ES2631137A1 - Use of an aqueous composition comprising nacl, aloe and chamomile for the treatment and/or prevention of nasal congestion (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Use of an aqueous composition comprising nacl, aloe and chamomile for the treatment and/or prevention of nasal congestion. The present invention provides the use of an aqueous composition comprising: (I) from 0.5 to 3% by weight of nacl, (II) from 0.1 to 1% by weight of aloe vera extract, and (III) from 0.5 to 5% by weight of chamomile extract, for the preparation of a medicament for the prevention and/or treatment of nasal congestion. The compositions may also contain mint. The invention also provides the compositions described above for nasal lavage. (Machine-translation by Google Translate, not legally binding)

Description

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DESCRIPTION

Use of an aqueous composition comprising NaCI, Aloe and chamomile for the treatment and / or prevention of nasal congestion

The present invention relates to the field of sanitary products for nasal hygiene, prevention and treatment of nasal congestion. More specifically, it refers to new compositions with decongestant effect.

STATE OF THE TECHNIQUE

The nose constitutes the entrance door of the air to the upper respiratory tract. The nasal mucosa (inner part of the nose) filters the inspired air in order to eliminate dust, germs and any irritating particles it may contain. Subsequently, it heats and moistens to prevent the lungs and the tubes that lead to them from drying out. Also the nose contributes to smell and taste. Occasionally, changes in atmospheric conditions (temperature and pressure) as well as exposure to infectious agents, irritants and allergens produces an inflammatory response in the mucosa of the nostrils and sinuses. When this inflammation occurs it gives rise to rhinosinusitis. Rhinosinusitis is characterized by a hypersecretion of mucus and nasal obstruction (congestion or rhinorrhea), which makes breathing difficult causing great discomfort and complications such as headaches and ears. The persistence of nasal congestion may also favor infection by pathogens leading to bronchitis, otitis or even pneumoma.

Proper nasal cleaning is beneficial to free the nasal cavities of contaminating particles, viruses, bacteria and other impurities that can cause inflammation of the mucosa, thus preventing nasal congestion and its complications. When congestion is already evident, it should be eliminated by an indicated treatment. In this regard, several medications have been proposed for the treatment of nasal passages. In general, these medications contain an alpha stimulant or vasoconstrictor such as ephedrine, NeoSynephrine (phenylephrine hydrochloride) or Afrin (oxymetazoline hydrochloride) can be used as a decongestant. But such medications have several possible side effects, such as atrophy of the nasal mucous membranes, increased blood pressure, cardiac irregularities and effect

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rebound, so prolonged use is not generally advised. Another treatment consists in the local administration of preparations containing essential oils and / or aromatic terpenic derivatives. Its local decongestant action, however, is not scientifically well established and its use, alone or in combination, can become dangerous to health due to the risk of causing local irritations or problems of the central nervous system. This risk increases when these preparations contain alcohol, even in low proportions, or antiseptic substances that can be irritating to nasal mucous membranes. Babies, young children or the elderly are particularly exposed to all these risks

On the other hand, seawater has traditionally been used to rinse the nasal passage, as part of a treatment for rhinosinusitis problems. But sea water alone has no decongestant effect and its use in nasal cleaning or irrigation is also associated with significant discomfort.

In view of the above, it is clear that it is necessary to provide new strategies for proper nasal hygiene, as well as to prevent and cure nasal congestion, which does not suffer from the aforementioned disadvantages.

EXPLANATION OF THE INVENTION

The inventors have designed new decongestant compositions that have advantages in terms of effectiveness and comfort, while not presenting harmful side effects. These compositions comprise natural ingredients, in particular, sea water, Aloe vera extract and chamomile extract, which makes them very suitable for use in susceptible population groups, such as children, the elderly or pregnant women.

Thus, a first aspect of the invention relates to an aqueous composition comprising: (i) from 0.5 to 3% by weight of NaCl; (ii) from 0.1 to 1% by weight of Aloe vera extract; and (iii) from 0.5 to 5% by weight of chamomile extract, for use in the prevention and / or treatment of nasal congestion. This aspect can be reformulated as the use of a composition comprising: (i) from 0.5 to 3% by weight of NaCl; (ii) from 0.1 to 1% by weight of Aloe vera extract; and (iii) from 0.5 to 5% by weight of chamomile extract, for the preparation of a medicine for prevention and / or

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Treatment of nasal congestion. The invention also relates to a method for the prevention and / or treatment of nasal congestion comprising the administration of an aqueous composition comprising: (i) from 0.5 to 3% by weight of NaCl; (ii) from 0.1 to 1% by weight of Aloe vera extract; and (iii) 0.5 to 5% by weight of chamomile extract.

The concentrations of the ingredients of the compositions according to the invention always refer to percentages by weight over the total weight of the aqueous composition (ie,% weight, which is also expressed as% w / w).

Together, the components (NaCl, Aloe vera extract and chamomile extract) of the composition designed by the inventors provide a greater decongestant effect while constituting an ideal means for nasal cleaning and hygiene. In a particular embodiment the decongestant composition according to the invention is also suitable for nasal lavage. Nasal lavage (or nasal irrigation), is the personal hygienic practice in which the nasal cavity is washed to remove dirt and excess mucus from the nose and sinuses. Nasal irrigation in a broader sense may also refer to the use of a saline nasal spray or nebulizers to moisten the mucous membranes and exert a decongestant and washing effect. Nasal lavage (or irrigation) is very important to relieve the discomfort of congestion and also to prevent congestion, since allergen, infectious or irritating residues that can cause it are removed from the nostrils. Therefore the composition according to the invention is also useful for nasal hygiene. The composition according to the invention is also useful for nasal irrigation.

For both uses (decongestion and nasal washing or irrigation), the composition according to the invention has the advantage that it provides a moisturizing effect and its application is more pleasant for the user. In addition, the composition, based on purely natural elements, has a high level of safety, without adverse effects, is environmentally friendly and suitable for use in risk patients such as pregnant women, children or the elderly. All the foregoing also allows the composition according to the invention to be used for longer periods compared to other compositions known in the state of the art without general discomfort, rebound effect or addictive behaviors. Additionally, the

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Synergies established between the components of the invention provide a greater decongestant effect and greater well-being for the user.

In the present application the term "extract" is used in the conventional sense to refer to concentrated preparations of compounds obtained by extracting the active constituents from the source, usually a botanical source, with suitable means. Such extracts contain one or more active ingredients and can be incorporated into pharmaceutical or cosmetic compositions in a variety of ways, including a pure or semi-pure component, a solid or liquid extract, or a solid plant material.

In general, botanical extracts contain not only one, but multiple components, many of them active. Sometimes, the beneficial effect is derived from the combination of many of these active components. In other cases there is a particular component that is primarily responsible for most of the activity.

The term "extract" as used herein also includes "synthetic" extracts, that is, several combinations of known components and / or components that combine to substantially mimic the composition and / or activity of a botanical extract of natural origin. Synthetic extracts will have two or more, three or more, or four or more active ingredients in common with that of the natural source. Natural or synthetic extracts that are enriched in one or more components are also considered part of the present invention.

Aloe vera (also known as sabila, Barbados aloe or Curacao aloe, among others) is a succulent plant that comes from hot and desert sites, although it has adapted to a wide variety of temperate climates. The most used are the leaves, each composed of three layers. The inner layer is a transparent gel that contains a high amount of water and active compounds such as polysaccharides glucosides, enzymes and minerals that are responsible for many of the properties of this plant. The intermediate layer or latex is a bitter yellow sap that contains anthraquinones and laxative glucosides. The thick outer layer, called the cortex, has the function of protection and synthesis of carbohydrates and proteins. In general, the healing properties of Aloe vera are known since ancient times and their use

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in topical compositions it is common for its antipruritic, healing, antiseptic, antioxidant, anti-inflammatory and moisturizing effect. However, its use in contraceptive and nasal hygiene compositions has not been described to date.

Aloe vera extract is the extract obtained from the leaves of this plant. The procedures for obtaining said extract are known in the state of the art. The processes adapted to the pharmaceutical, cosmetic and food industry eliminate the irritating components that can be contained in Aloe vera leaves. These extracts may be derived from Aloe Vera gel, latex, or both. The compositions according to the present invention may contain Aloe Vera extract containing the components of the gel, latex or both, but preferably the extract is derived from the gel and contains a high proportion of polysaccharides. Any of the varieties of Aloe vera extract are easily available through commercial suppliers.

The pure Aloe Vera gel extract consists of approximately 95% water and 5% active components. Mucilaginous polysaccharides are the active ingredients responsible for the biological activity of Aloe Vera gel and among them, acemanan is the most relevant. The remaining solids that make up the Aloe vera gel, and which can also contribute to its therapeutic activity, are organic salts and acids (glutamic, malico, salicylic, dtrico, magnesium lactate, calcium oxalate), enzymes (cellulase, carboxypeptidase, bradykininase, catalase, amylase, oxidase, tyrosinase), tannins, sterols, triglycerides, amino acids (lysine, histidine, glutamine, arginine, aspartic acid, asparagine, threonine, serine, glutamic acid, glycine, alanine, valine, methionine, isoleucine, leucine, leucine , phenylalanine and tryptophan), RNA and traces of alkaloids, of vitamins (beta-carotene, B1, B2, B3, B6, C, E, choline, folic acid) and minerals (aluminum, boron, barium, calcium, chromium, copper, iron, potassium, magnesium, sodium, phosphorus, strontium, silicon). The pure extract of Aloe Vera gel can be concentrated and filtered to remove water and increase the proportion of active agents. The Aloe vera extract used in the compositions according to the present invention is preferably a substantially pure liquid gel (> 95% pure aloe vera gel). These liquid gel extracts may contain a dry extract of aloe between 1 and 5%.

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Chamomile or chamomile is the common name of several daisy-like plants of the Asteraceae family that are normally used to infuse herbs to serve various medicinal purposes. Relevant active compounds present in chamomile include apigenin and alpha-bisabolol. It also contains sesquiterpenes, terpenoids, flavonoids, coumarins such as herniarine and umbelliferone, phenylpropanoids such as chlorogenic acid and caffeic acid, flavones such as apigenin and luteolin, flavanols such as quercetin and rutin, and polyacetylenes.

Chamomile extract can be obtained by procedures known in the state of the art or through commercial suppliers. The extract is preferably liquid extract. These liquid extracts may contain a dry chamomile extract between 1 and 5%.

The sodium chloride of the composition according to the invention can come from various sources. For example, you can add: pure NaCl, concentrated sea water or purified water. All these sources of NaCl are accessible through commercial suppliers. In particular, the NaCl of the composition of the invention can be provided by the addition to the concentrated seawater composition or by the addition of concentrated seawater and purified water. In this case, the composition also contains other salts and elements that may contribute to the decongestant effect and / or proper nasal hygiene.

In a particular embodiment, the composition according to the invention comprises: (i) from 0.7 to 2.8% by weight of NaCl; (ii) from 0.3 to 0.8% by weight of Aloe vera extract; and (iii) from 0.8 to 3.5% by weight of chamomile extract.

In some particular embodiments the composition according to the invention also contains mint. In one embodiment the mint is peppermint. Peppermint is a sterile hybrid obtained from the crossing of aquatic mint (mentha aquatica) and peppermint (mentha spicata), which occasionally occurs spontaneously in temperate regions of Europe. The main active components of peppermint include essential oils (containing terpenes, mainly menthol, neomenthol, isomenthol, neoisomenthol, piperitols, piperitenol, isopiperitenol) and flavonoids (diosmoside, diosmetoside, eriocytroside, luteolol 7 rutoside,

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hesperidoside). In a realization the composition contains mint aroma. Peppermint aroma can be obtained by procedures known in the state of the art or through commercial suppliers. The mint aroma is preferably a liquid mint extract. In a particular embodiment, the mint aroma concentration is 0.005 to 0.05% by weight, or 0.01 to 0.02% by weight, for example 0.015% by weight. In another particular embodiment, the composition contains menthol or some of its stereoisomers instead of the mint extract or aroma.

The composition for the prevention or treatment of nasal congestion according to the invention may be isotonic or hypertonic depending on the concentration of NaCl it contains. In one embodiment the composition contains 2 to 3% by weight of NaCl and, therefore, is hypertonic. In a particular embodiment the composition contains from 2.2 to 2.8% by weight of NaCl, more particularly 2.5% by weight of NaCl. The hypertonic compositions of the invention provide the advantage of exerting a decongestant effect without causing side effects. In another embodiment, the composition contains 0.5 to 1.5% by weight of NaCl and is therefore isotonic. In another particular embodiment the composition contains 0.7 to 1.1% by weight of NaCl, particularly 0.9% by weight of NaCl. The isotonic solutions of the invention are effective in preventing congestion and are preferable for use in babies.

In one embodiment, the composition according to the invention comprises (i) from 2 to 3% by weight of NaCl; (ii) from 0.3 to 0.8% by weight of Aloe vera extract; (iii) from 0.8 to 3.5% by weight of chamomile extract and from 0.005 to 0.05% of peppermint aroma. In a particular embodiment, the composition comprises (i) from 2.2 to 2.8% by weight of NaCl; (ii) from 0.4 to 0.6% by weight of Aloe vera extract; (iii) from 1.5 to 2.5% by weight of chamomile extract and from 0.01 to 0.02% of peppermint aroma. In another particular embodiment, the composition comprises (i) 2.5% by weight of NaCl; (ii) 0.5% by weight of Aloe vera extract; (iii) 2% by weight of chamomile extract and 0.015% of mint aroma.

In one embodiment, the composition according to the invention comprises (i) from 0.5 to 1.5% by weight of NaCl; (ii) from 0.3 to 0.8% by weight of Aloe vera extract; (iii) from 0.8 to 3.5% by weight of chamomile extract and from 0.005 to 0.05% of peppermint aroma. In a particular embodiment, the composition comprises (i) from 0.7 to 1.1% by weight of NaCl; (ii) from 0.4 to 0.6% by weight of Aloe vera extract; (iii) from 1.5 to 2.5%

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by weight of chamomile extract and 0.01 to 0.02% peppermint aroma. In another particular embodiment, the composition comprises (i) 0.9% by weight of NaCl; (ii) 0.5% by weight of Aloe vera extract; (iii) 2% by weight of chamomile extract and 0.015% of mint aroma.

The compositions defined above of the present invention may have a liquid or thick consistency until semi-solid. As an example, the composition according to the invention can be presented as a liquid, ointment, cream or gel to be applied to the nose or as a solution or dispersion for dripping or sprinkling in the nose.

As a vehicle for liquid administration forms, mainly aqueous systems are suitable. As vehicles for thick or semi-solid preparations such as ointments, creams or gels, paraffin hydrocarbons, petrolatum, lanolin products and other base materials, which increase viscosity and can be used in pharmacy are suitable, for example; in the case of hydrophilic gels, for example water, glycerin or sorbitol, which gel with suitable swelling agents, such as poly (acrylic acids), cellulose derivatives, starch or tragacanth. Mainly in the case of compositions containing salt, the thickening is selected so that it can be largely prevented from flowing into the pharynx cavity.

The preparation according to the invention may also contain, in addition to the active substances and vehicles, other pharmaceutical adjuvants and / or additives compatible with the active ingredients, such as: fillers, solvents, diluents, binders, humectants, stabilizers, colorants, flavorings, preservatives, propellant agents, buffers, etc.

In a particular embodiment, the composition according to the invention contains propylene glycol. The concentration of propylene glycol in the composition can be from 0.5 to 5% by weight, or from 1 to 3% by weight. In a particular embodiment the composition according to the invention comprises 2% propylene glycol.

The present invention also provides an aqueous composition for the prevention and / or treatment of nasal congestion and / or for nasal lavage that is

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characterized by the absence of excipients. In a particular embodiment, therefore, the invention provides an aqueous composition for the prevention and / or treatment of nasal congestion and / or for nasal lavage consisting of: (i) from 0.5 to 3% by weight of NaCl ; (ii) from 0.1 to 1% by weight of Aloe vera extract, and (iii) from 0.5 to 5% by weight of chamomile extract. In another embodiment the invention provides an aqueous composition for the prevention and / or treatment of nasal congestion and / or for nasal lavage consisting of: (i) from 0.5 to 3% by weight of NaCl; (ii) from 0.1 to 1% by weight of Aloe vera extract, (iii) from 0.5 to 5% by weight of chamomile extract and mint or menthol aroma. When the composition contains mint aroma, its concentration is 0.005 to 0.05% by weight.

In a preferred embodiment the composition of the invention is for intranasal administration, preferably in the form of a nasal spray or nasal spray. The invention also provides a nasal spray or nasal nebulizer comprising the composition according to the invention.

Nasal congestion may be caused by various conditions, either infectious, allergic processes, polyps, etc. These include: common cold (cold), flu, sinus infection, allergic rhinitis or other allergies, polyps and vasomotor rhinitis. In a particular embodiment, the compositions described above are for use in the prevention and / or treatment of common cold (flu), flu, sinus infection, allergic rhinitis, polyps and vasomotor rhinitis.

Throughout the description and claims the word "comprises" and its variants are not intended to exclude other technical characteristics, additives, components or steps. In addition, the word "understand" includes the case "consists of". For those skilled in the art, other objects, advantages and characteristics of the invention will be derived partly from the description and partly from the practice of the invention. The following examples are provided by way of illustration, and are not intended to be limiting of the present invention. In addition, the present invention covers all possible combinations of particular and preferred embodiments indicated herein.

EXAMPLES

Decongestant compositions for nasal spray or nasal spray.

The following compositions have been formulated:

Table 1. Compositions for nasal spray

 component

 Units (g) Units (g)% (w / w) of the total

 Sea water 1

 23.4375 93.75 78,125

 Purified water

 5,208 20,832 17.36

 Chamomile extract

 0.6 2.4 2

 Propylene glycol

 0.6 2.4 2

 Aloe Vera Extract

 0.15 0.6 0.5

 Mint Aroma

 0.0045 0.018 0.015

 TOTAL

 30.0 120.0 100

5 (1) The concentration of NaCl provided by seawater is 2.5% (solution

hypertonic)

The compositions were administered in the form of a nasal spray to a panel of users, their acceptance among users being greater than similar products available in the market.

Excerpts

The extracts used in the elaboration of the compositions of table 1 were the following:

a) Aloe vera extract. The aloe extract used was 71010 ALOVERIA® (CAS No. 902 760 000). This extract is a transparent liquid gel obtained directly from fresh leaves of the plant. It contains 99.6% pure Aloe Vera gel and 20 excipients (sodium benzoate, ascorbic acid, sodium bisulfite and potassium sorbate. Table 2 contains more information on this extract, including its composition (non-exhaustive list).

Table 2. 71010 ALOVERIA®

 Dry extract

 1.5 -2.5%

 pH

 4.5-5.5

 Density

 0.980 -1.020 g / ml

 Composition

 Polysaccharides> 0.2 g

 Acemanan> 0.1 g

 Raw fiber> 0.05 g

 Essential amino acids> 35 ppm

 Protemes> 0.18 g

 fat <0.12

 Anthraquinones (barbaloin) <2 ppm

b) Chamomile extract. The chamomile extract used was obtained from the company Genox Farma. It is a Kquido extract of flowers of Matricaria chamomilla L obtained by percolation by mixing alcohol and water. Table 3-5 contains more information about this extract.

Table 3. Chamomile extract (Genox Farma)

 Dry extract

 2.0-4.0%

 pH

 4.0-7.0

 Density

 0.980-0.995 g / ml

 alcohol

 23-27 °

 Water

 69-75%

c) Mint aroma. The mint aroma used was obtained from the company IFF 10 (AROMA MENTA LIQ SC397979 MP061). Table 4 contains more information about this product.

Table 4. AROMA MENTA LIQ SC397979 MP061

 Consistency

 liquid

 Density

 0.890-0.910 g / ml

 refraction index ND20

 1,450 -1,470

 Specific gravity D25 / 25 ° C

 0.869 - 0.909

 Flash point

 73 ° C

Claims (15)

5 10 fifteen twenty 25 30 1. Use of an aqueous composition comprising: (i) 0.5 to 3% by weight of NaCl (ii) from 0.1 to 1% by weight of Aloe vera extract, and (iii) 0.5 to 5% by weight of chamomile extract for the preparation of a medication for the prevention and / or treatment of nasal congestion. 2. Use according to claim 1, wherein the composition is also for nasal lavage. 3. Use according to any of claims 1-2, wherein the extracts are liquid extracts. 4. Use according to any of claims 1-3, wherein the composition further comprises mint. 5. Use according to claim 4, wherein the composition contains mint aroma at a concentration of 0.005 to 0.05% by weight. 6. Use according to any of claims 1-5, wherein the composition comprises: (i) from 0.7 to 2.8% by weight of NaCl (ii) from 0.3 to 0.8% by weight of Aloe vera extract, and (iii) from 0.8 to 3.5% by weight of chamomile extract. 7. Use according to any of claims 1-6, wherein the composition contains from 0.7 to 1.1% by weight of NaCl. 8. Use according to any of claims 1-6, wherein the composition contains from 2.2 to 2.8% by weight of NaCl. 9. Use according to claim 8, wherein the composition also comprises 0.01 to 0.02% by weight of mint aroma. 10. Use according to any of claims 1-9, wherein the composition is characterized by the absence of excipients. 11. Use according to any of claims 1-9, wherein the composition also comprises pharmaceutically acceptable excipients and / or vehicles. 12. Use according to claim 11, wherein the composition contains propylene glycol. 13. Use according to claim 12, wherein the concentration of propylene glycol is 0.5 to 5% by weight. 14. Use according to any of claims 1-13, wherein the composition is administered as a nasal spray or nasal spray. 15. Use according to any of claims 1-14, wherein the nasal congestion It is caused by a common cold (cold), flu, sinus infection, allergic rhinitis, polyps or vasomotor rhinitis. 16. Nasal spray or nasal nebulizer comprising the composition as defined in any of claims 1, 3-14.