JP2013063961A - Topical anti-inflammatory analgesic preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a topical anti-inflammatory analgesic preparation that eliminates unevenness in coating when coating a composition filled in a roll-on container having a metal coating ball, enables effective coating of a medical component in a composition, and enhances improvement effects on lumbago, stiff shoulders and muscle pain.SOLUTION: The topical anti-inflammatory analgesic preparation includes: a liquid composition containing (A) an anti-inflammatory analgesic component, (B) a lower alcohol, and (C) menthol, wherein a content of the component (B) is 30-70 mass%; and the roll-on container having the metal coating ball filled with the composition.

Description

  The present invention relates to an external anti-inflammatory analgesic product in which a liquid composition is filled in a container having a metal-coated ball.

  There exists a thing made from sponge as an application | coating container which apply | coats a composition to an application | coating site | part. However, the sponge container may be worn and deteriorated due to friction during application, and sometimes breaks. In addition, dripping often occurs when used in the application target part, and contamination of clothing is a problem. If a small amount is applied in order to eliminate dripping, the application area is reduced, so that there is a problem that the active ingredient does not spread over the entire affected area and the effect is reduced. Moreover, the effect by the pressing pressure at the time of application is low. As a means for solving this, there is one in which the application part has a roll-on shape. However, this has a problem that uneven coating occurs during application. In view of the above, there has been a demand for a technique for eliminating coating unevenness at the time of coating a composition filled in a roll-on container having a coated ball.

Japanese Patent Application Laid-Open No. 2005-186997

  The present invention has been made in view of the above circumstances, eliminates uneven application during application of a composition filled in a roll-on container, can effectively apply medicinal components in the composition to the target application site, and lower back pain An object of the present invention is to provide an external anti-inflammatory analgesic product that improves the stiff shoulder and muscle pain improvement effects.

  As a result of intensive studies to achieve the above object, the inventors of the present invention contain (A) an anti-inflammatory analgesic component, (B) a lower alcohol and (C) menthol, and the content of the (B) component is 30 to 70 mass. % Liquid composition is filled in a roll-on container with metal-coated balls and applied to the target application site from a roll-on container with metal-coated balls, improving the stiffness and eliminating coating unevenness during application. As a result, it was found that (A) anti-inflammatory analgesic component in the composition can be effectively applied, and the improvement effect of lower back pain, stiff shoulders, and muscle pain has been dramatically improved, and the present invention has been made. It is a thing. Furthermore, it has been found that the above-described effect is further enhanced when the filled composition has a specific contact angle and wettability with the metal-coated ball material.

Accordingly, the present invention provides the following external anti-inflammatory analgesic products.
[1]. A liquid composition containing (A) an anti-inflammatory analgesic component, (B) a lower alcohol and (C) menthol, wherein the content of the component (B) is 30 to 70% by mass, and a metal coating filled with this liquid composition An external anti-inflammatory analgesic product comprising a roll-on container having a ball.
[2]. The external anti-inflammatory analgesic product according to [1], wherein the metal-coated ball is made of stainless steel.
[3]. The external anti-inflammatory analgesic product according to [1] or [2], wherein the liquid composition has a contact angle with the metal-coated ball material of 30 degrees or less and a wettability of 2.9 seconds or less.
[4]. The external anti-inflammatory analgesic product according to [1], [2] or [3], wherein the content of the component (A) is 0.5 to 10% by mass.
[5]. (C) External anti-inflammatory analgesic product in any one of [1]-[4] whose content of a component is 0.1-10 mass%.
[6]. The external anti-inflammatory analgesic product according to any one of [1] to [5], wherein the size of the metal-coated ball is 3 to 30 mmφ.

  According to the present invention, a composition containing an anti-inflammatory analgesic component that eliminates uneven application of the filled liquid composition to the target application site and dramatically improves low back pain, stiff shoulders, and muscle pain improvement effects. However, an external anti-inflammatory analgesic product filled in a roll-on container can be provided.

Hereinafter, the present invention will be described in detail.
The external anti-inflammatory analgesic product of the present invention comprises (A) an anti-inflammatory analgesic component, (B) a lower alcohol and (C) menthol, and (B) a liquid composition having a content of 30 to 70% by mass, And a roll-on container having a metal-coated ball filled with the liquid composition.

[Roll-on container with metal-coated balls]
A roll-on container having a coating ball has a coating ball that rotates, presses the coating ball against the portion to be coated, and rolls it to apply the filled composition to the portion to be coated. A roll-on container having a coating ball has an advantage that it can be easily applied without getting a hand dirty, but has a problem that uneven coating tends to occur. As the roll-on container, it is important to have an application ball, and the container body that stores the liquid is not particularly limited. As a container, what was described in Unexamined-Japanese-Patent No. 2005-186997 is mentioned, for example.

  The application ball portion is a metal application ball (metal sphere), and the shape is not particularly limited, but a shape close to a true sphere is preferable from the viewpoint of easy rotation. Moreover, the metal sphere which gave rust prevention or the antirust process is preferable. Even when combined with the liquid composition of the present invention when made of plastic, it is difficult to increase the contact angle and wettability, it becomes difficult to eliminate coating unevenness, and the desired effect of improving the stiffness is low. Moreover, there is a concern about deterioration such as cracking due to the liquid composition. In addition, the material of the metal coated ball is preferably stainless (steel) from the viewpoint of the effect of eliminating coating unevenness by the combination with the liquid composition of the present invention, the stability of the liquid composition, and the corrosiveness of the metal coated ball. As stainless steel, SUS201 (JIS standard, the same applies hereinafter), 202, 301, 302, 303, 304, 305, 316, 316L, 317, 329J1, 403, 405, 420, 430, 430LX, 630, titanium treatment, chrome treatment Etc. Among these, SUS304, SUS316, SUS316L, and titanium-treated metal spheres are preferable, and SUS304 is more preferable. Although the number of metal spheres may be one or more, one is preferable from the viewpoint of portability.

  The size of the metal-coated ball is appropriately selected according to the portion to be coated. For example, in the case of improving shoulder stiffness, 3 to 30 mmφ is preferable, 5 to 25 mmφ is more preferable, and 8 to 18 mmφ is further increased. preferable. If the diameter of the metal-coated ball is too small, the amount of liquid applied to the coating distance tends to be small, and the effect of improving the stiffness tends to be low. Since the distance (number of times) of roll finger pressure that stimulates is reduced, the pressing effect is not obtained so much and the stiffness improving effect tends to be low.

[Liquid composition]
The liquid composition of the present invention contains (A) an anti-inflammatory analgesic component, (B) a lower alcohol and (C) menthol, and the content of the (B) component is 30 to 70% by mass.

(A) Anti-inflammatory analgesic component (A) By mix | blending component (A), the liquid composition with which the roll-on container which has a metal application | coating ball | bowl was filled (henceforth abbreviated as the filled liquid composition may be abbreviate | omitted) is an application object. Can be applied evenly, resulting in an improvement in lower back pain, stiff shoulders, and muscle pain.
The anti-inflammatory analgesic component is not limited as long as it has an anti-inflammatory analgesic effect. Can be used singly or in appropriate combination of two or more. Among these, felbinac, diclofenac sodium, loxoprofen sodium and indomethacin are preferable.

  The amount of the component (A) that can be obtained with the drug varies and cannot be generally specified, but by setting it to 0.5% by mass or more in the composition, lower back pain, stiff shoulders, muscle pain The effect of improvement can be acquired more, 0.5-10 mass% is preferable, and 1-5 mass% is more preferable. Even if it exceeds 10 mass%, the effect is not so high, and it may be difficult to maintain the homogeneity of the composition.

(B) Lower alcohol Lower alcohol (1 to 4 carbon atoms) is not particularly limited, and examples thereof include ethyl alcohol, methyl alcohol, n-propyl alcohol, isopropyl alcohol, n-butyl alcohol, and 2-methyl. Examples include -1-propanol, 2-butanol, and 2-methyl-2-propanol. Among these, ethyl alcohol (ethanol) is preferable from the viewpoints of non-uniform coating, low back pain, shoulder stiffness, muscle pain improving effect, odor, irritation, and the like.

  (B) Content of a component is 30-70 mass% in a composition, and 40-70 mass% is more preferable. When the content of the component (B) is less than 30% by mass, the contact angle exceeds 30 degrees and uneven coating occurs. Moreover, there exists a possibility that the solubility of (A) anti-inflammatory analgesic component may worsen and the homogeneity of a liquid composition may not be maintained. On the other hand, if it exceeds 70% by mass, skin irritation may occur depending on the person.

(C) Menthol As menthol, well-known things, such as 1-menthol and dl-menthol, can be used, and it can be used individually by 1 type or in combination of 2 or more types. By blending the components (A) to (C) in combination, the liquid composition can be applied to the application target without uneven application, and the effect of improving lower back pain, shoulder stiffness and muscle pain is improved.

  (C) 0.1-10 mass% is preferable in a composition, as for content of a component, 0.5-8 mass% is more preferable, and 3-8 mass% is further more preferable. By setting it in such a range, it is possible to obtain more effects of improving application uniformity, low back pain, stiff shoulders, and muscle pain. In addition, when it exceeds 10 mass%, there exists a possibility that the homogeneity of a liquid composition may not be maintained.

  By setting it as the structure of this invention, the liquid composition with which this invention was filled can be apply | coated to an object without application | coating nonuniformity, and the stiffening improvement effect improves. In addition, the contact angle between the liquid composition and the metal-coated ball material (referring to the material of the metal-coated ball, which uses the same material plate as the metal-coated ball in the measurement of the contact angle and wettability of the present invention) is 30 degrees or less. The wettability is preferably 2.9 seconds or less. By setting it as such a range, an application | coating nonuniformity can be suppressed more. The lower limit is not particularly limited, but a contact angle of 10 degrees and a wettability of 0 seconds (already less than 15 degrees at the time of contact) can be selected.

  Selection of the contact angle and wettability with the metal-coated ball material as an index that allows the filled liquid composition of the present invention to be applied to the object without unevenness of application, and a contact angle of 30 degrees or less, wettability 2 It is a new finding of the present inventor that the object can be achieved by selecting 9 seconds or less. In addition, it is set as the liquid composition which contains (A) anti-inflammatory analgesic component of this invention, (B) lower alcohol, and (C) menthol, and content of (B) component is 30-70 mass%, The contact angle and wettability with the metal-coated ball material can be set within the above ranges.

  The contact angle is an index of the compatibility of the liquid composition and the metal-coated ball. When the contact angle exceeds 30 degrees, the liquid film becomes thick, and the liquid may be uneven and uneven and may be easily emitted. The wettability is an index of the ease with which the liquid composition spreads on the surface of the coated ball. By setting it to 2.9 seconds or less, the wettability spreads quickly on the surface, so that the liquid composition is applied to the coated ball of about 3 to 30 mmφ. Smoothly fed continuously, so that the liquid composition can be transferred continuously. The contact angle and wettability can be confirmed with a metal plate made of the same material as that of the metal-coated ball. However, by making the contact angle and wettability range, a container having a metal-coated ball of about 3 to 30 mmφ is used. It was found that application unevenness to the target application site of the liquid composition was eliminated when applied.

The contact angle is determined by the following measurement method.
The contact angle is measured by a contact angle measuring device according to a conventional method. From the droplet image captured by the CCD camera, the boundary between solids / gas-liquid is automatically determined, curve fitting is performed, and the contact angle is measured. When the liquid composition is dropped onto a metal plate made of the same material as the metal-coated ball at a flow rate of 6 μL / s from a height of about 4 mm, the left and right contacts of the liquid composition immediately after contact with the metal plate Measure the angle. From the measured results, the average contact angle on the left and right is recorded in 10 degree increments, and this is defined as the contact angle of the preparation. For example, 10 degrees is 4.5 to 14.4 degrees.

The wettability is determined by the following measurement method.
The time (seconds) from when the contact angle started to be measured until the left and right average contact angles were less than 15 degrees was defined as wettability.

  The liquid composition of the present invention is preferably such that the entire liquid composition is homogeneous as a solution, suspension, or emulsion. By doing in this way, the improvement effect of a back pain, a stiff shoulder, and a muscular pain can be ensured from the beginning of use until the use is completed, and the effect can be maintained uniformly. In the present invention, “homogeneous” means that the components, density, quality, etc. are uniform and uniform.

  In the liquid composition of the present invention, one kind of drugs and additives other than the component (A), which are usually used in low back pain, stiff shoulders, anti-inflammatory analgesic compositions, are used as long as the effects of the present invention are not impaired. It can mix | blend individually or in combination of 2 or more types as appropriate. When there are many components other than blood flow promoting components such as arnica tincture, anti-inflammatory analgesic components, lower alcohols, and menthol, not only is it difficult to prepare a homogeneous liquid composition, but the contact angle and wettability to the metal-coated ball material are also increased. descend.

  Examples of the refreshing agent include essential oils such as camphor, dl-camphor, peppermint oil, spearmint oil, and peppermint oil.

  The surfactant is not particularly limited as long as it is a surfactant used in general external preparations such as cosmetics, pharmaceuticals, and quasi drugs. Examples of the lipophilic nonionic surfactant include glycerin fatty acid ester, alkyl glyceryl ether, polyoxyethylene glycerin fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene sorbit fatty acid ester, polyoxyethylene hydrogenated castor Oil, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil fatty acid ester, polyglycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, propylene glycol fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene Polyoxypropylene copolymer, polyoxyethylene alkylphenyl ether, polyoxyethylene Le bit beeswax, and include sucrose fatty acid esters and the like. The hydrophilic nonionic surfactant is not particularly limited as long as it is a hydrophilic nonionic surfactant used in general external preparations such as cosmetics, pharmaceuticals, and quasi drugs. For example, self-emulsifying glycerin Fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene sorbit fatty acid ester, polyoxyethylene lanolin, polyoxyethylene lanolin alcohol, polyoxyethylene phytosterol, polyoxyethylene phytostanol, polyoxyethylene core Stanol ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyglycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, propylene Glycol fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene alkylphenyl ether, and sucrose fatty acid ester (sucrose stearate ester, sucrose palmitate ester, sucrose palmitate ester, Sugar myristic acid ester, succinic acid oleic acid ester, sucrose lauric acid ester) and the like. A combination of these can also be used. In addition to the aforementioned nonionic surfactants, fatty acid soaps such as sodium laurate and sodium palmitate, sulfates such as sodium lauryl sulfate and sodium POE lauryl sulfate, sodium lauroyl sarcosine, sodium cocoyl-N-methyltaurate, Examples include acylated amino acid salts such as sodium lauryl glutamate, anionic surfactants such as phosphate ester salts such as sodium monolauryl phosphate, and cationic surfactants such as quaternary ammonium salts. Of these, nonionic surfactants are preferred as the surfactant.

  The higher alcohol is not particularly limited, and examples thereof include myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, oleyl alcohol, cetostearyl alcohol, octyldodecanol and the like.

  The higher fatty acid is not particularly limited, and examples thereof include lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, and behenic acid.

  The sterols are not particularly limited. For example, animal sterols such as cholesterol, cholestanol, lanosterol, and dehydrocholesterol, plant sterols such as β-sitosterol, stigmasterol, campesterol, and ergosterol, myco Examples include sterols derived from microorganisms such as sterol and timosterol. These may be used as they are or may be subjected to chemical treatment such as hydrogenation for stabilization.

  Oily components include hydrocarbons such as squalane and liquid paraffin, vegetable oils such as olive oil, macadamian nut oil, jojoba oil, animal oils such as beef tallow, cetyl palmitate, isopropyl myristate, myristyl myristate, phytosteryl hydroxystearate, Examples thereof include polyglycerin fatty acid esters, esters such as polycondensates such as (hydroxystearic acid / stearic acid / eicosandioic acid) polyglyceryl, and silicones such as dimethyl silicone, phenylmethyl silicone, and cyclomethicone.

  Examples of the polyhydric alcohol include polyethylene glycol, propylene glycol, 1,3-butylene glycol, dipropylene glycol, glycerin and the like. Among these, 1,3-butylene glycol is preferable from the viewpoint of suppressing coating unevenness. Propylene glycol is not preferable because it is not sticky and feels bad to use, and a liquid composition containing no propylene glycol is preferred.

  Examples of the solvent include water. 15-65 mass% is preferable in a composition, and, as for content at the time of mix | blending water, 25-60 mass% is more preferable.

  In consideration of contamination of clothing, pigments are often not blended, but legal pigments (dyes, pigments, lakes) and the like can be blended as necessary.

  Examples of the fragrances include essential oils and synthetic fragrances. Examples include essential oils such as eucalyptus oil, lavender oil, rosemary oil, lemon oil, orange oil and grapefruit oil, and synthetic fragrances such as lavender fragrance, herb fragrance, rosemary fragrance, citrus fragrance and grapefruit fragrance.

  Examples of preservatives include parabens and sodium benzoate.

  Examples of the viscosity modifier include water-soluble polymers such as hydroxypropylmethylcellulose, hyaluronic acid, polyvinyl alcohol, carboxyvinyl polymer, carrageenan, xanthan gum, and pullulan.

  pH adjusters / buffers include organic acids such as citric acid, lactic acid and malic acid, inorganic acids such as hydrochloric acid, phosphoric acid and boric acid, sodium citrate, sodium hydroxide, triethanolamine, diethanolamine, monoethanolamine , Diisopropanolamine, trometamol and the like. The pH of the liquid composition of the present invention is preferably 5-9.

  Other topical stimulants such as nonylic acid vanillyl amide, lactyl menthyl and cantharis tincture, benzyl nicotinate, nicotinic acid benzyl ester, capsaicin, chili pepper tincture, carpronium chloride, herb extract such as assembly extract, herbal ingredients such as salamander extract , Anti-inflammatory agents such as glycyrrhetinic acid, glycyrrhizic acid, glycyrrhizin, guaiazulene, NMF components such as amino acids, water-soluble collagen, elastin, glycyrrhizic acid, salicylic acid, glycyrrhetinic acid, ceramide and other skin roughening agents, pantothenic acid, tocopherol, tocopherol acetate , Vitamin E, vitamin E acetate, retinol, vitamin A acid and other anti-aging agents, various vitamins and their derivatives, ascorbic acid, ascorbyl palmitate, ascorbyl stearate Ascorbyl tetraisopalmitate, ascorbic acid glucoside, arbutin, can be mentioned ellagic acid, rucinol, glycine zinc complex, whitening agents such as tranexamic acid and its derivatives, sodium edetate hydrate such as a chelating agent.

  The amount of the components other than (A), (B) and (C) described above is preferably 50% by mass or less, more preferably 20% by mass or less, and further preferably 15% by mass or less in the composition.

  Although the preparation method of the liquid composition of this invention is not specifically limited, For example, it can obtain by mixing with normal stirring and emulsification apparatuses, such as a paddle mixer and a homomixer.

  The liquid composition of the present invention is suitable as an external anti-inflammatory analgesic composition, and is also suitable as a liquid composition for filling a roll-on container having a metal-coated ball. In addition, the roll-on container which has a metal application | coating ball | bowl is as having mentioned above.

[External anti-inflammatory analgesic product]
In the present invention, the external anti-inflammatory analgesic product refers to a product provided with the liquid composition and a roll-on container having a metal-coated ball filled with the liquid composition. The effects include lower back pain, muscle pain, stiffness reduction and improvement. Stiffness is not particularly limited, such as lower back stiffness, stiff shoulders, stiff feet, etc. It can be demonstrated.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, unless otherwise specified, “%” in the composition represents mass%, and each component amount in the table represents AI.

[Examples 1 to 27, Comparative Examples 1 to 5]
A liquid composition having a composition shown in Tables 1 to 8 (which was in the range of pH 5 to 9 at 25 ° C.) was prepared and filled into a roll-on container (made of polypropylene) having one coated ball in the table. did.
The following measurement and evaluation were performed about the liquid composition after filling. The results are also shown in the table.

(1) Contact angle When the liquid composition is dropped onto a metal plate (size 50 mm × 50 mm, thickness 1 mm) of the same material as the metal-coated ball at a flow rate of 6 μL / s from a height of about 4 mm at a flow rate of 6 μL. The right and left contact angles of the liquid composition immediately after contact with the metal plate were measured. As the contact angle measuring device, EKO INSTRUMENTS Co., Ltd. automatic contact angle measuring device OCA series was used. The left and right average contact angles are recorded in 10 degree increments. For example, 10 degrees is 4.5 to 14.4 degrees.

(2) Wettability The time (seconds) from when the contact angle began to be measured until the left and right average contact angles were less than 15 degrees was measured in increments of 0.1 seconds.

(3) Application unevenness The test subject (5 persons) applied the liquid composition filled in the container 10 times at a distance of about 15 cm. The coating unevenness at that time was confirmed to be that the liquid continued (no coating unevenness) or the liquid did not continue (coating unevenness). In addition, the thing in which dripping was recognized is set as x even if coating nonuniformity is not observed. A result is shown by the following evaluation criteria.
<Evaluation criteria>
A: No coating unevenness was observed in all subjects.
○: There were more subjects whose application unevenness was not observed.
(Triangle | delta): There were many subjects whose application | coating nonuniformity was observed.
X: Application unevenness was observed / drip was observed in all subjects.

(4) Shoulder stiffness improvement Five subjects who measured the coating unevenness evaluated the shoulder stiffness improvement effect by the following 7-step evaluation after the feeling of use disappeared. The results are shown as the average score of 5 people.
<Evaluation criteria for stiff shoulder improvement>
7: Very satisfied 6: Very satisfied 5: Somewhat satisfied 4: Neither satisfied 3: Somewhat dissatisfied 2: Somewhat dissatisfied 1: Very dissatisfied

  The liquid composition of Example 1 was measured and evaluated in the same manner as in Example with a polypropylene (PP) and polyethylene (PE) plastic plate (made by Hosokawa Seisakusho, material-like surface, size 50 mm × 50 mm, thickness 3 mm). (The size of the coated ball was 11.1 mm in diameter). The results are shown in the table below.

Claims (6)

  A liquid composition containing (A) an anti-inflammatory analgesic component, (B) a lower alcohol and (C) menthol, wherein the content of the component (B) is 30 to 70% by mass, and a metal coating filled with this liquid composition An external anti-inflammatory analgesic product comprising a roll-on container having a ball.   The external anti-inflammatory analgesic product according to claim 1, wherein the metal-coated ball is made of stainless steel.   The external anti-inflammatory analgesic product according to claim 1 or 2, wherein the liquid composition has a contact angle with the metal-coated ball material of 30 degrees or less and a wettability of 2.9 seconds or less.   The external anti-inflammatory analgesic product according to claim 1, wherein the content of the component (A) is 0.5 to 10% by mass.   (C) Content of a component is 0.1-10 mass%, The anti-inflammatory analgesic product for external use of any one of Claims 1-4.   The external anti-inflammatory analgesic product according to any one of claims 1 to 5, wherein the metal-coated ball has a size of 3 to 30 mmφ.