GB2490126A - Opuntia ficus indica, powdered psyllium husk and chitosan composition for reducing fat absorption - Google Patents

Opuntia ficus indica, powdered psyllium husk and chitosan composition for reducing fat absorption Download PDF

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Publication number
GB2490126A
GB2490126A GB1106540.6A GB201106540A GB2490126A GB 2490126 A GB2490126 A GB 2490126A GB 201106540 A GB201106540 A GB 201106540A GB 2490126 A GB2490126 A GB 2490126A
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powdered
weight
chitosan
opuntia ficus
plant material
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GB201106540D0 (en
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Jeremy John Stephens
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716Glucans
    • A61K31/722Chitin, chitosan
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/33Cactaceae (Cactus family), e.g. pricklypear or Cereus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/68Plantaginaceae (Plantain Family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

A composition for oral ingestion comprising powdered plant material from Opuntia ficus indica, powdered Psyllium (plantago ovata) husk and chitosan. Preferably, the composition comprises 1 to 4 parts by weight (100mg to 400mg) powdered plant material from Opuntia ficus indica; 0.5 to 1.5 part by weight (50mg to 150mg) powdered psyllium husk and 0.5 to 1.5 parts by weight (50mg to 150mg) chitosan. Preferably the powdered plant material from Opuntia ficus indica is derived from leaves of cladodes of the plant in which at least 75% by weight of the powder particles have sizes 230 to 280µm. Preferably the composition is contained within a capsule and is useful for binding lipids passing through the gastrointestinal tract and thereby preventing or reducing absorption of the lipids.

Description

A COMPOSITION FOR REDUCING FAT ABSORPTION
This invention relates to a composition for reducing the absorption of fats from the gastrointestinal tract.
Background of the invention
The incidence of obesity has increased dramatically over the past few decades in most developed countries and one reason for this has been a very large increase in the amount of fat consumed by the average member of the public. A great many solutions to this problem have been proposed ranging from special diets and exercise regimes, lipid-reducing food supplements and diet-suppressing drugs to surgical interventions such as gastric bands.
Various natural, semi-synthetic and synthetic substances have been developed and used for the purpose of binding lipids in the gastrointestinal (01) tract in order to reduce or prevent absorption of the lipids. For example, synthetic polymer resins which may be polyamines or anionic polymeric resins have been proposed and used for binding to bile acids thereby preventing their reuptake and use in the biosynthesis of cholesterol. Examples of substances of this type are disclosed in GB929391 (Merck). A problem with bile acid sequestering resins has been their lack of palatability. Consequently, much research has been expended in finding combinations of the resins with agents that improve the palatability of the resins.
For example, US560 1837 discloses combinations of psyllium husk and cholestyramine for treating hypercholesterolemia. US5286481 discloses combinations of an anion-exchange resin such as cholestyramine, colestipol or polidexide and bran for use in weight-reduction.
Other examples of substances for use in binding bile acids or other lipids such as triglycerides are disclosed in DE4136325 (Hoechst), which discloses cyclodextrins as bile acid adsorption agents useful for treating hyperlipidaemia, and US200410126444 (Dallas etaL), which discloses the use of powdered plant material from the cladodes of cacti for binding dietary fats.
Chitosan has been used for binding and preventing the absorption of dietary fats.
Chitosan is a deacetylated form of chitin, an amino polysaccharide (poly-N-acetyl glucosamine) found in the exoskeleton of arthropods (e.g., crustaceans such as lobsters and crabs) and also found in some plants and fungi. Chitosan is similar in structure and properties to dietary fibre (e.g., vegetable bran, cellulose) but, unlike like bran and cellulose, chitosan has the ability to bind fat and other lipids in the intestine. A known problem with chitosan, as disclosed in W099/21 566 (Rexall Sundown), is that when chitosan is consumed in the quantities required for dietary fat reduction, constipation can result. Indeed, W09912 1566 discloses that the use of chitosan as a dietary supplement must be of short duration or other ingredients or supplements added to combat the undesirable effects of the chitosan.
W099/21566 proposes the addition of aloin, which contains aloe saponins, in order to offset the constipating effect of chitosan. U54999341 discloses the use of soy sapon ins to offset the constipating effect of the chitosan. U52007/0048392 (Oben) discloses the use of combinations of chitosan and a plant extract from a plant of the Cissus, Vernonia or Brillantasia families.
Psyllium seed husks are portions of the seeds of the plant Plantago ovata, (genus Plantago), a native of India. They are soluble in water, expanding and becoming mucilaginous when wet. Psyllium seed husks have also been used for binding dietary fats and preventing their absorption. However, although Psyllium seed husks act as a laxative in relatively small amounts, they can cause constipation when administered in the larger amounts needed for dietary fat removal.
Thus, at present, although numerous substances and combinations of substances have been used for binding dietary lipids in the GI tract so as to prevent uptake of the lipids, many are associated with problems that can limit their effectiveness and the extent to which they are used in many sections of the general population.
Summary of the invention
The present invention provides an improved composition for binding dietary lipids in the GJ tract and thereby preventing or reducing absorption of the Jipids. In this way, the compositions provide a means of combatting obesity and hyperlipidaemia.
Accordingly, in a first aspect, the invention provides a composition for oral ingestion comprising powdered plant material from Opuntia ficus indica; powdered Psyllium husk and chitosan.
The composition may contain from 1 to 4 parts by weight of the powdered plant material from Opuntia ficus indica; from 0.5 to 1.5 parts by weight of powdered Psyllium husk and from 0.5 to 1.5 parts by weight of chitosan.
More particularly, the composition may contain from 100 mg to 400 mg of the powdered plant material from Opuntia ficus indica; from 50 mg to 150 mg of the powdered Psyllium husk and from 50 mg to 150 mg of the chitosan.
For example, the composition may contain from 200 mg to 300 mg of the powdered plant material from Opuntia ficus md/ca; from 75 mg to 125 mg of the powdered Psyllium husk and from 75 mg to 125 mg of the chitosan.
In one preferred embodiment, the composition contains from approximately 250 mg of the powdered leaf material from Opuntia ficus md/ca; approximately 100 mg of the powdered Psyllium husk and approximately 100 mg of the chitosan.
The compositions of the invention may be presented in the form of capsules.
The compositions of the invention may also be presented as medical devices, the term medical device as used herein referring to a substance which whilst providing a medical benefit to a subject, is not absorbed significantly from the subject's GI tract and does not exert its actions by pharmacological means.
The composition, capsule or medical device of the invention as defined herein may be used for binding lipids passing through the gastrointestinal tract and thereby preventing or reducing absorption of the lipids.
Psyllium seed husks are portions of the seeds of the plant Plantago ovata, (genus Plantago), a native of India. They are soluble in water, expanding and becoming mucilaginous when wet.
In the compositions of the present invention, the Psyllium seed husks may be presented in powder form wherein at least 99.5% by weight of the particles forming the powder have a particle size (e.g. diameter) of 600 pM or less. Such particles will pass through a 30 mesh sieve. In one embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 400 pM or less. Such particles will pass through a 40 mesh sieve. In another embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 300 pM or less. Such particles will pass through a 50 mesh sieve. In a further embodiment, at least 95% by weight of the particles have a particle size (e.g. diameter) of 210 pM or less.
Such particles will pass through a 70 mesh sieve. In another embodiment, at least 75% by weight of the particles will pass through a 50 to 60 mesh sieve and have particle sizes in the range from 230 to 280 pM.
The chitosan used in the compositions of the present invention is produced commercially by deacetylation of chitin, which is the structural element in the exoskeleton of crustaceans (crabs, shrimp, etc.) and cell walls of fungi. The degree of deacetylation is typically in the range 60-1 00 %, for example from 50-90% or 60- 80%. The average molecular weight of the chitosan is typically between 3,800 and 20,000 daltons, for example from 5,000 to 15,000 daltons, or from 5,000 to 10,000 daltons, or from 7,500 to 12,500 daltons..
The chitosan is presented in the form of a powder. The chitosan may be presented in powder form wherein at least 99.5% by weight of the particles forming the powder have a particle size (e.g. diameter) of 600 pM or less. Such particles will pass through a 30 mesh sieve. In one embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 400 pM or less. Such particles will pass through a 40 mesh sieve. In another embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 300 pM or less. Such particles will pass through a 50 mesh sieve. In a further embodiment, at least 95% by weight of the particles have a particle size (e.g. diameter) of 210 pM or less. Such particles will pass through a 70 mesh sieve. ln another embodiment, at least 75% by weight of the particles will pass through a 50 to 60 mesh sieve and have particle sizes in the range from 230 to 280 pM.
Opuntia ficus indica is a cactus found in Central and South America. The cactus produces "cladodes" or truncated branches of the stem that contain chlorophyll and are adapted to carry out photosynthesis. The cladodes have a leaf-like appearance but are not true leaves. In the present context, the term "leaf material from Opuntia ficus indica" refers to the cladodes.
The term plant material" includes material derived from the cladodes or from other parts of the plant such as the plant stem.
In one preferred embodiment, the plant material is derived from the cladodes or leaves of the plant.
The cladodes or other parts of the plant are dried and then ground to a powder in which at least 99.5% by weight of the particles have a maximum dimension (e.g. S diameter) of less than 300 pM. More typically, at least 70% by weight of the particles have a maximum dimension (e.g. diameter) of less than 100 pM.
Further details of the preparation of powdered plant material from Opuntia ficus indica may be found in US2004/0 126444.
The powdered plant material is presented in the form of a powder. The plant material may be presented in powder form wherein at least 99.5% by weight of the particles forming the powder have a particle size (e.g. diameter) of 600 pM or less.
Such particles will pass through a 30 mesh sieve. In one embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 400 pM or less. Such particles will pass through a 40 mesh sieve. In another embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 300 pM or less. Such particles will pass through a 50 mesh sieve. In a further embodiment, at least 95% by weight of the particles have a particle size (e.g. diameter) of 210 pM or less. Such particles will pass through a 70 mesh sieve. In another embodiment, at least 75% by weight of the particles will pass through a 50 to 60 mesh sieve and have particle sizes in the range from 230 to 280 pM.
The compositions of the invention are typically administered with or without (but preferably with or shortly before or after) meals one or more times per day. For example, the compositions may be administered from two to four times per day.
The compositions may be administered so that the daily intakes of the three components are as follows: Powdered plant material from Opuntia ficus indica: 100 mg to 1600 mg Powdered Psyllium husk: 50 mg to 600 mg Chitosan: 50 mg to 600 mg The compositions of the invention bind fats and other lipids in the GI tract and carry them through so that they are excreted with the faeces. In this way, the fats and other lipids cannot be absorbed by the body. By mopping up a large proportion of the fats in food consumed by a subject, obesity and hyperlipidaemia may be prevented.
The invention will now be illustrated but not limited, by reference to the following
specific example.
EXAMPLE I
Capsule formulation I Into a two part capsule shell formed from hydroxypropyl methylcellu lose is filled a mixture of powdered Opuntia ficus indica, Psyllium husk and chitosan in the following proportions: Opuntia ficus indica powder 250 mg Pysyllium husk powder 100 mg chitosan powder 100 mg The capsules are taken as a food supplement, two capsules being administered with each meal up to a total of six capsules per day.
It will readily be apparent that numerous modifications and alterations may be made to the specific embodiments of the invention described above without departing from the principles underlying the invention. All such modifications and alterations are intended to be embraced by this application.

Claims (12)

  1. CLAIMS1. A composition for oral ingestion comprising powdered plant material from Opuntia ficus indica; powdered Psyllium husk and chitosan.
  2. 2. A composition according to claim I comprising from I to 4 parts by weight of the powdered plant material from Opuntia ficus indica; from 0.5 to 1.5 parts by weight of powdered Psyllium husk and from 0.5 to 1.5 parts by weight of chitosan.
  3. 3. A composition according to claim 2 containing from 100 mg to 400 mg of the powdered plant material from Opuntia ficus indica; from 50 mg to 150 mg of the powdered Psyllium husk and from 50 mg to 150 mg of the chitosan.
  4. 4. A composition according to claim 3 containing from 200 mg to 300 mg of the powdered plant material from Opuntia ficus indica; from 75 mg to 125 mg of the powdered Psyllium husk and from 75 mg to 125 mg of the chitosan.
  5. 5. A composition according to claim 4 containing from approximately 250 mg of the powdered plant material from Opuntia ficus indica; approximately 100 mg of the powdered Psyllium husk and approximately 100 mg of the chitosan.
  6. 6. A composition according to any one of claims I to 5 wherein the powdered plant material from Opuntia ficus md/ca is derived from leaves or cladodes of the plant.
  7. 7. A composition according to any one of claims I to 6 wherein the powdered plant material from Opuntia f/cus md/ca is presented in the form of a powder in which at least 75% by weight of the particles have particle sizes in the range from 230 to 280 pM.
  8. 8. A composition according to any one of claims I to 7 wherein the powdered Psyllium husk is presented in the form of a powder in which at least 75% by weight of the particles have particle sizes in the range from 230 to 280 pM.
  9. 9. A composition according to any one of claims I to 8 wherein the chitosan is presented in the form of a powder in which at least 75% by weight of the particles have particle sizes in the range from 230 to 280 pM.
  10. 10. A capsule containing a composition according to any one of claims I to 9.
  11. 11. A medical device comprising a composition according to any one of claims I to9.
  12. 12. A composition, capsule or medical device according to any one of claims I to 11 for use in binding lipids passing through the gastrointestinal tract and thereby preventing or reducing absorption of the lipids.
GB1106540.6A 2011-04-18 2011-04-18 Opuntia ficus indica, powdered psyllium husk and chitosan composition for reducing fat absorption Withdrawn GB2490126A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2501242A (en) * 2012-03-23 2013-10-23 Ajit Ramanial Patel A composition for the treatment of obesity

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047372A2 (en) * 1998-07-10 2001-07-05 Vanson, Inc. Absorbing fat chitosan
US20020137729A1 (en) * 2000-07-21 2002-09-26 Babish John G. Combinations of psyllium and chitosan for synergistic adsorption of triglyceride
US20040126444A1 (en) * 2001-04-11 2004-07-01 D'huart Jean-Baptiste Cactaceae-based formulation having the property of fixing fats and method for obtaining same
KR20100084027A (en) * 2009-01-15 2010-07-23 세종대학교산학협력단 Composition of nanochitosan for lowering cholesterol and triglyceride in blood
US20100323045A1 (en) * 2007-11-06 2010-12-23 Finzelberg Gmbh & Co. Kg Extract formulation of opuntia ficus indica

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047372A2 (en) * 1998-07-10 2001-07-05 Vanson, Inc. Absorbing fat chitosan
US20020137729A1 (en) * 2000-07-21 2002-09-26 Babish John G. Combinations of psyllium and chitosan for synergistic adsorption of triglyceride
US20040126444A1 (en) * 2001-04-11 2004-07-01 D'huart Jean-Baptiste Cactaceae-based formulation having the property of fixing fats and method for obtaining same
US20100323045A1 (en) * 2007-11-06 2010-12-23 Finzelberg Gmbh & Co. Kg Extract formulation of opuntia ficus indica
KR20100084027A (en) * 2009-01-15 2010-07-23 세종대학교산학협력단 Composition of nanochitosan for lowering cholesterol and triglyceride in blood

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
https://web.archive.org/web/20081026094448/https://www.neopuntia.com/uk/Lipophilic-properties_2_9.html available online 26 October 2008 (wayback machine) accessed 2 August 2012 *
Journal of Medicine, vol. 33, No 1-4, 2002, pages 209-225 *
The Journal of Nutrition, vol. 135, No. 10, 2005, pages 2399-2404 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2501242A (en) * 2012-03-23 2013-10-23 Ajit Ramanial Patel A composition for the treatment of obesity

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