JP2010018550A - Liniment for skin - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a liniment for the skin, precisely exhibiting antiinflammatory effects and antiallergic effects by using mangosteens having useful physiological effects and clarifying the proper added amount. <P>SOLUTION: The liniment for the skin contains a chitosan derivative mixture containing α-mangosteen in an amount of from 1 μmol to 100 mmol based on 1 kg of a base for the liniment for the skin. It is shown in the examples 1 to 6 that large therapeutic effects are exhibited when the liniments for the skin are used, and it is determined that significant therapeutic effects against contact dermatitis, bedsore and allergic inflammatory are present. As a result, it is cleared that the content of ≥1 μmol of the chitosan derivative mixture containing the α-mangosteen based on 1 kg of the base for the liniment for the skin is required. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to a skin application agent that can relieve skin symptoms such as diaper rash, bed slipping, and atopic dermatitis, and more particularly to a skin application agent having an anti-inflammatory effect.

  Conventionally, skin treatments containing corticosteroids have been widely used for the treatment of skin diseases, particularly intractable skin diseases such as atopic dermatitis and contact dermatitis, and their pharmacological effects are high. It is known. However, corticosteroids may cause side effects on the application site, and drugs absorbed transdermally may cause systemic side effects. is needed. For this reason, there is a need for a skin application agent that has few side effects and has an equivalent or better therapeutic effect on skin diseases, in place of corticosteroids.

  As an application agent for skin replacing such a corticosteroid, Patent Document 1 discloses an invention of an external skin ointment characterized by comprising a gelled hydrocarbon base, vitamin E and squalane.

On the other hand, Patent Document 2 discloses that a mangosteen extract mainly composed of α-mangosteen, β-mangosteen, and γ-mangosteen extracted from the fruit mangosteen peel is useful for anti-inflammatory action and anti-allergic action. It describes that it has a physiological effect (medicine effect), and discloses an invention of a mangosteen preparation in which such a mangosteen extract is dispersed in an aqueous ethanol solution of 40% or less.
JP-A-10-087487 JP 2007-106674 A

  However, in the technique described in Patent Document 2, a physiological effect useful when a mangosteen extract mainly composed of α-mangosteen, β-mangostin, and γ-mangosteen is dispersed in an aqueous ethanol solution at what concentration. Is not described, and a specific production method and composition of a mangosteen preparation capable of surely obtaining an anti-inflammatory action / anti-allergic action is not shown. Therefore, the mangosteen extract is very expensive, and there is a risk of side effects if the specific content is not appropriately determined. Therefore, there is a problem that a practical mangosteen preparation cannot be produced. .

  Therefore, the present invention has been made to solve such a problem, and by using mangosteens having a useful physiological action, the appropriate addition amount is clarified, so that it is possible to reliably prevent the low price. It is an object of the present invention to provide a skin coating agent capable of obtaining an inflammatory effect and an antiallergic effect.

  The skin application agent according to the invention of claim 1 is a skin application agent applied to the skin in order to relieve skin symptoms, and α-mangosteen or α is applied to 1 kg of the skin application agent base. -A xanthone derivative mixture containing mangosteen is contained in the range of 1 µmol to 500 mmol, more preferably in the range of 10 µmol to 10 mmol.

  Here, α-mangostin is a kind of xanthone derivative, and the xanthone derivative is a kind of polyphenol and has a useful physiological action including an antioxidant action. The mangosteen extract mainly composed of α-mangostin, β-mangostin, and γ-mangosteen is a xanthone derivative having a xanthone skeleton, and in this specification, claims, and abstract, it is referred to as “xanthone derivative”. The term is used almost synonymously with the term “mangosteens”.

  In addition, examples of “skin symptoms” include rash, itching, eczema, hives, rough skin, rash, sore, moist, diaper rash, bedsores, atopic dermatitis, contact dermatitis, drug eruption, psoriasis, etc. it can. Furthermore, as a “skin coating base”, as a hydrophobic (oil-based) base, petrolatum (yellow petrolatum, white petrolatum), paraffin, plastibase, beeswax, etc. and additives such as glycol, glycerin, etc. Examples of those added and hydrophilic bases include emulsion bases (creams), water-soluble bases, suspension bases (jelly gels), and the like.

  The skin coating agent according to the invention of claim 2 is the structure of claim 1, wherein the base for skin coating agent is 60 parts by weight to 100 parts by weight, more preferably 70 parts by weight to 90 parts by weight, And glycol (diol compound) 5 to 20 parts by weight, more preferably 10 to 15 parts by weight.

  Here, yellow petrolatum and white petrolatum are known as “petrol”, and “glycol (diol compound)” is ethylene glycol (1,2-ethanediol), propylene glycol (1,2-propanediol), Butylene glycol (1,3-butanediol), diethylene glycol, and the like are known.

  The skin coating agent according to the invention of claim 3 is the structure of claim 1 or claim 2, wherein the base for skin coating agent is 3 to 15 parts by weight, more preferably 5 parts by weight to glycerin. It contains 10 parts by weight.

  The skin application agent according to a fourth aspect of the present invention is the skin application composition according to any one of the first to third aspects, wherein the xanthone derivative mixture contains γ-mangostin within a range of 5 wt% to 30 wt%. To do.

  The skin coating agent according to the invention of claim 1 is used in a range of 1 μmol to 500 mmol of α-mangostin alone or a xanthone derivative mixture containing α-mangostin with respect to 1 kg of the base for skin coating agent. Contains.

  Here, α-mangostin is a kind of xanthone derivative, and further, a xanthone derivative is a kind of polyphenol and has a useful physiological action including an antioxidant action, α-mangosteen, β- The mangosteen extract mainly composed of mangosteen and γ-mangosteen is a xanthone derivative having a xanthone skeleton.

  It was found that by adding within 1 μmol to 500 mmol per kg, the anti-inflammatory and anti-allergic effects can be obtained reliably, without side effects, and at a practical price. Based on this, the present invention has been completed.

  In addition, the present inventors have found that anti-inflammatory effects and anti-allergic effects obtained when mangosteens are added to a skin coating agent are mainly due to α-mangostin, and based on this finding, The invention has been completed. Therefore, by containing only α-mangostin or a mixture of xanthone derivatives containing α-mangostin within a range of 1 μmol to 500 mmol with respect to 1 kg of the base for skin application, anti-inflammatory effect and anti-allergic effect are ensured. Can be obtained.

  That is, when the addition amount of the xanthone derivative mixture containing α-mangosteen or α-mangosteen is less than 1 μmol with respect to 1 kg of the skin coating base, the addition amount of the xanthone derivative is too small to ensure the anti-inflammatory effect. An antiallergic effect cannot be obtained. On the other hand, when the addition amount exceeds 500 mmol with respect to 1 kg of the skin coating base, the xanthone derivative is added in too much amount, and a very expensive xanthone derivative is added in a large amount. As a result, the cost of the product becomes too high to be practical.

  Furthermore, by containing only α-mangostin or a mixture of xanthone derivatives containing α-mangostin within a range of 10 μmol to 10 mmol with respect to 1 kg of the skin coating base, it is more reliable and more practical. Since an anti-inflammatory effect and an anti-allergic effect can be obtained at a low price, it is more preferable.

  Thus, by using mangosteens having useful physiological actions and clarifying their appropriate addition amount, a skin coating agent that can reliably obtain anti-inflammatory and anti-allergic effects at low cost It becomes.

  In the skin coating agent according to the invention of claim 2, the base for skin coating agent contains 60 parts by weight to 100 parts by weight of petrolatum and 5 parts by weight to 20 parts by weight of glycol (diol compound).

  The present inventors have conducted extensive experimental research on the composition of an appropriate base for skin application when applying mangosteens to the skin application of skin application, and as a result, 60 parts by weight to 100 parts by weight of petrolatum. It has been found that by using a base for skin coating composition containing 5 parts by weight and 5 parts by weight to 20 parts by weight of a glycol (diol compound), a more prominent anti-inflammatory effect / anti-allergic effect can be surely obtained. The present invention has been completed based on this finding. Here, when the base for skin application agent contains 70 parts by weight to 90 parts by weight of petroleum jelly and 10 parts by weight to 15 parts by weight of glycol, the anti-inflammatory effect / Since an antiallergic effect can be acquired, it is more preferable.

  In this way, by using mangosteens having useful physiological actions and clarifying their appropriate addition amount, skin that can surely obtain more prominent anti-inflammatory and anti-allergic effects at low cost It becomes a coating agent.

  In the skin coating composition according to the invention of claim 3, the skin coating composition base contains 3 to 15 parts by weight of glycerin.

  In applying mangosteen to the skin coating agent of the skin coating agent, the present inventors conducted extensive experimental research on the composition of the appropriate base for skin coating agent, and as a result, 3 parts by weight to 15 parts by weight of glycerin. It has been found that by using a base for a skin coating agent containing parts by weight, a more prominent anti-inflammatory effect / anti-allergic effect can be surely obtained, and the present invention has been completed based on this finding. is there. Here, when the base for skin application agent contains 5 to 10 parts by weight of glycerin, a remarkable anti-inflammatory effect / anti-allergic effect can be obtained even more reliably. More preferred.

  Thus, by using mangosteens having useful physiological actions and clarifying their appropriate addition amount, a skin coating agent that can reliably obtain anti-inflammatory and anti-allergic effects at low cost It becomes.

  In the skin coating composition according to the invention of claim 4, the xanthone derivative mixture contains γ-mangostin within a range of 5 wt% to 30 wt%.

  The present inventors have conducted extensive experimental studies on the appropriate content of γ-mangostin associated with α-mangostin in the xanthone derivative mixture in applying mangosteens to the skin coating agent of the skin coating agent. It has been found that when the derivative mixture contains γ-mangostin in the range of 5% by weight to 30% by weight, an anti-inflammatory effect and an anti-allergic effect can be obtained more reliably and at low cost. Based on this, the present invention has been completed.

  Thus, by using mangosteens having useful physiological actions and clarifying their appropriate addition amount, a skin coating agent that can reliably obtain anti-inflammatory and anti-allergic effects at low cost It becomes.

  Embodiments of the present invention will be described below. First, the manufacturing method of the skin coating agent which concerns on embodiment of this invention is demonstrated with reference to FIG. FIG. 1 is a diagram showing the structural formula of xanthone derivatives including α-mangostin.

  In the skin coating agent according to the present embodiment, white petrolatum is used as the base for skin coating, propylene glycol (1,2-propanediol) and glycerin are used as additives, and a mixture of propylene glycol and glycerin is first used. The coating agent for skin is manufactured by melt | dissolving (alpha) -mangostin in this and mixing this with white petrolatum. Here, as shown in FIG. 1, xanthone derivatives such as α-mangostin are one type of polyphenol having a xanthone skeleton.

  In addition, in the skin coating agent which concerns on this Embodiment, although no other additive is used, a wetting agent, antiseptic | preservative, disinfectant | microbicide, an antibacterial agent, etc. can also be added as needed. Wetting agents, preservatives, bactericides, and antibacterial agents include polyethylene glycol (PEG), methylparaben, cetylpyridinium chloride, sansol, edetic acid, and other wetting agents, preservatives, bactericides, and antibacterial agents. You can also

  Next, a method for evaluating the anti-inflammatory effect / anti-allergic effect of the skin coating agent according to the present embodiment will be described.

  First, as Comparative Example 1, a skin coating agent having the same composition as the skin coating agent according to the present embodiment was prepared except that it did not contain α-mangosteen and a xanthone derivative mixture containing α-mangosteen at all. . In addition, as Example 1, Example 2, Example 3, Example 4, Example 5 and Example 6, the xanthone derivative mixture containing α-mangosteen was contained in 1 μmol, 10 μmol, 100 μmol, 1 mmol, 10 mmol and 100 mmol, respectively. A prepared skin application agent was prepared.

  Furthermore, as Comparative Example 2, a skin coating agent containing 0.5 μmol of a xanthone derivative mixture containing α-mangosteen was prepared. Table 1 shows the compositions of the skin coating agents according to Example 1, Example 2, Example 3, Example 4, Example 5, Example 6, Comparative Example 1, and Comparative Example 2.

  As shown in Table 1, the composition of the skin coating composition according to Examples 1 to 6 and Comparative Examples 1 and 2 was the skin coating composition except for the addition amount of the xanthone derivative mixture containing α-mangosteen. The contents of white petrolatum as a base for use and propylene glycol and glycerin as additives are exactly the same at 80 parts by weight, 12 parts by weight and 8 parts by weight, respectively.

  Here, as the xanthone derivative mixture containing α-mangostin, trade name Panaxanthone (registered trademark) manufactured by Mitsumata Medical Co., Ltd. was used. This panaxanthone was a xanthone derivative mixture containing 80% by weight of α-mangosteen, 12% by weight of γ-mangostin, and 8% by weight of other xanthone derivatives.

  Then, the skin coating agent according to Examples 1 to 6 and the skin coating agent according to Comparative Examples 1 and 2 manufactured in this way were divided into 8 groups of 10 elderly people who are wearing disposable diapers. This was applied to the lower back and buttocks for 1 week, and the effect on diaper rash and bed slip was evaluated. As an evaluation method, for each group, the skin condition was divided into equal groups and scored by judging according to the following criteria.

As a result, it was evaluated as a preferable result that the amount of decrease in the total score was larger.
There is no redness and it is absolutely beautiful. ... 0 points There is a little redness or rash, but it is normal. ... 1 point There is some redness and rash, but it is not pathological. 2 points Redness and rash, slightly morbid. 3 points Redness and rash are severe, and treatment is required. Table 4 shows the evaluation results.

  As shown in Table 2, the group using the skin coating composition according to Comparative Example 1 had no significant change in the total score compared to before the test, and contained no xanthone derivative mixture containing α-mangostin. It can be seen that no therapeutic effect is seen in the non-skin application. Further, as shown in Table 2, when the skin coating composition according to Comparative Example 2 was used, it was a decrease of only 3 points, and it cannot be said that there was a significant therapeutic effect.

  On the other hand, when the skin coating composition according to Example 1 to Example 6 was used, it was greatly reduced to 7 to 18 points, and a significant therapeutic effect on rash, bedsore and allergic inflammation. It is determined that there is. Therefore, in order to reliably obtain an anti-inflammatory effect / anti-allergic effect, in the skin coating agent impregnated in the skin coating agent, the xanthone derivative mixture containing α-mangosteen is used with respect to 1 kg of the skin coating agent base. It became clear that it was necessary to contain 1 μmol or more.

  Further, as shown in Table 2, when the skin coating agents according to Example 2, Example 3, Example 4, Example 5 and Example 6 were used, 10 points, 14 points, 16 points, 18-point and 18-point greatly decreased, and in Examples 3 to 6, bed sores were completely cured, and it was determined that there was a more remarkable therapeutic effect on rash, bed sores, and allergic inflammation. The Moreover, in Example 6, compared with Example 5, although the content of the xanthone derivative mixture containing α-mangosteen is increased 10 times, no significant improvement in the therapeutic effect is observed.

  Therefore, in order to reliably obtain a more prominent anti-inflammatory effect and anti-allergic effect at a lower cost, the xanthone derivative mixture containing α-mangosteen in the skin coating agent is added to 1 kg of the skin coating base. On the other hand, it became clear that it was more preferable to make it contain in the range of 10 micromol-10 mmol.

  Thus, in the skin coating agents according to Examples 1 to 6 of the present embodiment, by using mangosteens having a useful physiological action, by clarifying the appropriate addition amount, An anti-inflammatory effect and an anti-allergic effect can be reliably obtained at a low price.

  Furthermore, in the skin coating agents according to Examples 2 to 5 of the present embodiment, by using mangosteens having a useful physiological action, the appropriate addition amount is clarified, thereby reducing the price. Thus, more prominent anti-inflammatory and anti-allergic effects can be obtained with certainty.

  In the present embodiment, only the case where a xanthone derivative mixture containing α-mangosteen is used as the mangosteen has been described, but the anti-inflammatory effect obtained when the mangosteen is added to the skin application agent of the skin application agent -Since the antiallergic effect is mainly due to α-mangostin, the same action and effect can be obtained even when α-mangostin is used alone.

  In the present embodiment, as the xanthone derivative mixture containing α-mangosteen, a xanthone derivative mixture containing 80% by weight of α-mangosteen, 12% by weight of γ-mangosteen, and 8% by weight of other xanthone derivatives is used. However, as long as it is a xanthone derivative mixture containing α-mangostin, the other components and weight% are not limited thereto.

  Furthermore, in the present embodiment, the composition of the base for skin coating composition is 80 parts by weight of white petrolatum, 12 parts by weight of propylene glycol (1,2-propanediol), and 8 parts by weight of glycerin. The composition of the base for coating agent is not limited to these components and parts by weight. The composition of the base for skin application is preferably 60 to 100 parts by weight of white petrolatum, 5 to 20 parts by weight of propylene glycol and 3 to 15 parts by weight of glycerin. More preferably, it is 70 to 90 parts by weight, 10 to 15 parts by weight of propylene glycol, and 5 to 10 parts by weight of glycerin.

  In this embodiment, the case where propylene glycol (1,2-propanediol) is used as the glycol (diol compound) has been described. However, the glycol (diol compound) is not limited to this, and ethylene Other glycols such as glycol (1,2-ethanediol), butylene glycol (1,3-butanediol), diethylene glycol and the like may be used. It is to be noted that the use of propylene glycol (1,2-propanediol) and / or butylene glycol (1,3-butanediol) as glycol (diol compound) has extremely low transdermal toxicity, so that safety is ensured. From the point of view, it is more preferable.

  In practicing the present invention, the configuration, composition, blending, ingredients, shape, quantity, material, size, manufacturing method, etc. of other parts of the skin coating agent are also limited to this embodiment and each example. Is not to be done.

  In addition, since the numerical value quoted in the embodiment of the present invention does not indicate a critical value but indicates a preferable value suitable for implementation, even if the numerical value is slightly changed, the implementation is denied. is not.

FIG. 1 is a diagram showing the structural formula of xanthone derivatives including α-mangostin.

Claims (4)

A skin application agent applied to the skin to relieve skin symptoms,
The skin coating agent characterized by containing (alpha) -mangosteen or the xanthone derivative mixture containing (alpha) -mangostin within the range of 1 micromol-500 mmol with respect to 1 kg of the base for skin coating agents.   The skin coating agent according to claim 1, wherein the base for skin coating contains 60 parts by weight to 100 parts by weight of petroleum jelly and 5 parts by weight to 20 parts by weight of glycol (diol compound). .   The skin coating agent according to claim 1 or 2, wherein the skin coating base comprises 3 parts by weight to 15 parts by weight of glycerin.   The skin application agent according to any one of claims 1 to 3, wherein the xanthone derivative mixture contains γ-mangosteen within a range of 5 wt% to 30 wt%.

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