Nasal irrigation composition

Abstract

To provide a composition for washing a nasal cavity that has an excellent refreshing feel and an excellent foreign matter removal effect.SOLUTION: A composition for washing a nasal cavity contains a monoterpene, a divalent alcohol, and a thickener and gives an excellent refreshing feel after use and also gives a markedly excellent foreign matter removal effect.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a nasal irrigation composition having excellent cooling sensation and foreign substance removing effect.

Background Art

[0002] The nasal mucosa is an epithelial tissue that is directly exposed to the outside world and reacts sensitively to external stimuli. When foreign substances such as pollen, microorganisms, and house dust adhere to the nasal mucosa, it is known that it causes intolerable discomfort or develops various diseases such as allergic diseases and infectious diseases. To prevent or improve such nasal mucosal symptoms, it is effective to remove foreign substances adhering to the mucosa with a nasal irrigation composition.

[0003] Since the nasal irrigation composition is directly applied to the nasal mucosa, it is necessary to formulate it in consideration of sensory aspects such as the feeling of use. Furthermore, it is also important that the nasal irrigation composition is formulated so that foreign substances in the nasal cavity can be effectively removed. Conventionally, various nasal irrigation compositions have been proposed to improve the feeling of use and functionality. For example, Patent Document 1 describes that a nasal irrigation composition containing at least one selected from the group consisting of peppermint oil and citrus essential oil, peppermint oil, and l-menthol can obtain excellent cooling sensation and washing effect. In addition, Patent Document 2 describes that a cleaning solution containing minerals eluted from fossil shells into distilled water as a main component can effectively clean foreign substances such as pollen in the nasal cavity.

[0004] In recent years, as nasal irrigation using a nasal irrigation composition has become established, there has been a demand for further improvement in the feeling of use and functionality of the nasal irrigation composition.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Patent Document 2

[0006] The object of this invention is to provide a nasal irrigation composition that has excellent cooling sensation and foreign matter removal effect. [Means for solving the problem]

[0007] The inventors of the present invention conducted diligent research to solve the aforementioned problems and found that a nasal irrigation composition containing a monoterpene, a dihydric alcohol, and a thickening agent provides an excellent refreshing sensation after use and exhibits a remarkably superior foreign matter removal effect. The present invention was completed by further research based on these findings.

[0008] In other words, the present invention provides inventions in the following embodiments. Item 1. A nasal irrigation composition containing a monoterpene, a dihydric alcohol, and a thickening agent. Item 2. The nasal lavage composition according to Item 1, further comprising a parahydroxybenzoic acid ester and / or a quaternary ammonium salt. Item 3. The nasal lavage composition according to item 1 or 2, wherein the thickening agent is a cellulose-based thickening agent and / or a polyvinyl-based thickening agent. Item 4. A nasal lavage composition according to any one of items 1 to 3, contained in a container capable of dispensing its contents into the nasal cavity in droplet form by dropping or spraying. [Effects of the Invention]

[0009] The nasal irrigation composition of the present invention can provide an excellent refreshing sensation and effectively remove foreign substances adhering to the nasal mucosa, such as pollen, microorganisms, and house dust. [Modes for carrying out the invention]

[0010] The nasal irrigation composition of the present invention is characterized by containing a monoterpene, a dihydric alcohol, and a thickening agent. By including these three components, the nasal irrigation composition of the present invention dramatically improves the feeling of freshness compared to when a monoterpene is included alone, and also provides a significantly superior foreign matter removal effect. The nasal irrigation composition of the present invention will be described in detail below.

[0011] [Monoterpenes] The nasal irrigation composition of the present invention contains a monoterpene. A monoterpene is a known component having a structure containing two isoprene units in its molecule and possessing a cooling effect. The type of monoterpene used in the present invention is not particularly limited, as long as it is applicable to the nasal cavity, but examples include alcohol-based monoterpenes such as menthol, thymol, geraniol, linalool, borneol, cineole, and terpineol; aldehyde-based monoterpenes such as citral, citronellal, perillaldehyde, and safranal; and ketone-based monoterpenes such as camphor, menthone, carbomenthone, and ionone. If optical isomers exist, these monoterpenes may be d-isomers, l-isomers, or dl-isomers. These monoterpenes may be used individually or in combination of two or more.

[0012] Furthermore, in this invention, essential oils containing monoterpenes may be used as monoterpenes. Essential oils containing monoterpenes can be appropriately selected from known ones, but examples of essential oils containing menthol include peppermint oil, spearmint oil, and peppermint menthol. Note that, when using essential oils containing monoterpenes, the descriptions of monoterpene content and ratios in this specification are values ​​converted to the amount of monoterpenes contained in the essential oil.

[0013] Among these monoterpenes, menthol is preferred, and l-menthol is even more preferred, from the viewpoint of providing an even better cooling sensation.

[0014] The monoterpene content in the nasal irrigation composition of the present invention can be appropriately set depending on the type of monoterpene used, the degree of cooling sensation to be imparted, etc., but for example, 0.001 to 3% by weight is preferred, and from the viewpoint of imparting an even better cooling sensation, 0.005 to 1% by weight is preferred, and more preferably 0.01 to 0.25% by weight is preferred.

[0015] [Dihydric alcohol] The nasal irrigation composition of the present invention contains a dihydric alcohol. The dihydric alcohol used in the present invention is not particularly limited, as long as it is applicable to the nasal cavity, but examples include dihydric lower alcohols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, isoprene glycol, diethylene glycol, and dipropylene glycol.

[0016] These dihydric alcohols may be used individually or in combination of two or more.

[0017] Among these dihydric alcohols, propylene glycol and 1,3-butylene glycol are preferred from the viewpoint of providing an even better cooling sensation.

[0018] The dihydric alcohol content in the nasal irrigation composition of the present invention can be, for example, 0.01 to 10% by weight, preferably 0.1 to 5% by weight, and more preferably 0.3 to 2% by weight, from the viewpoint of providing an even better cooling sensation.

[0019] In the nasal irrigation composition of the present invention, the ratio of monoterpenes to dihydric alcohols is not particularly limited, but for example, 0.1 to 1500 parts by weight of dihydric alcohol per 1 part by weight of monoterpenes is preferred, and from the viewpoint of providing an even better cooling sensation, 0.5 to 500 parts by weight, more preferably 0.5 to 50 parts by weight, and even more preferably 1 to 20 parts by weight of dihydric alcohol per 1 part by weight of monoterpenes is preferred.

[0020] [Thickener] The nasal cavity irrigation composition of the present invention contains a thickener. The thickener used in the present invention is not particularly limited as long as it is applicable in the nasal cavity. Examples thereof include cellulose-based thickeners, polyvinyl-based thickeners, thickening polysaccharides, acrylic acid-based thickeners, and the like.

[0021] Specific examples of the cellulose-based thickeners include carmellose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose, ethylcellulose, hydroxyethyl cellulose, hydroxyethyl cellulose, and the like. These cellulose-based thickeners may be in the form of salts. Examples of the cellulose-based thickeners in the form of salts include sodium carmellose and the like.

[0022] Specific examples of the polyvinyl-based thickeners include carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, and polyvinyl methyl ether.

[0023] Specific examples of the thickening polysaccharides include xanthan gum, guar gum, locust bean gum, carrageenan, alginic acid, and the like. These thickening polysaccharides may be in the form of salts. Examples of the thickening polysaccharides in the form of salts include sodium alginate and the like.

[0024] Specific examples of the acrylic acid-based thickeners include acrylic acid-methacrylic acid alkyl copolymer, sodium polyacrylate bentonite, and the like.

[0025] These thickeners may be used alone or in combination of two or more.

[0026] Among these thickeners, from the viewpoint of further improving the foreign matter removal effect, cellulose-based thickeners, polyvinyl-based thickeners, and thickening polysaccharides are preferred; more preferably, carmellose and / or its salts, hydroxypropyl methylcellulose, hydroxypropylcellulose, carboxyvinyl polymer, and xanthan gum; even more preferably, carmellose and / or its salts; and particularly preferably, carmellose sodium.

[0027] The amount of thickener in the nasal irrigation composition of the present invention can be appropriately set depending on the type of thickener used, the viscosity to be imparted, etc., but for example, the total amount of thickener is preferably 0.005 to 2% by weight, preferably 0.05 to 1% by weight, and more preferably 0.1 to 0.5% by weight, from the viewpoint of further improving the foreign matter removal effect.

[0028] In the nasal lavage composition of the present invention, the ratio of monoterpenes to thickeners is not particularly limited, but for example, the total amount of thickeners is 0.01 to 500 parts by weight per 1 part by weight of monoterpenes, and from the viewpoint of further improving the foreign matter removal effect, the total amount of thickeners is preferably 0.1 to 150 parts by weight, more preferably 0.1 to 30 parts by weight, and even more preferably 0.5 to 15 parts by weight per 1 part by weight of monoterpenes.

[0029] [Parahydroxybenzoic acid esters and / or quaternary ammonium salts] The nasal irrigation composition of the present invention may also contain a parahydroxybenzoic acid ester and / or a quaternary ammonium salt in addition to the above-mentioned components. When the nasal irrigation composition of the present invention contains a parahydroxybenzoic acid ester and / or a quaternary ammonium salt, it can not only provide preservative properties but also further enhance the feeling of freshness.

[0030] Parahydroxybenzoic acid esters are alkyl esters or benzyl esters of parahydroxybenzoic acid. Examples of alkyl groups in the alkyl esters of parahydroxybenzoic acid include linear or branched alkyl groups having 1 to 5 carbon atoms. Specific examples of parahydroxybenzoic acid esters include methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, isobutyl parahydroxybenzoate, and benzyl parahydroxybenzoate. Among these parahydroxybenzoic acid esters, methyl parahydroxybenzoate is preferred from the viewpoint of further enhancing the cooling sensation.

[0031] Examples of quaternary ammonium salts include benzalkonium chloride, cetylpyridinium chloride, benzethonium chloride, decalinium chloride, alkyldimethylammonium chloride, alkyltrimethylammonium chloride, methylbenzethonium chloride, and lauroylcoraminoformylmethylpyridinium chloride. These quaternary ammonium salts may also be in the form of solvates such as hydrates. Among these quaternary ammonium salts, benzalkonium chloride is preferred from the viewpoint of further enhancing the cooling sensation.

[0032] The nasal irrigation composition of the present invention may contain either a parahydroxybenzoic acid ester or a quaternary ammonium salt, or a combination of a parahydroxybenzoic acid ester and a quaternary ammonium salt may be used.

[0033] When using a combination of parahydroxybenzoic acid ester and quaternary ammonium salt, there are no particular restrictions on their ratio, but for example, the total amount of quaternary ammonium salt is 0.01 to 20 parts by weight, preferably 0.1 to 10 parts by weight, and more preferably 1 to 5 parts by weight, per 100 parts by weight of total amount of parahydroxybenzoic acid ester.

[0034] When the nasal lavage composition of the present invention contains a parahydroxybenzoic acid ester, the content is preferably, for example, 0.005 to 0.5% by weight, preferably 0.01 to 0.4% by weight, and more preferably 0.05 to 0.3% by weight, from the viewpoint of further improving the refreshing sensation. Furthermore, when the nasal lavage composition of the present invention contains a quaternary ammonium salt, the content is preferably, for example, 0.00005 to 0.1% by weight, preferably 0.0001 to 0.1% by weight, and more preferably 0.001 to 0.05% by weight, from the viewpoint of further improving the refreshing sensation.

[0035] When the nasal lavage composition of the present invention contains a parahydroxybenzoic acid ester, the ratio of monoterpene to parahydroxybenzoic acid ester is not particularly limited, but for example, per 1 part by weight of monoterpene, the total amount of parahydroxybenzoic acid ester is preferably 0.01 to 500 parts by weight, more preferably 0.1 to 100 parts by weight, and more preferably 0.1 to 10 parts by weight, from the viewpoint of further improving the cooling sensation. Furthermore, when the nasal lavage composition of the present invention contains a quaternary ammonium salt, the ratio of monoterpene to quaternary ammonium salt is not particularly limited, but for example, per 1 part by weight of monoterpene, the total amount of quaternary ammonium salt is preferably 0.0001 to 1 part by weight, more preferably 0.0005 to 0.1 parts by weight, and more preferably 0.0005 to 0.1 parts by weight, of 1 part by weight of monoterpene.

[0036] [Nonionic surfactants] The nasal irrigation composition of the present invention may optionally contain a nonionic surfactant. The nonionic surfactant used in the present invention is not particularly limited, as long as it is applicable to the nasal cavity, but examples include polyoxyethylene sorbitan fatty acid esters and polyoxyethylene hydrogenated castor oil. These nonionic surfactants may be used individually or in combination of two or more.

[0037] Among these nonionic surfactants, polyoxyethylene sorbitan fatty acid esters are preferred. The average number of moles of ethylene oxide (EO) added to the polyoxyethylene sorbitan fatty acid ester is not particularly limited, but for example, it is 5 to 40 moles, preferably 10 to 30 moles, and more preferably 15 to 25 moles. The number of carbon atoms in the fatty acid constituting the polyoxyethylene sorbitan fatty acid ester is not particularly limited, but for example, it is 10 to 22, preferably 14 to 22, and more preferably 16 to 20. Specific examples of polyoxyethylene sorbitan fatty acid esters include polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan trioleate, polyoxyethylene sorbitan tristearate, and polyoxyethylene sorbitan monostearate. Among these polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan monooleate (polysorbate 80) with an average number of moles of ethylene oxide (EO) added is preferred. These nonionic surfactants may be used individually or in combination of two or more.

[0038] Examples of the nonionic surfactant content in the nasal irrigation composition of the present invention include 0.005 to 5% by weight, preferably 0.01 to 2% by weight, and more preferably 0.1 to 0.5% by weight.

[0039] [Inorganic salts of alkali metals] The nasal lavage composition of the present invention may contain an alkali metal inorganic salt as needed to adjust osmotic pressure, etc. The alkali metal inorganic salt is not particularly limited as long as it is applicable to the nasal cavity, but examples include alkali metal chlorides and alkali metal carbonates. Specifically, alkali metal chlorides include sodium chloride and potassium chloride. Specifically, alkali metal carbonates include sodium bicarbonate, sodium carbonate, potassium bicarbonate, and potassium carbonate. These alkali metal inorganic salts may be used individually or in combination of two or more. Among these inorganic salts, alkali metal chlorides are preferred, and sodium chloride is preferred. When alkali metal inorganic salts are included, the content of the inorganic salt is not particularly limited, but examples include 0.01 to 5% by weight, preferably 0.1 to 3% by weight, and more preferably 0.3 to 2% by weight.

[0040] [Other ingredients] In addition to the components described above, the nasal lavage composition of the present invention may contain other bases and additives necessary for formulation, etc., to the extent that they do not impair the effects of the present invention. Such bases and additives are not particularly limited as long as they are pharmaceutically acceptable, but examples of additives include monohydric lower alcohols having 1 to 5 carbon atoms, inorganic salts, trihydric alcohols, inorganic salts of alkaline earth metals, colorants, viscosity modifiers, pH adjusters, wetting agents, stabilizers, antioxidants, ultraviolet absorbers, buffers, solubilizers, solubilizers, chelating agents, and fragrances. These bases and additives may be used individually or in combination of two or more.

[0041] [Dosage form / Application / Product form] The nasal irrigation composition of the present invention is a liquid preparation, which is prepared by adding predetermined amounts of each component to water, dissolving them, and subjecting the mixture to sterilization as necessary.

[0042] The nasal irrigation composition of the present invention is used for irrigating the nasal cavity. Methods for irrigating the nasal cavity using the nasal irrigation composition of the present invention include, for example, introducing the nasal irrigation composition of the present invention into one nostril and flushing it out of that nostril; introducing the nasal irrigation composition of the present invention into the nasal cavity and flushing it out through the mouth; introducing the nasal irrigation composition of the present invention into one nostril and flushing it out of the other nostril. Furthermore, when introducing the nasal irrigation composition of the present invention into the nasal cavity, it may be introduced in droplet form (especially mist form) or as a liquid stream.

[0043] The nasal irrigation composition of the present invention is used in a container that can dispense its contents into the nasal cavity. This container may be capable of dispensing the contents in droplet form by dripping or spraying, or it may be capable of dispensing the contents as a liquid stream. Because the nasal irrigation composition of the present invention contains a thickening agent, it has properties suitable for dispensing in droplet form (especially mist form). Therefore, a suitable example of a container for the nasal irrigation composition of the present invention is a container that can dispense the contents in droplet form into the nasal cavity by dripping or spraying. [Examples]

[0044] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0045] Test Example 1 Nasal irrigation compositions (liquids) with the compositions shown in Table 1 were prepared. The refreshing sensation and foreign body removal effect of the obtained nasal irrigation compositions were evaluated using the following method.

[0046] <Method for evaluating the feeling of coolness> First, the nasal irrigation composition was placed in a container that can spray a mist into the nasal cavity (a commonly used nasal spray container). Ten subjects sprayed the nasal irrigation composition (approximately 0.15 ml per nostril) into each nostril to irrigate their nasal cavity, and evaluated the feeling of freshness after nasal irrigation. The feeling of freshness was evaluated on a five-point scale: "highly refreshing and very pleasant," "somewhat refreshing and somewhat pleasant," "neither," "somewhat insufficient refreshing," and "insufficient refreshing." The percentage of subjects who evaluated the feeling as "highly refreshing and very pleasant" or "somewhat refreshing and somewhat pleasant" was calculated as the refreshingness score.

[0047] <Method for evaluating the effectiveness of foreign matter removal> First, a nasal irrigation composition was placed in a container capable of spraying a mist into the nasal cavity (a commonly used nasal spray container). Next, approximately 3 ml of the nasal irrigation composition was sprayed in a mist into one nostril, and the nasal cavity was irrigated by flushing out the composition from that nostril. After irrigation, nasal discharge was collected from the irrigated nostril and used as the test sample. Nasal discharge from the other nostril was collected without irrigation and used as the control sample. The total number of particles between 2 and 125 μm was measured in the collected test and control samples using a particle counter. The total number of particles in the control sample was set to 1, and the relative ratio of the total number of particles in the test samples was calculated as the foreign body removal effect score. This evaluation was conducted on 10 subjects, and the average value of the foreign body removal effect score was calculated and rounded to two decimal places to obtain the foreign body removal effect score.

[0048] The results are shown in Table 1. When no thickener was included and monoterpenes and glycerin were present, the cooling sensation and foreign matter removal effect were insufficient (Comparative Example 1). Furthermore, when no thickener was included and monoterpenes and dihydric alcohols were present, an improvement in cooling sensation was observed compared to Comparative Example 1, but the foreign matter removal effect was insufficient (Comparative Examples 2 and 3).

[0049] In contrast, when a thickening agent was included along with monoterpenes and dihydric alcohols, the cooling sensation was enhanced, and the foreign matter removal effect was dramatically improved (Examples 1-8). In particular, when carmellose sodium was used as the thickening agent, the foreign matter removal effect was remarkably improved (Examples 1, 6, and 8). Furthermore, when parahydroxybenzoic acid esters and / or quaternary ammonium salts were included, the cooling sensation was remarkably improved (Examples 6-8). In addition, when the nasal lavage compositions of Examples 1-8 were modified by changing propylene glycol to 1,3-butylene glycol, the cooling sensation and foreign matter removal effect were evaluated, and the cooling sensation and foreign matter removal effect were improved in the same way as in Examples 1-8. Furthermore, when the nasal lavage compositions of Examples 1-8 were modified by changing the propylene glycol content to 2% by weight, the cooling sensation and foreign matter removal effect were evaluated, and the cooling sensation and foreign matter removal effect were improved in the same way as in Examples 1-8.

[0050] [Table 1]

[0051] Test Example 2 Nasal irrigation compositions were prepared by replacing the carboxyvinyl polymer in Examples 4 and 7 of Table 1 with xanthan gum. When the cooling sensation and foreign body removal effect were evaluated in the same manner as in Test Example 1, the cooling sensation and foreign body removal effect were improved, similar to Examples 4 and 7.

[0052] Prescription examples Nasal irrigation compositions were prepared with the compositions shown in Table 2. The cooling sensation and foreign body removal effect of the obtained nasal irrigation compositions were evaluated using the same method as in Test Example 1. All of the nasal irrigation compositions from Formulation Examples 1 to 7 exhibited excellent cooling sensation and foreign body removal effects.

[0053] [Table 2]

Claims

1. A nasal lavage composition comprising menthol, a dihydric lower alcohol, carmellose or a salt thereof, and a parahydroxybenzoic acid ester.

2. Furthermore, the nasal lavage composition according to claim 1 further contains a quaternary ammonium salt.

3. The nasal lavage composition according to claim 1 or 2, contained in a container capable of dispensing its contents into the nasal cavity in droplet form by dropping or spraying.

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