Mucosal components

Abstract

The present invention aims to provide a mucosal application composition with reduced metal corrosiveness. [Solution] A mucosal application composition comprising (A) an alkali metal chloride, (B) a dihydric alcohol, and (C) water, wherein the content of component (A) is 0.5 to 18% by weight, has reduced metal corrosiveness.

Description

Technical Field

[0001] The present invention relates to a mucosal application composition with reduced metal corrosiveness.

Background Art

[0002] With the recent increase in awareness of hygiene and protection for mucous membranes, compositions for the care of mucous membranes may be applied to mucous membranes. Since mucous membranes have a structure that is more sensitive to irritation than the skin, mucosal application compositions are used in a state where alkali metal chlorides adjusted to the same osmotic pressure concentration as body fluids are formulated as isotonic agents, thereby reducing irritation to the applied mucous membranes.

[0003] For example, Patent Document 1 shows that a mucosal application composition containing 0.002 to 0.1% by weight of benzalkonium chloride, 0.65% by weight of sodium chloride, 0.5% by weight of glycerin, 98 to 99% by weight of water, etc. suppresses the formation of precipitates and maintains good usability.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] Mucosal cleaning is typically performed in areas with water. Furthermore, these areas often contain metal components, and metal objects are frequently found in such locations. When a mucosal cleaning composition is used, it can adhere to metal surfaces in these areas. If left unwashed, the alkali metal chloride salts used as isotonic agents in the composition can cause metal corrosion. Additionally, because relatively large quantities of the mucosal cleaning composition are used at once, it is often prepared as a concentrated solution and diluted to the appropriate concentration before use. This dilution process can exacerbate the problem of corrosion if the concentrated solution adheres to metal surfaces in the area.

[0006] Therefore, the present invention aims to provide a mucosal application composition with reduced metal corrosiveness. [Means for solving the problem]

[0007] As a result of diligent research, the inventors discovered that by incorporating a dihydric alcohol into a mucosal application composition containing an alkali metal chloride salt at a predetermined concentration and water, metal corrosivity is reduced. This invention was completed by further research based on this finding.

[0008] In other words, the present invention provides inventions in the following embodiments. Item 1. A mucosal application composition comprising (A) an alkali metal chloride, (B) a dihydric alcohol, and (C) water, wherein the content of component (A) is 0.5 to 18% by weight. Item 2. The mucosal application composition according to Item 1, wherein the content of component (A) is 5 to 18% by weight. Item 3. The mucosal application composition according to Item 1 or 2, wherein the content of component (B) per 1 part by weight of component (A) is 0.1 parts by weight or more. Item 4. A mucosal application composition according to any one of items 1 to 3, further comprising (D) polyoxyethylene sorbitan fatty acid ester. [Effects of the Invention]

[0009] According to the present invention, a mucosal application composition with reduced metal corrosiveness is applied. [Modes for carrying out the invention]

[0010] The mucosal application composition of the present invention comprises (A) an alkali metal chloride (hereinafter also referred to as "component (A)"), (B) a dihydric alcohol (hereinafter also referred to as "component (B)"), and (C) water (hereinafter also referred to as "component (C)"), characterized in that the content of component (A) is 0.5 to 18% by weight. The mucosal application composition of the present invention will be described in detail below.

[0011] (A) Alkali metal chloride The mucosal application composition of the present invention contains an alkali metal chloride salt as component (A) at a predetermined concentration.

[0012] Examples of alkali metal chloride salts include sodium chloride and potassium chloride. These alkali metal chloride salts may be used individually or in combination. Among these alkali metal chloride salts, sodium chloride is preferred.

[0013] The content of component (A) in the mucosal application composition of the present invention is 0.5 to 18% by weight. Therefore, depending on the content of component (A), the mucosal application composition of the present invention can be used as is without dilution at the time of use, or it can be used after diluting with water at the time of use. Because the mucosal application composition of the present invention has excellent metal corrosion reduction properties, even if it contains a high concentration of component (A) which inherently increases metal corrosivity, it can effectively reduce metal corrosion. From this viewpoint, a preferred example of the content of component (A) in the mucosal application composition of the present invention is a high concentration that becomes suitable for mucosal application when diluted with water at the time of use, and specifically, this includes 3 to 18% by weight, preferably 4 to 18% by weight, more preferably 5 to 18% by weight, 5 to 15% by weight, 5 to 12% by weight, 5 to 10% by weight, 5 to 8% by weight, or 5 to 7% by weight.

[0014] (B) Dihydric alcohol The mucosal application composition of the present invention contains a dihydric alcohol as component (B). A mucosal application composition containing 0.5 to 18% by weight of component (A) and component (C) is corrosive to metals, but the mucosal application composition of the present invention can reduce metal corrosivity by further incorporating component (B).

[0015] The dihydric alcohols used in the present invention are not particularly limited, but examples include alkylenediols and polyalkylene ether diols. Examples of alkylenediols include ethylene glycol, propylene glycol, 1,3-butylene glycol, and isoprene glycol. Examples of polyalkylene ether diols include diethylene glycol and dipropylene glycol. These dihydric alcohols may be used individually or in combination of two or more.

[0016] Among these dihydric alcohols, alkylenediol is preferred from the viewpoint of further enhancing the metal corrosion inhibitory effect, propylene glycol and / or 1,3-butylene glycol is more preferred, and propylene glycol is even more preferred.

[0017] The content of component (B) in the mucosal application composition of the present invention is not particularly limited, but examples include an amount in which the content of component (B) per 1 part by weight of component (A) is 0.1 parts by weight or more, and from the viewpoint of further enhancing the metal corrosion inhibitory effect, preferably an amount of 0.3 parts by weight or more, more preferably 0.5 parts by weight or more, even more preferably 0.7 parts by weight or more, 1 part by weight or more, 1.5 parts by weight or more, or 2 parts by weight or more. The upper limit of the content of component (B) in the mucosal application composition of the present invention is not particularly limited, but examples include an upper limit of an amount in which the content of component (B) per 1 part by weight of component (A) is 4 parts by weight or less, 3 parts by weight or less, 2.5 parts by weight or less, 2 parts by weight or less, 1 part by weight or less, or 0.8 parts by weight or less.

[0018] Regarding the specific content of component (B) in the mucosal application composition of the present invention, it is determined by the content of component (A) and the content of component (B) with respect to component (A) described above. For example, it is 0.1% by weight or more, preferably 0.3% by weight or more, more preferably 1% by weight or more, still more preferably 3% by weight or more, and even more preferably 4% by weight or more. Although there is no particular limitation on the upper limit of the specific content of component (B) in the mucosal application composition of the present invention, for example, it is 15% by weight or less, 12.5% by weight or less, 10% by weight or less, 7% by weight or less, or 5% by weight or less.

[0019] (C)Water The mucosal application composition of the present invention contains water as component (C). Examples of water include purified water, distilled water, sterilized water, deep ocean water, and the like.

[0020] In the mucosal application composition of the present invention, the content of component (C) is not particularly limited, and examples include 60 to 99% by weight, preferably 65 to 96% by weight, and more preferably 70 to 92% by weight.

[0021] (D) Polyoxyethylene sorbitan fatty acid ester The mucosal application composition of the present invention can contain polyoxyethylene sorbitan fatty acid ester as component (D) for the purpose of further enhancing the metal corrosion inhibition property. [[ID=]17]

[0022] The polyoxyethylene sorbitan fatty acid ester used in the present invention is not particularly limited, and examples include polyoxyethylene sorbitan trioleate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan tristearate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monolaurate, and the like.

[0023] Although there is no particular limitation on the average number of moles of ethylene oxide (EO) added to the above polyoxyethylene sorbitan fatty acid ester, for example, it is 5 to 40 moles.

[0024] These polyoxyethylene sorbitan fatty acid esters may be used individually or in combination of two or more types.

[0025] Among the polyoxyethylene sorbitan fatty acid esters mentioned above, from the viewpoint of further enhancing the ability to suppress metal corrosion, preferred examples include polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, and polyoxyethylene sorbitan monolaurate, with polyoxyethylene sorbitan monooleate being the most preferred.

[0026] Furthermore, among the polyoxyethylene sorbitan fatty acid esters mentioned above, those with a preferably 10 to 30 moles of ethylene oxide (EO), more preferably 15 to 25 moles, and even more preferably 18 to 22 moles, are recommended from the viewpoint of further enhancing the ability to suppress metal corrosion.

[0027] Specifically, among the polyoxyethylene sorbitan fatty acid esters mentioned above, from the viewpoint of further enhancing the ability to suppress metal corrosion, polyoxyethylene sorbitan monooleate (polyoxyethylene (18-22) sorbitan monooleate) in which 18 to 22 moles of ethylene oxide (EO) are added is particularly preferred.

[0028] The amount of component (D) in the mucosal application composition of the present invention is not particularly limited, but for example, the amount of component (D) per 1 part by weight of component (A) is 0.05 parts by weight or more, and from the viewpoint of further enhancing the metal corrosion inhibitory effect, preferably it is 0.1 parts by weight or more, more preferably 0.3 parts by weight or more, and even more preferably 0.4 parts by weight or more, 0.6 parts by weight or more, 0.8 parts by weight or more, or 0.9 parts by weight or more. The upper limit of the amount of component (D) in the mucosal application composition of the present invention is not particularly limited, but for example, the upper limit of the amount of component (D) per 1 part by weight of component (A) is 4 parts by weight or less, 2 parts by weight or less, 1 part by weight or less, 0.7 parts by weight or less, or 0.5 parts by weight or less.

[0029] Furthermore, when the mucosal application composition of the present invention contains component (D), the amount of component (D) is such that, for example, the amount of component (D) per 1 part by weight of component (B) is 0.08 parts by weight or more. From the viewpoint of further enhancing the metal corrosion inhibitory effect, preferably it is 0.2 parts by weight or more, more preferably 0.4 parts by weight or more, even more preferably 0.5 parts by weight or more, 0.8 parts by weight or more, or 1 part by weight or more. There is no particular upper limit to the amount of component (D) when the mucosal application composition of the present invention contains component (D), but for example, the upper limit of the amount of component (D) per 1 part by weight of component (B) is such that it is 5 parts by weight or less, 2.5 parts by weight or less, 1.5 parts by weight or less, 0.8 parts by weight or less, or 0.6 parts by weight or less.

[0030] The specific content of component (D) in the mucosal application composition of the present invention is determined by the content of component (A) and the content of component (D) relative to component (A) and / or component (B) described above, but for example, it can be 0.5% by weight or more, preferably 1% by weight or more, more preferably 3% by weight or more, and even more preferably 4% by weight or more. There is no particular upper limit to the specific content of component (D) in the mucosal application composition of the present invention, but for example, it can be 20% by weight or less, 15% by weight or less, 10% by weight or less, or 6% by weight or less.

[0031] Other ingredients In addition to the components described above, the mucosal application 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 include lower monohydric alcohols having 1 to 5 carbon atoms, aqueous bases such as glycerin, oily bases, surfactants (other than the above component (D)), preservatives, colorants, viscosity modifiers, pH adjusters, wetting agents, stabilizers, antioxidants, UV absorbers, chelating agents, buffers, solubilizers, preservatives, and other additives. These bases and additives may be used individually or in combination of two or more. The content of these bases and additives can be appropriately set depending on the formulation form, etc.

[0032] In addition to the components described above, the mucosal application composition of the present invention may contain other pharmacological components as needed, provided that they do not impair the effects of the present invention. Examples of such pharmacological components include vitamins, antihistamines, local anesthetics, anti-inflammatory agents, mucosal protective agents, blood circulation promoting components, cooling agents, mucopolysaccharides, and the like. These pharmacological components may be used individually or in combination of two or more. When these pharmacological components are included, their content should be appropriately determined according to the type of pharmacological component used, the desired effect, etc.

[0033] form The form of the mucosal application composition of the present invention is not particularly limited as long as it is in a fluid form, and examples include liquid preparations and semi-solid preparations (ointments, gels, etc.). Preferably, a liquid preparation that can be easily dropped or splashed onto metal surfaces present in wet areas when applied to mucous membranes is preferred. Preferably, it can be designed as a concentrated liquid preparation that can be diluted with water at the time of use to prepare a mucosal application liquid composition with a concentration of each component suitable for application to mucous membranes.

[0034] Purpose The mucosal application composition of the present invention is used either as is without dilution, or after being diluted with water at the time of use to prepare a mucosal application liquid composition in which the concentration of each component is suitable for application to mucous membranes, it is used for the purpose of application to mucous membranes. The site of the mucous membrane is not particularly limited, and examples include the mucous membranes of the nasal cavity, eyes, pharynx, oral cavity, ears, vagina, bladder, rectum, etc., with the mucous membrane of the nasal cavity being preferred. Furthermore, the form of application to the mucous membrane is not particularly limited as long as it is a form in which the mucosal application composition of the present invention comes into contact with the mucous membrane, and examples include washing and application, but washing is preferred.

[0035] The method of using the mucosal application composition of the present invention is not particularly limited as long as the effect of application is achieved, but examples include: dropping it onto the mucous membrane; spraying it onto the mucous membrane with a sprayer, etc.; injecting it with a catheter, etc.; in the case of the nasal cavity, pouring the cleaning solution into the nasal cavity and spitting it out through the mouth, or pouring the cleaning solution into one nostril and spitting it out through the other nostril; in the case of the eyes, pouring the cleaning solution into an eye cup and washing the eyes; in the case of the oral cavity, rinsing the mouth with it and brushing with it; in the case of the vagina, injecting it into the vaginal cavity and letting it flow out through the vaginal opening, etc. [Examples]

[0036] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0037] Liquid mucosal application compositions were prepared with the compositions shown in Tables 1 and 2. These mucosal application compositions are applicable to the nasal mucosa. Of the mucosal application compositions shown in Tables 1 and 2, the mucosal application compositions of Comparative Examples 1-3 and Examples 1 and 2 are formulated to be applied directly to the mucosa without dilution, while the mucosal application compositions of Comparative Examples 4-8 and Examples 3-10 are formulated as concentrated mucosal application compositions that are diluted with water before use. 50 ml of the obtained mucosal application composition was placed in a beaker (50 ml capacity), and the metals shown in Tables 1 and 2 were immersed in it and left at room temperature for one day. The degree of metal corrosion after standing was observed. When corrosion occurs in the metal that has come into contact with the mucosal application composition, the metal dissolves into the mucosal application composition, causing browning and / or precipitate formation. Therefore, the degree of metal corrosion was evaluated based on the presence and degree of browning and precipitate formation in the mucosal application composition. Specifically, the corrosiveness was evaluated based on the following criteria.

[0038] ◎: Clear and uncolored (non-corrosive) ○: Slightly browned but clear (only slightly corrosive) △: Browned and with fine sediment (corrosive) △△: Browned and showing significant precipitate formation (moderately corrosive) ×: Dark brown coloration and more precipitate formation (highly corrosive). ××: It has turned a very dark brown and large precipitates have formed (it is quite corrosive).

[0039] [Table 1]

[0040] [Table 2]

[0041] As shown in the results in Tables 1 and 2 above, the mucosal application composition containing the indicated amount of sodium chloride showed corrosiveness to metals (Comparative Example 1), and the metal corrosiveness did not improve even when glycerin, a trihydric alcohol, was further added; in fact, it sometimes worsened (Comparative Examples 2 and 3). In concentrated mucosal application compositions with a high concentration of sodium chloride, the metal corrosiveness worsened particularly (Comparative Examples 4 to 8). In contrast, when propylene glycol, a dihydric alcohol, was added to the mucosal application composition containing the indicated amount of sodium chloride, the metal corrosiveness was significantly reduced (Examples 1 to 10). Furthermore, it was confirmed that the metal corrosiveness was significantly reduced when 1,3-butylene glycol, a dihydric alcohol, was added instead of propylene glycol, similar to Examples 1 to 10.

Claims

1. A composition for use on mucous membranes, comprising (A) an alkali metal chloride, (B) a dihydric alcohol, and (C) water, wherein the content of component (A) is 0.5 to 18% by weight.

2. The mucosal application composition according to claim 1, wherein the content of component (A) is 5 to 18% by weight.

3. The mucosal application composition according to claim 1 or 2, wherein the content of component (B) per 1 part by weight of component (A) is 0.1 parts by weight or more.

4. The mucosal application composition according to any one of claims 1 to 3, further comprising (D) a polyoxyethylene sorbitan fatty acid ester.

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