JP7134746B2 - emulsion composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to emulsified compositions and the like, and more particularly to oral emulsified compositions and the like.

Compositions containing a relatively small amount of water and a relatively large amount of hydrocarbon oil usually have poor stability over time, and even if emulsified using an emulsifier, the hydrocarbon oil often separates after long-term storage. is. Therefore, it has been difficult to use them for various uses (for example, compositions for oral cavity).

JP 2014-189550 A JP 2009-95253 A

An object of the present invention is to prepare an emulsified composition having good stability over time while containing a hydrocarbon oil.

The present inventors found that an emulsified composition containing a hydrocarbon oil, sorbitol, and a polyglycerol monofatty acid ester and/or an alkyl glycoside may have good stability over time while containing a hydrocarbon oil. Further improvements have been made to complete the present invention.

The invention includes, for example, the subject matter described in the following sections.
Section 1.
(A) a hydrocarbon oil,
An emulsified composition containing (B) sorbitol and (C) polyglycerol monofatty acid ester and/or alkyl glycoside.
Section 2.
Item 1. The composition according to Item 1, which is for oral cavity use.
Item 3.
Item 3. The composition according to item 1 or 2, wherein the hydrocarbon oil is paraffin.
Section 4.
Item 4. The composition according to any one of items 1 to 3, wherein the polyglycerin monofatty acid ester is a monoester of a fatty acid having 8 to 24 carbon atoms and polyglycerin.
Item 5.
Polyglycerin monofatty acid ester consists of polyglycerin monocaprate, polyglycerin monolaurate, polyglycerin monomyristate, polyglycerin monostearate, polyglycerin monopalmitate, and polyglycerin monooleate Item 4. The composition according to any one of Items 1 to 3, which is at least one selected from the group.
Item 6.
Item 6. The composition according to any one of Items 1 to 5, wherein the polyglycerin of the polyglycerin monofatty acid ester contains an average of 4 to 12 glycerin units.
Item 7.
Item 7. The composition according to any one of Items 1 to 6, wherein the water content is 20% by mass or less.
Item 8.
Item 8. The composition according to any one of items 1 to 7, which further comprises glycerin and/or propylene glycol and is non-aqueous.
Item 9.
Item 9. The composition according to any one of Items 1 to 8, which is gel-like or cream-like.

Provided is an emulsified composition containing a hydrocarbon oil and having excellent stability over time. The emulsified composition can be preferably used for various purposes. For example, it can be used for the oral cavity. In this case, it is possible to provide an oral emulsified composition that has excellent stability over time while containing a hydrocarbon oil.

Each embodiment included in the present invention will be described in further detail below. The present invention preferably includes, but is not limited to, an emulsifying composition, uses of the emulsifying composition (particularly for oral use), a method for producing the composition, and the like, and the present invention is disclosed herein. includes all

Emulsified compositions encompassed by the present invention contain (A) hydrocarbon oil, (B) sorbitol, and (C) polyglycerol monofatty acid ester and/or alkyl glycoside. Hereinafter, the emulsified composition may be referred to as "the emulsified composition of the present invention". Moreover, the composition which used the said emulsified composition for oral cavity may be described as "the emulsified composition for oral cavity of this invention." Furthermore, the components (A) to (C) are sometimes referred to as "(A) component", "(B) component", "(C) component", and the like.

Examples of hydrocarbon oils include squalane, paraffin, microcrystalline wax, petrolatum, ceresin, limonene, turpentine oil, and the like. Known hydrocarbon oils used in oral compositions are particularly preferred, and squalane and paraffin are particularly preferred. Paraffin is preferred. As the squalane, both animal squalane and vegetable squalane can be used. For example, shark squalane, olive squalane and the like can be preferably used. As the paraffin, liquid paraffin is preferable, and light liquid paraffin is more preferable. A hydrocarbon oil can be used individually by 1 type or in combination of 2 or more types.

Examples of polyglycerin monofatty acid esters include those having 8 to 24 carbon atoms (8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, or 24) monoesters of saturated or unsaturated fatty acids and polyglycerol are preferred.

The number of carbon atoms in the fatty acid is more preferably 8-22, still more preferably 10-20, and even more preferably 12-18. Further, the fatty acid may be a saturated fatty acid or an unsaturated fatty acid. In the case of an unsaturated fatty acid, the number of carbon-carbon double bonds is preferably 1, 2, 3, or 4. is more preferable. Examples of the fatty acid include capric acid, lauric acid, myristic acid, stearic acid, palmitic acid, palmitoleic acid, margaric acid, oleic acid, linoleic acid, and behenic acid. , stearic acid, palmitic acid and oleic acid are preferred. Natural fatty acids such as coconut oil fatty acid and palm oil fatty acid may also be used, including these fatty acids. That is, since the natural fatty acid contains the specific fatty acid, the emulsified composition using the natural fatty acid is included in the emulsified composition using the specific fatty acid.

The polyglycerin may also contain an average of 4 to 12 (4, 5, 6, 7, 8, 9, 10, 11, or 12) glycerin units (-OCH ₂ CH(OH)CH ₂ -). More preferably, it contains an average of 5-10 glycerin units.

Specific examples of preferred polyglycerin monofatty acid esters include polyglycerin monocaprate, polyglycerin monolaurate, polyglycerin monomyristate, polyglycerin monostearate, polyglycerin monopalmitate, and polyglycerin monooleate and the like.

Polyglycerol monofatty acid ester can be used individually by 1 type or in combination of 2 or more types.

An alkyl glycoside is a compound having a structure in which a higher alcohol and sugar are glycosidic bonded.

Examples of the higher alcohol include alkyl alcohols having 6 to 18 carbon atoms (6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, or 18). 16 alkyl alcohols are more preferred. The alkyl alcohol may be linear or branched, preferably linear. In addition, it is preferable that the alkyl alcohol has one OH group.

The sugar (sugar that forms a glycosidic bond with a higher alcohol) may be a monosaccharide or a polysaccharide. Di- or trisaccharides are preferred. Preferred monosaccharides are, for example, glucose and maltose, with glucose being particularly preferred. As the polysaccharide, for example, at least one selected from the group consisting of glucose and maltose is preferably bound by multiple glycosidic bonds, and particularly preferred is a polysaccharide in which glucose is glycosidic bonded. The glycosidic bond can be an α or β glycosidic bond.

The HLB of the component (C) used is preferably about 10 to 18, for example, although it is not particularly limited as long as the effects of the present invention are exhibited. The upper or lower limit of the range is, for example, 10.5, 11, 11.5, 12, 12.5, 13, 13.5, 14, 14.5, 15, 15.5, 16, 16.5, 17 , or 17.5.

The contents of components (A), (B), and (C) in the emulsified composition of the present invention are not particularly limited as long as the emulsified composition can be prepared and the effects of the present invention are not impaired. .

For example, about 5 to 60 parts by mass of component (B) is preferable for 60 parts by mass of component (A). The upper or lower limit of the mass part ratio range is, for example, , 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49 , 50, 51, 52, 53, 54, 55, 56, 57, 58, or 59 parts by weight. Although not particularly limited, for example, about 5 to 50 or 5 to 40 parts by weight is more preferable, and about 10 to 35 or 10 to 30 parts by weight is even more preferable.

Further, for example, about 0.5 to 10 parts by mass of component (C) is preferable for 60 parts by mass of component (A). The upper or lower limit of the mass part ratio range may be, for example, 1, 2, 3, 4, 5, 6, 7, 8, or 9 parts by mass. Although not particularly limited, for example, 1 to 9 or 2 to 9 parts by weight is more preferable, and 3 to 8 parts by weight is even more preferable.

In addition, as long as the effects of the present invention are not impaired, there is no particular limitation. It is more preferably contained, more preferably about 50 to 70% by mass, even more preferably about 55 to 65% by mass. In addition, the component (B) is preferably contained in an amount of about 5 to 59% by mass, more preferably about 5 to 45% by mass, and may be included in an amount of about 10 to 40% by mass or about 15 to 35% by mass. More preferably, about 20 to 30 parts by mass is even more preferable. In addition, component (C) is preferably contained in an amount of about 0.5 to 10% by mass, more preferably about 1 to 9% by mass or about 2 to 9% by mass, and is included in an amount of about 3 to 8% by mass. is more preferred.

The emulsion composition of the present invention may contain water. However, it preferably contains a relatively small amount of water. Specifically, for example, the water content is preferably 20% by mass or less, and more preferably 19, 18, 17, 16, or 15% by mass or less. Further, the upper limit of the water content range is 14, 13, 12, 11, 10, 9, 8, 7, 6, 5, 4, 3, 2, 1, or 0.5% by mass. good.

The emulsified composition of the present invention may be a composition that does not contain water (ie, a non-aqueous composition). However, the case where the composition contains an amount of water that is difficult to remove as an inevitable impurity is included in the "non-aqueous composition" herein.

When the emulsified composition of the present invention is a non-aqueous composition, it preferably further contains (D) glycerin and/or propylene glycol. In addition, hereinafter, these components may be described as "(D) component".

The content of glycerin and/or propylene glycol (component D) in the non-aqueous composition is 30 parts by mass or more when the total amount of components (B) and (D) contained is 100 parts by mass. It is preferably less than 100 parts by mass. The lower or upper limit of the mass ratio is 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, or 99 may For example, the lower limit of the weight part ratio may preferably be 35, 40, 45, 50, 55, 60, 65, or 70 parts by weight.

The emulsified composition of the present invention is stably maintained in an emulsified state. For example, it is preferable that the hydrocarbon oil does not separate (phase separation does not occur) when left standing at room temperature (25° C.) for one week after preparation.

The form of the emulsified composition of the present invention is not particularly limited as long as it is emulsified, but it is preferably in the form of gel or cream, for example.

As a method for preparing the emulsified composition of the present invention, for example, components (B) and (C) are first stirred and mixed, and then while stirring is continued, component (A) is gradually added to the mixture and mixed. method. Mixing can be performed with a known stirrer (for example, disper mixer, etc.). If a large amount of component (A) is added at once, it may not be uniformly mixed, so it is preferable to add the component (A) little by little.

When preparing the oral emulsion composition of the present invention, the component (B) is preferably dissolved in water or a polyhydric alcohol (i.e., an aqueous sorbitol solution or a sorbitol polyhydric alcohol solution). . As polyhydric alcohol here, (D) component is preferable. In particular, when preparing a non-aqueous composition, it is preferable to use the sorbitol polyhydric alcohol solution.

As the sorbitol aqueous solution used for the preparation, an aqueous sorbitol solution of 75% by mass or less is preferable, and an aqueous sorbitol solution of 70% by mass or less is more preferable. The sorbitol polyhydric alcohol solution used for the preparation is preferably a sorbitol polyhydric alcohol solution of 70% by mass or less, more preferably a sorbitol polyhydric alcohol solution of 60, 50, 40, or 30% by mass or less.

The emulsified composition of the present invention can be used for various purposes. A composition containing a relatively large amount of hydrocarbon oil (especially a composition containing a hydrocarbon oil and a surfactant) is used as an oral composition because there is a high possibility that the separation of the hydrocarbon oil will significantly impair the feeling of use. Although this is not common, the emulsified composition of the present invention can be preferably used as an oral composition because of its high stability.

The oral emulsified composition of the present invention is not particularly limited, but may be used in accordance with conventional methods such as toothpaste, liquid dentifrice, mouthwash, gel, ointment, paste, and gum. It can be made into a usual dosage form such as

To the extent that the effects of the present invention are not impaired, the oral emulsified composition of the present invention may contain known components that can be contained in oral compositions, as long as the effects of the present invention are not impaired. . The oral emulsified composition of the present invention to which such components are added is prepared, for example, by adding and mixing the components together when the components (B) and (C) are first stirred and mixed. be able to.

Examples of such known ingredients include abrasives, wetting agents, fragrances, activators, sweeteners, preservatives, colorants, pH adjusters, stabilizers, flavoring agents, astringents, thickeners, and others. and the like. In addition, such a well-known component can be used individually by 1 type or in combination of 2 or more types.

Abrasives include dicalcium phosphate dihydrate and anhydrate, calcium phosphate, tricalcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, anhydrous silicic acid, silica gel, aluminum silicate, calcium silicate, Insoluble sodium metaphosphate, magnesium tertiary phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, hydroxyapatite, synthetic resin, bioactive glass, and the like can be used.

Wetting agents include, for example, alcohols (monohydric alcohols or polyhydric alcohols), more specifically ethanol. As the polyhydric alcohol, a dihydric or trihydric alcohol is preferably exemplified. Dihydric alcohols and trihydric alcohols are not particularly limited, but preferred examples include ethylene glycol, propanediol, diethylene glycol, polyethylene glycol, 1,3-butylene glycol, glycerin and the like. As propanediol, both propylene glycol (1,2-propanediol) and 1,3-propanediol can be preferably used. Among them, propylene glycol, 1,3-propanediol, 1,3-butylene glycol and glycerin are preferred, and propylene glycol and glycerin are particularly preferred. Wetting agents can be used alone or in combination of two or more.

Examples of fragrances include menthol, anethole, carvone, eugenol, limonene, peppermint oil, spearmint oil, wintergreen, methyl salicylate, cionaire, thymol, clove oil, eucalyptus oil, rosemary oil, sage oil, lemon oil, and orange oil. , ocimene oil, citronellol, methyl eugenol and the like.

Sweeteners include, for example, saccharin sodium, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, asparatylphenylalanyl methyl ester, α-methoxycinnamic aldehyde, xylit, sucralose, palatinose, stevia. fin, erythritol and the like.

Examples of antiseptics include parabens such as methylparaben, ethylparaben, propylparaben and butylparaben, sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride.

Examples of the coloring agent include legal dyes such as Blue No. 1, Yellow No. 4, Red No. 202, and Green No. 3, mineral dyes such as ultramarine, enhanced ultramarine, and Prussian blue, and titanium oxide.

Examples of pH adjusters include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, phytic acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, and the like. be done.

Stabilizers include, for example, sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate and the like.

Examples of flavoring agents include tea extract, dry distillation of tea, propolis extract, sodium glutamate and the like.

Examples of astringents include sodium bicarbonate, aluminum lactate, zinc compounds and the like.

Thickeners include, for example, cellulose derivatives such as hydroxypropylcellulose, hydroxypropylmethylcellulose and hydroxymethylethylcellulose; gums such as xanthan gum, locust bing gum, carrageenan, tragacanth gum, karaya gum, gum arabic and gellan gum; polyvinyl alcohol; Synthetic binders such as sodium, carboxyvinyl polymer, polyvinylpyrrolidone, thickening silica, aluminum silica gel, inorganic binders such as Veegum, sodium alginate, pectin, agar, gelatin, soybean polysaccharides, sodium chondroitin sulfate, sodium hyaluronate etc.

Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; potassium salts such as potassium nitrate and potassium chloride; strontium salts such as strontium chloride; , protease, enzymes such as lytic enzymes (retech enzymes); tranexamic acid, ε-aminocaproic acid, aluminum chlorohydroxyallantoin, allantoin, dihydrocholesterol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, isopropylmethylphenol, glycerophosphate, chlorophyll, gluconic acid Copper, sodium chloride, water-soluble inorganic phosphate compounds, pyrrolidonecarboxylic acid, chlorhexidine salts, triclosan, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride; dl-α-tocopherol acetate, pyridoxine acetate, ascorbic acid or salts thereof, etc. of vitamins; basic amino acids such as arginine, lysine, citrulline, ornithine, creatine, histidine, diaminobutanoic acid, diaminopropionic acid or salts thereof; flavonoids, polyphenols such as phenolic acid; aloe, ginkgo biloba, agaricus, oolong tea, Chamomile, Chinese quince, Gymnema, Kumazasa, Sweet tea, Tochu tea, Houttuynia cordata, Hatomugi, Megusurinoki, Wormwood, Green tea, Rooibos, Lemon balm, Rosemary, Crabmin, Rakanka, Perilla, Cranberry, Yarrow, Elder, Licorice, Mint, Eucalyptus, Guarana , licorice, bodaiju, hops, cacao, mulberry leaves, thyme, plant extracts such as Scutellaria root, lactic acid bacteria, hydrogen peroxide and the like.

The amounts of these known components to be blended can be appropriately adjusted with reference to the amounts blended in ordinary oral compositions, as long as the effects of the present invention are not hindered.

In this specification, the term "comprising" includes "consisting essentially of" and "consisting of." In addition, the present invention encompasses all arbitrary combinations of the constituent elements described herein.

Also, the various characteristics (property, structure, function, etc.) described for each of the embodiments of the invention described above may be combined in any way to identify subject matter encompassed by the invention. That is, the invention encompasses all subject matter consisting of any and all possible combinations of the features described herein.

The present invention will be described in more detail below, but the present invention is not limited to the following examples. In addition, hereinafter, "%" indicates "% by mass" unless otherwise specified. In addition, unless otherwise specified, the compounding amount of each component described in each table is expressed in "% by mass". The sorbitol used was all D-sorbitol. In addition, among the raw materials listed in each table, those that do not include words representing the number of fatty acid bonds (eg, di, tri, etc.) represent "mono". (For example, polyglyceryl-10 laurate means polyglyceryl-10 monolaurate.) POE stands for polyoxyethylene and PEG for polyethylene glycol, respectively.

Study 1
According to the compositions shown in Tables 1 and 2, 35% 70% sorbitol solution (70% sorbitol aqueous solution), 60% light liquid paraffin, and 5% each of various surfactants were mixed to prepare emulsified compositions. Mixing was performed in more detail as follows. Glycerin or 70% sorbitol solution and various surfactants were added to a container (beaker) and mixed by manual stirring using a glass rod or by stirring with a disper mixer. At this time, heating was performed as necessary. Light liquid paraffin was added little by little while stirring was continued.

Immediately after preparation, each composition obtained was visually observed to confirm the presence or absence of phase separation. Those in which the gel state (emulsified state) was maintained without phase separation were evaluated as ◯, and those in which the oil phase was separated were evaluated as x (evaluation of preparation feasibility). Further, the resulting composition was filled in a glass container, allowed to stand at room temperature (25° C.) for 1 week, and then visually observed again for evaluation in the same manner (evaluation of stability for 1 week). The results are also shown in Tables 1 and 2.

The alkyl glycoside used in Table 1 is Plantacare 1200UP (BASF), more specifically, an aqueous solution of polyglycoside of alkyl alcohol having 12 to 16 carbon atoms. The water content is about 47-50%.

Consideration 2
In order to study the stability of the resulting composition when the amount of light liquid paraffin and the amount of polyglycerol monofatty acid ester are changed, compositions were prepared in the same manner as described above according to the compositions shown in Tables 3 and 4. product preparation and stability evaluation. The evaluation results are also shown in Tables 3 and 4.

In addition, in Table 3, the viscosity of the obtained emulsified composition increased as the amount of light liquid paraffin increased. Further, in Table 4, the smaller the amount of polyglycerol monofatty acid ester (specifically, the amount of polyglyceryl-10 laurate), the lower the viscosity of the emulsion composition obtained.

Consideration 3
Consideration was given to preparing compositions with lower water content.

Among the raw materials used in Examinations 1 and 2 above, the 70% sorbitol solution is a 70% sorbitol aqueous solution, so water is contained in the prepared composition. Therefore, sorbitol (powder) was used to prepare a sorbitol aqueous solution (80 to 90% sorbitol solution) with an increased sorbitol content, and an attempt was made to use this in the preparation of a composition. An 80-90% sorbitol solution could be prepared by dissolving sorbitol (powder) in water while heating, but sorbitol precipitated when the solution was returned to room temperature. Moreover, when preparing a composition using an 80 to 90% sorbitol solution, sorbitol precipitated when the temperature was lowered, and an emulsified composition (gel-like) was not obtained.

Therefore, next, we searched for a polyhydric alcohol capable of dissolving sorbitol (powder). According to the composition shown in Table 5, sorbitol (powder) was dissolved in various polyhydric alcohols to prepare 70%, 50%, or 30% sorbitol polyhydric alcohol solutions. The results are also shown in Table 5.

Using the obtained sorbitol polyhydric alcohol solution, according to the composition shown in Table 6, composition preparation and stability evaluation were performed in the same manner as described above. The evaluation results are also shown in Table 6. Of the examples shown in Table 6, sorbitol powder was used instead of the sorbitol polyhydric alcohol solution only for the preparation of Comparative Example 6-1, but the sorbitol powder did not dissolve even when heated.

Claims (7)

(A) a hydrocarbon oil,
(B) sorbitol, and (C) an emulsified composition containing polyglycerol monofatty acid ester and/or alkyl glycoside ,
An emulsion composition for oral cavity containing 40 to 80% by mass of (A), 10.5 to 38.5% by mass of (B), 1 to 5% by mass of (C), and 20% by mass or less of water . A composition according to claim 1 , wherein the hydrocarbon oil is paraffinic. 3. The composition according to claim 1, wherein the polyglycerin mono-fatty acid ester is a monoester of a fatty acid having 8 to 24 carbon atoms and polyglycerin. Polyglycerin monofatty acid ester consists of polyglycerin monocaprate, polyglycerin monolaurate, polyglycerin monomyristate, polyglycerin monostearate, polyglycerin monopalmitate, and polyglycerin monooleate 3. The composition according to claim 1 or 2 , which is at least one selected from the group. A composition according to any preceding claim, wherein the polyglycerin of the polyglycerin monofatty acid ester contains an average of 4 to 12 glycerin units. The composition according to any one of claims 1 to 5 , further comprising glycerin and/or propylene glycol and being non-aqueous. The composition according to any one of claims 1 to 6 , which is gel or cream.