[go: up one dir, main page]

WO2007109884A1 - Composition piégeant les matières grasses comprenant un polysaccharide cationique non digestible et un agent émulsifiant - Google Patents

Composition piégeant les matières grasses comprenant un polysaccharide cationique non digestible et un agent émulsifiant Download PDF

Info

Publication number
WO2007109884A1
WO2007109884A1 PCT/CA2007/000483 CA2007000483W WO2007109884A1 WO 2007109884 A1 WO2007109884 A1 WO 2007109884A1 CA 2007000483 W CA2007000483 W CA 2007000483W WO 2007109884 A1 WO2007109884 A1 WO 2007109884A1
Authority
WO
WIPO (PCT)
Prior art keywords
fat
composition
chitosan
trapping
emulsifying agent
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CA2007/000483
Other languages
English (en)
Other versions
WO2007109884A8 (fr
Inventor
Tien Canh Le
Catherine Dupuis
Claudia Schlegel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LABORATOIRES MAUVES Inc
Original Assignee
LABORATOIRES MAUVES Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by LABORATOIRES MAUVES Inc filed Critical LABORATOIRES MAUVES Inc
Priority to CA002644585A priority Critical patent/CA2644585A1/fr
Publication of WO2007109884A1 publication Critical patent/WO2007109884A1/fr
Publication of WO2007109884A8 publication Critical patent/WO2007109884A8/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • 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
    • A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
    • A23L29/275—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of animal origin, e.g. chitin
    • 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
    • A23L33/21—Addition of substantially indigestible substances, e.g. dietary fibres
    • A23L33/28—Substances of animal origin, e.g. gelatin or collagen
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716—Glucans
    • A61K31/722—Chitin, chitosan
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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

Definitions

  • the present invention relates to a composition for trapping fat in the digestive tract, thus preventing its degradation and absorption.
  • Medications currently approved for weight loss in the United States fall into two broad categories: i) those that are aimed at decreasing food intake by reducing the appetite or increasing satiety (appetite suppressants) and ii) those that are aimed at decreasing nutrient absorption.
  • a third category i.e. medications that increase energy expenditure (such as ephedrine) and other investigational compounds, is not currently approved as a treatment for obesity in the United States.
  • appetite suppressants work primarily by increasing the availability of anorexigenic neurotransmitters notably, norepinephrine, serotonin, dopamine, or some combination of these neurotransmitters in the central nervous system.
  • Noradrenergic drugs available in the United States include phentermine, diethylpropion, phendimetrazine, and benzphetamine. Amphetamines are no longer recommended (and are not approved for use) for weight loss because of the potential for their abuse. All of the above medications are approved by the Food and Drug Administration (FDA) for use lasting «a few weeks» only (generally presumed to be 12 weeks or less) for the treatment of obesity. These drugs used in combination may be just as effective as either drug alone, with the added advantages of the need for lower doses of each agent and perhaps fewer side effects. Although the combination has not been approved by the FDA, in 1996 the total number of prescriptions in the United States for fenfluramine and phentermine exceeded 18 million.
  • Serotonergic agents act by increasing the release of serotonin, inhibiting its reuptake, or both such as Fenfluramine (Pondimin) and dexfenfluramine (Redux). These drugs were withdrawn from the market in the United States in 1997 due to their association with valvular heart disease and pulmonary hypertension. Their efficacy in controlled studies appeared similar to that of the noradrenergic agents.
  • Another inhibitor of both norepiphedrine et serotonin reuptake approved by the FDA for weight loss is Sibutramine (Meridia) which, unlike fenfluramine and dexfenfluramine, has not been implicated in the development of valvular heart disease. However, adverse reactions such as hypertension, dry mouth, headache, insomnia, and constipation were reported.
  • OrlistatTM acts as a gastro-intestinal lipase inhibitor preventing hydrolysis of fat (triglycerides) into absorbable free fatty acids and monoacylglycerols.
  • OrlistatTM might be viewed as an analog of a diuretic.
  • the loss of calories as undigested triglycerides would be similar to the loss of sodium with diuretics.
  • the centrally active noradrenergic and serotonergic drugs approved by the FDA for treatment of obesity may be analogous to the earlier drugs used to treat hypertension.
  • Orlistat, found under the commercial name Xenical ® belongs to a new class of anti-obesity drugs. It prevents the lipolysis of dietary triglycerides (TG), and thus reduces the subsequent intestinal absorption of fat.
  • Human pancreatic lipase (HPL) has been the main target in the development of Orlistat.
  • HGL human gastric lipase
  • Orlistat has also been investigated in vitro but studies have not yet been carried out by way of test meals. In most clinical studies, the effects of Orlistat have been estimated indirectly from the fecal fat excretion levels, but the inhibition exerted on digestive lipases and the levels of lipolysis have not been measured simultaneously in vivo.
  • Adverse effects of Orlistat include flatulence with discharge, fecal urgency, fecal incontinence, steatorrhea, oily spotting, and increased frequency of defecation. These side effects are usually mild to moderate, and generally decrease in frequency with ongoing treatment. Orlistat also decreases absorption of fat-soluble vitamins, primarily vitamin D, an effect that can be counteracted by daily administration of a multivitamin at least two hours before or after a dose of Orlistat. - A -
  • statins PulravacholTM, LipitorTM, CrestorTM, etc.
  • the main activity of statins consists of inhibiting the enzyme HMG-CoA reductase, which is the rate-limiting enzyme of the mevalonate pathway of cholesterol synthesis.
  • HMG-CoA reductase the rate-limiting enzyme of the mevalonate pathway of cholesterol synthesis.
  • dietary supplements and herbal preparations are not prospectively reviewed for safety or efficacy by the FDA, who takes action only if a dietary supplement is shown to present «a significant or unreasonable risk».
  • Producers of a dietary supplement cannot claim that it treats a disease (including obesity), but may claim that it reduces the risk of a disease in a population.
  • fat burners thermoogenics
  • Xenadrine Hydroxycut
  • Diet Fuel etc.
  • Xenadrine is a thermogenic formula containing various important ingredients such as ephedrine, caffeine, aspirin (E/C/A) and synephrine.
  • Greenway Greenway, F.L. 2001. Obes. Rev., 2, 199-211 reported that ephedrine can reduce body weight.
  • This component is the primary active constituent of the botanical Ephedra sinica (or ma-huang, an evergreen shrub native to central Asia), which has been studied alone and in combination with caffeine. Results showed that the combination of ephedrine and caffeine is effective for reducing body weight and appears to outweigh the risks.
  • Hydroxycut is also a thermogenic weight loss supplement which possesses a similar formulation of Xenadrine composed of hydroxycitric acid, L- Carnitine, green tea extract, ephedrine, guaranine (caffeine extracted from guarana) and willow bark (herbal extracted from aspirin). These ingredients create a cause and effect resulting in appetite suppression and fat burning.
  • the Diet Fuel it is a formulation which includes milk protein-based products (such as whey protein concentrate, whey protein isolate, calcium caseinate, egg albumen, and soy protein isolate), maltodextrin, fructo- oligosaccharides, fructose and mineral mixture of chromium, boron, selenium, etc.
  • milk protein-based products such as whey protein concentrate, whey protein isolate, calcium caseinate, egg albumen, and soy protein isolate
  • maltodextrin such as whey protein concentrate, whey protein isolate, calcium caseinate, egg albumen, and soy protein isolate
  • maltodextrin such as whey protein concentrate, whey protein isolate, calcium caseinate, egg albumen, and soy protein isolate
  • maltodextrin such as maltodextrin, fructo- oligosaccharides, fructose and mineral mixture of chromium, boron, selenium, etc.
  • a dietary fiber, guar gum, derived from the Indian cluster bean (Cyamopsis tetragonolobus) was assessed as an effective agent in lowering body weight.
  • Pittler and Ernst (Pittler MH, Ernst E. 2001. Am. J. Med., 110, 724-730) showed that guar gum is not effective in reducing body weight, and adverse effects relate to the gastro-intestinal system.
  • Yohimbe (Pausinystalia yohimbe) is a tall evergreen tree that is native to Central Africa. Yohimbine, an ⁇ -2 receptor antagonist, is the main active constituent of the ground bark of P. yohimbe. Most clinical studies relate to the effects of this isolated constituent of yohimbe bark. At present, therefore, it is unclear whether Yohimbine is effective in reducing body weight, and few adverse effects have been reported.
  • One aim of the present invention is to provide a composition for trapping lipids and excretion of lipids (one of the major causes of obesity), by preventing their degradation and absorption, resulting in excretion of same.
  • a fat- trapping composition comprising:
  • a method for treating obesity in a mammal comprising the step of orally administering to the mammal an effective amount of a fat-trapping composition as defined herein.
  • a method for reducing absorption of dietary fat in a mammal comprising the step of orally administering to the mammal a therapeutic amount of a fat-trapping composition as defined herein.
  • a method for treating and/or reducing hypertriglyceridemia in a mammal comprising the step of orally administering to the mammal a therapeutic amount of a fat-trapping composition as defined herein.
  • polymers can be employed in the invention described herein.
  • Preferred polymers are cationic polysaccharides.
  • the polysaccharides must not be degraded or digested in the intestinal tract.
  • the present invention also relates to a method for treating obesity, a method for reducing the absorption of dietary fat, and a method for treating hypertriglyceridemia in a patient with the composition of the present invention.
  • the composition of the present invention can also be used for the manufacture of a medicament for the treatment of the above-mentioned conditions.
  • the methods comprise the step of orally administering to a mammal, such as a human, a therapeutically effective amount of the fat-trapping composition described herein.
  • the administration of the composition of the present invention prevents adsorption of fat from the body.
  • the fat-binding composition is administered in combination with other dietary supplements or dietary fibers, as described herein.
  • the term "in combination" in this context includes both simultaneous and sequential administration, but preferably a sequential application where the composition is administered first.
  • the fat- binding polymer and lipase inhibitor when used in combination, can be employed together in the same dosage form or, as disclosed herein, preferably in separate dosage forms taken at the same time or within a certain period of time, wherein both the fat-binding composition and the dietary supplements or the dietary fibers are present in a therapeutically effective amount.
  • Frat-trapping composition or “Fat-trapping formulation”, as these terms are used interchangeably herein, relates to a formulation or a composition which absorbs, binds or otherwise associates with fat thereby preventing fat digestion, hydrolysis, or absorption in the gastro-intestinal tract.
  • Fats are solids or liquid oils generally consisting of glycerol esters of fatty acids.
  • Sources of fats include both animal and vegetable fats, for example, triglyceride esters of saturated and/or unsaturated fatty acids, free fatty acids, diglycerides, monoglycerides, phospholipids and cholesterol esters are fats, as defined herein.
  • the terms "therapeutically effective amount” and “therapeutic amount” are synonymous.
  • the terms refer to an amount which is sufficient to treat obesity, reduce the absorption of fat or treat hypertriglyceridemia.
  • the dosage of the fat-trapper formulation to be administered to a patient will vary depending among other things on the weight of the patient, age, sex and the general health of the patient. The dosage can be determined with regard to established medical practice.
  • the amount of fat- trapper formulation administered can be in the range of from about 0.1 g to about 30 g a day.
  • the fat-trapper formulation of the invention can be formulated using conventional inert pharmaceutical adjuvant materials into dosage forms which are suitable for oral administration.
  • the oral dosage forms include tablets, capsules, suspension, solutions, and the like.
  • the identity of the inert adjuvant materials which can be used in formulating the fat-trapper formulation of the invention will be immediately apparent to persons skilled in the art.
  • Fig. 1 illustrates FTIR spectra of lecithin, chitosan and lecithin/chitosan complex.
  • the composition aims to trap and promote the excretion of lipids such as triglycerides, fatty acids and bile acids, as well as cholesterol and other sterols.
  • the composition consists of mixing a polysaccharide to be used as a matrix (i.e. chitosan) with an emulsifying agent entrapped therein and used as enhancer (i.e. lecithin) which present a high affinity to the various fatty matters thus increasing the lipid binding capacity of the composition.
  • a suitable gelling agent i.e.
  • hydroxyl citric acid sodium salt and/or xanthan gum are able to form a stable complex which prevents the fat release from the matrix and promotes their excretion.
  • Other dietary fibers, dietary supplements (i.e. hoodia extract) and/or additives (flavoring agent, masking agent, preservative agents, etc.) could also be added to the formulation.
  • the composition also referred to as a fat trapper in this invention includes:
  • a cationic polysaccharide i.e. chitosan
  • an emulsifying agent i.e. lecithin
  • an enhancer which can increase the fat binding capacity of chitosan in the gastric medium and also play a role in stabilizing the chitosan/fat complex during intestinal transit;
  • dietary fibers i.e. xanthane gum, fructose- oligosaccharide, inuline, etc.
  • dietary supplements hydroxycitric acid sodium salt or HCA extracted from Garcinia cambogia, phaseolamine extracted from white kidney bean, Phaseolus vulgaris and hoodia extracted from Hoodia gordonii, etc.
  • the matrix is generally selected from cationic (positively charged) polysaccharides such as chitosan or other aminopolysaccharides.
  • Chitosan is a deacetylated form of chitin, an aminopolysaccharide found in the shell of the crustacean (shrimp or crab) or the exoskeleton of the arthropod and certain fungi. Chitosan is indigestible by mammalian digestive enzymes.
  • chitosan can bind some amounts of fats; and ii) the amount of fat binding and excretions can be significant and lead to weight loss.
  • a fat binding capacity of chitosan to fats in the stomach interferes with the complex chitosan/fat due to the presence of other substances (i.e. bile acids) and changes of environment (pH value, viscosity, etc.) during intestinal transit.
  • the molecular weight of chitosan essentially plays an important role in the binding capacity of the lipids.
  • an experiment was carried out dispersing an amount of 1.0 g of chitosan (purchased from Marinard Biotech, Riviere-au-Renard, QC, Canada) at various molecular weights (75-1500 kDa, DDA 85%) in 94.0 g of simulated gastric fluid (pH 1.2 according to USP method 27) at 37 0 C. Thereafter, an amount of 5.0 g of triolein was added under agitation in order to maintain conditions imitating those in the human stomach. After 1 h, the shaker was stopped and the quantity of separated triolein was determined.
  • chitosan possessing a low (400 kDa) or high (800 kDa) Mw with any DDA shows a complete destabilization of complex chitosan/triolein in the presence of bile acids.
  • the destabilization of complex chitosan/triolein by bile acids was approximately 80%.
  • the important feature is that these bioadhesive properties of the mucosa intestine could constitute a main factor in destabilizing the complex chitosan fats, as well as the bile acids. In addition, this phenomenon can increase the intestinal transit time which could cause adverse effects, such as flatulence or constipation, in certain people.
  • the destabilization of .the complex chitosan/fat could be due to several factors, mainly the bile acids under intestinal conditions. Great attention has been directed to address these destabilization problems of the chitosan and lipids.
  • an emulsifying agent preferably a natural emulsifying agent such as a phosphoglyceride
  • the addition of an emulsifying agent to the chitosan can improve the stability of the complex chitosan/fat.
  • emulsifying agents which possess negative charges such as phosphatidylinositol, phosphatidic acids or zwitterion molecules or phosphoglycerides (phosphatidylcholine, phosphatidylethanolamine, phosphatidyl-serine, etc.).
  • the reason for the use of emulsifying agents possessing a negative charge in this embodiment consists in creating ionic interactions with chitosan (i.e. a positively charged polysaccharide) in order to generate a stable and resistant matrix under gastrointestinal conditions.
  • lecithin is preferably used, because it is nontoxic, commercially available at low cost and approved by the Food and Drug Administration (FDA) for human consumption.
  • Lecithin is a mixture consisting mainly of phospholipids (phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, etc.), glycolipids and triglycerides. Lecithin may be isolated from soy beans, sun flower or egg yolk, etc.
  • the emulsifying agent used in combination with chitosan is necessary to enhance the affinity of the matrix with fats and the stabilization of the matrix during gastro-intestinal transit. It is worth noting that preferably chitosan with Mw 100-1000 kDa and DDA 75-99% is used.
  • the daily quantities could be varied 0.1 to 5.0 g/day and the emulsifying agent quantities could be from about 0.25 to 10.0 g/ day.
  • these dietary supplements or fibers are used to improve the resistance of the matrix and/or to avoid the possible side effects of chitosan (i.e. constipation).
  • these dietary supplements or fibers are preferably administered subsequently to the composition of the present invention, and more preferably after a meal.
  • These dietary fibers can, for example, be anionic polysaccharides (e.g. pectin, xanthan gum, alginate, carrageenan, etc. or any combination thereof) which could gel with the complex chitosan/fat and promote its excretion.
  • Uncharged compounds such as inuline, guar gum or FOS (fructo- oligosaccharide), etc., can also be included in the formulation.
  • the advantage in using these natural molecules is that they are non-toxic (edible) and readily available at low cost.
  • Other dietary supplements can also be added to the formulation.
  • These other dietary supplements can be, for example, HCA sodium salt extract (from Garcinia cambogia), phaseolamine extract (from white kidney bean Phaseolus vulgaris which contains an alpha-amylase inhibitor), hoodia extract (from Hoodia gordonii which is responsible for its appetite-suppressant effect), corosolic acid extract (from banana leaves), fructo-oligosaccharide (FOS), inuline, guaranine, theobromine, theophyllin, tannic acid, forskolin (Coleus forskolii), rosalin (Rhodiola rosea), polyphenols (primrose oil, green tea, pomegranate, etc.), phytosterols (tribulus, maca, acai, etc.), xanthones (mangostino), 5-hydroxytryptophane (from Griffonia simplicifolia), boswellic acid (Boswellia serrata
  • composition of the present invention can also be formulated into a liquefied form such as a syrup or juice mixture.
  • flavoring and/or savoring agents and preservative agents can also added to the formulation.
  • composition of the present invention is preferably administered after a meal.
  • quantity of additive compounds it varies from one compound to another.
  • the quantity of HCA used after a meal can be varied from about 0.1 g to 5 g/ day, whereas pectins could reach up to 10 g/ day.
  • pectins could reach up to 10 g/ day.
  • One skilled in the art will know the amount of any desired additive compounds to be used.
  • chitosan disperses in gastric fluid (pH 1.2-2.5) and associates with the emulsifying agent (such as lecithin) via ionic interaction between the amino group of chitosan and the phosphate group of phospholipids.
  • emulsifying agent such as lecithin
  • Fig. 1 FTIR analysis using a Spectrum 100 (Perkin-Elmer Instruments, FT-IR spectrometer Norwalk, USA) equipped with a Universal Attenuated Total Reflectance (UATR) device recording in the spectral region of 1800-600 cm “1 with 256 scans at 4 cm "1 resolution. All spectra were normalized over the range using the Spectrum software version 3.02.
  • the band of chitosan spectrum at 1512 cm "1 assigned to the NH 2 scissoring vibration of the primary amino group was not (or weakly) present in the chitosan/lecithin spectrum.
  • This event was due to the formation in acidic medium of a chitosan ionized form and to the ionic interaction of the amino groups of chitosan with the phosphate groups of phospholipids in lecithin.
  • the absorption band of phosphate groups was shifted from 1236 cm "1 in the lecithin to 1230 cm "1 in the chitosan/lecithin mixture which indicates the ionic interaction has taken place.
  • the chitosan/lecithin association attracts fat droplets and forms particles in the stomach before they are exposed to the action of the bile acids and the pancreatic enzymes in the intestine.
  • these particles reach the intestinal tract (pH ⁇ 7.0), they became more and more stable due to the pH change causing chitosan gelation, forming a matrix.
  • This phenomenon is interesting because it promotes the formation of a stable barrier which separates the fat from the bile acids and the lipases.
  • a gelling agent i.e. HCA, pectin, xanthan gum or a combination thereof
  • HCA hydroxycellulose
  • pectin hydroxycellulose
  • xanthan gum a combination thereof
  • the matrix surroundings can limit the access of lipases to fats and/or restrict the migration of fats from the matrix to the outside environment. This phenomenon prevents the lipolysis and the micelles formation of fat with the bile acids which can contact the epithelial cells of the intestine from where the absorption would normally take place.
  • the chitosan a cationic polymer
  • the chitosan is susceptible to interact with the lipases by ionic interactions, and possibly leads to a certain decrease in the lipolysis activity.
  • the undigested matrix of chitosan/fat complex travels through the intestine and is then excreted.
  • the composition of the present invention can be formulated into various forms, such as tablets, capsules, suspension, solution, powder or used as a supplement in food.
  • the daily doses could be varied from 0.1 to 30 g of matrix/day and at least as many additives.
  • Chitosan with Mw ⁇ 1000 kDa with DDA >75 % is preferably used. To obtain better results, it is recommended to consume the matrix composition approximately 20-30 minutes before a meal and the other diet supplement separately at the end of a meal.
  • chitosan and lecithin are commercially available in powder form and in this case, chitosan (approximately 150 kDa and DDA, 90 %) and lecithin are simply mixed together in a proportion of 1 :5 respectively to obtain a homogeneous mixture.
  • HCA and xanthan gum can be further added in a ratio of HCA/xanthan gum of 3:1.
  • the resulting powder mixture can be used as an additive in juices or food.
  • the resulting powder could be compressed directly.
  • the capsule With regard to the capsule, the latter is carried out by a powder filling machine.
  • Phosphatidylcholine enriched lecithin may be obtained by fractionation in ethanol. While most other phospholipids do not dissolve well in ethanol, phosphatidylcholine does. Practically, an amount of 100 g of lecithin is dispersed in 1 L of absolute ethanol at 40 0 C. After 2 h stirring, the supernatant is separated and the ethanol is removed by evaporation at 75-80 0 C. The remaining residue constitutes the phosphatidylcholine enriched lecithin fraction.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Organic Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dispersion Chemistry (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une composition servant à piéger les lipides ou les matières grasses, ce qui empêche de cette manière leur décomposition et leur absorption dans l'appareil digestif. La composition piégeant les matières grasses de l'invention comprend un polysaccharide cationique comestible mais non digestible (de préférence le chitosan) et au moins un agent émulsifiant (de préférence un phosphoglycéride tel que la lécithine), s'associant dans l'estomac et formant dans l'intestin une matrice servant à piéger la matière grasse. En outre, la présente invention concerne des procédés servant à traiter l'obésité, à réduire l'absorption de matière grasse alimentaire et à traiter et/ou réduire l'hypertriglycéridémie, en administrant oralement la composition piégeant les matières grasses de l'invention.
PCT/CA2007/000483 2006-03-24 2007-03-23 Composition piégeant les matières grasses comprenant un polysaccharide cationique non digestible et un agent émulsifiant Ceased WO2007109884A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA002644585A CA2644585A1 (fr) 2006-03-24 2007-03-23 Composition piegeant les matieres grasses comprenant un polysaccharide cationique non digestible et un agent emulsifiant

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US74374006P 2006-03-24 2006-03-24
US60/743,740 2006-03-24

Publications (2)

Publication Number Publication Date
WO2007109884A1 true WO2007109884A1 (fr) 2007-10-04
WO2007109884A8 WO2007109884A8 (fr) 2007-11-08

Family

ID=38540747

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA2007/000483 Ceased WO2007109884A1 (fr) 2006-03-24 2007-03-23 Composition piégeant les matières grasses comprenant un polysaccharide cationique non digestible et un agent émulsifiant

Country Status (2)

Country Link
CA (1) CA2644585A1 (fr)
WO (1) WO2007109884A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITUA20161937A1 (it) * 2016-03-23 2017-09-23 S I I T S R L Servizio Int Imballaggi Termosaldanti Preparazione per il controllo del peso corporeo a base di chitosano e cellulosa
US9833642B2 (en) 2009-08-28 2017-12-05 Mary Kay Inc. Skin care formulations
US10130673B2 (en) 2006-01-19 2018-11-20 Mary Kay Inc. Compositions comprising kakadu plum extract or acai berry extract
US11806352B2 (en) 2010-05-19 2023-11-07 Upfield Europe B.V. Theobromine for increasing HDL-cholesterol

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4223023A (en) * 1978-10-12 1980-09-16 Ivan Furda Nonabsorbable lipid binder
US5932561A (en) * 1997-10-24 1999-08-03 Rexall Sundown, Inc. Dietary composition with lipid binding properties for weight management and serum lipid reduction
CA2514952A1 (fr) * 2003-02-06 2004-08-19 Advanced Biopolymers As Produit alimentaire au chitosane

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4223023A (en) * 1978-10-12 1980-09-16 Ivan Furda Nonabsorbable lipid binder
US5932561A (en) * 1997-10-24 1999-08-03 Rexall Sundown, Inc. Dietary composition with lipid binding properties for weight management and serum lipid reduction
CA2514952A1 (fr) * 2003-02-06 2004-08-19 Advanced Biopolymers As Produit alimentaire au chitosane

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
HAN L.-K.: "Reduction in fat storage during chitin-chitosan treatment in mice fed a high-fat diet", INTERNATIONAL JOURNAL OF OBESITY, vol. 23, 1999, pages 174 - 179 *
NAUSS J.L. ET AL.: "The Binding of Micelar Lipids to Chitosan", LIPIDS, vol. 18, 1983, pages 714 - 719 *
NI MHURCHU C. ET AL.: "Chitosan for overweight or obesity (review)", COCHRANE DATABASE SYST. REV., vol. 20, no. 3, July 2005 (2005-07-01), pages 1 - 44 *
PITTLER M.H. AND ERNST E.: "Dietary supplements for body-weight reduction: a systematic review", AM. J. CLIN. NUTR., vol. 79, no. 4, April 2004 (2004-04-01), pages 529 - 536, XP009060450 *
YLITALO R. ET AL.: "Cholesterol-lowering properties and safety of chitosan", ARZNEIMITTELFORSCHUNG, vol. 52, no. 1, 2002, pages 1 - 7 *

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10675323B2 (en) 2006-01-19 2020-06-09 Mary Kay Inc. Topical compositions comprising acai berry extract
US12186357B2 (en) 2006-01-19 2025-01-07 Mary Kay Inc. Compositions comprising kakadu plum extract or acai berry extract
US10130673B2 (en) 2006-01-19 2018-11-20 Mary Kay Inc. Compositions comprising kakadu plum extract or acai berry extract
US10918591B2 (en) 2006-01-19 2021-02-16 Mary Kay Inc. Compositions comprising kakadu plum extract or acai berry extract
US10668124B2 (en) 2006-01-19 2020-06-02 Mary Kay Inc. Compositions comprising kakadu plum extract or acai berry extract
US10434340B2 (en) 2009-08-28 2019-10-08 Mary Kay Inc. Skin care formulations
US11123578B2 (en) 2009-08-28 2021-09-21 Mary Kay Inc. Skin care formulations
US11596813B2 (en) 2009-08-28 2023-03-07 Mary Kay Inc. Skin care formulations
US11679284B2 (en) 2009-08-28 2023-06-20 Mary Kay Inc. Skin care formulations
US12097393B2 (en) 2009-08-28 2024-09-24 Mary Kay Inc. Skin care formulations
US9833642B2 (en) 2009-08-28 2017-12-05 Mary Kay Inc. Skin care formulations
US11806352B2 (en) 2010-05-19 2023-11-07 Upfield Europe B.V. Theobromine for increasing HDL-cholesterol
ITUA20161937A1 (it) * 2016-03-23 2017-09-23 S I I T S R L Servizio Int Imballaggi Termosaldanti Preparazione per il controllo del peso corporeo a base di chitosano e cellulosa

Also Published As

Publication number Publication date
WO2007109884A8 (fr) 2007-11-08
CA2644585A1 (fr) 2007-10-04

Similar Documents

Publication Publication Date Title
RU2637133C2 (ru) Пищевое волокно для применения при лечении побочного эффекта питания или лекарственного средства в отношении желудочно-кишечного тракта
JP3668241B2 (ja) 脂質代謝改善用組成物
RU2566050C2 (ru) Композиция для снижения всасывания входящего в рацион жира
CA2967284C (fr) Composition de fibres alimentaires
WO1999021566A1 (fr) Composition dietetique ayant des proprietes de liaison aux lipides servant a gerer le poids et a reduire le lipide serique
WO2019038668A1 (fr) Composition synthétique pour réduire les symptômes d'allergie
KR20160121534A (ko) 식이 지방 흡수를 감소시키는데 사용하기 위한 오크라를 포함하는 조성물
US20040126444A1 (en) Cactaceae-based formulation having the property of fixing fats and method for obtaining same
US20100216742A1 (en) Soluble Fiber Combinations for Weight Control and Improving Parameters of Cardiovascular Health
WO2007109884A1 (fr) Composition piégeant les matières grasses comprenant un polysaccharide cationique non digestible et un agent émulsifiant
Preuss et al. Chitosan as a dietary supplement for weight loss: a review
Jung et al. L-ascorbic acid addition to chitosan reduces body weight in overweight women
JP2006506464A (ja) 食事性繊維およびコレステロール低下物質で造られたコレステロール低下剤
US20020137729A1 (en) Combinations of psyllium and chitosan for synergistic adsorption of triglyceride
US20070167395A1 (en) Compositions and methods for treating diabetes
TW200401645A (en) Enteric fat absorption inhibitors containing plant extract and foods containing the same
EP2016946B1 (fr) Composition de coprécipité de chitosane et de dioxyde de silicium pour une utilisation en tant qu'agent thérapeutique
JP2011074028A (ja) リパーゼ阻害剤及びこれを含有する飲食品
MXPA04010692A (es) Composicion para el tratamiento de la obesidad e hiperlipidemia.
US20040247709A1 (en) Composition and method for treating upper abdominal pain and cramping
CA3155818A1 (fr) Composition a liberation retardee comprenant un medicament a revetement enterosoluble charge dans une matrice d'enveloppe de psyllium
HK1183208A (en) Composition for reducing absorption of dietary fat
HK1183208B (en) Composition for reducing absorption of dietary fat

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 07719417

Country of ref document: EP

Kind code of ref document: A1

DPE1 Request for preliminary examination filed after expiration of 19th month from priority date (pct application filed from 20040101)
WWE Wipo information: entry into national phase

Ref document number: 2644585

Country of ref document: CA

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 07719417

Country of ref document: EP

Kind code of ref document: A1

DPE1 Request for preliminary examination filed after expiration of 19th month from priority date (pct application filed from 20040101)