Formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases

Abstract

A formulation is provided for the reduction of inflammation due to gastric disorders, injuries, or diseases comprising one or more phenylethanoid glycosides.

Description

[0001] DESCRI PTION

[0002] FORMULATION FOR THE REDUCTION OF INFLAMMATION DUE TO GASTRIC DISORDERS, INJURIES, OR DISEASES

[0003] The present invention relates to a formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases, as specified in the preamble of the first claim.

[0004] In particular, the present invention targets inflammation caused by gastroesophageal reflux or injuries to gastric mucosa, such as ulcers, or other inflammations that may result from conditions affecting the gastric apparatus.

[0005] As known, gastroesophageal reflux is a condition where gastric juices from the stomach flow back into the esophagus.

[0006] Normally, the muscle at the base of the esophagus, called the lower esophageal sphincter, closes after food passes into the stomach, preventing the food and gastric acids from moving back up into the esophagus. However, in cases of malfunction of this muscle or excessive abdominal pressure, for example, due to pregnancy or obesity, gastric content may reflux upwards, causing unpleasant symptoms.

[0007] Common symptoms of gastroesophageal reflux include heartburn, acidic regurgitation manifesting as a sensation of acidic liquid rising in the throat, chest pain, chronic cough, hoarseness, and difficulty swallowing, and overproduction of mucus in the upper airways.

[0008] In some cases, chronic reflux can cause damage to the esophagus, such as inflammation, ulcers, or esophagitis.

[0009] The causes of reflux may vary and include factors such as poor dietary habits, obesity, pregnancy, certain diseases like hiatal hernia, some drugs, and smoking.

[0010] Lifestyle changes, such as dietary modifications, avoiding large meals before bedtime, weight loss if necessary, and avoiding foods that trigger symptoms, can help manage reflux.

[0011] For this purpose, international guidelines provide for the use of drugs to reduce gastric acid production for a period not exceeding two months. Specifically, conventional drugs include proton pump inhibitors or prokinetic drugs. Alternatively, for severe or chronic reflux, international guidelines recommend surgical interventions to resolve the problem.

[0012] In chronic inflammation, the biochemical mechanism involved is similar to that of acute inflammation but differs in its persistence and prolonged activation of the immune system over time.

[0013] This process can lead to sustained tissue damage and progression of various pathological conditions.

[0014] Some key aspects of the biochemical mechanism of chronic inflammation include, for example, the persistent activation of the immune system. In this sense unlike acute inflammation, chronic inflammation is characterized by the prolonged and sustained activation of the immune system, often without a clear signal to terminate the inflammatory response.

[0015] Additionally, chronic inflammation may manifest as continuous release of inflammatory mediators, therefore the immune system cells such as macrophages and lymphocytes continue to release cytokines, interleukins, prostaglandins, and other inflammatory mediators into the inflamed tissue.

[0016] Constant exposure to inflammatory mediators can therefore lead to persistent tissue damage, as immune cells may harm healthy surrounding tissues while attempting to combat the inflammation. Moreover, connective tissue cells may become involved in the process, producing excess collagen and leading to scar formation or fibrotic tissue.

[0017] In some cases, chronic inflammation may be associated with autoimmune diseases, where the immune system mistakenly attacks healthy tissues, keeping the inflammation active. This can also exacerbate other chronic diseases, such as rheumatoid arthritis, Crohn's disease, ulcerative colitis, heart diseases, and other conditions.

[0018] The known technique described has several important drawbacks.

[0019] Specifically, the drugs used to reduce inflammation act solely on gastric acid production or selectively stimulate intestinal motor function.

[0020] Furthermore, traditional anti-inflammatory drugs, whether NSAIDs or corticosteroids, are gastrolesive and cannot be used for these purposes.

[0021] Thus, drugs, rather than addressing the inflammation directly, aim to circumvent or limit the factors generating the very inflammation.

[0022] Consequently, none of the drugs can directly interfere with the inflammatory cascade.

[0023] In this context, the technical task underlying the present invention is to devise a formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases capable of substantially overcoming at least part of the cited drawbacks.

[0024] Within this technical task, an important object of the invention is to obtain a formulation for reducing inflammation due to gastric disorders, injuries or diseases which is capable of modulating, at a molecular level, the pathway of the inflammatory cascade.

[0025] Therefore, another object of the invention is to directly target the inflammation.

[0026] In conclusion, another task of the invention is to reduce the likelihood of the growth of chronic, cellular, or basal inflammations. The technical task and the specified objects are achieved by a formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases as claimed in the appended Claim 1 .

[0027] Preferred technical solutions are highlighted in the dependent claims.

[0028] In the present document, measurements, values, shapes, and geometric references (such as perpendicularity and parallelism), when associated with words like "approximately" or similar terms such as "substantially" or "essentially", are to be understood as allowing for measurement errors or inaccuracies due to production and / or manufacturing errors and, above all, to allow for a slight deviation from the value, measure, shape, or geometric reference with which it is associated.

[0029] For example, such terms, when associated with a value, preferably indicate a deviation not exceeding 10% of the value itself.

[0030] Additionally, terms like "first", "second", "upper", "lower", "primary", and "secondary", unless otherwise specified, do not necessarily identify an order, a priority of relation, or relative position but may simply be used to distinguish different components more clearly one from the other.

[0031] Unless otherwise specified, as evident from the following discussions, terms such as "treatment", "computing", "determination", "computation", or similar refer to the action and / or processes of a computer or similar electronic computation device that manipulates and / or transforms data represented as physical quantities, such as electronic magnitudes of records of a computing system and / or memories, into other data similarly represented as physical quantities within computer systems, records, or other information storage, transmission, or display devices.

[0032] Unless otherwise indicated, the measurements and data reported in this text are to be considered as performed in International Standard Atmosphere ICAO (ISO 2533:1975).

[0033] The formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases broadly comprises one or more phenylethanoid glycosides.

[0034] Phenylethanoid glycosides, also referred to by the acronym PhGs, are a class of water-soluble natural products widely distributed in the plant kingdom, many of which are isolated from medicinal plants.

[0035] They schematically include at least one sugar moiety and two functional groups ester-linked to the hydroxyls of the sugars. The functional groups are preferably caffeic acid and / or hydroxytyrosol.

[0036] In particular, the phenylethanoid glycosides present in the formulation may include one or more of Oleuropein, Verbascoside, Echinacoside, Lamiuside-A, Ligustroside, Forsythoside, Plantamaioside, and Cystanoside.

[0037] More specifically, the phenylethanoid glycosides may include or consist of at least Verbascoside from the family Verbenaceae or Orobanchaceae and Lamiuside-A from the family Lamiaceae.

[0038] If the phenylethanoid glycosides in the formulation include Verbascoside and Lamiuside-A, the latter are preferably present in the formulation in a reciprocal ratio of between 7 and 8, for example, between 7.3 and 7.7, more specifically 7.5.

[0039] In a formulation where Verbascoside is present in an amount of approximately 22.5 mg, Lamiuside-A may be present in an amount of approximately 3 mg.

[0040] In a preferred, but not exclusive, embodiment, the formulation further includes a plant extract.

[0041] If present, the plant extract preferably includes Mucilages. More specifically, the plant extract is rich in Mucilages and therefore predominantly consists of Mucilages, preferably in amounts exceeding 50% of the total plant extract, more specifically, for example, exceeding 60%, and even more preferably exceeding 70%.

[0042] The plant extract could also essentially consist of Mucilages.

[0043] Moreover, the Mucilages are preferably Mucilages derived from the family Malvaceae.

[0044] Naturally, in the preferred embodiment of the formulation, wherein both phenylethanoid glycosides and plant extracts are present, the latter may be present in specific proportions.

[0045] For instance, phenylethanoid glycosides and plant extracts are present in a reciprocal ratio of between 1.6 and 2.6 in the formulation. More specifically, phenylethanoid glycosides and plant extracts may be present in a reciprocal ratio of between 1.9 and 2.3 in the formulation. Appropriately, phenylethanoid glycosides and plant extracts could be present in a reciprocal ratio of 2.1 in the formulation.

[0046] In a preferred embodiment of the formulation, the phenylethanoid glycosides include Verbascoside in an amount of approximately 22.5 mg and Lamiuside-A in an amount of approximately 3 mg, additionally, the plant extract includes Mucilages in an amount of approximately 12 mg.

[0047] Naturally, the formulation could consist of Verbascoside, Lamiuside-A, and Mucilages in the specified amounts.

[0048] The formulation may further be in solid, liquid, or gel form.

[0049] For instance, according to the above the formulation may be in the form of an orosoluble tablet. Alternatively, the formulation may be in other forms, preferably any protected ingestion form, such as sachets, soft-gels, lozenges, or other forms.

[0050] In conclusion, the formulation enables the creation of a novel food supplement or even a new pharmaceutical product. In this sense, the food supplement or pharmaceutical product comprises at least the formulation as previously described, but may also include other active ingredients or components.

[0051] The formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases according to the invention achieves significant advantages.

[0052] Indeed, the formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases allows for the molecular-level modulation of the inflammatory cascade pathway.

[0053] Specifically, the phenylethanoid glycosides exhibit various biochemical activities, including the modulation of TNF-alpha and NFkB-mediated inflammatory cascade pathways.

[0054] Additionally, in the preferred embodiment of the invention, the presence of a plant extract rich in Mucilages enables reduced transit time through the digestive tract for the ingested product and provides more effective topical action on damaged membranes.

[0055] Therefore, in general, the formulation for the reduction of inflammation due to gastric disorders, injuries, or diseases is effective in directly interfering with inflammation and is therefore particularly suited for therapies addressing chronic gastric conditions.

[0056] The invention is susceptible to variations falling within the scope of the inventive concept defined by the claims.

[0057] Within this scope, all details can be replaced by equivalent elements, and the materials, shapes, and dimensions can be any.

Claims

C LA I M S1. Formulation for use in the reduction of inflammation due to gastric disorders, injuries, or diseases, characterised by comprising one or more phenylethanoid glycosides.

2. Formulation according to claim 1 , wherein said phenylethanoid glycosides comprise one or more of Oleuropein, Verbascoside, Echinacoside, Lamiuside-A, Ligustroside, Forsythoside, Plantamaioside, and Cystanoside.

3. Formulation according to the preceding claim, wherein said phenylethanoid glycosides comprise at least Verbascoside from the family Verbenaceae or Orobanchaceae and Lamiuside-A from the family Lamiaceae.

4. Formulation according to the preceding claim, wherein said Verbascoside and said Lamiuside-A are present in a reciprocal ratio of between 7 and 8 in said formulation.

5. Formulation according to any preceding claim, further comprising a plant extract.

6. Formulation according to the preceding claim, wherein said plant extract comprises Mucilages from the family Malvaceae.

7. Formulation according to any one of claims 5-6, wherein said phenylethanoid glycosides and said plant extract are present in a reciprocal ratio of between 1 .6 and 2.6 in said formulation.

8. The formulation according to any preceding claim, in solid, liquid, or gel form.

9. Formulation according to the preceding claim, in the form of an orosoluble tablet.

10. Food supplement comprising a formulation according to any preceding claim.