Spray-type external composition

Abstract

To provide a spray-type external composition that is free from stickiness, obtains a sufficient moisturizing effect by combining heparinoid, a specific amount of surfactant and a specific amount of oil solution, and furthermore, can realize very fine droplets in both of a solubilization type and an emulsification type, solves a problem on spray of uniformly spraying a cosmetic on entire face, and also has excellent stability.SOLUTION: A spray-type external composition is constituted of the following components (A) to (C): (A) heparinoid, (B) surfactant, and (C) oil solution, where a content mass ratio B / C between component B and component is 1 to 20.SELECTED DRAWING: Figure 1

Description

[Technical Field]

[0001] The present invention relates to a spray-type external composition, whether solubilized or emulsified, that can produce very fine droplets and has excellent stability and moisturizing properties. [Background technology]

[0002] Heparinoids are used as active ingredients in topical skin preparations because they have excellent moisturizing, blood circulation promoting, and anti-inflammatory effects. While milk and cream types have been the mainstream of topical preparations containing heparinoids, in recent years, the variety of formulations has expanded to include foam types and other types (see, for example, Patent Documents 1 and 2). Spray-type formulations are excellent in usability because they can be sprayed evenly regardless of the contours of the face and can be applied to the desired area, and the fact that they can be sprayed without touching the hands and fingers is also advantageous from the perspective of preventing viral infections. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Patent Publication No. 2016-180012 [Patent Document 2] Patent Publication No. 2020-59756 Summary of the Invention [Problem to be solved by the invention]

[0004] However, so-called spray-type cosmetics containing heparinoids have the problem that unless they adhere to the skin surface as fine droplets, they lack uniformity, making it difficult to feel a sufficient moisturizing effect compared to formulations that are normally sprayed. Therefore, when high concentrations of polyhydric alcohols or water-soluble polymers are added to enhance moisturizing effects, it is sometimes difficult to form fine droplets and spray evenly. There are also concerns about a decrease in the feel of use, such as stickiness and a decrease in penetration. On the other hand, when oils are added and emulsified with surfactants to enhance moisturizing effects, the viscosity can increase, making the product difficult to spray, or, conversely, the viscosity can be low, causing creaming. In spray-type formulations containing heparinoids, formulation technologies that combine heparinoids with oils and surfactants to enhance moisturizing effects have not been explored. [Means for solving the problem]

[0005] In view of this situation, the present inventors have conducted extensive research and found that by combining a heparinoid, a surfactant, and an oil in a specific content ratio, a sufficient moisturizing effect can be obtained without stickiness. Furthermore, the inventors have found that, by realizing extremely fine droplets in both the solubilized and emulsified types, it is possible to solve the problem of spraying a spray-type topical composition evenly over the entire face and to obtain a spray-type topical composition with excellent stability.

[0006] That is, the present invention provides the following. [1] The following components (A) to (C): (A) Heparinoids (B) Surfactant (C) Oil The spray-type external composition is composed of the above, and the content ratio B / C of component (B) to component (C) is 1 to 20. [2] When the topical composition is filled into a spray container and sprayed horizontally, the angle between a horizontal line from the nozzle and a line connecting the nozzle and the highest point of the mist 200 mm horizontally above the nozzle is 15 degrees or more. [3] The spray-type external composition contains the component (B) in an amount of 0.01 to 1% by mass. [4] The spray-type external composition contains the component (C) in an amount of 0.01 to 1% by mass. [5] The component (B) is a nonionic surfactant having an HLB of 11 or more. [6] A spray-type external composition in which the component (C) has a molecular weight of 500 or less. [7] The spray-type external composition is a spray-type composition, wherein the spray-type container is an aerosol-type container. [Effects of the Invention]

[0007] According to the present invention, a spray-type external composition can be provided which, whether solubilized or emulsified, can produce very fine droplets when sprayed, thereby enabling uniform spraying onto the skin, and which has excellent moisturizing properties and stability. [Brief explanation of the drawings]

[0008] [Figure 1] FIG. 1 is a diagram showing the spread of mist from the spray-type external composition of the present invention. DETAILED DESCRIPTION OF THE INVENTION

[0009] The present invention will be described in detail below. In this specification, the symbol "to" means a range including the numerical values ​​before and after it. The term "spray-type external composition" as used herein refers to an external composition that is filled into a non-aerosol or aerosol container and used.

[0010] The spray-type topical composition of the present invention is not particularly limited as long as it is applied to the skin. Specifically, it may be in the form of any of a pharmaceutical product, a quasi-drug, or a cosmetic, and is preferably a quasi-drug.

[0011] Component (A) Heparinoid The heparinoid (component (A)) used in the present invention is a polysulfated ester of mucopolysaccharide, specifically cellulose sulfate, chitin sulfate, chitosan sulfate, pectin sulfate, chondroitin sulfate, inulin sulfate, alginate sulfate, glycogen sulfate, starch sulfate, polyvinyl alcohol sulfate, polyglucose sulfate, polylactose sulfate, laminarin sulfate, galactan sulfate, levan sulfate, and polysulfates thereof and salts thereof. Heparinoids are known to have moisturizing and blood circulation-promoting effects. In the present invention, heparinoids described in the Japanese Pharmacopoeia 2002 Standards for Pharmaceuticals and Medical Devices are preferably used. The heparinoids defined in the Japanese Pharmacopoeia Standards for Pharmaceuticals and Medical Devices are primarily composed of polysulfated esters of chondroitin sulfate.

[0012] The amount of organic sulfate groups in the heparinoid is not particularly limited, and any can be used, but the amount of organic sulfate groups is preferably 20 to 40% by mass (hereinafter simply abbreviated as %) from the viewpoints of moisturizing effect, usability, etc. The amount of organic sulfate groups in component (A) in the present invention can be measured by the method described in the quantitative determination method for "heparinoids" in the Japanese Pharmacopoeia Non-Drug Standards 2002.

[0013] The content of component (A) in the present invention is not particularly limited, but is preferably 0.01% or more, more preferably 0.1% or more, and preferably 0.5% or less, based on the total amount of the spray-type topical composition. This range is more preferable because it provides a non-sticky and more excellent moisturizing effect.

[0014] Component (B) Surfactant The surfactant, component (B) used in the present invention, is not particularly limited, and any surfactant commonly used in cosmetics can be used, including nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants. While the type of surfactant is not particularly limited, from the viewpoint of stability over time, it is preferable to use a nonionic surfactant with an HLB of 11 or higher, and more preferably an HLB of 13 or higher. The HLB (Hydrophile-Lipophile Balance) used in the present invention is an index showing the balance between hydrophilicity and lipophilicity, and is calculated by Oda and Teramura et al. using the following formula (1): HLB = inorganic value (IV) / organic value (OV) × 10 (Equation 1) (See Yoshio Koda, "Organic Conceptual Diagram - Fundamentals and Applications", pp. 11-17, Sankyo Publishing, 1984)

[0015] Specific examples include polyoxyethylene alkyl ether phosphate, alkyltrimethylammonium chloride, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, polyoxyethylene sorbitan fatty acid ester, etc., with polyoxyethylene hydrogenated castor oil being more preferred. Preferred examples of surfactants include polyoxyethylene (60 mol) hydrogenated castor oil (HLB 14), polyoxyethylene (80 mol) hydrogenated castor oil (HLB 15), polyoxyethylene hydrogenated castor oil monoisostearate (50 E.O.) (HLB 12), etc. One or more of these can be appropriately selected and used.

[0016] The content of component (B) in the present invention is not particularly limited, but is preferably 1% or less, more preferably 0.01% or more, and even more preferably 0.1% or more, based on the total amount of the topical composition. This range is preferable because it allows for less stickiness and allows for the formation of very fine droplets.

[0017] Component (C) Oil The oily agent of component (C) used in the present invention is not particularly limited as long as it is one that is commonly used in ordinary cosmetics and the like, and examples thereof include hydrocarbons, oils and fats, waxes, esters, fatty acids, silicone oils, fluorine-based oils, and the like, regardless of their physical properties such as solid, paste, or liquid, their polarity or non-polarity, and their origins such as vegetable oil, mineral oil, or synthetic oil. However, in order to reduce stickiness when sprayed onto the skin and to improve stability over time, it is preferable for the molecular weight to be 500 or less, and more preferably 400 or less.

[0018] In the present invention, specific examples of the component (C) oil include propylene glycol dicaprate, cetyl 2-ethylhexanoate, glyceryl tri-2-ethylhexanoate, isopropyl myristate, isopropyl palmitate, di-2-ethylhexyl succinate, glyceryl tri(caprylate-caprate), cetyl octanoate, isotridecyl isononanoate, myristyl lactate, dialkyl carbonate, etc. One or more of these may be appropriately selected and used.

[0019] The content of component (C) in the present invention is not particularly limited, but is preferably 1% or less, more preferably 0.01% or more, and even more preferably 0.1% or more, based on the total amount of the topical composition. This range is preferred because it provides better moisturizing properties and stability over time.

[0020] In the present invention, the mass ratio B / C of components (B) and (C) is 1 to 20. If it is outside this range, the stability over time will be poor and it will be difficult to achieve very fine droplets. In order to improve the stability over time and achieve very fine droplets, the mass ratio B / C is preferably 1.5 to 10.

[0021] In addition to the above components (A) to (C), the topical composition of the present invention may contain other bases and additives, such as water, emulsifying aids, moisturizing agents, UV absorbers, anti-fading agents, antioxidants, preservatives, cosmetic ingredients, and fragrances, as appropriate, within the scope of the present invention.

[0022] The water is not particularly limited as long as it is commonly used in cosmetics and the like, but examples thereof include purified water, hot spring water, ion-exchanged water, deep sea water, tap water, or steam-distilled water from plants as a base, and one or more types can be appropriately selected and used as needed. Other bases include glycols such as propylene glycol, 1,3-butylene glycol, dipropylene glycol, and polyethylene glycol; sugar alcohols such as glycerin, diglycerin, and polyglycerin; sorbitol, maltitol, and glucose; and lower alcohols such as ethanol. Preservatives include parahydroxybenzoic acid esters and phenoxyethanol. Additives include antioxidants such as tocopherol and ascorbic acid, anti-inflammatory agents such as dipotassium glycyrrhizinate and allantoin, and moisturizing amino acids such as L-arginine, L-aspartic acid, DL-alanine, glycine, L-serine, and L-theanine.

[0023] The topical composition of the present invention may be in the form of a solubilized or emulsified formulation, and is preferably in a liquid form, specifically, one having a viscosity of 1000 mPa·S or less at 25°C as measured using a Brookfield rotational viscometer.

[0024] The method for producing the topical skin preparation of the present invention is not particularly limited, and it can be prepared by a conventional method. For example, a method can be mentioned in which components (B) and (C) are mixed and dissolved in a solution in which (A) has been dissolved, and then added, and any optional components are added and mixed thereto to prepare the preparation.

[0025] The spray-type topical composition of the present invention is characterized by producing very fine droplets when sprayed from a container having a spray mechanism under conditions suitable for spraying onto the face. However, since it is extremely difficult to measure the particle size of the sprayed droplets, this is substituted by measuring the state of the sprayed mist. The topical composition of the present invention is preferably a topical composition filled in a container in which the angle between the spray direction from the nozzle of the container and the highest point 200 mm vertically above the spray direction is 15 degrees or more. By making the droplets of the spray-type topical composition very fine, the angle becomes 15 degrees or more, allowing for more uniform spraying over the entire face. Measurements are taken five times consecutively, and the average value is calculated by excluding the maximum and minimum values.

[0026] To evaluate the sprayability of the present invention, a Z-155-C110 container manufactured by Takemoto Container Co., Ltd. was used to fill the sample. The container containing the sample was placed on a horizontal surface, and the pressing part of the container was pressed with an average load of 800 to 1000 g for 0.4 seconds to eject the topical composition.

[0027] To evaluate the sprayability of the present invention, the spray state of the topical composition is filmed with a camera. The camera is installed at the same height as the nozzle of the container. The camera is fixed at a position 150 mm horizontally from the nozzle in the spray direction and 500 mm vertically from the nozzle, the sample is sprayed, and the sprayed mist is filmed with the camera. The frame rate of the camera used is 30 FPS. An image taken 0.4 seconds after spraying is selected and a still image (2048 x 1536 pixels) is extracted.

[0028] The extracted image is analyzed using the image analysis software "PHOTOSHOP ELEMENT VER.11.0 (ADOBE)" to measure the fog state. Using this software, the captured image is converted to grayscale, the contrast is adjusted (+50), and the image is converted to two gradations (threshold 60). In the image processed by this software, the angle of the fog spread in the vertical direction above, 200 mm from the nozzle, is measured as shown in Figure 1.

[0029] The type of container for spraying the topical composition of the present invention may be either non-aerosol or aerosol, but the effects of the present invention are more pronounced in non-aerosol containers because they can be sprayed over the entire face without the use of a propellant. [Example]

[0030] The effects of the present invention will be explained using the following examples and comparative examples, although the technical scope of the present invention is not limited to the following examples.

[0031] Examples 1 to 8 and Comparative Examples 1 to 5: Aerosol-type topical compositions The compositions shown in Tables 1 and 2 were prepared, and the spray angle, moisture retention, non-stickiness, and presence or absence of separation of the samples were evaluated by the following methods. The results are shown in Table 1.

[0032] [Table 1]

[0033] [Table 2] Note 1: EMALEX RWIS 150 (manufactured by Nippon Emulsion Co., Ltd.) Note 2: NIKKOL HCO-60 (manufactured by Nikko Chemicals Co., Ltd.) Note 3: Heparinoid (Maruho Co., Ltd.) Note 4: NIKKOL IPM-EX (manufactured by Nikko Chemicals Co., Ltd.) Note 5: Hicall K-230 (manufactured by Kaneda Co., Ltd.)

[0034] (Method of manufacturing a spray-type external composition) A: Mix and dissolve components (1) to (4) and components (10) to (14). B: Mix and dissolve components (5) to (9) at 60°C. C: B was added to A and mixed uniformly to obtain a sample.

[0035] (Evaluation methods 1 and 2: Moisture retention, non-stickiness) The moisturizing effect and non-stickiness were tested by a panel of five cosmetic evaluation specialists. The obtained samples were placed in Z-155-C110 containers manufactured by Takemoto Container Co., Ltd., and each sample was sprayed three times over the entire face. Each panelist then rated the moisturizing effect and non-stickiness after use on a four-point scale using the absolute evaluation below, and the average was calculated from the total scores of all panelists for each sample, and judged according to the four-point scale below.

[0036] (moisturizing properties) <Absolute evaluation criteria> (Rating): (Evaluation) 4 points: Strong moisturizing feeling 3 points: Moisturizing 2 points: Weak moisturizing feeling 1 point: No moisturizing sensation <4-level evaluation criteria> (Judgment): (Average score) ◎: Over 3.25 points: Very good ○: Over 2.5 points, 3.25 points or less: Good △: Over 1.75 points and 2.5 points or less: Slightly poor × : 1.75 points or less : Defective

[0037] (non-sticky) <Absolute evaluation criteria> (Rating): (Evaluation) 4 points: No stickiness on the skin 3 points: Not too sticky on the skin 2 points: Skin feels slightly sticky 1 point: Skin feels sticky <4-level evaluation criteria> (Judgment): (Average score) ◎: Over 3.25 points: Very good ○: Over 2.5 points, 3.25 points or less: Good △: Over 1.75 points and 2.5 points or less: Slightly poor × : 1.75 points or less : Defective

[0038] (Evaluation method 3: droplet fineness) The obtained sample was placed in a Z-155-C110 container manufactured by Takemoto Container Co., Ltd. The container containing the sample was placed on a horizontal surface, and the pressing part of the container was pressed with an average load of 800 to 1000 g for 0.4 seconds to eject the sample. The camera was installed at the same height as the nozzle of the container. The camera was fixed 150 mm horizontally and 500 mm vertically from the nozzle. The sample was ejected, and the ejected mist was captured as a video. The frame rate of the camera used was 30 FPS. An image taken 0.4 seconds after ejection was selected and a still image (2048 x 1536 pixels) was extracted. The extracted image was used to measure the mist state using image analysis software (Adobe Photoshop Element Ver. 11.0). Using the image analysis software PHOTOSHOP ELEMENT VER.11.0 made by ADOBE, the captured image was converted to grayscale, and the contrast was adjusted (+50), and two-tone (threshold 60) was used to capture the image 200 mm from the nozzle. The angle of the fog spread in the vertical direction above the point was measured. Measurements were taken five times consecutively, and the average value was calculated excluding the maximum and minimum values.

[0039] 4-level evaluation criteria (Judgment): (Judgment criteria) A: The mist spread angle is 20 degrees or more B: The mist spread angle is between 15 degrees and 20 degrees C: The mist spread angle is between 10 degrees and 15 degrees D: The mist spread angle is less than 10 degrees

[0040] (Evaluation method 4: Stability over time (50°C / 1 month)) The stability over time was evaluated by storing the samples in Z-155-C110 containers manufactured by Takemoto Container Co., Ltd. at a constant temperature of 50°C for one month, then visually inspecting the samples and evaluating the stability according to the following two-stage evaluation criteria.

[0041] Two-stage evaluation criteria [Judgment]:[Evaluation] ○: No separation observed ×: Separation is observed

[0042] As is clear from the results in Tables 1 and 2, the samples of Examples 1 to 8 of the present invention were superior in moisturizing properties and non-stickiness compared to the samples of Comparative Examples 1 to 5, and also in droplet size and stability over time.

[0043] In contrast, Comparative Example 1, which did not contain component (A), had insufficient moisturizing properties. Furthermore, it was not possible to prepare a sample from Comparative Example 2, which did not contain component (B). Comparative Example 3, in which the amounts of component (B) and component (C) exceeded the appropriate ranges, did not provide a satisfactory level of non-stickiness. Comparative Example 4, which did not contain component (C), had insufficient droplet fineness and moisturizing properties. Comparative Example 5, in which the amounts of component (B) and component (C) were below the appropriate ranges, did not maintain stability over time.

[0044] Example 9: Aerosol-type topical composition (Undiluted solution components) (%) (1) Heparinoid 0.3 (2) Polyoxyethylene hydrogenated castor oil 0.2 (3) Isostearic acid 0.15 (4) Phytosterol 0.005 (5) Isopropyl myristate 0.05 (6) Tocopherol 0.001 (7) Dipropylene glycol 10 (8) Ethanol 5 (9) Methylparaben 0.15 (10) Glyceryl-N-(2-methacryloyloxyethyl)carbamate-stearyl methacrylate copolymer 0.05 (11) Glycerin 1 (12) L-Theanine 0.005 (13) Purified water remainder

[0045] (Manufacturing method) A: Mix ingredients (1), (10) to (12) uniformly with a portion of (13). B: Mix and dissolve components (2) to (7) at 80°C. C: Add B to a portion of (13) heated to 80°C and mix evenly. D: (8) and (9) are mixed uniformly. E: A, C, and D were mixed uniformly to obtain a sample. 50 g of the stock solution was filled into an aluminum pressure-resistant container, the valve was then fixed, and nitrogen was filled in until the product pressure was 0.7 MPa, to obtain an aerosol sample.

Claims

1. The following components (A) to (C): (A) Heparinoids (B) Surfactant (C) Oil A spray-type external composition containing the above components, wherein the mass ratio B / C of the components (B) to (C) is 1 to 20.

2. A spray-type topical composition according to claim 1, wherein when the topical composition is filled into a spray-type container and sprayed horizontally, the angle formed by a horizontal line from the nozzle and a line connecting the nozzle and the highest point of the mist 200 mm horizontally above the nozzle is 15 degrees or more.

3. 2. The spray-type external composition according to claim 1, wherein the content of component (B) is 0.01 to 1% by mass.

4. 2. The spray-type external composition according to claim 1, wherein the content of component (C) is 0.01 to 1% by mass.

5. 2. The spray-type external composition according to claim 1, wherein the component (B) is a nonionic surfactant having an HLB of 11 or more.

6. 2. The spray-type external composition according to claim 1, wherein the component (C) has a molecular weight of 500 or less.

7. The spray-type external composition according to any one of claims 2 to 6, wherein the spray-type container is an aerosol-type container.

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