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WO2004035025A1 - Agent d'administration orale contenant un comprime de farine de konjak, insoluble ou peu soluble dans l'eau ou dans les liquides gastriques et intestinaux - Google Patents

Agent d'administration orale contenant un comprime de farine de konjak, insoluble ou peu soluble dans l'eau ou dans les liquides gastriques et intestinaux Download PDF

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Publication number
WO2004035025A1
WO2004035025A1 PCT/EP2003/011310 EP0311310W WO2004035025A1 WO 2004035025 A1 WO2004035025 A1 WO 2004035025A1 EP 0311310 W EP0311310 W EP 0311310W WO 2004035025 A1 WO2004035025 A1 WO 2004035025A1
Authority
WO
WIPO (PCT)
Prior art keywords
substances
compressed
carrier material
konjac flour
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/EP2003/011310
Other languages
German (de)
English (en)
Inventor
Günther Beisel
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to AU2003271719A priority Critical patent/AU2003271719A1/en
Publication of WO2004035025A1 publication Critical patent/WO2004035025A1/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
    • 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
    • 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
    • A23L19/00—Products from fruits or vegetables; Preparation or treatment thereof
    • A23L19/10—Products from fruits or vegetables; Preparation or treatment thereof of tuberous or like starch containing root crops
    • A23L19/115—Konjak; Konntaku
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
    • A23P10/00—Shaping or working of foodstuffs characterised by the products
    • A23P10/20—Agglomerating; Granulating; Tabletting
    • A23P10/28—Tabletting; Making food bars by compression of a dry powdered mixture
    • 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
    • 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 present invention relates to an agent for oral ingestion, containing a material which swells in water and gastrointestinal fluids, a method for its preparation and its use for the manufacture of agents for producing a satiety effect and for the manufacture of orally administrable medicaments, nutritional supplements or foods with Delayed and gentle drug release.
  • German patent DE 4025912 a means for oral administration is known which consists of a container which is detachable in the stomach and releases the contents. This is filled with a substance that increases its volume in the stomach after it is released, thereby suggesting a feeling of satiety in the body.
  • DE 100 44 846 A1 discloses means for oral ingestion which contains at least one substance which increases the viscosity of a liquid in order to produce a long-lasting saturation effect and at least one further compound which increases the residence time of the viscosity-increasing substance in order to prolong a saturation effect in the stomach ,
  • the means are therefore based on two compounds that are coordinated in terms of their effect.
  • the agents are used as granules and therefore do not form bodies of a defined size in the stomach.
  • konjac also known as konjac gum or konjac glucomannan
  • food additive E425. it is used especially as a fiber additive or for texture improvement.
  • a targeted use to produce a saturation effect is not yet known.
  • the use of konjac flour as a powder in hard gelatin capsules as a saturant is generally known. After opening the capsules, the powdered konjac flour is released from the capsules.
  • the smaller lumps of gel that are formed have no defined dimensions, so that a certain size of the gel and therefore a longer stomach time is not achieved.
  • the object of the present invention is accordingly to provide an agent with a satiety effect for oral administration which does not have the disadvantages of the previous agents as described.
  • an agent comprising a material which swells like a gel in water and gastrointestinal liquids, in the form of a compressed product from konjac flour.
  • the agent according to the invention consists wholly or partly of konjac flour which is obtained from the konjac root of the konjac plant (amorphallus).
  • the root of the konjac plant is the konjac flour, the essential component of which is the polysaccharide glucomannan.
  • Konjak glucomannans are able to form gel-like solutions or solid gels with water or gastrointestinal fluids.
  • Konjak-glucomannan is weakly branched via bonds on the C3 of hexose units of the main chain (for every 50th to 60th hexose unit) (SHIMAHARA, 1975; Agri. Biol. Chem. Vol. 39 (2), 293-299; KATO, 1973, Agr. Biol. Chem. Vol. 37 (9), 2045-2051). It also contains an acetyl group of 19 hexose units (MAEKAJI, 1974, Agr. Biol. Chem., 38, 315-321), which is important for the solubility behavior of konjac mannan
  • konjak flour is brought into a form before ingestion, which form one or more gel bodies with defined sizes in the stomach after release.
  • the konjak flour is optionally processed with the addition of further substances to form compressed products which, after passing through the esophagus in the stomach, absorb liquid within seconds, preferably within 60 to 240 seconds, particularly within 120 to 180 seconds, or with a delay within 30 to 60 minutes - in individual cases even within hours - swell to gel bodies with a size that exceeds the original size of the compressed material.
  • the compressions according to the invention preferably contain 70-100% konjac glucomannan based on the total mass of the composition they contain 75-97.5%, particularly preferably 80-95% konjac glucomannan.
  • auxiliary substances can be substances that are usually used as technological auxiliary substances in the pharmaceutical field or in food, e.g. Fillers, disintegrants, lubricants, mold release agents, surfactants, wetting agents and hydrophilizing or hydrophobizing substances. Fatty acids are also used as auxiliary substances, which may delay the transport of the gel bodies in the gastrointestinal tract.
  • the agent according to the invention can be used as pharmaceutically active substances, foods or food supplements, e.g. Contain vitamins, fiber, proteins, minerals as well as other food substances, stimulants or flavorings.
  • the agents according to the invention can also contain active ingredients.
  • Active substances in the sense of the invention are understood to mean all substances with a pharmaceutical or biological effect.
  • Examples include betamethasone, thioetic acid, sotalol, salbutamol, norfenefrin, solymarin, dihydroergotamine, buflumedil, etofibrate, indomethacin, oxazepam, beta-acetyldigoxim, piroxicam, haloperidol, ISMN, amitirptylin, diflipinolinol, diclipinolinol, diclipinolinol, diclipinolinol, diclipinolinol, diclipinolinol, diclipinolinin, diclipinolinacin Methylprednisolone, clonidine, fenofibrate, allopurinol, pirenzepin, levothyroxine, tamoxifen, metildigoxin, o- (beta-hydroxyethy
  • acetaminophen paracetamol
  • acetohexamide acetyldigoxime
  • acetylsalicylic acid acromycin
  • anipamil benzocaine
  • beta-carotene beta-carotene
  • choramphenicol chlordiazepoxide
  • chlormadinoacetate chlorthiazide
  • cinnarizine donazepamethonone
  • clonazepamoxinone clonazepamoxinone
  • clonazepamoxinone clonazepamoxinone
  • clonazepamoxinone clonazepamoxinone
  • Digoxin dihydroergotamine, drotaverine, flunitrazepam, furosemide
  • Gramicidin griseofluvin
  • hydroflumethazig indimet
  • Mefrusid, methandrostenolone, methylprednisolone, methylsulfadiazine ( sulfaperin), nalidixic acid, nifedipine, nitrazepam, nitrofurantoin, nystatin, ostradiol, papaverine, phenacetin, phenobarbital, phenylbutazone, phenytoin, prednisone, sulfinadamol, sulfonamethamidolamidamidonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamid, sulfonamol, sulfonamid, sulfonamol, sulfona
  • retarding substances can also be added to the agent according to the invention.
  • auxiliaries or mixtures thereof such as lipids, including fatty alcohols, eg cetyl alcohol, stearyl alcohol and cetostearyl alcohol; Glycerides, for example glycerol monostearate or mixtures of mono-, di- and triglycerides of vegetable oils; hydrogenated oils such as hydrogenated castor oil or hydrogenated cottonseed oil; Waxes, for example beeswax or carnauba wax; solid hydrocarbons, eg paraffin or earth wax; Fatty acids, eg stearic acid; certain cellulose derivatives, for example ethyl cellulose or acetyl cellulose; Polymers or copolymers, such as polyalkylenes, for example polyethylene, polyvinyl compounds, for example polyvinyl chloride or polyvinyl acetate, and also vinyl chloride-vinyl acetate copolymers and copolymers with crotonic acid, or polymers and copolymers of acrylates
  • lipids including
  • the volume of the decompressed structure is 10 to 40 cm 3, preferably 12 to 30 cm 3 , particularly preferably 14 to 25 cm 3 .
  • the volume in the compressed state is 0.5 to 3 cm 3 , preferably 0.60 to 1.25 cm 3 , particularly preferably 0.75 to 1 cm 3 .
  • the agent according to the invention can have any shape in the decompressed state. However, cuboid or rectangular or round configurations are preferred.
  • the surfaces in this case are 6 to 60 cm 2 .
  • the compressed agent should, after exiting the esophagus, preferably two to one hundred times, particularly preferably four to fifty times, very particularly preferably ten to forty times, very particularly preferably fifteen to thirty-five times its Can expand volume in the stomach.
  • the agents according to the invention can take the form of round tablets, oblong tablets, microtablets or pellets.
  • the compressed products according to the invention are preferably compacts of a shape which facilitates swallowing and passage through the esophagus, such as round tablets or oblong tablets. Tablets can be in the form of coated or layered tablets, which may contain the compressions according to the invention on the inside.
  • the compressed products can be used without coatings or with coverings such as film coatings, coatings or applied hydrophilic or lipophilic auxiliaries.
  • the compresses can be coated by soaking the moldings at higher temperatures, if necessary.
  • the hydrophilic or lipophilic auxiliaries can be liquid or solid. Examples of film coatings include cellulose derivatives or polyacrylates, if appropriate Saliva-resistant properties.
  • Hydrophilic auxiliaries are glycerol, propylene glycol or macrogols. Hydrophobic auxiliaries are waxes, fats or oils.
  • the compressed product can also be introduced into containers. Capsules in different shapes and made of different materials are used as containers. Containers can also be used by pressing flat film-like materials made of polymers or fibrous materials.
  • the compressed products can be produced in a conventional manner by pressing the powdery starting components which contain the konjac flour.
  • these compressions can also be provided with coverings in the manner described or introduced into capsules in capsules.
  • the compressed products can be produced by pressing the konjac flour into a capsule.
  • a device can be used for this purpose, into which the capsule is inserted. With the help of a stamp, the compressed production can take place.
  • the manufacturing process is such that the contents of the capsule are not in the form of a loose powder, but rather in the form of a compact which forms swelling bodies of a defined size in the stomach.
  • the expanding compressions can be processed with gas-forming adjuvants such as calcium carbonate, which react in the acidic environment of the stomach with the formation of carbon dioxide and reduce the density of the gel body formed.
  • gas-forming adjuvants such as calcium carbonate
  • the gas formation also makes it possible to increase the strength of the gel body modify and facilitate transport and dissolution in the gastrointestinal tract.
  • the agent according to the invention is taken orally.
  • the carrier material passes through the mouth, throat and esophagus passage by adding drinking liquid and light chewing or swallowing movements.
  • the carrier substance expands in the stomach and remains in the stomach for several hours. As a result, a long-term feeling of satiety or fullness can be achieved, which results in reduced food intake.
  • the intake of the compresses according to the invention can also bring about a lowering of the cholesterol level. It is believed that the effect on the hindrance of the transport of cholesterol in the jejunum and the bile acids (cholesterol metabolites) in the ileum depends. Thus, the effect of the compresses according to the invention is not limited to the stomach alone, but is extended to other parts of the gastrointestinal Wings expanded.
  • Konjak flour is pressed without additives on an eccentric tablet press into an oblong tablet (1.8 x 0.7 cm).
  • the oblong tablet has an individual weight of 0.85 g.
  • Konjak flour is compressed to oblong tablets with the addition of fatty acids and magnesium trisilicate on an eccentric tablet press.
  • One tablet weighs 0.76 g.
  • Konjak flour is impregnated with a surfactant before processing.
  • Sorbitan palmitate is homogeneously distributed on the konjac flour by trituration. Powder mixture:
  • the lower capsule part 1 of a gelatin capsule is introduced into a support mold 2, filled with the powder mixture 3 from production example 3 and compressed with the stamp 4 in the capsule to form a compact.
  • the capsule lower part is ejected from the support mold and closed with the capsule upper part (not shown).

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

Abstract

L'invention concerne un agent d'administration orale, lequel contient une substance, fabriquée à partir de farine de konjak, sous forme de gel gonflant dans l'eau et dans les liquides gastriques et intestinaux. La présente invention porte également sur l'utilisation de cette composition.
PCT/EP2003/011310 2002-10-14 2003-10-13 Agent d'administration orale contenant un comprime de farine de konjak, insoluble ou peu soluble dans l'eau ou dans les liquides gastriques et intestinaux Ceased WO2004035025A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003271719A AU2003271719A1 (en) 2002-10-14 2003-10-13 Agent for oral administration, containing a tablet made of konjac flour and which is insoluble or poorly soluble in water or in a gastrointestinal medium

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10247910A DE10247910A1 (de) 2002-10-14 2002-10-14 Mittel zur Erzeugung eines langanhaltenden Sättigungseffektes
DE10247910.0 2002-10-14

Publications (1)

Publication Number Publication Date
WO2004035025A1 true WO2004035025A1 (fr) 2004-04-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/011310 Ceased WO2004035025A1 (fr) 2002-10-14 2003-10-13 Agent d'administration orale contenant un comprime de farine de konjak, insoluble ou peu soluble dans l'eau ou dans les liquides gastriques et intestinaux

Country Status (3)

Country Link
AU (1) AU2003271719A1 (fr)
DE (1) DE10247910A1 (fr)
WO (1) WO2004035025A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU102736B1 (de) 2021-03-29 2022-09-30 Gollus Anne Sättigendes Kombinationserzeugnis und Verfahren zu dessen Herstellung

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS56161319A (en) * 1980-05-19 1981-12-11 Shin Etsu Chem Co Ltd Easily swellable glucomannan tablet
FR2660529A1 (fr) * 1990-04-09 1991-10-11 Ennagram Utilisation du glucomannane pour la preparation d'un produit dietetique, et produit dietetique comprenant du glucomannane.
WO1994015643A1 (fr) * 1992-12-30 1994-07-21 Fmc Corporation Excipient a liberation, prolongee, facile a produire, a base de glucomannane de konjac
EP0835654A1 (fr) * 1996-10-11 1998-04-15 Shimizu Chemical Corporation Préparations pharmaceutiques pour administration orale à libération contrÔlée contenant du glucomannan
WO2001091586A2 (fr) * 2000-05-31 2001-12-06 Vladimir Vuksan Compositions de konjac mannan et de ginseng, procedes et utilisations
DE20120348U1 (de) * 2001-12-17 2002-04-11 Easyway AG, 40789 Monheim Mittel zur oralen Einnahme
DE20119843U1 (de) * 2001-12-06 2002-04-18 Beisel, Günther, 40789 Monheim Mittel zur Behandlung von Übergewicht und weiteren Symptomen

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3217071A1 (de) * 1982-05-06 1983-11-10 Rüdiger Dr. 6365 Rosbach Gröning Arzneimittel fuer die perorale applikation mit verbesserter biologischer verfuegbarkeit der wirkstoffe
DE10044846A1 (de) * 2000-09-11 2002-04-04 Guenther Beisel Mittel mit verlängerter Magenverweilzeit zur Erzeugung eines langanhaltenden Sättigungseffektes sowie dessen Verwendung

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS56161319A (en) * 1980-05-19 1981-12-11 Shin Etsu Chem Co Ltd Easily swellable glucomannan tablet
FR2660529A1 (fr) * 1990-04-09 1991-10-11 Ennagram Utilisation du glucomannane pour la preparation d'un produit dietetique, et produit dietetique comprenant du glucomannane.
WO1994015643A1 (fr) * 1992-12-30 1994-07-21 Fmc Corporation Excipient a liberation, prolongee, facile a produire, a base de glucomannane de konjac
EP0835654A1 (fr) * 1996-10-11 1998-04-15 Shimizu Chemical Corporation Préparations pharmaceutiques pour administration orale à libération contrÔlée contenant du glucomannan
WO2001091586A2 (fr) * 2000-05-31 2001-12-06 Vladimir Vuksan Compositions de konjac mannan et de ginseng, procedes et utilisations
DE20119843U1 (de) * 2001-12-06 2002-04-18 Beisel, Günther, 40789 Monheim Mittel zur Behandlung von Übergewicht und weiteren Symptomen
DE20120348U1 (de) * 2001-12-17 2002-04-11 Easyway AG, 40789 Monheim Mittel zur oralen Einnahme

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Section Ch Week 198204, Derwent World Patents Index; Class B05, AN 1982-06728E, XP002267707 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU102736B1 (de) 2021-03-29 2022-09-30 Gollus Anne Sättigendes Kombinationserzeugnis und Verfahren zu dessen Herstellung

Also Published As

Publication number Publication date
AU2003271719A1 (en) 2004-05-04
DE10247910A1 (de) 2004-04-22

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