FIELD OF THE INVENTION

The present invention concerns a composition for the treatment of intestinal gas and bloating, and its corresponding formulation.

The compositions are used to reduce the presence of gas in the digestive system, responsible for intestinal bloating.

BACKGROUND OF THE INVENTION

The presence of gas in the gastrointestinal tract is a physiological condition that does not cause any disorder in most individuals. However, in altered psychological, chemical, anatomical or physiological conditions, the accumulation of gas in the intestine can cause uncomfortable symptoms that can compromise the quality of life.

Abdominal bloating is a common symptom that affects up to 76% of patients with functional gastrointestinal disorders (such as functional dyspepsia and/or irritable bowel syndrome) and 6-13% of the healthy population. The term abdominal bloating is ambiguous in meaning and includes heterogeneous symptoms, since it is the subjective sensations of individuals who report feeling a full and contracted abdomen, sensations of bloating/distended abdomen, abdominal pressure or also a sensation of excessive gas in the abdomen. Usually patients who complain of an excessive presence of gastrointestinal gas also report a feeling of bloating, tension and/or abdominal pain, burning, spasms, excessive belching or flatulence. All in all, these are particularly annoying symptoms that negatively affect the quality of life.

The causes of abdominal bloating can be numerous, including: an increase in the volume of the intestinal lumen due to the presence of gas, feces or liquids; a compromised abdominal evacuation; an increase in the tension of the abdominal muscles; or an amplification of intestinal stimuli.

Despite its clinical, social and economic importance, the pathophysiology of abdominal bloating is complex and not fully understood, so much so that no universally effective treatment is reported. The formation of gastrointestinal gases, in fact, depends on numerous factors and still today it is difficult to measure the excess of gas using modem diagnostic techniques.

The homeostasis of gastrointestinal gases depends on the balance between their formation and their elimination. Under physiological conditions, the production of gases is the result of: ingestion of air (0 ₂ and N ₂ ); chemical 5 reactions, such as the interaction between bicarbonate and acids that occurs in the stomach and produces enormous quantities of carbon dioxide (C0 ₂ ); processes of gaseous diffusion from the blood (C0 ₂ , N ₂ and 0 ₂ ); metabolism of bacteria (C0 ₂ , H ₂ , CH ₄ , and various traces of gases containing sulfur). The elimination of gastrointestinal gases can instead occur through belching, absorption, bacterial iu iciulcman n emu ev utauuu.

Many individuals complain of excess gastrointestinal gas. The presence of higher than normal levels of gastrointestinal gas can be caused by aerophagia, a functional disorder in which patients ingest air in disproportionate quantities, causing excessive entry of gas into the gastric lumen.

15 Gases in the intestine also originate from intraluminal production due to the metabolism of bacteria. In the intestine, in fact, the bacterial microflora plays an important role in the balance between the production and consumption of intestinal gases and can be considered another determining factor in the qualitative and quantitative production of gastrointestinal gases. The bacteria 0 present in the intestinal lumen, mainly in the colon, are responsible for the fermentation of non-digestible substrates deriving from the normal diet (starches, oligosaccharides, fibers) with the consequent release of hydrogen, carbon dioxide and methane.

The production of gas, both from a qualitative and quantitative point of view, 5 is determined by the quantity of metabolites that reach the intestinal lumen, mainly carbohydrates not completely absorbed in the small intestine. In fact, most of the carbohydrates ingested are polymers that have to be digested into simple sugars before being absorbed. The incomplete digestion of these substances and malabsorption in the intestine can lead to their accumulation in 0 the colon, where they act as a substrate for bacterial fermentation, resulting in the formation of excess gas.

Compositions already exist for the treatment of the presence of gas in the intestine, generally based on an anti-foaming agent. One disadvantage of existing compositions is that they act only on the symptoms and not on the phenomena at the origin of intestinal bloating.

For example, the excessive production of intestinal gases is very often due to the incomplete digestion and consequent malabsorption of some foods introduced with the diet. In persons with digestive difficulties, it may happen that these foods, in particular carbohydrates, are not adequately transformed by the enzymes of the organism. These substances, traveling through the digestive canal, are not absorbed and come into contact with the intestinal bacterial flora in the colon, where they are transformed by the bacteria with consequent overproduction of gas.

Another disadvantage lies in their formulation, commonly in the form of ingestible or dissolvable tablets. They require water to be used for swallowing, or they must remain in the mouth for a long time so that they dissolve.

The publication Arendt T. et al., 1998 describes the treatment of tympanites disturbances using a preparation combining rhizolipase and simethicone. The preparation is in the form of chewable gum. Simethicone is an anti-foaming agent that contains dimethicone (dimethylpolysiloxane) and silicon dioxide or silica gels and is also known as “activated dimethicone”.

The publication Auld J. M., 1979 describes the treatment of abdominal disorders attributable to gastrointestinal gas with a combination agent containing simethicone and pancreatin, which is a mixture of enzymes, mainly amylase, lipase and protease. The composition is in the form of a tablet.

GB 1 154 256 describes compositions of alkylpolysiloxane in tablet form, to aid digestion and prevent the formation of gas. This document describes the preparation of a tablet which contains aerosil, dimethylpolysiloxane, that is, dimethicone, and pancreatin.

DE 20 2008 015 430 U describes a composition for the treatment of tympanites, flatulence and excessive formation of gas comprising polysiloxane, in particular dimethicone or simethicone, and an enzyme, in particular protease.

US 2007/0020249 Al describes a composition for the prevention and treatment of symptoms of gastrointestinal disorders which comprises at least one probiotic organism, simethicone and at least one enzyme, for example alpha- galactosidase, protease (papain), glucanase, xylanase, pectinase and phytase. There is therefore a need to perfect a composition for the treatment of intestinal gas and bloating, and the corresponding formulation, 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 further reduce the

5 presence of gases in the intestine, also acting on the phenomena at their origin, thus preventing them from forming.

Another purpose of the present invention is to provide a formulation for the treatment of intestinal gas and bloating which is easy and quick for the patient to take.

Ϊ0 The Applicant has devised, tested and embodied fne 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.

15 The dependent claims describe other characteristics of the present invention or variants to the main inventive idea.

In accordance with the above purposes, the composition for the treatment of intestinal gas and bloating according to the present description comprises simethicone as an anti-foaming agent. The simethicone is responsible for the 0 mechanism of action, which is exerted through an exclusively physical action, thanks to the capacity to lower the surface tension at the interface between liquid and air.

In accordance with some embodiments, the composition comprises, in addition to simethicone, one or more digestive enzymes, preferably a mixture of digestive 5 enzymes.

The digestive enzymes help to improve the digestion of food (breaking it down into smaller elements that are easily absorbed by the intestine) thus counteracting the effects related to a possible malabsorption thereof, including the hyperproduction of gas following its fermentation. 0 Advantageously, the enzymes are selected from the group consisting of alpha- galactosidases, amylases, proteases, glucoamylases, lipases, cellulases, lactases and pectinases. Even more advantageously, the mixture of enzymes comprises all the enzymes of this group. Preferably, the composition also comprises at least one excipient intended to make the composition safer and/or more pleasant to take. Even more preferably, the composition comprises a plurality of excipients. These excipients can be substances with stabilizing, flavoring and/or acidifying activity.

Preferably, the composition also comprises at least one flavoring substance, and at least one sweetening substance.

Preferably, the composition can also comprise other excipients, such as for example a diluent agent, and/or an anti-agglomeration agent that makes the powder flow more easily.

According to one aspect, the composition is formulated in an orodispersible powder.

Preferably, the formulation is made available in single-dose sachets, for example of 2 grams each.

Advantageously, the single-dose sachets are made available in pouches containing a plurality of sachets, for example from 10 to 24 sachets.

According to another aspect, the invention concerns a container device, of the single-dose sachet type, comprising the composition for the treatment of intestinal gas and bloating as above, in the formulation as above.

Advantageously, the single-dose sachet has a substantially tubular shape, hermetically closed at both ends. Even more preferably, the sachet comprises a longitudinal closure that extends between its ends.

DETAILED DESCRIPTION OF SOME EMBODIMENTS

We will now refer in detail to the possible embodiments of the invention, of which one or more examples are shown in the attached drawings. Each example is supplied by way of illustration of the invention and shall not be understood as a limitation thereof. For example, one or more characteristics shown or described insomuch as they are part of one embodiment can be varied in, or adopted on, or in association with, other embodiments to produce other embodiments. It is understood that the present invention shall include all such modifications and variants.

Before describing these embodiments, we must also clarify that the present description is not limited in its application to details of the construction and disposition of the components as described in the following description using the attached drawings. The present description can provide other embodiments and can be obtained or executed in various other ways. We must also clarify that the phraseology and terminology used here is for the purposes of description only, and cannot be considered as limitative.

5 The composition for the treatment of intestinal gas and bloating comprises simethicone as an anti-foaming agent.

Simethicone is a silicone belonging to the family of polydimethylsiloxanes, characterized by a polymeric structure consisting of a succession of silicon and oxygen atoms (polydimethylsiloxane) mixed with silicon dioxide or a Si0 ₂ silica r\ - -U gci.

Simethicone is a hydrophobic ingredient that is stable at elevated temperatures, and comes as a colorless and odorless liquid. It is a physiologically inactive, non-toxic agent, particularly safe when administered orally. It is not absorbed by the gastrointestinal tract and does not interfere in any way5 whatsoever with the digestive processes.

The anti-foaming action is exerted through a physical mechanism of reduction of the surface tension of the gas bubbles present in the gastrointestinal tract. The mixture of polydimethylsiloxane and hydrophobic silica disperses on the surface of aqueous liquids, forming a low surface tension film that breaks easily. In this0 way, the gas contained in the bubbles present in the gastrointestinal tract is released and unites to form entities of larger sizes (coalescence) which are easily eliminated.

Preferably, the composition also comprises at least one digestive enzyme, supporting the main anti-foaming action carried out by simethicone, and which5 helps to improve the digestion of food, counteracting the effects related to a possible malabsorption thereof. In fact, it has been verified that the excessive production of intestinal gas is due, among other reasons, to the incomplete digestion and consequent malabsorption of some foods introduced with the diet. In subjects with digestive difficulties, it may happen that these foods, in0 particular carbohydrates, are not adequately transformed by the body’s enzymes. As they travel through the digestive tract, these substances are not absorbed and come into contact with the intestinal bacterial flora at colon level, where they are transformed by bacteria with consequent overproduction of gas. A reduction in fermentation at colon level can be achieved by administering digestive enzymes, which promote the breaking down of food introduced into the body through the diet into smaller elements easily absorbable in the small intestine. In this way, the quantity of fermentable substrate that reaches the colon is greatly reduced and consequently there is a reduction in the development of excess gas by the intestinal bacterial flora.

Preferably, the simethicone is present in proportions comprised between 1 and 20% by weight with respect to the total weight of the composition, preferably between 2 and 10%, more preferably between 3 and 7%, even more preferably between 3 and 5%.

Preferably, the composition comprises a mixture of digestive enzymes.

Even more preferably, the enzymes are selected from the group consisting of alpha-galactosidases, amylases, proteases, glucoamylases, lipases, cellulases, lactases and pectinases.

Advantageously, the composition for the treatment of intestinal gas and bloating comprises a mixture of all these digestive enzymes. In this way, the composition operates an optimal breaking down of the food present in the digestive system, since it is more complete.

It should be noted that the enzyme or mixture of enzymes is supplied possibly including its own excipients, such as for example maltodextrin or suchlike.

Preferably, the enzyme or mixture of enzymes is present in proportions comprised between 1 to 15% by weight with respect to the total weight of the composition, more preferably between 2 and 10%, even more preferably between 3 and 5%.

In accordance with some embodiments, in the composition of the present description, the sum of simethicone and enzyme or mixture of enzymes ranges from 2 to 35%, in particular from 4 to 20%, more particularly from 6 to 12% by weight with respect to the total weight of the composition.

The Applicant has therefore found that the presence of simethicone and of a mixture of enzymes which comprises alpha-galactosidases, amylases, proteases, glucoamylases, lipases, cellulases, lactases and pectinases, advantageously in the quantities indicated according to the various embodiments described here, allows to obtain a composition which surprisingly has a high efficacy for the treatment of intestinal gas and bloating.

Preferably, according to some embodiments, the composition described here is free of probiotic organisms.

Preferably, in addition to simethicone and the mixture of digestive enzymes, the composition can also comprise at least one excipient intended to make the composition safer and/or more pleasant to take. Even more preferably, the composition comprises a plurality of excipients, with different functionalities. These excipients can be substances with stabilizing, flavoring and/or acidifying activity At least one flavoring substance and/or at least one sweetening substance are advantageously added to the simethicone and to the mixture of digestive enzymes. These products are intended to improve the organoleptic properties of the composition, making it more pleasant to take for the user. One example of a sweetening substance is xylitol. For example, the sweetening substance is present between 8 and 12%, in particular between 9 and 11%, by weight with respect to the weight of the composition.

For example, the flavoring substances can be combined with flavor coadjuvant substances. For example, the flavoring substances can be such as to give a chocolate or citrus flavor. In particular, in the first case, the flavoring substances can comprise cocoa powder, a chocolate flavoring and a cream flavoring. In the second case, on the other hand, the flavoring substances can comprise an orange flavoring, a lemon and lime flavoring and citric acid. In these examples, therefore, the flavorings can be combined with flavor coadjuvant substances, such as in this specific case citric acid for the citrus flavor and cocoa powder for the chocolate and cream flavor.

Preferably, the composition can also comprise other excipients, such as for example a diluent agent, and/or an anti-agglomeration agent.

One example of a diluent agent is sorbitol. The diluent agent is intended to give the powder a volume suitable for it to be taken orally, in particular for it to be swallowed, and to promote its dissolution in saliva. For example, the diluent agent is present between 70 and 80% by weight with respect to the weight of the composition.

One example of an anti-agglomeration agent is silicon dioxide. This substance is intended to make the powders flow more easily and guarantee a correct distribution thereof during the production process. For example, the anti agglomeration agent is present between 2 and 5%, in particular between 3 and 4% by weight with respect to the weight of the composition.

According to one aspect of the invention, the formulation for the treatment of intestinal gas and bloating comprises the composition described above in the form of orodispersible powder. This formulation has the advantage of being ready for use. In addition, oral administration in particular of the digestive enzymes can be useful in controlling the production of gas with a reduction in the symptoms related to intestinal bloating, and in improving the quality of life of patients with functional disorders of the gastrointestinal tract, such as irritable bowel syndrome. Furthermore, with such formulation, using the composition does not require particular skills, it is therefore not required that a professional operator administer it, and it can be used autonomously by the informed patient in his/her home. Furthermore, such a formulation is more convenient to take compared to known tablets, since it does not require water for its ingestion and does not have to be kept in the mouth for a certain amount of time in order for it to dissolve.

Alternatively, the composition can be formulated in the form of a powder that is soluble or dispersible in water, or in a liquid form.

Preferably, the formulation is made available in single-dose sachets. This packaging allows the user to carry the composition in question with him/her, and to take it at any time of the day and in any place whatsoever, not necessarily at his/her home. The single doses of composition are for example of 2 grams each, but others are possible according to requirements and/or the applied dosages. Preferably, the sachets are hermetically closed so as to prevent the orodispersible powder from coming into contact with external humidity.

It is also possible to provide that the formulation is conditioned in multi-dose sachets.

Preferably, the single-dose sachet has a substantially tubular shape, hermetically closed at both ends. Even more preferably, the sachet comprises a longitudinal closure that extends between its ends. This packaging is known as a stick pack. However, it is possible to provide a sachet of any other type whatsoever that is able to enclose the formulation in a hermetic manner, for example with the four sides sealed, possibly equipped with a delivery tube (particularly suitable when the composition is in liquid form).

Advantageously, the single-dose sachets are made available in pouches containing a plurality of sachets, for example 10, 12, 18, 20 or 24 sachets. Advantageously, an instruction manual on how to take and preserve the composition in question is also supplied in the pouch.

According to another aspect of the invention, the formulation of the invention has to be taken during or after each of the three main daily meals.

Two alternative examples of composition according to the invention are presented below.

Example 1

The first example of composition has a chocolate flavor. The composition is as follows (the percentages are to be understood by weight with respect to the total weight of the composition):

Example 2

The second example of composition has a citrus flavor. The composition is as follows (the percentages are to be understood by weight with respect to the total weight of the composition):

Example 3

The third example of composition has a chocolate flavor. The composition is as follows (the percentages are to be understood by weight with respect to the total weight of the composition): Example 4

The fourth example of composition has a citrus flavor. The composition is as follows (the percentages are to be understood by weight with respect to the total weight of the composition):

It should be noted that the citric acid, for example present in the formulations of examples 2 and 4 as above, strengthens the citrus flavor in order to improve the organoleptic properties of the product, and consequently the pleasantness for the user. The cocoa powder in examples 1 and 3 can perform a similar function, strengthening the chocolate and cream flavor.

In the examples above, the enzyme mixture can include its own excipients, such as for example maltodextrin or suchlike.

It is dear that modifications and/or additions of ingredients may be made to the composition for the treatment of intestinal gas and bloating and to the corresponding formulation as described heretofore, without departing from the field and scope of the present invention as defined by the claims. In particular, with reference to the two examples above, the proportions of simethicone and digestive enzymes can vary, even significantly.

It is also clear that, although the present invention has been described with reference to some specific examples, a person of skill in the art shall certainly be able to achieve many other equivalent forms of composition for the treatment of intestinal gas and bloating, having the characteristics as set forth in the claims and hence all coming within the field of protection defined thereby.