JP2022026218A - External composition - Google Patents

Abstract

To provide an external composition that is excellent in foamability and the persistence of the bubbles, while enabling the bubbles to run out quickly.SOLUTION: An external composition contains (A1 component) sorbitol, (B component) polyoxyethylene polyoxypropyleneglycol, and (C component) heparin analog.SELECTED DRAWING: None

Description

The present invention relates to an external composition or the like.

Dosage forms of external preparations include, for example, ointments, creams, lotions and the like. Since ointments and creams are semi-solid, it is difficult to spread them over a wide area. In addition, since the lotion is liquid, it is suitable for spreading over a wide area, but it is difficult to use because the liquid may drip during use.

On the other hand, in recent years, a foaming agent that is simple and can be widely used has attracted attention. Since the foaming agent is in a foamy state at the time of ejection, dripping is suppressed, and since it is a liquid, it is also suitable for spreading over a wide area. As the foaming agent, a foaming agent using a non-gas type foam discharging device such as a pump type foam discharging device using a nonionic surfactant is desirable for the purpose of suppressing irritation to the skin. Patent Document 1 proposes that foam is retained for a long time by combining a nonionic surfactant and a certain amount or more of alcohol.

Japanese Unexamined Patent Publication No. 2016-121146

In the course of research by the present inventor, the foaming agent of the prior art has good foam durability and suppresses dripping, but the foam does not disappear easily even when spread, and the spread portion is whitened. I focused on having the problem that it looks like it was done (the problem that the bubbles are not broken).

Therefore, it is an object of the present invention to provide an external composition having good foaming and foam sustainability, but also good foam breaking.

As a result of diligent research in view of the above problems, the present inventor has produced an external composition containing (A1 component) sorbitol, (B component) polyoxyethylene polyoxypropylene glycol, and (C component) heparinoid. If so, we have found that the above problems can be solved. The present inventor has completed the present invention as a result of further research based on this finding. That is, the present invention includes the following aspects.

Item 1. An external composition containing (A1 component) sorbitol, (B component) polyoxyethylene polyoxypropylene glycol, and (C component) heparinoid.
Item 2. Item 2. The external composition according to Item 1, wherein the A1 component contains D-sorbitol.
Item 3. Item 2. The external composition according to Item 1 or 2, wherein the content of the A1 component in the external composition is 0.1 to 40% by mass.
Item 4. Item 4. The external composition according to any one of Items 1 to 3, further comprising (A2 component) glycerin.
Item 5. Item 2. The external composition according to Item 4, wherein the content of the A2 component in the external composition is 0.5 to 45% by mass.
Item 6. Item 2. The external composition according to any one of Items 1 to 5, wherein the content of the component B in the external composition is 0.05 to 10% by mass.
Item 7. Item 6. The external composition according to any one of Items 1 to 6, wherein the content of the C component in the external composition is 0.01 to 10% by mass.
Item 8. Item 2. The external composition according to any one of Items 1 to 7, wherein the content of water in the external composition is 25% by mass or more.
Item 9. Item 6. The external composition according to any one of Items 1 to 8, which is used for application to the skin.
Item 10. Item 6. The external composition according to any one of Items 1 to 9, which is for a foam discharge device.
Item 11. Item 6. The external composition according to Item 10, wherein the foam discharging device is a non-gas type foam discharging device.
Item 12. An external preparation prepared by filling a container provided with a foam discharge device with the external composition according to any one of Items 1 to 11.

According to the present invention, it is possible to provide an external composition having good foaming and foam sustainability, but also good foam breakage.

In the present specification, the expressions "contains" and "contains" include the concepts of "contains", "contains", "substantially consists" and "consists of only".

The present invention, in one aspect thereof, is an external composition containing (A1 component) sorbitol, (B component) polyoxyethylene polyoxypropylene glycol, and (C component) heparinoid (in the present specification, "the present invention". It may be referred to as "external composition of the invention"). This will be described below.

Sorbitol (A1 component) is a sugar alcohol and includes both D-sorbitol and L-sorbitol. In one aspect of the present invention, among these, D-sorbitol is preferably mentioned from the viewpoint of foaming, foam sustainability, foam breakage and the like.

The A1 component can be used alone or in combination of any two or more.

In one aspect of the present invention, the A1 component preferably contains D-sorbitol.

The content of the A1 component in the external composition of the present invention is not particularly limited as long as foaming, foam sustainability, and foam breakage can be satisfactorily exhibited. The content is, for example, 0.1 to 40% by mass. The content is preferably 0.2 to 40% by mass, more preferably 0.4 to 35% by mass, and further preferably 0.5 to 30% by mass from the viewpoints of foaming, foam sustainability, foam breakage and the like. From the viewpoint of foaming, foam sustainability, foam breakage, etc., in a preferred embodiment of the present invention, the lower limit of the content is, for example, 1% by mass, 2% by mass, 3% by mass, 4% by mass, 5% by mass, It can be 6% by weight, 7% by weight, 8% by weight, 9% by weight, 10% by weight.

The external composition of the present invention preferably contains glycerin (A2 component) from the viewpoint of foaming, foam persistence, foam breakage and the like (particularly, foam persistence).

When the external composition of the present invention contains an A2 component, the content of the A2 component in the external composition of the present invention is not particularly limited as long as foaming, foam sustainability, and foam breakage can be satisfactorily exhibited. The content is, for example, 0.5 to 45% by mass. The content is preferably 1 to 45% by mass, more preferably 2 to 40% by mass, still more preferably 4 to 35% by mass, still more preferably 6 from the viewpoint of foaming, foam sustainability, foam breakage and the like. It is -30% by mass, particularly preferably 6 to 25% by mass, and particularly preferably 8 to 25% by mass.

When the external composition of the present invention contains an A2 component, the total content of the A1 component and the A2 component in the external composition of the present invention is preferably from the viewpoint of foaming, foam sustainability, foam breakage and the like. 1 to 85% by mass, more preferably 2 to 75% by mass, still more preferably 4 to 70% by mass, still more preferably 5 to 65% by mass, particularly preferably 7 to 55% by mass, and even more preferably 9 to 50%. It is mass%. In one aspect of the invention, the lower limit of the content may be, for example, 12% by weight, 14% by weight, 16% by weight, 18% by weight, or 19% by weight.

When the external composition of the present invention contains an A2 component, the content ratio of the A1 component to the A2 component in the external composition of the present invention is the A1 component 1 from the viewpoint of foaming, foam sustainability, foam breakage, etc. The A2 component is preferably 0.05 to 45 parts by mass, more preferably 0.1 to 40 parts by mass, still more preferably 0.2 to 35 parts by mass, and even more preferably 0.3 to 30 parts by mass with respect to parts by mass. In a more preferable embodiment of the present invention, the A2 component is preferably 0.4 to 10 parts by mass, 0.5 to 5 parts by mass, 0.6 to 3 parts by mass, and 0.8 to 2 parts by mass with respect to 1 part by mass of the A1 component.

In one aspect of the present invention, the external composition of the present invention may contain a polyhydric alcohol other than the A1 component and the A2 component. Other polyhydric alcohols include, for example, sugar alcohols other than A1 component and A2 component, propylene glycol, dipropylene glycol, 1,3-butylene glycol, 1,2-pentanediol, 1,2-hexanediol, 1,3. , 6-Hexanetriol, polyethylene glycol, polypropylene glycol and the like. However, in that case, it is preferable that the content of the other polyhydric alcohol is lower from the viewpoint of foaming, foam sustainability, foam breakage and the like.

Other polyhydric alcohols can be used alone or in combination of any two or more.

In the external composition of the present invention, the total content of the A1 component and the A2 component in the polyhydric alcohol (when the external composition of the present invention does not contain the A2 component, it means the content of the A1 component), or. The total content of sugar alcohol in the polyhydric alcohol is, for example, 70% by mass or more, preferably 80% by mass or more, more preferably 85% by mass or more, still more preferably 90% by mass or more, still more preferably 95% by mass or more. , Particularly preferably 97% by mass or more, particularly preferably 98% by mass or more, and particularly preferably 99% by mass or more. The content is 100% by mass or less.

In one aspect of the invention, the external composition of the invention comprises other polyhydric alcohols (eg, 1,3-butylene glycol, macrogol 400, and 1) in terms of foaming, foam persistence, foam breakage, and the like. , At least one polyhydric alcohol selected from the group consisting of 3,6-hexanetriol) is preferably lower in content. The content of the polyvalent alcohol (for example, 1,3-butylene glycol) in the external composition of the present invention is, for example, 0% by mass or more and less than 5% by mass, preferably 0% by mass or more and less than 4% by mass. It is preferably 0% by mass or more and less than 3% by mass, more preferably 0% by mass or more and less than 2% by mass, still more preferably 0% by mass or more and less than 1% by mass, particularly preferably 0% by mass or more and less than 0.5% by mass, and particularly further. It is preferably 0% by mass or more and less than 0.1% by mass, and more preferably 0% by mass or more and less than 0.01% by mass. In one aspect of the invention, the content can be 0% by weight.

Polyoxyethylene polyoxypropylene glycol (component B) is a nonionic surfactant containing oxyethylene units and oxypropylene units. The average number of moles of ethylene oxide added per oxyethylene unit is not particularly limited, but is, for example, 10 to 300, preferably 50 to 250, and more preferably 100 to 200. The average number of moles of propylene oxide added in an oxypropylene unit is not particularly limited, but is, for example, 10 to 300, preferably 20 to 150, and more preferably 25 to 70.

The HLB value of polyoxyethylene polyoxypropylene glycol is not particularly limited as long as it can satisfactorily exhibit foaming, foam sustainability, and foam breakage. The HLB value is, for example, 10 to 20, preferably 12 to 18.

The B component can be used alone or in combination of any two or more.

The content of the component B in the external composition of the present invention is not particularly limited as long as foaming, foam sustainability, and foam breakage can be satisfactorily exhibited. The content is, for example, 0.02 to 15% by mass. The content is preferably 0.05 to 12% by mass, more preferably 0.05 to 10% by mass, still more preferably 0.1 to 9% by mass, still more preferably 0.2, from the viewpoints of foaming, foam sustainability, foam breakage and the like. It is -9% by mass, particularly preferably 0.3-9% by mass, and even more preferably 0.4-9% by mass. From the viewpoint of foaming, foam sustainability, foam breakage, etc., in a preferred embodiment of the present invention, the upper limit of the content is, for example, 8% by mass, 7% by mass, 6% by mass, 5% by mass, 4% by mass, It can be 3% by mass, 2% by mass, 1% by mass, or 0.8% by mass.

In one aspect of the present invention, the external composition of the present invention may contain a surfactant other than the component B. Other surfactants include, for example, nonionic surfactants containing polyoxyalkylene units (eg, polyoxyalkylene fatty acid ester, polyoxyalkylene cured castor oil, polyoxyalkylene alkyl ether, etc.), glycerin fatty acid ester, sorbitan fatty acid. Nonionic surfactants such as esters and aliphatic alkanolamides; anionic surfactants; cationic surfactants; amphoteric surfactants and the like can be mentioned. However, in that case, the content of the other surfactant is preferably lower from the viewpoint of skin irritation, foaming, foam persistence, foam breakage and the like.

Other surfactants may be used alone or in combination of any two or more.

In the external composition of the present invention, the content of the B component in the surfactant or the nonionic surfactant containing the polyoxyalkylene unit (including the B component, preferably the B component and the polyoxyalkylene fatty acid ester, The total content of (with at least one selected from the group consisting of polyoxyalkylene cured castor oil and polyoxyalkylene alkyl ether) is, for example, 70% by mass or more, preferably 80% by mass or more, more preferably 85% by mass or more. It is more preferably 90% by mass or more, still more preferably 95% by mass or more, particularly preferably 97% by mass or more, particularly preferably 98% by mass or more, and particularly preferably 99% by mass or more. The content is 100% by mass or less.

In the external composition of the present invention, the content of the component B in the nonionic surfactant is, for example, 70% by mass or more, preferably 80% by mass or more, more preferably 85% by mass or more, still more preferably 90% by mass. As described above, it is more preferably 95% by mass or more, particularly preferably 97% by mass or more, particularly preferably 98% by mass or more, and particularly preferably 99% by mass or more. The content is 100% by mass or less.

The content of other surfactants (particularly, anionic surfactants, cationic surfactants, and amphoteric surfactants) in the external composition of the present invention is, for example, 0% by mass or more and less than 5% by mass. , Preferably 0% by mass or more and less than 4% by mass, more preferably 0% by mass or more and less than 3% by mass, further preferably 0% by mass or more and less than 2% by mass, still more preferably 0% by mass or more and less than 1% by mass, in particular. It is preferably 0% by mass or more and less than 0.5% by mass, more preferably 0% by mass or more and less than 0.1% by mass, and even more preferably 0% by mass or more and less than 0.01% by mass. In one aspect of the invention, the content can be 0% by weight.

The heparinoid (component C) is a polysulfated mucopolysaccharide such as chondroitin polysulfate, and is a known drug known to have a moisturizing effect, a blood flow increasing effect, and the like. The origin of the heparinoid is not particularly limited, but is, for example, one obtained by polysulfating mucopolysaccharide, one extracted from edible animal tissue (for example, lung containing bovine tracheal cartilage), and the like. Can be mentioned. As the heparin-like substance, a heparin-like substance contained in the Japanese Pharmacopoeia non-Japanese Pharmacopoeia drug standard can be preferably used.

The C component can be used alone or in combination of any two or more.

The content of the C component in the external composition of the present invention is not particularly limited as long as it can exert a medicinal effect and does not significantly impair foaming, foam sustainability, foam breakage and the like. The content is, for example, 0.01 to 10% by mass, 0.05 to 3% by mass, or 0.1 to 1% by mass.

In one aspect of the present invention, the external composition of the present invention may contain other components other than the above. Other components include, for example, ester oils (eg, triacetin, triethyl citrate, tri (capryl, capric acid) glycerin, diisopropyl adipate, diethyl adipate, diethyl dibasic acid such as diethyl sebacate, isopropyl myristate, etc. Cetyl palmitate, hexyl laurate, monobasic acids such as benzyl acetate, etc.), hydrocarbons (eg, liquid paraffin, squalane, etc.), solvents (eg, benzyl alcohol, methyl ethyl ketone, N-alkylpyrrolidone, alkylene carbonate, acetone, etc.) Ethanol, isopropanol, propylene glycol, 1,3-butylene glycol, etc.), water-soluble polymers (eg, carboxyvinyl polymer, hydroxymethyl cellulose, hydroxypropyl cellulose, methyl cellulose, chitosan, povidone, polyvinyl alcohol, etc.), preservatives, preservatives , Stabilizers and the like.

The content of other components in the external composition of the present invention is not particularly limited as long as it does not significantly impair foaming, foam persistence, foam breakage and the like. The content is, for example, 0 to 10% by mass, 0 to 5% by mass, 0 to 2% by mass, 0 to 1% by mass, or 0 to 0.1% by mass.

The external composition of the present invention usually contains water from the viewpoints of foaming, foam sustainability, foam breakage and the like. The content of water in the composition of the present invention is, for example, 15% by mass or more, preferably 20% by mass or more, more preferably 25% by mass or more, still more preferably 30% by mass or more, still more preferably 35% by mass or more. , Particularly preferably 40% by mass or more, particularly preferably 50% by mass or more, and even more preferably 60% by mass or more. The upper limit of the content can be, for example, 95% by mass, 90% by mass, 85% by mass, or 80% by mass. The above lower limit and upper limit can be arbitrarily combined.

The external composition of the present invention can be used for application to the skin. Since the composition for external use of the present invention has good foam durability, it can be easily spread because it suppresses dripping when discharged in the form of foam and also has good foam breakage. The external composition of the present invention is preferably in the form of an external composition for skin such as a medicine for external skin and cosmetics. The external composition of the present invention is used in such a manner that it is not removed after application, and is distinguished from a cleaning agent intended to be removed (for example, washed away) with water after being used by whipping.

The external composition of the present invention can be prepared by mixing each component with a solvent. The composition of the present invention is preferably in a solubilized state. The solubilized state means a state in which the surfactant forms micelles and the substance insoluble in the solvent is transparently and uniformly dissolved to form a one-phase solution. The solubilized state includes the state of a microemulsion. The microemulsion is a thermodynamically stable micelle solution composed of emulsified particles having a fine particle size of 100 nm or less. The solubilized state can be confirmed by the transparent appearance. In addition, the solubilized state can be confirmed by measuring the particle size by a conventional method. The solubilized composition can be obtained by dissolving each component under heating, if necessary, and then cooling.

The external composition of the present invention can be used for a foam discharge device. Here, the foam discharge device means a device provided with a mechanism for foaming. That is, the external composition of the present invention is intended to be foamed and used by a foam ejection device. The foam ejection device is preferably a non-gas type foam ejection device from the viewpoint of irritation to the skin. Examples of the non-gas type foam discharge device include a screen type foam discharge device. The screen-type foam ejection device means a mechanism that pressurizes a liquid, passes it through a net-like screen, mixes it with air, and foams it. Examples of the screen type foam discharge device include a pump type foam discharge device, a tube type foam discharge device, a squeeze type foam discharge device, and the like. Among these, the pump type foam discharge device is preferable.

As the foam discharge device, a known one, a commercially available one, or the like can be adopted. For example, in the case of a pump-type foam discharge device, those described in JP-A-2012-45525, JP-A-2008-307478 and the like can be used.

The external composition of the present invention can be used by filling a container equipped with a foam ejection device. From this point of view, the present invention also relates to, in one aspect, an external preparation, which comprises filling a container provided with a foam ejection device with the external composition of the present invention. The “external agent” is the same as the above-mentioned external composition of the present invention.

Hereinafter, the present invention will be described in detail based on examples, but the present invention is not limited to these examples.

Test example 1. Foam evaluation test 1
Compositions 1 to 10 for filling a container equipped with a foam discharge device were prepared according to the formulation shown in Table 1 (the unit of the number is parts by mass). Specifically, each component was weighed, dissolved by heating at 80 ° C., solubilized under stirring, and then cooled to room temperature with stirring to obtain compositions 1 to 16. These compositions were filled in a pump-type foam discharger container and subjected to a test.

The details of the materials used are as follows.
・ 70% D-sorbitol solution (manufactured by dissolving D-sorbitol (manufactured by Fuji Film Wako Pure Chemical Industries, Ltd., trade name: D-sorbitol (Wako first grade)) in purified water)
・ Glycerin (manufactured by Fuji Film Wako Pure Chemical Industries, Ltd., product name: glycerin (special grade reagent))
-Polyoxyethylene polyoxypropylene glycol (manufactured by NOF Corporation, trade name: Pronon 188P)

A fixed amount of each of the compositions 1 to 10 was discharged onto the slide glass from the pump-type foam discharge device container. Foaming immediately after discharge was visually observed and evaluated on a 4-point scale according to the following evaluation criteria. In addition, the sustainability of the foam was evaluated on a 4-point scale according to the following evaluation criteria by visually observing the change in the state of the foam after allowing it to stand for 5 minutes from the discharge. Regarding the foaming immediately after discharge, the evaluation of ◯ or higher was judged to be good foaming, and the evaluation of foam sustainability of Δ or higher was judged to be good sustainability.

<Evaluation criteria for foaming immediately after ejection>
◎: Foaming with good foam quality (fine texture, foaming).
◯: Foams.
Δ: Weak foaming.
×: Does not form bubbles.

<Evaluation criteria for foam sustainability>
⊚: No change is observed in the bubbles.
◯: The bubble height becomes low.
Δ: The area occupied by bubbles on the slide glass becomes smaller.
X: There are no bubbles.

On the other hand, a certain amount of each of the compositions 1 to 10 was discharged from the pump-type foam discharger container to one arm of the subject and spread toward the fingertips. However, the spreading operation was performed only once. Foam breakage was evaluated on a three-point scale according to the following evaluation criteria. Δ The above evaluation was judged to be good for foam breakage.

<Evaluation criteria for bubble breakage>
◯: After spreading once, foam remained on the arm, but the foam disappeared within 1 minute.
Δ: After spreading once, foam remained on the arm, and the foam remained even after 1 minute had passed. However, by spreading it many times, the bubbles disappeared and no whitening was observed.
X: After spreading once, foam remained on the arm, and then after spreading many times, foam remained and whitening was observed on the arm.

The results are shown in Table 1.

As shown in Table 1, the foams obtained from the compositions 1 to 10 had good foaming and foam sustainability, but also had good foam breakage.

Test example 2. Foam evaluation test 2
The composition 11 for filling a container equipped with a foam ejection device was prepared in the same manner as in Test Example 1 according to the formulation shown in Table 2 (the unit of the number is parts by mass). Foaming immediately after ejection, foam persistence, and foam breakage were evaluated in the same manner as in Test Example 1.

The results are shown in Table 2.

As shown in Table 2, the foam obtained from the composition 11 had good foaming and foam sustainability, but also had good foam breakage.

Claims (10)

An external composition containing (A1 component) sorbitol, (B component) polyoxyethylene polyoxypropylene glycol, and (C component) heparinoid. The external composition according to claim 1, wherein the A1 component comprises D-sorbitol. The external composition according to claim 1 or 2, wherein the content of the A1 component in the external composition is 0.1 to 40% by mass. The external composition according to any one of claims 1 to 3, further comprising (A2 component) glycerin. The external composition according to claim 4, wherein the content of the A2 component in the external composition is 0.5 to 45% by mass. The external composition according to any one of claims 1 to 5, wherein the content of the component B in the external composition is 0.05 to 10% by mass. The external composition according to any one of claims 1 to 6, wherein the content of the C component in the external composition is 0.01 to 10% by mass. The external composition according to any one of claims 1 to 7, wherein the content of water in the external composition is 25% by mass or more. The external composition according to any one of claims 1 to 8, which is for a foam discharge device. An external preparation agent comprising the external composition according to any one of claims 1 to 10 filled in a container provided with a foam discharge device.