KR20110056526A - Antihistamine and antihistamine-like nasal application, products, and method - Google Patents

Abstract

A method and product for applying to the nasal area or nasal cavity of a human to reduce the undesirable effects of allergic rhinitis. The formulations form a barrier that prevents airborne allergens from contacting the nasal mucosa, while at the same time electrostatically pushing, adsorbing and trapping particulate allergens and changing their shape to mitigate the effects of allergic rhinitis. The formulation is. It may be more effective by adding an antihistamine compound.

Description

Antihistamine and antihistamine-like nasal application, products, and method

Notes of Related Applications

This US patent application claims the benefit of pending US Provisional Patent Application No. 61 / 091,887 filed on August 28, 2008 and its US Patent Application No. 12 / 466,382 filed May 14, 2009. Both applications are incorporated by reference throughout this specification.

Field of invention

The present invention relates to a protective composition that acts against the attack of various air allergens entering the body through the airways and / or nasal mucosa. Typically these allergens in particular include pollen, dust mites, molds and animal dandruff. The present invention also relates to products developed to date that generate an electrostatic field near or around the nasal passage to limit the flow of airborne material into the nasal passage. This traps pollutants, reducing the influx of airborne contaminants into the nasal passages and preventing them from entering the body and stimulating allergic reactions. The present invention also relates to formulations having an antihistamine or pseudo-antihistamine effect on the body to treat allergic reactions caused by such aerial allergens.

Background of the Invention

Many suffer from allergens in the air in spring and autumn. The main pollutant in spring is pollen. The main pollutant during the fall season is hives ragweed pollen. However, many people suffer from allergic reactions all year round. Most of these reactions are due to pollen, dust mites, mold, and white mold. In the allergic season, many suffering people must block their nasal passages and breathe through their mouths. However, for most people, the nasal passages and mucous membranes serve as the main entrance to most of the allergens. Nasal air is a natural filter for airborne particles, so it is desirable to breathe through the human nose. It prevents particulates from entering into the lower respiratory system. The mechanism of the immune system to deal with allergens is that the cells in the nasal mucosa within 15 minutes after the allergen comes into contact with the cells present in the nasal mucosa, eyes, and lungs, the chemical regulator (histamine is one example of many things produced). To produce. This occurs because the immune system recognizes pollutants, particulates, and / or anything that can enter the body from the outside air. This allergic reaction is supposed to remove them from the body or make them ineffective. Unfortunately, in most cases these allergic reactions are more harmful than good. Mild allergic reactions include substances such as histamine that cause nasal swelling, sneezing, coughing, itching of the throat and itching of the eyes. In some instances, allergic reactions can act to cause hives and even hypersensitivity shocks. The term histamine is used here in a broad sense, involving several different kinds of mediators. Most of these coordinators play a role in generating allergic reactions at different stages. Thus, approved available palliative therapies act differently for other types of modulators that may cause allergic reactions. When allergens in the air come in contact with the nasal mucosa, it becomes difficult for people to breathe through their noses.

Histamine released by the body is a much more exaggerated immune response when allergens enter the body. When allergens touch the mucous membranes in the nasal passages, the immune system is attacked by harmful substances. When histamine is released into the bloodstream, a person develops allergic rhinitis, which is manifested as a “runny” or “itchy” nose, sneezing, “watery eyes”, itching of the neck, etc. This is the first 15 minutes. It can happen immediately or within four to eight hours, and many prescription and over-the-counter anti-histamine drugs are designed to inhibit the production of histamine and other modulators in the body.

People may also receive costeroids or immunotherapy injections designed to reduce or alter the immune response to allergens to reduce or eliminate allergic reactions. Tears and itching of the throat may involve reactions to allergens in the nose. This is the main starting point. If allergens in the nose can be prevented from coming into contact with the mucous membranes, allergic reactions can be greatly reduced.

Anti-histamines can work in two ways. In the first method, anti-histamine drugs should be taken orally to provide systemic stability. Many such anti-histamines can make the user sleepy, which is quite undesirable. There are anti-histamine drugs that do not cause sleepiness, but most of them have other undesirable side effects. In the second method, anti-histamine drugs act topically. These are anti-histamine nasal sprays and eye drops. There are fewer side effects here. Although these nasal sprays act locally on the nose, some systemic absorption occurs. Here, inhibition of histamine production begins locally,

In practice it works both locally and systemically. In addition, allergens in the air continue to exist in the immune system, primarily through the nose, even if the histamine response is inhibited.

Patent documents such as US Pat. No. 5,468,488, US Pat. No. 5,674,481, and US Pat. No. 6,844,005 are applicable to the outer periphery of the nasal cavity and are electrostatically charged compositions that adsorb opposite materials of opposite charges to be inhaled separately. This is described. These compositions produce an electrostatic field that helps filter out materials of opposite charge.

Formulations that can be applied externally to the nasal area with creams, ointments, lotions, gels, or other topical formulations, or when spraying liquids into the nasal passages, trapping allergens, preventing contact with mucous membranes and reducing allergic reactions. It would be desirable if it existed. It would also be desirable to include antihistamine or pseudo-antihistamine products that can reduce allergic reactions. Topical nasal decongestants may also be included. Such products are generally known and are also used for the treatment of allergies. And most of these products are now sold on the market. One such product is sold under the exclusive trademark Antithistine and is used for itchy eyes. Other products that are pseudo-antihistamines are Nasonex (momentasone furate monohydrate-corticosteroid, mometasone furoate monohydrate-a corticosteroid) and Afrin Nasal Spray.

Purpose of the Invention

It is therefore an object of the present invention to provide a formulation which can be easily applied to the outer periphery of the nasal cavity and / or just slightly inside the edge of the nasal cavity which can electrostatically adsorb airborne allergens and trap and harm them. Purpose.

It is another object of the present invention to provide a formulation which is capable of electrostatically adsorbing allergens in the air and spraying in the nose which can trap and harm the allergens in the air.

It is another object of the present invention to provide a spray, cream, ointment, lotion, gel, or other topically applied formulation as described which has the additional property of separating the mucosa from the adhesion of the captured allergen.

It is another object of the present invention to locally inhibit histamine production by adding anti-histamine drugs to the above formulations.

Other objects of the present invention will become apparent to those of ordinary skill in the art upon encountering the present disclosure. For all the foregoing purposes, the above mentioned deficiencies in the prior art are solved by the teachings of the present invention.

Summary of the Invention

These and other objects of the present invention, when applied to a surface, in aqueous or non-aqueous base formulations that create a barrier and generate an electrostatic field to electrostatically adsorb and trap the air's allergens that are opposite charges in the periphery of the surface. Unexpectedly obtained by a method of providing a formulation with at least one polymeric quaternization compound. The barrier prevents the allergens from contacting the mucosa and reduces its deleterious effects. In combination with known antihistamine drugs, allergic reactions can be reduced with or without synergism from both types of action.

Detailed description of the invention

The present invention includes methods and formulations to be produced. The formulation is included in a gel that is applied in and around the nasal passages or in a liquid that is sprayed into the nasal passages. The film or barrier separates the mucosa when contacting the inner surface of the nasal cavity.

The formulations include commonly used cationic agents that produce an electrostatic field. This has the effect of adsorbing allergens with opposite charges.

The barrier can then capture the infiltrating allergen. This reduces allergic rhinitis, including the release of histamine and other modulators without the use of other local or systemic drugs.

The effect of this is to reduce allergic reactions. For example, if a formulation is applied and a reaction occurs in an individual who is allergic to hives ragweed pollen when the number of pollen reaches a threshold, the reaction may not begin to occur until the pollen number is significantly higher.

Preliminary observations of test subjects for the formulations of the present invention show a decrease in total and specific IgE protein. Within a short time after application, these subjects appear to virtually disappear or diminish their allergic rhinitis.

First, the eyes and neck stop the itching, the "sniffles" stop, and the last object can breathe comfortably through the nose. In most but not all subjects, symptoms disappear in the reverse order of appearance at the onset of an allergic reaction.

The previous product adsorbed or pushed away the particles of electrostatically charged air that were applied in the region around the nasal passages. These particles, pushed away from the applied product, never entered the nasal cavity. These particles adsorbed to the applied product never came into the nasal cavity because they were captured and captured in the product itself.

Thus, the number of particles entering the nasal passages was significantly reduced. At some point the previous product was removed by wiping and reapplied as needed. The products of the present invention act differently from these conventional products. This also means applying in the nasal passages in addition to applying around the nasal passages.

The products of the present invention adsorb air allergens and create barriers between air and mucous membranes in the nasal cavity. It can be in the form of a gel or a spray. Not only does it prevent the air allergens from adhering to the mucosa, but the air allergens come into contact with the product itself and become harmless.

In order to carry out the invention, formulations with at least one cationic agent known in the art, such as quaternary ammonium compounds, are prepared. These compounds may be used alone or together to form static electricity on or around the surface to which the compound is applied, including surfaces such as skin, textiles (wovens and nonwovens), and hard surfaces such as floors, walls, wood, metals, plastics, and the like. You can generate chapters.

The formulations are generally based on aqueous, but may include non-aqueous solvents that are compatible with the other formulation ingredients and used to be compatible with the surface to which it is applied. Preferably, the formulation is an aqueous formulation. In addition, the compositions include, but are not necessarily required to, various thickeners, gelling agents, flavors, colorants, emollients, wetting agents, and other suitable ingredients that are generally compatible with other components of the end use application and formulation.

Most airborne particles such as pollen and dust are small but not as small as most microorganisms. Although some must be observed under a microscope, many can be seen with the naked eye. The form of these fine particles includes a fibrous expansion structure that can adhere to the mucosa. In many respects it resembles a lint ball or a ball of cotton candy. This expansion is responsible for initiating an allergic reaction.

However, when the formulation of the present invention is applied to the nasal and nasal periphery, the moment the allergen particles contact the membrane, their shape changes and the dilatation structure becomes flat. In this way the particulates become less harmful. Particulates cannot enter the mucous membranes causing allergic reactions. Even if they are removed after they are first caught, they are caught in the nose hair and become ineffective. It is true that some particulates remain active (possibly in the bronchus or lungs). However, the threshold of the individual to capture most of these particles and make them ineffective increases.

The effectiveness of the product can be increased by combining antihistamine compounds as known in the art. However, the combination of electrostatic fields with local application of antihistamines can produce a three-step synergistic effect. First, most allergen particulates are prevented from adhering to the nasal mucosa by the barrier. Secondly, the particles are captured and their shape is changed so that the effects of the particles are lost. Finally, because allergic reactions are milder, anti-histamines are more effective in eliminating or reducing the effects of the response.

The formulation of the invention is:

·water;

At least one quaternized thickener;

Preservatives;

Emulsifiers;

Biocides; And

Neutralizing agent added to adjust and achieve pH in the range of 5.0 to 6.8.

In an exemplary embodiment of the formulation, the amount of water is from 60 to 90% by weight, quaternized thickener (at least one must be present)-0.5 to 5.0% by weight; Preservative-0.1 to 1.0% by weight; Emulsifiers-from 0.1 to 3.0% by weight; And biocide-0.1 to 1.0% by weight.

In an exemplary embodiment of the formulation, the quaternized thickener may include, but is not limited to, at least one of the following:

Polyquaternium-10;

Polyquaternium-22;

Polyquaternium-67;

Polyquaternium-91.

In an exemplary embodiment of the formulation, the emulsifier may include, but is not limited to, at least one of the following:

Cetyl alcohol;

Cetearyl alcohol;

Glyceryl stearate;

Ceeareth-20.

In an exemplary embodiment of the formulation, the emollient may include, but is not limited to, at least one of the following:

C 10-30 Cholesterol / Lanosterol Esters;

Ethylhexyl palmitate;

Hydrogenated Polyisobutene.

In an exemplary embodiment of the formulation, the preservative includes, but is not limited to, at least one of the following:

Phenoxyethanol;

Methylparabens;

Butyl parabens;

Ethylparabens;

Propylparabens;

Isobutyl paraben.

Examples of typical formulations include the following ingredients:

ingredient Percent range function water 80%-90% Solvents, humectants Polyquaternium-10 2%-5% Conditioner, Quaternary, Thickener Polyquaternium-67 1%-2% Conditioner, Quaternary, Thickener Phenoxyethanol, methyl paraben, butyl paraben, ethyl paraben,
Propylparaben,
Isobutyl paraben One% Preservative Phenoxyethanol 0.2% -0.3% Preservatives, masking agents Polyquaternium-22 1%-2% Conditioner, Grade 4 Setronium Chloride 2% Conditioner, Level 4 C10-30 Cholesterol / Lanosterol Ester 0.2%-0.3% Softener Cetyl alcohol 2% Thickeners, emulsifiers Cetiaryl alcohol, glyceryl stearate,
PEG-40 stearate,
Cetearette-20 2%-3% Emulsifier Benzalkonium chloride 0.5% Biocides, Conditioners, Quaternization Hydroxypropyl, trimonium hydrolized silk 0.5% Conditioner, Level 4 Sodium hydroxide 0.025% corrector

Formulations for the first embodiment of the invention are shown in Table 1. The function of each component is shown in this table. As can be seen from the table, the composition consists mainly of water. The other components consist of 10-30% by weight. The pH range of the composition is 6.1-6.5 and the viscosity varies between 50,000-110,000 cps. Specific gravity ranges from 0.96-1.02.

Other typical formulations are as follows:

ingredient percent function water 80% -90% Solvents, humectants Quaternium-91,
Cetrimonium methosulfate,
Cetiaryl Alcohol 1% -4% conditioner for hair Stearyl alcohol 2% Thickener Cetyl alcohol 0.5% Thickener C10-30 Cholesterol
Lanosterone ester One% Softener Ethylhexyl palmitate 3% -5% Softener Glyceryl stearate,
PEG-100 Stearate 1% -3% Emulsifier

Table 2 shows the formulations for the second embodiment of the invention. As apparent from Table 2, quaternium-91 is used in this embodiment instead of polyquaternium-10, polyquaternium-22, and polyquaternium-67 from the first embodiment.

ingredient percent function water 80% -90% Solvents, humectants Dipropylene glycol 2% -4% Softener Acetamide MEA One% Wetting agent Gluconolactone,
Sodium benzoate One% Preservative Quaternium-91,
Cetrimonium Methosulfate,
Cetiaryl Alcohol 1% -4% conditioner for hair Cetiaryl Alcohol,
Cocoa glucoside 1% -4% Thickener Cetyl alcohol 0.1% -1.5% Thickener C10-30 cholesterol,
Lanosterol Esters 0.5% -1.5% Softener Ethylhexyl palmitate 2% -6% Softener Glyceryl stearate,
PEG-100 Stearate 1% -4% Emulsifier Hydrolyzed Hydroxypropyl Trimonium 0.5% Skin conditioner Oat Protein water,
Hydrolyzed Algin One% Skin conditioner

Table 3 shows the formulations for the third embodiment of the invention. Note that in the second and third embodiments, the quaternium-91 component is present in the same percentage.

ingredient percent function water 75% -85% menstruum,
Moisturizer,
Surfactants Gluconolactone,
Sodium benzoate One% Preservative Quaternium-91,
Set Limonium 1% -4% conditioner for hair Methosulfate,
Cetiaryl Alcohol Stearyl alcohol 1% -3% Thickener Cetyl alcohol 0.1% -1.5% Thickener C10-30 Cholesterol
Lanosterone ester 1% -3% Softener Ethylhexyl palmitate 2% -6% Softener Glyceryl stearate,
PEG-100 Stearate 1% -4% Emulsifier Polyquaternium-22 0.5% -3% conditioner for hair Ethoxyethanol 0.5% Preservative Sodium hydroxide 3% corrector

Table 4 shows the formulation for the fourth embodiment. Note that both quaternium-91 and polyquaternium-22 are used.

ingredient percent function water 70% -80% Solvents, humectants Gluconolactone,
Sodium benzoate One% Preservative Quaternium-91,
Cetrimonium methosulfate,
Cetiaryl Alcohol 1% -4% conditioner for hair Stearyl alcohol 1% -3% Thickener Cetyl alcohol 0.1% -1.5% Thickener C10-30 Cholesterol
Lanosterone ester 1% -3% Softener Hydrogenated polybutene 3% -6% Softener Glyceryl stearate,
PEG-100 Stearate 1% -4% Emulsifier Polyquaternium-22 2% -5% conditioner for hair Phenoxyethanol 0.5% Preservative Hydroxy Trimonium Hydrolyzed Silk 0.5% conditioner for hair Hydrolyzed Milk Protein 0.25% conditioner for hair Sodium hydroxide 3% -4% corrector

Table 5 shows the formulation for the fifth embodiment of the present invention.

ingredient percent function water 75% -85% Solvents, humectants Polyquaternium-67 0.5% -2% Conditioner / Quat (Quat) Phenoxyethanol,
Methylparaben,
Butyl Paraben,
Ethyl paraben,
Propylparaben,
Isobutyl paraben One% Preservative Polyquaternium-22 1% -4% Conditioner / Level 4 Cetyl trimonium ammonium chloride 1% -3% Conditioner / Level 4 Stearyl alcohol 1% -2% Thickener Cetyl alcohol 1% -2% Thickener C10-30 Cholesterol Lanosterone Ester 0.5% -2% Softener Hydrogenated polyisobutene 3% -6% Softener Glyceryl stearate,
PEG-100 Stearate 1% -4% Emulsifier Hydroxypropyl Trimonium Hydrolyzed Silk 0.5% Conditioner / Level 4 Benzylconium chloride 1% -3% Conditioner / Level 4 Sodium hydroxide One% corrector

Table 6 shows the formulation, which is the sixth embodiment of the present invention. Note that it includes benzylconium chloride as well as polyquaternium-67 and polyquaternium-22.

All formulations described in Tables 1-6 representing six embodiments of the present invention work in the manner described above. The same result can be obtained by varying the percentage of active and inactive ingredients. Changing the percentage of active ingredient affects the consistency of the formulation. The components and amounts thereof can be varied by methods used by those skilled in the art without undue experimentation to achieve the desired results.

Claims (34)

A method of applying the formulation to the nasal area or nasal cavity of a person to reduce the undesirable effects of allergic rhinitis, which comprises:
a) creating a barrier that prevents airborne allergen particulates from contacting the nasal mucosa;
b) electrostatically adsorbing the allergen particles; And
c) entrapping the allergen microparticles in the formulation.
The method of claim 1, further comprising changing the shape of the captured allergen particulates such that they cannot cause allergic rhinitis.
The method of claim 1, further comprising applying an anti-histamine compound to locally inhibit the production of histamine.
The method of claim 1, further comprising applying a corticosteroid.
The method of claim 1, further comprising applying a topical nasal decongestant.
A formulation applied to the nasal area or nasal cavity of a person that reduces the undesirable effects of allergic rhinitis, wherein the formulation is:
a) means for creating a barrier that prevents the allergen particulates from contacting the nasal mucosa;
b) means for electrostatically adsorbing the allergen particulates;
c) means for trapping the allergen microparticles in the formulation; And
d) means for changing the shape of the captured allergen microparticles such that the allergen microparticles cannot cause allergic rhinitis.
A formulation that reduces the undesirable effects of allergic rhinitis by application to the nasal area or nasal cavity of a human comprising at least one cationic agent, and wherein the formulation,
a) creates a barrier that prevents airborne allergens from contacting the nasal mucosa;
b) Formulations that generate and capture an electrostatic field that adsorbs air allergens around the nasal area or around the nasal cavity.
8. The formulation of claim 7, wherein said at least one cationic agent is a polymeric quaternary ammonium compound.
8. The formulation of claim 6 or 7, further comprising a liquid that facilitates spraying into the nasal cavity of a human.
The formulation of claim 9, wherein the liquid is water.
8. The formulation of claim 6 or 7, further comprising a gel or cream to facilitate manual application of the formulation to the human nose area and around the nasal cavity.
8. The formulation of claim 6 or 7, further comprising an antihistamine compound.
8. The formulation of claim 6 or 7, further comprising a topical nasal decongestant.
8. The formulation of claim 6 or 7, further comprising a corticosteroid.
It is a formulation that is applied to the nasal area or nasal cavity of a person to reduce the undesirable effect of allergic rhinitis, which formulation is:
2 to 5% by weight of polyquaternium-10;
1 to 2 weight percent of polyquaternium-67; And
A formulation comprising 1 to 2% by weight of polyquaternium-22.
The formulation of claim 15 further comprising setronium chloride and benzylalkonium chloride.
The formulation of claim 15 further comprising at least one emulsifier.
18. The formulation of claim 17, wherein said emulsifier is cetyl alcohol.
The formulation of claim 15 further comprising at least one preservative.
The formulation of claim 15 further comprising at least one emollient.
The formulation of claim 15 further comprising at least one masking agent.
The formulation of claim 15 further comprising at least one thickener.
A formulation that is applied to the nasal area or nasal cavity of a human to reduce the undesirable effects of allergic rhinitis, wherein the formulation is:
Quaternium-91;
Polyquaternium-10;
Polyquaternium-22;
Polyquaternium-67; And
Benzalkonium chloride.
A formulation comprising at least one selected from the group consisting of.
The formulation of claim 23, wherein the formulation further comprises at least one emulsifier.
The formulation of claim 23, further comprising at least one preservative.
The formulation of claim 23, further comprising at least one emollient.
The formulation of claim 23, further comprising at least one masking agent.
The formulation of claim 23, further comprising at least one thickener.
A formulation that is applied to the nasal area or nasal cavity of a human to reduce the undesirable effects of allergic rhinitis, wherein the formulation is:
a) water;
b) at least one quaternized thickener;
c) preservatives;
d) emulsifiers;
e) biocides; And
f) A formulation comprising a neutralizing agent added to adjust and achieve a pH in the range of 5.0 to 6.8.
The formulation of claim 29, wherein the formulation is:
a) in the range of 60 to 90% by weight of water;
b) quaternized thickener in the range from 0.5 to 5.0% by weight;
c) preservative in the range from 0.1 to 1.0% by weight;
d) emulsifier in the range from 0.1 to 3.0% by weight; And
e) A formulation which is a biocide in the range of 0.1 to 1.0% by weight.
The formulation of claim 29, wherein the formulation is:
Polyquaternium-10,
Polyquaternium-22,
Polyquaternium-67, and
A formulation further comprising a thickener selected from the group consisting of polyquaternium-91.
The method of claim 29, wherein the emulsifier is:
Cetyl Alcohol,
Cetearyl alcohol,
Glyceryl stearate, and
A formulation selected from the group consisting of ceteareth-20.
The method of claim 29, wherein the emulsifier is:
C 10-30 cholesterol / lanosterol esters,
Ethylhexyl palmitate, and
Formulations selected from the group consisting of hydrogenated polyisobutenes.
The method of claim 29, wherein the preservative is:
Phenoxyethanol,
Methylparaben,
Butyl Paraben,
Ethyl paraben,
Propylparaben, and
A formulation selected from the group consisting of isobutylparabens.