WO2024252015A1 - Utilisation de compositions contenant des glucides sous forme de comprimé pour le traitement d'états hypoglycémiques - Google Patents

Utilisation de compositions contenant des glucides sous forme de comprimé pour le traitement d'états hypoglycémiques Download PDF

Info

Publication number
WO2024252015A1
WO2024252015A1 PCT/EP2024/065870 EP2024065870W WO2024252015A1 WO 2024252015 A1 WO2024252015 A1 WO 2024252015A1 EP 2024065870 W EP2024065870 W EP 2024065870W WO 2024252015 A1 WO2024252015 A1 WO 2024252015A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
composition
tablets
coating
tablet form
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.)
Pending
Application number
PCT/EP2024/065870
Other languages
German (de)
English (en)
Inventor
Julius GRENNIGLOH
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.)
Euvorio GmbH
Original Assignee
Euvorio GmbH
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 Euvorio GmbH filed Critical Euvorio GmbH
Publication of WO2024252015A1 publication Critical patent/WO2024252015A1/fr
Anticipated expiration legal-status Critical
Pending 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. fats
    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
    • 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

Definitions

  • the invention relates to the use of special carbohydrate-containing compositions, in particular in tablet form, for the preparation of agents for the treatment of forms of hypoglycemia, in particular nocturnal hypoglycemia.
  • Diabetes mellitus is a metabolic disorder that affects the utilization of carbohydrates. It is caused in particular by a lack of insulin and can lead to chronic hyperglycemia with numerous subsequent damages.
  • the carbohydrates ingested with food are broken down into glucose, which is transferred through the intestinal wall into the blood and distributed throughout the body.
  • the body's own hormone insulin causes the glucose contained in the blood to enter the cells, where it is used to generate energy.
  • the insulin required for this is mainly produced in the pancreas. If the body does not produce any insulin or does not produce enough insulin, glucose cannot be transferred into the body's cells and therefore remains in the blood.
  • diabetes mellitus is usually treated with insulin. This creates the problem of correctly dosing the amount of insulin, i.e. adjusting it to the amount of carbohydrate. If too little insulin is given, too much glucose remains in the blood. If the insulin dosage is too high, hypoglycemia can occur. This type of hypoglycemia is a serious disorder that can be fatal in the worst case.
  • hypoglycemia can also occur at night.
  • people who suffer from diabetes wake up at night, for example, with outbreaks of sweat or are woken up by warning devices. This can happen, for example, if the person in question has eaten a meal in the evening or at night whose exact carbohydrate content is not known. The person is then dependent on estimating the carbohydrate content in order to then administer the appropriate amount of insulin. If the amount of carbohydrate is overestimated, the hypoglycemia mentioned above can then occur after insulin is administered.
  • Affected people often find it unpleasant to eat glucose, (sweet) fruit juices or bread, especially at night, to compensate for the hypoglycemia. In order to compensate for the sweet taste in the mouth, they would have to get up at night and brush their teeth again, for example.
  • the task therefore arises of providing a composition that is able to specifically raise the blood sugar level in the event of hypoglycemia, is easy to dose, but at the same time does not leave an unpleasant sweet taste in the mouth, so that the affected people can continue sleeping. This task is solved by using the compositions described below.
  • compositions for the treatment of nocturnal hypoglycemia are compositions that are described as "delayed and sustained release compositions".
  • the compositions are intended to be taken before going to bed and ensure a consistent supply of carbohydrates during the night. Treatment of acute nocturnal hypoglycemia is not possible due to the delayed release.
  • the document CN 115226896 describes other sustained release compositions of various carbohydrates, which are also not suitable for the treatment of acute nocturnal hypoglycaemia.
  • the document DE 2246013 A describes a process for the production of porous carbohydrate-containing tablets which solves various production problems of Tablet formulations are intended to solve this problem. Nocturnal hypoglycemia treatment is not mentioned here.
  • compositions for producing cell cultures These compositions are said to contain carbohydrates and are described as "sustained release" compositions. Use for the treatment of nocturnal hypoglycemia is not mentioned here.
  • the document CN 105963266 A describes glucose tablets that are also intended to be suitable for the treatment of hypoglycemia. Due to their composition, the tablets dissolve in the mouth and produce a sweet taste.
  • the present invention relates to the use of carbohydrate-containing compositions, in particular in tablet form, which only release the carbohydrates contained in the gastrointestinal tract, for the treatment of hypoglycemia, in particular nocturnal hypoglycemia.
  • compositions initially contain one or more saccharides as carbohydrates, such as dextrose, lactose, maltose, trehalose, sucrose or mixtures thereof.
  • carbohydrates such as dextrose, lactose, maltose, trehalose, sucrose or mixtures thereof.
  • a well-known carbohydrate mixture is, for example, maltodextrin.
  • the carbohydrates sometimes occur in various hydrate forms, i.e. they contain different amounts of water of crystallization.
  • Dextrose for example, is available as a monohydrate, but also as anhydrous anhydrate. Typically, all available stable hydrate forms can be used to produce the preparations according to the invention.
  • dextrose works quickly, whereas other carbohydrates have a delayed onset of action but can have a longer lasting effect. Mixtures of different carbohydrates can produce a rapid initial effect, which lasts longer when more complex carbohydrates are added.
  • the composition consists predominantly, i.e. more than 70%, of the saccharide or the saccharide mixture.
  • conventional agents are used to improve the processability or dissolution properties, such as stearates or cellulose.
  • the saccharide content is up to 95%, typically around 80%.
  • the inventive The most preferred saccharide is dextrose, especially as dextrose monohydrate.
  • the composition is first pressed into pellet-shaped tablet cores.
  • the individual tablet cores have diameters between 4 and 10 mm, preferably between 6 and 8 mm, and can have the usual shapes for such compositions, such as spherical, biconvex, faceted or curved. It goes without saying that they should not have any sharp edges for the purpose of ingestion, but otherwise the shape is practically arbitrary.
  • the prefabricated tablet cores are coated with a coating that is tasteless and ensures that the tablets do not dissolve in the mouth, but that the saccharides they contain are only released in the stomach.
  • the coating also makes the tablets easier to swallow.
  • Such coatings are known in principle. They are usually composed on the basis of starch and modified cellulose. The decisive factor for the coating is that it does not dissolve in the mouth, but rather quickly releases the tablet core in the stomach.
  • the following substance classes are preferably used for the coating according to the invention:
  • Cellulose and cellulose derivatives in particular carboxymethylcellulose, hydroxypropylmethylcellulose phthalate, methylcellulose, hydroxypropylmethylcellulose (hypromellose) and/or hydroxypropylcellulose
  • the most preferred coating agent is hydroxypropylmethylcellulose (hypromellose).
  • the coatings can also contain colorants.
  • food colorants are used, such as carotenoids (E 160a), berry colorants (anthocyanins, E 163), beetroot colorants (betanin, E 162), carmine (E 120), paprika extract (E 160c) and curcumin (E 100).
  • Particularly preferred are strongly coloring plant or fruit extracts, such as beetroot, spinach or elderberry juice and spices such as saffron and turmeric.
  • the tablet cores are preferably coated in a single process, resulting in modified film-coated tablets (coated tablets).
  • modified film-coated tablets coated tablets
  • the classic coating with several layers is of course also possible.
  • the tablets created from the tablet cores by coating typically have a diameter of between 4 and 10 mm and a mass of between 50 and 500 mg.
  • the individual tablets Preferably, have a diameter of 7 to 8 mm and a mass of 210 to 270 mg.
  • a person suffering from hypoglycemia can dose the composition according to the invention in tablet form using simple dosing devices, for example with a dosing spoon.
  • the spoon can be designed in such a way that a total amount of tablets is taken up that corresponds to a certain amount of carbohydrates, for example a carbohydrate unit, the typical calculation unit for diabetics.
  • carbohydrate units can then be taken from a storage container and taken orally.
  • a sip of water can be helpful in swallowing the tablets completely.
  • the tablets do not release any carbohydrates in the mouth within about 15 seconds, so that their sweet taste in the mouth is avoided.
  • the tablets only dissolve in the stomach and there quickly release the saccharides they contain, which then combat hypoglycemia by raising the blood sugar level.
  • the properties of the tablets described also allow their use in hypoglycaemia conditions that are not caused by diabetes, eg in endurance sports. For example, marathon runners may experience so-called “hunger bouts”, which is a form of hypoglycemia that is not caused by diabetes. Another form of hypoglycemia that is not caused by diabetes can occur when people have not eaten anything for a long time or have eaten very few carbohydrates (“fastin hypoglycemia”). Taking the tablets described in a controlled dose can also overcome such hypoglycemia.
  • a particular advantage of the tablets described is that, when taken as described, a state of hypoglycemia can be treated without the risk of triggering sugar addiction. Experts believe that sugar addiction is promoted by the connection between the sweet taste and the immediate rise in blood sugar, as occurs when eating common sweets (e.g. chocolate bars, gummy bears). Due to the lack of the sweet taste in the mouth, the reward system in the brain is apparently not activated, so that no addictive effects occur.
  • common sweets e.g. chocolate bars, gummy bears
  • the components listed above are mixed and pressed into tablet cores.
  • the coating is then applied using the composition listed below.
  • the tablets After drying, the tablets can be packaged.
  • Tablet size 7 or 8 mm tablet cores (curved)
  • Tablet cores are pressed. The coating is then applied with the composition specified below.
  • the tablets After drying, the tablets can be packaged.
  • Tablet size 7 or 8 mm tablet cores (curved)
  • Tablet cores are pressed. The coating is then applied with the composition specified below.
  • the tablets After drying, the tablets can be packaged.
  • Tablet size 7 or 8 mm tablet cores (curved)
  • the components listed above are mixed and pressed into dragee cores.
  • the coating is then applied using the composition listed below.
  • the dragees can be packaged.
  • Dragee size 7 or 8 mm dragee cores (curved)
  • the components listed above are mixed and pressed into dragee cores.
  • the coating is then applied using the composition listed below.
  • the dragees can be packaged.
  • Dragee size 7 or 8 mm dragee cores (curved)
  • the components listed above are mixed and pressed into tablet cores.
  • the coating is then applied using the composition listed below.
  • the tablets After drying, the tablets can be packaged.
  • Tablet size 7 or 8 mm tablet cores (curved)
  • the components listed above are mixed and pressed into tablet cores.
  • the coating is then applied using the composition listed below.
  • the tablets After drying, the tablets can be packaged.
  • Tablet size 7 or 8 mm tablet cores (curved)
  • the tablet cores produced according to Example 6a will be coated with a coating, which coating has the composition given below.
  • Tablet size Approx. 7 mm tablet cores (curved)
  • This protocol is applicable to all types of tablets intended for oral administration and intended to be swallowed directly rather than sucked.
  • test subjects not sensory trained, preferably about 100 people
  • test subjects are informed about the purpose of the test and give their consent to participate.
  • test subject receives a certain number of test tablets, corresponding to the usual dosage for the product being tested. - The test subjects keep the tablets in their mouth for 15 seconds before swallowing them.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne l'utilisation de compositions spécifiques contenant des glucides, en particulier sous forme de comprimés, pour la production d'agents pour le traitement de l'hypoglycémie, en particulier de l'hypoglycémie nocturne. Les compositions sont faciles à doser et ne laissent pas de goût sucré dans la bouche, mais libèrent les glucides présents rapidement dans l'estomac et sont donc particulièrement appropriées pour le traitement notamment de l'hypoglycémie nocturne.
PCT/EP2024/065870 2023-06-09 2024-06-10 Utilisation de compositions contenant des glucides sous forme de comprimé pour le traitement d'états hypoglycémiques Pending WO2024252015A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102023002336.1 2023-06-09
DE102023002336.1A DE102023002336A1 (de) 2023-06-09 2023-06-09 Kohlenhydrathaltige Zusammensetzungen in Drageeform

Publications (1)

Publication Number Publication Date
WO2024252015A1 true WO2024252015A1 (fr) 2024-12-12

Family

ID=91530301

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2024/065870 Pending WO2024252015A1 (fr) 2023-06-09 2024-06-10 Utilisation de compositions contenant des glucides sous forme de comprimé pour le traitement d'états hypoglycémiques

Country Status (2)

Country Link
DE (1) DE102023002336A1 (fr)
WO (1) WO2024252015A1 (fr)

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2246013A1 (de) 1972-09-20 1974-03-28 Boehringer Mannheim Gmbh Verfahren zur herstellung von poroesen tabletten
WO2014001267A2 (fr) * 2012-06-25 2014-01-03 Hennig Arzneimittel Gmbh & Co. Kg Forme galénique pour la libération de principes actifs
US20140180224A1 (en) 2011-07-14 2014-06-26 Jun Xia Composition, device and method for delayed and sustained release of brain energy molecules
WO2015148742A1 (fr) 2014-03-28 2015-10-01 Corning Incorporated Composition et procédé pour libération prolongée de culture cellulaire
US20160081941A1 (en) * 2013-05-09 2016-03-24 Farmaceutická Univerzita Brno Pharmaceutical composition with controlled release of metabolically active sugar
CN105963266A (zh) 2016-05-09 2016-09-28 天津力能斯伯尔科技有限公司 一种葡萄糖片及其制备方法
WO2020254940A1 (fr) * 2019-06-15 2020-12-24 Shrinivasan Shesha Iyengar Compositions à libération prolongée de glucose et procédés associés
CN115226896A (zh) 2021-04-22 2022-10-25 张婧 糖类缓释组合物及其制备方法

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2246013A1 (de) 1972-09-20 1974-03-28 Boehringer Mannheim Gmbh Verfahren zur herstellung von poroesen tabletten
US20140180224A1 (en) 2011-07-14 2014-06-26 Jun Xia Composition, device and method for delayed and sustained release of brain energy molecules
WO2014001267A2 (fr) * 2012-06-25 2014-01-03 Hennig Arzneimittel Gmbh & Co. Kg Forme galénique pour la libération de principes actifs
US20160081941A1 (en) * 2013-05-09 2016-03-24 Farmaceutická Univerzita Brno Pharmaceutical composition with controlled release of metabolically active sugar
WO2015148742A1 (fr) 2014-03-28 2015-10-01 Corning Incorporated Composition et procédé pour libération prolongée de culture cellulaire
CN105963266A (zh) 2016-05-09 2016-09-28 天津力能斯伯尔科技有限公司 一种葡萄糖片及其制备方法
WO2020254940A1 (fr) * 2019-06-15 2020-12-24 Shrinivasan Shesha Iyengar Compositions à libération prolongée de glucose et procédés associés
CN115226896A (zh) 2021-04-22 2022-10-25 张婧 糖类缓释组合物及其制备方法

Also Published As

Publication number Publication date
DE102023002336A1 (de) 2024-12-12

Similar Documents

Publication Publication Date Title
DE1617374C2 (de) Verfahren zum Herstellen eines pharmazeutischen Präparates mit verzögerter analgetischer Wirkung
DE60223254T2 (de) Verzögert freisetzende formulierungen von oxymorphon
DE69934505T2 (de) Im munde zerfallende tablette enthaltend ein benzimidazole
DE69521328T2 (de) Kaffein-formulierung mit verzögerter freisetzung
DE69826290T2 (de) Pharmazeutische zusammensetzungen zur kontrollierten freigabe von wirkstoffen
DE2808514A1 (de) Nitrofurantoin enthaltende tablette
US20050155519A1 (en) Granulation process
CH638987A5 (de) Langsam und gleichmaessig wirkstoffe freisetzende pharmazeutische zubereitung.
DE2542158A1 (de) Pharmazeutisches mittel fuer die verabreichung in der mundhoehle und verfahren zu seiner herstellung
EP0032562A1 (fr) Formes-retard pour l'administration du dipyridamol et procédés pour leur préparation
DE60017361T2 (de) Direktverpressbare matrix zur kontrollierten abgabe von einmaltäglichen dosen von clarithromycin
DE69429964T2 (de) Feste, therapeutische oder hygienische, mucoadhäsive Zusammensetzung zur Verabreichung durch Auftragen auf der Mund-schleimhaut oder der Nasen-schleimhaut
DE69624364T2 (de) Abführmittel enthaltend lactitol und psyllium
DE112011101605T5 (de) Pharmazeutische Zusammensetzung umfassend Hydromorphon und Naloxon
DE69008107T2 (de) Zubereitung mit verzögerter Freigabe eines Hydrochlorids eines basischen Arzneistoffs.
EP0450262A1 (fr) Préparation pharmaceutique à libération retardée du principe actif
DE112022006830T5 (de) Anwendung einer zusammensetzung aus traditioneller chinesischer medizin zur herstellung eines medikaments zur vorbeugung und behandlung von retinitis pigmentosa
EP2679216B1 (fr) Forme pharmaceutique pour la libération modifiée de bétahistine
EP2512440A1 (fr) Comprimé orodispersible contenant de la dapoxétine
EP2029101A2 (fr) Comprimé plat combiné pour le diabète de type 2
CH630262A5 (de) Neues orales roentgenkontrastmittel und verfahren zu seiner herstellung.
DE60216471T2 (de) Pharmazeutische zubereitungen mit einem cortisol synthese inhibitor
DE2718260A1 (de) Therapeutische zusammensetzung und verfahren zur herstellung einer tablette
CN108144066B (zh) 一种用于辅助吞咽口服固体药物的稳定的凝胶
DE68928415T2 (de) Verfahren und zusammensetzungen zur verabreichung von lipophilen heilmitteln in einer dosierung nach der gewünschten wirkung

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: 24732596

Country of ref document: EP

Kind code of ref document: A1

WWE Wipo information: entry into national phase

Ref document number: 2024732596

Country of ref document: EP

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 2024732596

Country of ref document: EP

Effective date: 20260109

ENP Entry into the national phase

Ref document number: 2024732596

Country of ref document: EP

Effective date: 20260109

ENP Entry into the national phase

Ref document number: 2024732596

Country of ref document: EP

Effective date: 20260109