested by product B shows that the functional food of the invention achieves the desired effect.
• NCCDPHP National Center for Chronic Disease Prevention and Health Promotion

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Food Science & Technology (AREA)
• Nutrition Science (AREA)
• Polymers & Plastics (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Mycology (AREA)
• Organic Chemistry (AREA)
• Emergency Medicine (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Obesity (AREA)
• Hematology (AREA)
• Diabetes (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Epidemiology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Child & Adolescent Psychology (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• General Preparation And Processing Of Foods (AREA)
• Medicinal Preparation (AREA)
• Fats And Perfumes (AREA)
• Furan Compounds (AREA)
• Medicines Containing Plant Substances (AREA)

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• 2004
  • 2004-03-15 FI FI20045076A patent/FI20045076L/fi not_active Application Discontinuation
• 2005
  • 2005-03-14 RU RU2006132453/13A patent/RU2386365C2/ru not_active IP Right Cessation
  • 2005-03-14 BR BRPI0509243-4A patent/BRPI0509243A/pt not_active IP Right Cessation
  • 2005-03-14 AT AT05717277T patent/ATE407575T1/de active
  • 2005-03-14 ES ES05717277T patent/ES2314636T3/es not_active Expired - Lifetime
  • 2005-03-14 JP JP2007503361A patent/JP2007529478A/ja active Pending
  • 2005-03-14 DE DE602005009676T patent/DE602005009676D1/de not_active Expired - Lifetime
  • 2005-03-14 US US10/592,398 patent/US20080038318A1/en not_active Abandoned
  • 2005-03-14 DK DK05717277T patent/DK1729598T3/da active
  • 2005-03-14 CN CN2005800153970A patent/CN1953670B/zh not_active Expired - Fee Related
  • 2005-03-14 WO PCT/FI2005/000151 patent/WO2005087025A1/en not_active Ceased
  • 2005-03-14 CA CA002559175A patent/CA2559175A1/en not_active Abandoned
  • 2005-03-14 EP EP05717277A patent/EP1729598B1/en not_active Expired - Lifetime
  • 2005-03-14 AU AU2005220626A patent/AU2005220626B2/en not_active Ceased

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