EP4199900A1 - Composition and formulation for treating constipation and abdominal bloating - Google Patents

Composition and formulation for treating constipation and abdominal bloating

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Publication number
EP4199900A1
EP4199900A1 EP20790080.4A EP20790080A EP4199900A1 EP 4199900 A1 EP4199900 A1 EP 4199900A1 EP 20790080 A EP20790080 A EP 20790080A EP 4199900 A1 EP4199900 A1 EP 4199900A1
Authority
EP
European Patent Office
Prior art keywords
composition
hereinbefore
formulation
weight
expulsion
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
EP20790080.4A
Other languages
German (de)
French (fr)
Inventor
Sara Pezzetta
Elena VATRI
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.)
Biofarma SRL
Original Assignee
Biofarma SRL
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Filing date
Publication date
Application filed by Biofarma SRL filed Critical Biofarma SRL
Publication of EP4199900A1 publication Critical patent/EP4199900A1/en
Pending legal-status Critical Current

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    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K31/74—Synthetic polymeric materials
    • A61K31/765—Polymers containing oxygen
    • A61K31/77—Polymers containing oxygen of oxiranes
    • 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
    • A61K31/74—Synthetic polymeric materials
    • A61K31/80—Polymers containing hetero atoms not provided for in groups A61K31/755 - A61K31/795
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1611—Inorganic compounds
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1664—Compounds of unknown constitution, e.g. material from plants or animals

Definitions

  • the present invention concerns a granular or powder composition for treating constipation and abdominal bloating, as well as a formulation which comprises the same composition.
  • Constipation is a common gastrointestinal disorder widespread throughout the world that affects both the adult and the child population.
  • constipation (costiveness) defines a syndrome generally associated with persistent difficulties or discomfort in the area of alvine functions. It is characterized by reduced frequency of defecation, difficulty in evacuating with the emission of hard and pellet-like stools, associated in a variable extent with a sensation of incomplete evacuation, a sensation of rectal-anal obstruction, a sensation of distension or abdominal pain or bloating.
  • Constipation is often accompanied by other symptoms of a gastrointestinal nature, including abdominal pain and distension and bloating, due to an excess of gas. In fact, if the stools remain in the intestine for a prolonged period, this leaves the intestinal flora more time for fermentation, with consequent hyper-production of gas.
  • the causes of constipation can be various and multifactorial. Constipation can be classified into primary or secondary constipation, on the basis of etiology. Primary or organic causes of constipation are the alterations of the neuromuscular mechanisms responsible for the control of gastrointestinal and anorectal functions, while secondary causes are linked to metabolic disorders, the intake of certain medicines, neurological disorders and primary diseases of the colon.
  • laxatives are also known, which have an impact on the transfer of water and electrolytes through the intestinal mucosa; they soften hardened stools and stimulate defecation.
  • laxatives can be divided into various types, the main ones being bulk-forming laxatives, lubricating laxatives, stimulating laxatives and osmotic laxatives.
  • Bulk-forming laxatives increase the volume of the non-absorbable solid residue, bringing considerable quantities of indigestible substances, in particular food fibers, which swell in contact with water. These laxatives make the stools denser and more voluminous and increase the amount of water they retain, which promotes evacuation.
  • Lubricating laxatives mix with the fecal matter, helping to soften and lubricate it. In this way, they facilitate the transit of the stools into the intestine by sliding.
  • Stimulating laxatives increase intestinal motility, in particular colic contractions to promote the progress of the stools toward the outside.
  • Osmotic laxatives are not absorbed but retain water and electrolytes in the colon, affecting the consistency of the stools so as to make them semi-solid or liquid.
  • Osmotic laxatives are the most frequently prescribed type of laxative, not only in the case of acute and chronic constipation, but also in preparation for diagnostic tests (e.g. colonoscopy) or surgery.
  • Osmotic laxatives comprise complex carbohydrates, such as lactulose or mannitol, or saline substances such as magnesium hydroxide or phosphates, or even polyethylene glycols (PEG), which are inert water-soluble polymers often with a high molecular weight.
  • complex carbohydrates such as lactulose or mannitol
  • saline substances such as magnesium hydroxide or phosphates, or even polyethylene glycols (PEG), which are inert water-soluble polymers often with a high molecular weight.
  • PEG polyethylene glycols
  • one purpose of the present invention is to propose a composition for treating constipation and abdominal bloating which can alleviate unwanted side effects, both in the short term and in the long term.
  • Another purpose of the present invention is to provide a formulation for treating constipation and abdominal bloating which is convenient and simple for users to take.
  • the Applicant has devised, tested and embodied the present invention to overcome the shortcomings of the state of the art and to obtain these and other purposes and advantages.
  • compositions and of a formulation for treating constipation and abdominal bloating are described, which overcome the limits of the state of the art and eliminate the defects present therein.
  • a granular or powder composition for treating constipation and abdominal bloating comprising a polyethylene glycol and an anti-foaming agent.
  • the polyethylene glycol is present in a quantity greater than or equal to 95% by weight of the total weight of the composition. More favorably, the polyethylene glycol has a concentration comprised between 95% and 99% by weight of the total weight of the composition.
  • the weight ratio between polyethylene glycol and simethicone PEG: Simethicone is greater than 90:1, more advantageously it is comprised between 99:1 and 140:1, even more advantageously it is comprised between 100:1 and 130:1.
  • the polyethylene glycol is macrogol, and has a molecular weight preferably comprised between 3000 and 5000 Da, more preferably equal to 3350 Da or 4000 Da.
  • the anti-foaming agent is dimethicone, preferably in activated form.
  • the dimethicone can be activated, for example by adding silicon oxide gel.
  • a specific example of dimethicone in activated form is simethicone.
  • the composition also comprises a sweetener.
  • the sweetener is an artificial sweetener, for example sucralose.
  • the composition can also comprise at least one insoluble fiber, or a mixture of insoluble fibers and/or soluble fibers, in order to increase the fecal mass and promote its expulsion.
  • the composition also comprises a bulk-forming laxative, more preferably a hydrophilic resin, even more preferentially polycarbophil calcium, in order to further promote the expulsion of the fecal mass and increase the elimination of gases.
  • a bulk-forming laxative more preferably a hydrophilic resin, even more preferentially polycarbophil calcium, in order to further promote the expulsion of the fecal mass and increase the elimination of gases.
  • the composition also comprises a stool softening substance, in order to promote the expulsion of the fecal mass.
  • the stool softening substance comprises mineral oil, vegetable oil and/or docusate sodium.
  • composition described here also comprises one or more magnesium mineral salts, in order to promote the expulsion of the fecal mass.
  • composition for treating constipation and abdominal bloating described here can also comprise an anti-caking agent, for the correct absorption and the correct dispersion of the activated dimethicone and to promote the fluidity of the powdered preparation.
  • an anti-caking agent is silicon dioxide.
  • composition also comprises specific enzymes, for example amylase and/or glycosidases.
  • the composition described here also comprises muco-polysaccharides in order to create a protective layer in the intestinal lumen and promote the expulsion of the fecal mass.
  • the muco-poly saccharide comprises hyaluronic acid and its salts.
  • composition described here also comprises a probiotic (even tyndalized) in order to contribute to the digestive process, and consequently promote the expulsion of the fecal mass and, at the same time, rebalance the intestinal bacterial flora.
  • a probiotic even tyndalized
  • the composition described here also comprises plant extracts titrated in polysaccharides, with calming, moisturizing, and soothing functions and a function of filming the intestinal mucosa, such as for example titrated polysaccharides extracted from Mallow, Altea, Linden.
  • the composition described here also comprises carboxymethylcellulose as a filming and protective agent of the intestinal lumen.
  • the composition described here also comprises vegetable and mineral oils with a lubricating and softening action on stools.
  • the composition described here also comprises sugar alcohols such as xylitol, glycerol, sorbitol, used to promote the organoleptic pleasantness of the preparation as well as because of their characteristics of recalling water and softening stools.
  • sugar alcohols such as xylitol, glycerol, sorbitol
  • the granular or powder composition described here comprises macrogol, activated dimethicone (for example simethicone), an anti-caking agent and a sweetener.
  • the anti-caking agent is silicon dioxide.
  • the sweetener is sucralose.
  • the macrogol has a concentration greater than 40%, preferably greater than 50%, more preferably greater than 95% by weight of the total weight of the composition
  • the activated dimethicone has a concentration comprised between 0.05% and 2.0% by weight
  • the anti-caking agent, where present has a concentration comprised between 0.05% and 2.0% by weight
  • the sweetener has a concentration lower than 0.5% by weight.
  • a formulation for treating constipation and abdominal bloating, which comprises the granular or powder composition indicated above.
  • the formulation is preferably in powder or granular form, preferably soluble in water or other liquids, it is made available as a gel or it is made available in a liquid solution for oral administration.
  • the formulation is made available as a gel, it also comprises viscosifying/texturizing rheological agents such as guar gum, xanthan gum, carboxymethylcellulose (CMC) and/or carbopol. These compounds allow to obtain the formulation as a gel.
  • viscosifying/texturizing rheological agents such as guar gum, xanthan gum, carboxymethylcellulose (CMC) and/or carbopol.
  • the formulation is made available in single-dose sachets or in multi-dose packs.
  • the present description also includes the intervals that derive from uniting or overlapping two or more intervals described, unless otherwise indicated.
  • the present description also includes the intervals that can derive from the combination of two or more values taken at different points, unless otherwise indicated.
  • Embodiments described here concern a composition for treating constipation and abdominal bloating comprising a PEG compound, in particular macrogol, both as a laxative agent as well as a main ingredient.
  • Macrogol represents more than 40% by weight of the composition, preferably more than 45%, more preferably more than 50%, even more preferably more than 95% by weight.
  • macrogol is present between 45% and 99% by weight of the composition, in particular between 95% and 99% by weight of the total weight of the composition.
  • Macrogol is a high molecular weight water-soluble inert polymer, capable of forming hydrogen bonds with water molecules, operating as a pure osmotic agent, which retains the water that accompanies administration in stools and opposes its reabsorption in the large intestine.
  • the mechanism through which macrogol acts determines a rehydration and softening of the stools, thus facilitating defecation.
  • Intestinal transit is accelerated in the colon and rectum since macrogol promotes the intraluminal movement of stools with a reduced consistency due to the increase in water content.
  • the increase in stool volume dilates the intestinal wall, accelerating intestinal transit in the colon and rectum and activating the urge to defecate.
  • Macrogol therefore acts simultaneously on the main symptoms of constipation, increasing the frequency of bowel movements and reducing the consistency of the stools. Macrogol is not absorbed or metabolized in the intestinal tract and does not lead to electrolyte imbalances, if taken with the indicated dose of liquid. The mode of action of macrogol is non-specific and is independent of the pathogenesis of the disorders.
  • Macrogol has a molecular weight preferably comprised between 3000 Da and 5000 Da. More particularly, the macrogol comprised in the composition according to the invention can have a molecular weight of 3350 Da or 4000 Da. These two types of macrogol differ only in terms of the molecular weight, since they are identical in all other characteristics, in particular in terms of efficacy and safety profile.
  • electrolyte-free macrogol-based products represents an effective and safe treatment for constipation and does not lead to electrolyte imbalances, both in adults and also in children. Therefore, it does not cause side effects following its intake and, therefore, can be considered a safe and well tolerated active ingredient.
  • composition according to the invention also comprises an anti-foaming agent, in particular dimethicone, preferably activated with the addition of silicon oxide gels.
  • an anti-foaming agent in particular dimethicone, preferably activated with the addition of silicon oxide gels.
  • activated dimethicone is simethicone.
  • Dimethicone is a silicone belonging to the family of polydimethylsiloxanes which has anti-foaming properties, which are the basis of its beneficial effects. Dimethicone has a polymeric structure consisting of a succession of silicon and oxygen atoms (polydimethylsiloxane), mixed with silica gel. The latter ingredient is hydrophobic, stable at high temperatures, physiologically inactive, non-toxic and safe when taken orally. It is not absorbed by the gastrointestinal tract and does not interfere with the digestive processes in any way whatsoever.
  • the anti-foaming action is exerted through a physical mechanism of reduction of the surface tension of the gas bubbles.
  • the mixture of polydimethylsiloxane and hydrophobic silica disperses on the surface of aqueous liquids, forming a low surface tension film that breaks easily. In this way, the gas contained in the bubbles present in the gastrointestinal tract is released and unites to form entities of a larger size (coalescence) which are easily eliminated.
  • activated dimethicone in particular simethicone, decreases the surface tension of the gas bubbles present in the gastrointestinal tract, facilitating their expulsion.
  • the elimination of gases reduces the sensation of bloating and abdominal distension.
  • dimethicone does not cause any side effects whatsoever following its intake, and therefore can be considered a safe and well-tolerated agent.
  • Numerous clinical studies have shown the efficacy and safety of using dimethicone in reducing the symptoms caused by excess gas in the intestine, regardless of its causes.
  • the activated dimethicone supports the main action of the composition, given by macrogol, and helps relieve the discomfort caused by bloating and flatulence, gastrointestinal symptoms that often accompany constipation.
  • dimethicone in particular activated dimethicone (for example simethicone) is present in a concentration comprised between 0.05% and 2%, more preferably between 0.1% and 1% of the composition.
  • activated dimethicone for example simethicone
  • constipation is often accompanied by gastrointestinal symptoms (including abdominal distention, meteorism, and flatulence) caused by excess gas. Gas is formed as a consequence of the prolonged stay of the stools in the intestine, which gives the intestinal bacterial flora more time for fermentation.
  • macrogol-based solutions can also be accompanied by flatulence and abdominal bloating.
  • activated dimethicone as a secondary ingredient in macrogol-based formulations for the asymptomatic treatment of constipation helps to alleviate the discomfort caused by these symptoms, without interfering in any way whatsoever with the main mechanism of action of the product that is conferred by macrogol.
  • the granular or powder composition described here, or the formulation comprising such composition can include one or more prebiotic and/or probiotic compounds.
  • prebiotic compounds such as one or more insoluble fibers
  • insoluble fibers include Psyllium cuticle or oat bran.
  • the one or more insoluble fibers it can also be provided to add one or more soluble fibers to the composition.
  • fibers include inulin, pectin, fructooligosaccharides (FOS) or psyllium seeds.
  • the expulsion of the fecal mass can be further promoted by adding, as optional compounds, at least one or more from calcium polycarbophil, which also increases the elimination of gases, mineral oil or docusate sodium as softening substances of the fecal mass, one or more from magnesium mineral salts, amylase and/or glycosidase type enzymes, hyaluronic acid as mucus- polysaccharide which create a protective layer in the intestinal lumen.
  • a probiotic which, in addition to promoting the expulsion of fecal matter, also has an action of rebalancing the intestinal bacterial flora.
  • an anti-caking excipient such as silicon dioxide
  • silicon dioxide has a concentration comprised between 0.05% and 2% by weight, more preferably between 0.1% and 1% by weight of the composition.
  • an artificial sweetener can be used.
  • an artificial sweetener is sucralose, but acesulfame K, aspartame or stevia, or a mixture of one or more of them can also be provided.
  • the sweetener is preferably concentrated to less than 0.5%, more preferably less than 0.1% by weight in the composition described here. It can also be provided to add a flavoring excipient, for example containing an orange flavor, a lemon flavor or any type of flavor whatsoever that has a pleasant taste.
  • composition can also advantageously contain carboxymethylcellulose CMC as a filming agent, plant extracts titrated in polysaccharides and/or sugar alcohols.
  • salts or electrolytes
  • the addition of electrolytes derives from their original use as solutions for bowel preparation before performing diagnostic tests or surgery.
  • the macrogol-based composition is to be administered in high doses and salts are added in order to limit the risk of hydro-electrolyte imbalances.
  • composition for treating constipation and abdominal bloating described here is advantageously formulated in granular or powder form, or in a gel or in a liquid solution for oral administration. Regardless of the formulation of the composition, it can be made available in single-dose sachets or in multi-dose packs (for example ajar or bottle).
  • the formulation can be packaged into stick-pack type sachets (for example the sachet known as T-Win® supplied by the Applicant), in turn packaged into a secondary packaging, for example a cardboard box.
  • a secondary packaging for example a cardboard box.
  • the singledose sachets can contain, for example, 4 g, 5 g and 10 g of powder or 10 ml or 20 ml of oral solution.
  • a multi-dose package can be provided, such as, for example, a jar or a bottle in which a predeterminate quantity of product is disposed.
  • a metering member typically a measuring cup, configured to take the correct dose of formulation.
  • the multi-dose package can contain, for example, 200 g, 250 g, 300 g, 400 g of powder or 480 ml of oral solution, depending on requirements.
  • the powder or granules should be diluted in water or other liquid and taken immediately.
  • the oral solution should be taken as it is and then followed by water.
  • the volumes of water or other liquids to be used for intake are predefined.
  • the doses are defined taking into account the population being treated and are specified as a function of age group and, in the case of children aged between 6 months and 12 years, also of the different weight brackets.
  • the dose should be increased or decreased, depending on the individual response to treatment, in order to allow a regular evacuation of soft stools.
  • the maximum dose provided does not normally exceed 20 g of powder or 40 ml of oral solution in the versions intended for children under the age of 12, and 40 g of powder or 80 ml of oral solution in the versions intended for adults and children over the age of 12.
  • compositions for treating constipation and abdominal bloating are given below.
  • EXAMPLE 1 The following composition is formulated in powder form and does not contain any flavoring excipient whatsoever. It comprises:
  • dimethicone 0.800 % (w/w)
  • Silicon dioxide 1.000 % (w/w)
  • composition is also formulated in powder form, and comprises one flavoring excipient.
  • dimethicone 0.800 % (w/w)
  • Silicon dioxide 1.000 % (w/w)
  • This example provides a liquid formulation of the composition according to the invention, and does not contain flavoring excipients. Since it is a liquid formulation, a solubilizing component such as polysorbate 80 is provided.
  • Citric acid 0.334 % (w/w)
  • this liquid formulation was obtained by diluting a powder formulation in which Macrogol is concentrated at 95.394% (w/w).
  • This example shows a liquid formulation of the composition, with a flavoring excipient. Since it is a liquid formulation, a solubilizing component such as polysorbate 80 is provided. Purified water 51.299 % (w/w)
  • Citric acid 0.334 % (w/w)
  • this liquid formulation was obtained by diluting a powder formulation in which Macrogol is concentrated at 95.002% (w/w).

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Abstract

The granular or powder composition for treating constipation and abdominal bloating comprises at least one polyethylene glycol PEG as a laxative agent and an antimeteoric agent. Such composition is made available in a formulation that can be a powder, in a solution for oral administration or a gel.

Description

“COMPOSITION AND FORMULATION FOR TREATING CONSTIPATION AND ABDOMINAL BLOATING”
FIELD OF THE INVENTION
The present invention concerns a granular or powder composition for treating constipation and abdominal bloating, as well as a formulation which comprises the same composition.
BACKGROUND OF THE INVENTION
Constipation is a common gastrointestinal disorder widespread throughout the world that affects both the adult and the child population.
The term “constipation” (costiveness) defines a syndrome generally associated with persistent difficulties or discomfort in the area of alvine functions. It is characterized by reduced frequency of defecation, difficulty in evacuating with the emission of hard and pellet-like stools, associated in a variable extent with a sensation of incomplete evacuation, a sensation of rectal-anal obstruction, a sensation of distension or abdominal pain or bloating.
An incomplete evacuation leads to greater reabsorption of water from the stools and can lead to the formation of a mass of consistent stools, hard and difficult to evacuate in the rectum-sigma, known as fecaloma.
Constipation is often accompanied by other symptoms of a gastrointestinal nature, including abdominal pain and distension and bloating, due to an excess of gas. In fact, if the stools remain in the intestine for a prolonged period, this leaves the intestinal flora more time for fermentation, with consequent hyper-production of gas.
The causes of constipation can be various and multifactorial. Constipation can be classified into primary or secondary constipation, on the basis of etiology. Primary or organic causes of constipation are the alterations of the neuromuscular mechanisms responsible for the control of gastrointestinal and anorectal functions, while secondary causes are linked to metabolic disorders, the intake of certain medicines, neurological disorders and primary diseases of the colon.
There are basic therapeutic measures for treating constipation, intended to modify the habits and behaviors that can promote it. These measures comprise information to the patients on symptoms, pathophysiology and potential causes of constipation, physiotherapy measures, increased physical exercise, increased consumption of food fiber and adequate intake of liquids.
In addition to these basic measures, laxatives are also known, which have an impact on the transfer of water and electrolytes through the intestinal mucosa; they soften hardened stools and stimulate defecation.
Based on their mechanism of action, laxatives can be divided into various types, the main ones being bulk-forming laxatives, lubricating laxatives, stimulating laxatives and osmotic laxatives.
Bulk-forming laxatives increase the volume of the non-absorbable solid residue, bringing considerable quantities of indigestible substances, in particular food fibers, which swell in contact with water. These laxatives make the stools denser and more voluminous and increase the amount of water they retain, which promotes evacuation.
Lubricating laxatives mix with the fecal matter, helping to soften and lubricate it. In this way, they facilitate the transit of the stools into the intestine by sliding.
Stimulating laxatives increase intestinal motility, in particular colic contractions to promote the progress of the stools toward the outside.
Finally, osmotic laxatives are not absorbed but retain water and electrolytes in the colon, affecting the consistency of the stools so as to make them semi-solid or liquid. Osmotic laxatives are the most frequently prescribed type of laxative, not only in the case of acute and chronic constipation, but also in preparation for diagnostic tests (e.g. colonoscopy) or surgery.
Osmotic laxatives comprise complex carbohydrates, such as lactulose or mannitol, or saline substances such as magnesium hydroxide or phosphates, or even polyethylene glycols (PEG), which are inert water-soluble polymers often with a high molecular weight.
One disadvantage of known laxative compositions is the onset of unpleasant side effects, in particular abdominal pain and bloating. These unwanted side effects can extend over time and have a negative impact on the quality of life of those who experience them.
There is therefore a need to perfect a composition for treating constipation and abdominal bloating which can overcome at least one of the disadvantages of the state of the art. In particular, one purpose of the present invention is to propose a composition for treating constipation and abdominal bloating which can alleviate unwanted side effects, both in the short term and in the long term.
Another purpose of the present invention is to provide a formulation for treating constipation and abdominal bloating which is convenient and simple for users to take.
The Applicant has devised, tested and embodied the present invention to overcome the shortcomings of the state of the art and to obtain these and other purposes and advantages.
SUMMARY OF THE INVENTION
The present invention is set forth and characterized in the independent claims. The dependent claims describe other characteristics of the present invention or variants to the main inventive idea.
In accordance with the above purposes, embodiments of a composition and of a formulation for treating constipation and abdominal bloating are described, which overcome the limits of the state of the art and eliminate the defects present therein.
In accordance with some embodiments, a granular or powder composition is provided for treating constipation and abdominal bloating comprising a polyethylene glycol and an anti-foaming agent. Favorably, the polyethylene glycol is present in a quantity greater than or equal to 95% by weight of the total weight of the composition. More favorably, the polyethylene glycol has a concentration comprised between 95% and 99% by weight of the total weight of the composition.
Advantageously, the weight ratio between polyethylene glycol and simethicone PEG: Simethicone is greater than 90:1, more advantageously it is comprised between 99:1 and 140:1, even more advantageously it is comprised between 100:1 and 130:1.
In accordance with some embodiments, the polyethylene glycol is macrogol, and has a molecular weight preferably comprised between 3000 and 5000 Da, more preferably equal to 3350 Da or 4000 Da.
Advantageously, the anti-foaming agent is dimethicone, preferably in activated form. The dimethicone can be activated, for example by adding silicon oxide gel. A specific example of dimethicone in activated form is simethicone.
Preferably, the composition also comprises a sweetener. More preferably, the sweetener is an artificial sweetener, for example sucralose.
In accordance with some embodiments, the composition can also comprise at least one insoluble fiber, or a mixture of insoluble fibers and/or soluble fibers, in order to increase the fecal mass and promote its expulsion.
Preferentially, the composition also comprises a bulk-forming laxative, more preferably a hydrophilic resin, even more preferentially polycarbophil calcium, in order to further promote the expulsion of the fecal mass and increase the elimination of gases.
According to some embodiments, the composition also comprises a stool softening substance, in order to promote the expulsion of the fecal mass. Preferably, the stool softening substance comprises mineral oil, vegetable oil and/or docusate sodium.
It is possible to provide that the composition described here also comprises one or more magnesium mineral salts, in order to promote the expulsion of the fecal mass.
Advantageously, the composition for treating constipation and abdominal bloating described here can also comprise an anti-caking agent, for the correct absorption and the correct dispersion of the activated dimethicone and to promote the fluidity of the powdered preparation. More advantageously, the anti-caking agent is silicon dioxide.
In order to contribute to the digestive process, and consequently further promote the expulsion of the fecal mass, it is advantageous to provide that the composition also comprises specific enzymes, for example amylase and/or glycosidases.
According to some embodiments, the composition described here also comprises muco-polysaccharides in order to create a protective layer in the intestinal lumen and promote the expulsion of the fecal mass. Preferentially, the muco-poly saccharide comprises hyaluronic acid and its salts.
Favorably, the composition described here also comprises a probiotic (even tyndalized) in order to contribute to the digestive process, and consequently promote the expulsion of the fecal mass and, at the same time, rebalance the intestinal bacterial flora.
According to some embodiments, the composition described here also comprises plant extracts titrated in polysaccharides, with calming, moisturizing, and soothing functions and a function of filming the intestinal mucosa, such as for example titrated polysaccharides extracted from Mallow, Altea, Linden.
According to some embodiments, the composition described here also comprises carboxymethylcellulose as a filming and protective agent of the intestinal lumen.
According to some embodiments, the composition described here also comprises vegetable and mineral oils with a lubricating and softening action on stools.
According to some embodiments, the composition described here also comprises sugar alcohols such as xylitol, glycerol, sorbitol, used to promote the organoleptic pleasantness of the preparation as well as because of their characteristics of recalling water and softening stools.
In accordance with some embodiments, the granular or powder composition described here comprises macrogol, activated dimethicone (for example simethicone), an anti-caking agent and a sweetener. Preferably, the anti-caking agent is silicon dioxide. More preferably, the sweetener is sucralose. Even more preferably, the macrogol has a concentration greater than 40%, preferably greater than 50%, more preferably greater than 95% by weight of the total weight of the composition, the activated dimethicone has a concentration comprised between 0.05% and 2.0% by weight, the anti-caking agent, where present, has a concentration comprised between 0.05% and 2.0% by weight, and the sweetener has a concentration lower than 0.5% by weight.
According to one aspect, a formulation is provided for treating constipation and abdominal bloating, which comprises the granular or powder composition indicated above. The formulation is preferably in powder or granular form, preferably soluble in water or other liquids, it is made available as a gel or it is made available in a liquid solution for oral administration.
Favorably, if the formulation is made available as a gel, it also comprises viscosifying/texturizing rheological agents such as guar gum, xanthan gum, carboxymethylcellulose (CMC) and/or carbopol. These compounds allow to obtain the formulation as a gel.
Advantageously, the formulation is made available in single-dose sachets or in multi-dose packs.
DESCRIPTION OF EMBODIMENTS
We will now refer in detail to the possible embodiments of the invention, of which one or more examples are supplied by way of a non-limiting example. The phraseology and terminology used here is also for the purposes of supplying nonlimiting examples.
Unless otherwise defined, all the technical and scientific terms used here and hereafter have the same meaning as commonly understood by a person with ordinary experience in the field of the art to which the present invention belongs. Even if methods and materials similar or equivalent to those described here can be used in practice and in the trials of the present invention, the methods and materials are described hereafter as an example. In the event of conflict, the present application shall prevail, including its definitions. The materials, methods and examples have a purely illustrative purpose and shall not be understood restrictively.
Unless otherwise indicated, all measurements are carried out at 25° C (ambient temperature) and at atmospheric pressure. Unless otherwise indicated, all temperatures are expressed in degrees Celsius.
All percentages and ratios indicated are understood to refer to the weight of the total composition (w/w), unless otherwise indicated.
All percentage intervals reported here are provided with the provision that the sum with respect to the overall composition is 100%, unless otherwise indicated.
All the intervals reported here shall be understood to include the extremes, including those that report an interval “between” two values, unless otherwise indicated.
The present description also includes the intervals that derive from uniting or overlapping two or more intervals described, unless otherwise indicated.
The present description also includes the intervals that can derive from the combination of two or more values taken at different points, unless otherwise indicated.
Where water is mentioned we mean purified water, unless otherwise specified. Embodiments described here concern a composition for treating constipation and abdominal bloating comprising a PEG compound, in particular macrogol, both as a laxative agent as well as a main ingredient. Macrogol represents more than 40% by weight of the composition, preferably more than 45%, more preferably more than 50%, even more preferably more than 95% by weight. For example, macrogol is present between 45% and 99% by weight of the composition, in particular between 95% and 99% by weight of the total weight of the composition.
Macrogol is a high molecular weight water-soluble inert polymer, capable of forming hydrogen bonds with water molecules, operating as a pure osmotic agent, which retains the water that accompanies administration in stools and opposes its reabsorption in the large intestine.
The mechanism through which macrogol acts determines a rehydration and softening of the stools, thus facilitating defecation. Intestinal transit is accelerated in the colon and rectum since macrogol promotes the intraluminal movement of stools with a reduced consistency due to the increase in water content. At the same time, the increase in stool volume dilates the intestinal wall, accelerating intestinal transit in the colon and rectum and activating the urge to defecate.
Macrogol therefore acts simultaneously on the main symptoms of constipation, increasing the frequency of bowel movements and reducing the consistency of the stools. Macrogol is not absorbed or metabolized in the intestinal tract and does not lead to electrolyte imbalances, if taken with the indicated dose of liquid. The mode of action of macrogol is non-specific and is independent of the pathogenesis of the disorders.
Macrogol has a molecular weight preferably comprised between 3000 Da and 5000 Da. More particularly, the macrogol comprised in the composition according to the invention can have a molecular weight of 3350 Da or 4000 Da. These two types of macrogol differ only in terms of the molecular weight, since they are identical in all other characteristics, in particular in terms of efficacy and safety profile.
It has been verified that the use, even on a continuous basis, of electrolyte-free macrogol-based products represents an effective and safe treatment for constipation and does not lead to electrolyte imbalances, both in adults and also in children. Therefore, it does not cause side effects following its intake and, therefore, can be considered a safe and well tolerated active ingredient.
The composition according to the invention also comprises an anti-foaming agent, in particular dimethicone, preferably activated with the addition of silicon oxide gels. An example of activated dimethicone is simethicone.
Dimethicone is a silicone belonging to the family of polydimethylsiloxanes which has anti-foaming properties, which are the basis of its beneficial effects. Dimethicone has a polymeric structure consisting of a succession of silicon and oxygen atoms (polydimethylsiloxane), mixed with silica gel. The latter ingredient is hydrophobic, stable at high temperatures, physiologically inactive, non-toxic and safe when taken orally. It is not absorbed by the gastrointestinal tract and does not interfere with the digestive processes in any way whatsoever.
The anti-foaming action is exerted through a physical mechanism of reduction of the surface tension of the gas bubbles. The mixture of polydimethylsiloxane and hydrophobic silica disperses on the surface of aqueous liquids, forming a low surface tension film that breaks easily. In this way, the gas contained in the bubbles present in the gastrointestinal tract is released and unites to form entities of a larger size (coalescence) which are easily eliminated.
In essence, activated dimethicone, in particular simethicone, decreases the surface tension of the gas bubbles present in the gastrointestinal tract, facilitating their expulsion. The elimination of gases reduces the sensation of bloating and abdominal distension.
It has been verified that, in adults and children, dimethicone does not cause any side effects whatsoever following its intake, and therefore can be considered a safe and well-tolerated agent. Numerous clinical studies have shown the efficacy and safety of using dimethicone in reducing the symptoms caused by excess gas in the intestine, regardless of its causes.
Advantageously, the activated dimethicone supports the main action of the composition, given by macrogol, and helps relieve the discomfort caused by bloating and flatulence, gastrointestinal symptoms that often accompany constipation.
Preferably, dimethicone, in particular activated dimethicone (for example simethicone) is present in a concentration comprised between 0.05% and 2%, more preferably between 0.1% and 1% of the composition.
As already mentioned, constipation is often accompanied by gastrointestinal symptoms (including abdominal distention, meteorism, and flatulence) caused by excess gas. Gas is formed as a consequence of the prolonged stay of the stools in the intestine, which gives the intestinal bacterial flora more time for fermentation.
The administration of macrogol-based solutions can also be accompanied by flatulence and abdominal bloating. The use of activated dimethicone as a secondary ingredient in macrogol-based formulations for the asymptomatic treatment of constipation helps to alleviate the discomfort caused by these symptoms, without interfering in any way whatsoever with the main mechanism of action of the product that is conferred by macrogol.
Although the effects deriving from macrogol and activated dimethicone are already satisfactory in themselves, it is possible to enhance them by adding one or more secondary components or ingredients, which however are to be intended as optional in the context of the present description.
In some embodiments, which can be combined with all the embodiments described here, the granular or powder composition described here, or the formulation comprising such composition, can include one or more prebiotic and/or probiotic compounds.
For example, it can be provided to add prebiotic compounds, such as one or more insoluble fibers, in the composition, which are added to the fecal mass and promote its expulsion from the gastrointestinal tract. Possible examples of insoluble fibers include Psyllium cuticle or oat bran.
In combination with, or as an alternative to, the one or more insoluble fibers, it can also be provided to add one or more soluble fibers to the composition. Examples of fibers include inulin, pectin, fructooligosaccharides (FOS) or psyllium seeds.
The expulsion of the fecal mass can be further promoted by adding, as optional compounds, at least one or more from calcium polycarbophil, which also increases the elimination of gases, mineral oil or docusate sodium as softening substances of the fecal mass, one or more from magnesium mineral salts, amylase and/or glycosidase type enzymes, hyaluronic acid as mucus- polysaccharide which create a protective layer in the intestinal lumen. There can also be provided, in addition or as an alternative to one or more of the components as above, the presence of a probiotic which, in addition to promoting the expulsion of fecal matter, also has an action of rebalancing the intestinal bacterial flora.
An anti-caking excipient, such as silicon dioxide, can also be included in the composition described here, in order to allow the correct absorption and the correct dispersion of the dimethicone and thus support its machinability and stability. If present, the silicon dioxide has a concentration comprised between 0.05% and 2% by weight, more preferably between 0.1% and 1% by weight of the composition.
In order to improve the palatability of the composition described here, it is preferable to provide that it be free of added salts. The degree to which the composition has an enjoyable taste can be further improved by adding a substance with a sweetening effect, in a minimal percentage. For example, an artificial sweetener can be used. One example of artificial sweetener is sucralose, but acesulfame K, aspartame or stevia, or a mixture of one or more of them can also be provided. The sweetener is preferably concentrated to less than 0.5%, more preferably less than 0.1% by weight in the composition described here. It can also be provided to add a flavoring excipient, for example containing an orange flavor, a lemon flavor or any type of flavor whatsoever that has a pleasant taste.
The composition can also advantageously contain carboxymethylcellulose CMC as a filming agent, plant extracts titrated in polysaccharides and/or sugar alcohols.
Finally, it should be noted that it is possible to add salts, or electrolytes, to the composition. The addition of electrolytes derives from their original use as solutions for bowel preparation before performing diagnostic tests or surgery. When used in this field, the macrogol-based composition is to be administered in high doses and salts are added in order to limit the risk of hydro-electrolyte imbalances.
Since the doses of macrogol and the volumes of liquids taken for treating constipation are significantly lower than those used for bowel cleansing, in this case it is possible to avoid the addition of electrolytes, with the advantage of reducing the total sodium load, improving the palatability of the product and potentially increasing the patient’s response to treatment.
The composition for treating constipation and abdominal bloating described here is advantageously formulated in granular or powder form, or in a gel or in a liquid solution for oral administration. Regardless of the formulation of the composition, it can be made available in single-dose sachets or in multi-dose packs (for example ajar or bottle).
For example, the formulation can be packaged into stick-pack type sachets (for example the sachet known as T-Win® supplied by the Applicant), in turn packaged into a secondary packaging, for example a cardboard box. In this way, the single doses are already prepared and ready for use for the user. The singledose sachets can contain, for example, 4 g, 5 g and 10 g of powder or 10 ml or 20 ml of oral solution.
Alternatively, a multi-dose package can be provided, such as, for example, a jar or a bottle in which a predeterminate quantity of product is disposed. In this case, it is advantageous to also provide a metering member, typically a measuring cup, configured to take the correct dose of formulation. The multi-dose package can contain, for example, 200 g, 250 g, 300 g, 400 g of powder or 480 ml of oral solution, depending on requirements.
The powder or granules should be diluted in water or other liquid and taken immediately. The oral solution should be taken as it is and then followed by water. The volumes of water or other liquids to be used for intake are predefined.
The doses are defined taking into account the population being treated and are specified as a function of age group and, in the case of children aged between 6 months and 12 years, also of the different weight brackets. The dose should be increased or decreased, depending on the individual response to treatment, in order to allow a regular evacuation of soft stools. The maximum dose provided does not normally exceed 20 g of powder or 40 ml of oral solution in the versions intended for children under the age of 12, and 40 g of powder or 80 ml of oral solution in the versions intended for adults and children over the age of 12.
Four examples of compositions for treating constipation and abdominal bloating according to the present description are given below.
EXAMPLE 1 The following composition is formulated in powder form and does not contain any flavoring excipient whatsoever. It comprises:
Macrogol 3350 or 4000 98.180 % (w/w)
Activated dimethicone (simethicone) 0.800 % (w/w)
Silicon dioxide 1.000 % (w/w)
Sucralose 0.020 % (w/w)
EXAMPLE 2
The following composition is also formulated in powder form, and comprises one flavoring excipient.
Macrogol 3350 or 4000 97.818 % (w/w)
Activated dimethicone (simethicone) 0.800 % (w/w)
Silicon dioxide 1.000 % (w/w)
Sucralose 0.020 % (w/w)
Orange flavor 0.362 % (w/w)
EXAMPLE 3
This example provides a liquid formulation of the composition according to the invention, and does not contain flavoring excipients. Since it is a liquid formulation, a solubilizing component such as polysorbate 80 is provided.
Purified water 51.499 % (w/w)
Polysorbate 80 FG-TEEN 80 0.800 % (w/w)
Macrogol 3350 or 4000 46.267 % (w/w)
Activated Dimethicone 0.400 % (w/w)
Potassium sorbate 0.090 % (w/w)
Sodium benzoate 0.090 % (w/w)
Sucralose 0.020 % (w/w)
Xanthan gum 0.500 % (w/w)
Citric acid 0.334 % (w/w)
It is noted that this liquid formulation was obtained by diluting a powder formulation in which Macrogol is concentrated at 95.394% (w/w).
EXAMPLE 4
This example shows a liquid formulation of the composition, with a flavoring excipient. Since it is a liquid formulation, a solubilizing component such as polysorbate 80 is provided. Purified water 51.299 % (w/w)
Polysorbate 80 FG-TEEN 80 0,800 % (w/w)
Macrogol 3350 or 4000 46.267 % (w/w)
Activated Dimethicone 0.400 % (w/w)
Potassium sorbate 0.090 % (w/w)
Sodium benzoate 0.090 % (w/w)
Sucralose 0.020 % (w/w)
Xanthan gum 0.500 % (w/w)
Citric acid 0.334 % (w/w)
Lemon flavor 0.200 % (w/w)
It is noted that this liquid formulation was obtained by diluting a powder formulation in which Macrogol is concentrated at 95.002% (w/w).
It is clear that modifications and/or additions of parts may be made to the composition and to the formulation for treating constipation and abdominal bloating as described heretofore, without departing from the field of the present invention as defined by the claims.

Claims

1. Granular or powder composition for treating constipation and abdominal bloating, comprising at least one polyethylene glycol (PEG) as a laxative agent, characterized in that polyethylene glycol is present in a quantity greater than or equal to 95% by weight of the total weight of the composition, and in that it comprises activated dimethicone as an antimeteoric agent.
2. Composition as in claim 1, characterized in that the proportion between polyethylene glycol and activated dimethicone is greater than 90:1.
3. Composition as in claim 1 or 2 characterized in that the polyethylene glycol is macrogol.
4. Composition as in claim 3, characterized in that the macrogol has a molecular weight selected between 3350 Da and 4000 Da.
5. Composition as in any claim hereinbefore, characterized in that the activated dimethicone is present between 0.05% and 2.0% by weight of the total weight of the composition.
6. Composition as in any claim hereinbefore, characterized in that it also comprises sucralose, acesulfame K, aspartame and/or stevia as a sweetener.
7. Composition as in claim 6, characterized in that the sucralose has a concentration lower than 0.5% by weight of the total weight of the composition.
8. Composition as in any claim hereinbefore, characterized in that it also comprises silicon dioxide as an anti-caking agent.
9. Composition as in claim 5, characterized in that the silicon dioxide has a concentration comprised between 0.05% and 2.0% by weight of the total weight of the composition.
10. Composition as in any claim hereinbefore, characterized in that it comprises at least one insoluble fiber in order to increase the fecal mass and promote its expulsion.
11. Composition as in any claim hereinbefore, characterized in that it comprises a bulk-forming laxative.
12. Composition as in claim 11, characterized in that the bulk-forming laxative is a hydrophilic resin.
13. Composition as in any claim hereinbefore, characterized in that it comprises mineral oil, vegetable oil and/or sodium docusate as a stool softener.
14. Composition as in any claim hereinbefore, characterized in that it comprises one or more magnesium mineral salts in order to promote the expulsion of the fecal mass.
15. Composition as in any claim hereinbefore, characterized in that it comprises amylase and/or glycosidases in order to promote the expulsion of fecal mass.
16. Composition as in any claim hereinbefore, characterized in that it also comprises hyaluronic acid and its salts as mucus-polysaccharide in order to create a protective layer in the intestinal lumen and promote the expulsion of fecal mass.
17. Composition as in any claim hereinbefore, characterized in that it comprises a probiotic, even in tyndalized form, in order to promote the expulsion of fecal matter and at the same time rebalance the intestinal bacterial flora.
18. Composition as in any claim hereinbefore, characterized in that said activated dimethicone is simethicone.
19. Formulation for treating constipation and abdominal bloating, characterized in that it comprises a composition as in any claim hereinbefore.
20. Formulation as in claim 19, characterized in that it is made available as a powder soluble in water or in other liquids.
21. Formulation as in claim 20, characterized in that it is made available as a liquid solution.
22. Formulation as in claim 20, characterized in that it is made available as a gel.
23. Formulation as in claim 22, characterized in that the gel is obtained with the addition of viscosifying/texturizing rheological agents such as guar gum, xanthan gum, carboxymethylcellulose CMC, carbopol.
24. Formulation as in claim 20, characterized in that it contains a flavor or a mixture of flavors.
25. Formulation as in claim 24, characterized in that said flavor or mixture of flavors are natural or artificial.
26. Formulation as in claim from 20 to 25, characterized in that it is made available in single-dose sachets or in multi-dose packs.
EP20790080.4A 2020-08-20 2020-08-20 Composition and formulation for treating constipation and abdominal bloating Pending EP4199900A1 (en)

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