TW202038892A - Water-in-oil emulsion composition containing nicotinamide - Google Patents

Water-in-oil emulsion composition containing nicotinamide Download PDF

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TW202038892A
TW202038892A TW108148043A TW108148043A TW202038892A TW 202038892 A TW202038892 A TW 202038892A TW 108148043 A TW108148043 A TW 108148043A TW 108148043 A TW108148043 A TW 108148043A TW 202038892 A TW202038892 A TW 202038892A
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polyglycerol
water
sorbitan
acid
emulsion composition
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TWI838448B (en
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岡真佐人
前澤閑久
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日商樂敦製藥股份有限公司
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    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • A61K8/894Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone modified by a polyoxyalkylene group, e.g. cetyl dimethicone copolyol
    • AHUMAN NECESSITIES
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    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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    • AHUMAN NECESSITIES
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    • A61Q19/00Preparations for care of the skin
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    • AHUMAN NECESSITIES
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Abstract

Provided is a water-in-oil emulsion composition having an excellent feel on use. A water-in-oil emulsion composition containing (A) 3 mass% or more of nicotinamide; (B) one or more surfactants selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants; and (C) one or more oil-soluble thickeners selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents is prepared.

Description

含有菸鹼醯胺之油中水型乳化組成物Water-in-oil emulsion composition containing nicotine amide

本發明係關於一種含有菸鹼醯胺之油中水型乳化組成物。The present invention relates to a water-in-oil emulsion composition containing nicotine amide.

已知菸鹼醯胺係維生素類的1種,到目前為止係於護膚領域中當作血液循環促進、抗發炎、腦醯胺合成促進等成分而使用的成分,進而亦具有作為美白、抗皺、抗衰老之效果(例如專利文獻1)。One type of nicotinic amine-based vitamins is known. So far, it is a component used in the field of skin care as blood circulation promotion, anti-inflammation, and brain amine synthesis promotion. It is also used as whitening, anti-wrinkle, Anti-aging effect (for example, Patent Document 1).

提出有一種含有菸鹼醯胺、特定的活性劑、及凡士林之水中油型乳化組成物(專利文獻2)。 [先前技術文獻] [專利文獻]An oil-in-water emulsion composition containing nicotine amide, a specific active agent, and petrolatum is proposed (Patent Document 2). [Prior Technical Literature] [Patent Literature]

[專利文獻1]日本特開2004-217629號公報。 [專利文獻2]日本特開2018-172304號公報。[Patent Document 1] JP 2004-217629 A. [Patent Document 2] Japanese Patent Application Laid-Open No. 2018-172304.

[發明所欲解決之課題][The problem to be solved by the invention]

一方面,油中水型組成物具有高保濕性及耐水性等優異之特性,另一方面,因容易產生分離等問題而難以賦予充分的穩定性,與水中油型組成物相比,製劑方面的課題較多。On the one hand, the water-in-oil composition has excellent characteristics such as high moisture retention and water resistance. On the other hand, it is difficult to provide sufficient stability due to problems such as separation. Compared with the oil-in-water composition, the formulation There are many topics.

本發明的目的在於提供一種含有高濃度的菸鹼醯胺之油中水型乳化組成物,該油中水型乳化組成物具有良好的穩定性及使用感。 [用以解決課題之手段]The object of the present invention is to provide a water-in-oil emulsion composition containing a high concentration of nicotine amide, which has good stability and a sense of use. [Means to solve the problem]

本發明者等人為了解決本課題而反覆進行了努力研究,結果發現,於本發明中,藉由製成含有(A)菸鹼醯胺、(B)特定的界面活性劑、以及(C)油溶性增黏劑之油中水型乳化組成物,能獲得使用感優異且穩定性優異之油中水型乳化組成物,從而完成了本發明。The inventors of the present invention have conducted diligent studies to solve this problem. As a result, they found that in the present invention, (A) nicotine amide, (B) a specific surfactant, and (C) The water-in-oil emulsified composition of the oil-soluble tackifier can obtain a water-in-oil emulsified composition with excellent feeling in use and excellent stability, thereby completing the present invention.

亦即,本發明提供下述所列舉之油中水型乳化組成物。 項1. 一種油中水型乳化組成物,含有:(A)菸鹼醯胺3質量%以上;(B)界面活性劑,係選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上;以及(C)油溶性增黏劑,係選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上。 項2. 如項1所記載之油中水型乳化組成物,其中前述(A)成分的含量為3質量%至10質量%。 項3. 如項1或2所記載之油中水型乳化組成物,其中前述(B)成分為選自由PEG(polyethylene glycol;聚乙二醇)-10二甲基矽酮、PEG-3二甲基矽酮、PEG-12二甲基矽酮、PEG/PPG(polypropylene glycol;聚丙二醇)-19/19二甲基矽酮、聚矽酮13、PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、甲基聚矽氧烷-鯨蠟基甲基聚矽氧烷-聚(氧乙烯-氧丙烯)甲基聚矽氧烷共聚物、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、雙丁基二甲基矽酮聚甘油-3、聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-3二矽氧烷二甲基矽酮;月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、山梨醇酐三油酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐三異硬脂酸酯、山梨醇酐硬脂酸酯、山梨醇酐倍半硬脂酸酯、山梨醇酐三硬脂酸酯;聚甘油-2三異硬脂酸酯、聚甘油-2異硬脂酸酯、聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-6縮合蓖麻醇酸酯、聚甘油-6五異硬脂酸酯、聚甘油-6五油酸酯、聚甘油-6五羥基硬脂酸酯、油酸甘油酯、倍半油酸甘油酯、三油酸甘油酯、倍半異硬脂酸甘油酯、異硬脂酸甘油酯、三異硬脂酸甘油酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、及三硬脂酸甘油酯所組成之群組中的1種以上。 項4. 如項1至3中任一項所記載之油中水型乳化組成物,其中前述(C)成分為選自由二甲基二硬脂基銨鋰膨潤石、苄基二甲基硬脂基銨鋰膨潤石、經氯化二硬脂基二甲基銨處理之矽酸鋁鎂、糊精棕櫚酸酯、糊精油酸酯、糊精硬脂酸酯、糊精肉豆蔻酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精(棕櫚酸/己基癸酸)酯、及菊糖硬脂酸酯、二丁基月桂醯麩胺醯胺、二丁基乙基己醯基麩胺醯胺所組成之群組中的1種以上。 項5. 如項1至4中任一項所記載之油中水型乳化組成物,其進而含有(D)紫外線吸收劑。 項6. 如項5所記載之油中水型乳化組成物,其中前述(D)成分的總含量為20質量%以下。 項7. 如項1至6中任一項所記載之油中水型乳化組成物,其進而含有(E)紫外線防禦劑。 項8. 如項1至7中任一項所記載之油中水型乳化組成物,其中前述(B)成分為選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的2種以上之界面活性劑。 項9. 如項1至7中任一項所記載之油中水型乳化組成物,其中前述(B)成分至少為選自矽酮系界面活性劑中的2種以上之界面活性劑之組合。 項10 如項1至7中任一項所記載之油中水型乳化組成物,其中前述(B)成分為(B)-1成分及(B)-2成分之組合,前述(B)-1成分係選自矽酮系界面活性劑中的1種以上之界面活性劑,前述(B)-2成分係選自由山梨醇酐硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、異硬脂酸甘油酯、倍半異硬脂酸甘油酯、油酸甘油酯、倍半油酸甘油酯、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、及聚甘油-10五油酸酯所組成之群組中的1種以上之界面活性劑。 項11. 如項1至10中任一項所記載之油中水型乳化組成物,其中前述(D)紫外線吸收劑為選自由水楊酸系紫外線吸收劑、肉桂酸系紫外線吸收劑、苯甲醯甲烷系紫外線吸收劑、苯甲酸酯衍生物紫外線吸收劑、三嗪衍生物紫外線吸收劑、亞苄基丙二酸酯衍生物紫外線吸收劑、奧克立林系紫外線吸收劑、咪唑磺酸衍生物紫外線吸收劑、及二苯甲酮衍生物紫外線吸收劑所組成之群組中的1種以上。 項12. 如項1至11中任一項所記載之油中水型乳化組成物,其中前述(D)紫外線吸收劑為選自由對甲氧基肉桂酸2-乙基己酯、4-第三丁基-4'-甲氧基二苯甲醯甲烷、2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯、2,4-雙-[{4-(2-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪、2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪、2-苯基苯并咪唑-5-磺酸所組成之群組中的1種以上。 [發明功效]That is, the present invention provides the water-in-oil emulsion composition listed below. Item 1. A water-in-oil emulsified composition containing: (A) Nicotinamide 3% by mass or more; (B) Surfactant, selected from silicone surfactants, sorbitan ester surfactants, and polyglycerol One or more of the group consisting of ester surfactants and glyceride surfactants; and (C) oil-soluble tackifiers, selected from clay-based tackifiers, dextrin fatty acid esters, and inulin fats One or more of the group consisting of acid ester and amino acid oil gelling agent. Item 2. The water-in-oil emulsion composition as described in Item 1, wherein the content of the component (A) is 3% by mass to 10% by mass. Item 3. The water-in-oil emulsion composition as described in item 1 or 2, wherein the aforementioned component (B) is selected from PEG (polyethylene glycol; polyethylene glycol)-10 dimethyl silicone, PEG-3 dimethyl silicone Ketones, PEG-12 Dimethicone, PEG/PPG (polypropylene glycol)-19/19 Dimethicone, Polysiloxane 13, PEG-9 Dimethicone Base silicone, methyl polysiloxane-cetyl methyl polysiloxane-poly(oxyethylene-oxypropylene) methyl polysiloxane copolymer, lauryl PEG-9 polydimethylsiloxane Ethyl Dimethicone, Dibutyl Dimethicone Polyglycerol-3, Polyglycerol-3 Polydimethylsiloxane Ethyl Dimethicone, Polyglycerol-3 Disiloxane Dimethyl Base silicone; lauryl polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone, sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, sorbitan Alcohol sesquistearate, sorbitan isostearate, sorbitan triisostearate, sorbitan stearate, sorbitan sesquistearate, sorbitan Tristearate; polyglycerol-2 triisostearate, polyglycerol-2 isostearate, polyglycerol-10 condensed ricinoleate, polyglycerol-10 five isostearate, poly Glycerol-10 pentaoleate, polyglycerol-10 pentastearate, polyglycerol-10 pentahydroxystearate, polyglycerol-6 condensed ricinoleate, polyglycerol-6 pentaisostearate , Polyglycerol-6 pentaoleate, polyglycerol-6 pentahydroxystearate, glyceryl oleate, glyceryl sesquioleate, glyceryl trioleate, glyceryl sesquiisostearate, isostearin One or more of the group consisting of glyceryl fatty acid, glyceryl triisostearate, glyceryl stearate, glyceryl sesquistearate, and glyceryl tristearate. Item 4. The water-in-oil emulsion composition according to any one of items 1 to 3, wherein the aforementioned component (C) is selected from the group consisting of dimethyl distearyl ammonium lithium bentonite and benzyl dimethyl stearyl ammonium Lithium bentonite, magnesium aluminum silicate treated with distearyl dimethyl ammonium chloride, dextrin palmitate, dextrin oleate, dextrin stearate, dextrin myristate, dextrin (palm Acid/ethylhexanoic acid) ester, dextrin (palmitic acid/hexyl decanoic acid) ester, and inulin stearate, dibutyl lauric acid glutamine amide, dibutyl ethyl hexyl glutamine amide One or more of the group consisting of amines. Item 5. The water-in-oil emulsion composition as described in any one of items 1 to 4, which further contains (D) an ultraviolet absorber. Item 6. The water-in-oil emulsion composition as described in Item 5, wherein the total content of the aforementioned (D) component is 20% by mass or less. Item 7. The water-in-oil emulsion composition as described in any one of items 1 to 6, which further contains (E) an ultraviolet protection agent. Item 8. The water-in-oil emulsion composition according to any one of items 1 to 7, wherein the aforementioned component (B) is selected from silicone surfactants, sorbitan ester surfactants, and polyglycerol ester surfactants , And 2 or more surfactants in the group consisting of glyceride surfactants. Item 9. The water-in-oil emulsion composition according to any one of items 1 to 7, wherein the aforementioned component (B) is at least a combination of two or more surfactants selected from silicone-based surfactants. Item 10 The water-in-oil emulsion composition according to any one of items 1 to 7, wherein the component (B) is a combination of component (B)-1 and component (B)-2, and component (B)-1 One or more surfactants selected from silicone surfactants. The aforementioned (B)-2 component is selected from sorbitan stearate, sorbitan isostearate, and sorbitan Hemiisostearate, sorbitan oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate, sesquiisostearate Glycerides, glyceryl oleate, glyceryl sesquioleate, polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol One or more surfactants in the group consisting of -10 pentaoleate. Item 11. The water-in-oil emulsion composition according to any one of items 1 to 10, wherein the aforementioned (D) ultraviolet absorber is selected from the group consisting of salicylic acid-based ultraviolet absorbers, cinnamic acid-based ultraviolet absorbers, and benzyl methane UV absorber, benzoate derivative UV absorber, triazine derivative UV absorber, benzylidene malonate derivative UV absorber, octocrelin-based UV absorber, imidazole sulfonic acid derivative One or more types of ultraviolet absorbers and ultraviolet absorbers of benzophenone derivatives. Item 12. The water-in-oil emulsion composition according to any one of items 1 to 11, wherein the aforementioned (D) ultraviolet absorber is selected from the group consisting of 2-ethylhexyl p-methoxycinnamate and 4-tert-butyl -4'-Methoxy dibenzyl methane, 2-[4-(diethylamino)-2-hydroxybenzyl]hexyl benzoate, 2,4-bis-[{4-(2 -Ethylhexyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[4-(2 -Ethylhexyloxycarbonyl)anilino]-1,3,5-triazine, 2-phenylbenzimidazole-5-sulfonic acid group consisting of one or more. [Invention Effect]

藉由本發明能夠提供一種穩定性優異之油中水型乳化組成物。The present invention can provide a water-in-oil emulsion composition with excellent stability.

本說明書中,含量的單位「質量%」與「g/100g」同義。In this manual, the unit of content "mass%" is synonymous with "g/100g".

高濃度含有具有多種有效性之菸鹼醯胺之製劑對於製成具有多功能性之製劑而言非常有用,但於油中水型乳化組成物中高濃度含有菸鹼醯胺之情形時,製劑變得不穩定或黏膩,而於黏著性之方面對使用感有影響。本發明者等人發現,獲得如此含有高濃度的菸鹼醯胺且兼顧良好的穩定性及使用感之油中水型組成物尤其非常困難。A formulation containing a high concentration of nicotine amide with multiple effectiveness is very useful for making a multi-functional formulation, but when a high concentration of nicotine amide is contained in a water-in-oil emulsion composition, the formulation changes It is unstable or sticky, and the adhesiveness has an impact on the feeling of use. The inventors of the present invention found that it is particularly difficult to obtain a water-in-oil type composition that contains such a high concentration of nicotine amine and has good stability and usability.

到目前為止的油中水型組成物的系統中,無法使高濃度的菸鹼醯胺穩定地乳化,而要求兼顧良好的使用感及充分的穩定性之含有高濃度的菸鹼醯胺之油中水型組成物。例如,藉由含有乳化性之矽酮彈性體、界面活性劑、及紫外線吸收劑等而具有特徵性使用感之油中水乳化型組成物,由於不僅不具有充分的穩定性,並且具有於施加剪切應力時會釋出水相此種與一般的乳化組成物不同的特徵性使用感,故而缺乏通用性。In the conventional water-in-oil type composition system, the high concentration of nicotine amide cannot be stably emulsified, and the oil containing high concentration of nicotine amide is required to have a good feeling of use and sufficient stability. Medium water type composition. For example, a water-in-oil emulsified composition that has a characteristic feeling of use by containing emulsifying silicone elastomers, surfactants, and ultraviolet absorbers, etc., not only does not have sufficient stability, but also has the advantages of application Under shear stress, it releases the characteristic feeling of use which is different from the general emulsified composition, which is the water phase, and therefore lacks versatility.

進而,雖然存在著藉由將乳化性之矽酮彈性體與固化劑組合而於相對高溫下的穩定性提高之油中水乳化型組成物,但難言具有充分的穩定性,調配有大量的固體蠟,使用感變得乾澀。Furthermore, although there is an oil-in-oil emulsified composition whose stability at relatively high temperatures is improved by combining an emulsifying silicone elastomer and a curing agent, it is hard to say that it has sufficient stability and a large amount of Solid wax makes the feeling dry.

本發明的油中水型乳化組成物含有:(A)菸鹼醯胺3質量%以上;(B)界面活性劑,係選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上;以及(C)油溶性增黏劑,係選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上。The water-in-oil emulsion composition of the present invention contains: (A) Nicotinamide 3% by mass or more; (B) Surfactant, selected from silicone surfactants, sorbitan ester surfactants, and poly One or more of the group consisting of glyceride surfactants and glyceride surfactants; and (C) oil-soluble tackifier, selected from clay-based tackifiers, dextrin fatty acid esters, and inulin One or more types of fatty acid esters and amino acid oil gelling agents.

[(A)菸鹼醯胺] 本發明的油中水型乳化組成物中所含之菸鹼醯胺係菸鹼酸(維生素B3 /維生素PP)的醯胺化合物,係水溶性維生素。菸鹼酸可為來自天然物之萃取物,亦可為藉由公知的方法所合成之物。具體而言,可使用日本藥典第17次修訂版中所收錄之成分。已知有血液循環促進作用、或肌膚粗糙改善作用、以及黑色素生成抑制作用或美白效果。Niacinamide based nicotinic acid (vitamin B 3 / vitamin PP) Amides of the compounds contained [(A) niacinamide] in water-in-oil emulsion composition of the present invention, the water-soluble vitamins. Nicotinic acid may be an extract from natural products, or it may be synthesized by a known method. Specifically, the ingredients included in the 17th revised edition of the Japanese Pharmacopoeia can be used. It is known to have blood circulation promotion effect, or rough skin improvement effect, and melanin production suppression effect or whitening effect.

本發明的油中水型乳化組成物中,(A)成分的含量相對於油中水型乳化組成物的總量可根據與其他成分之平衡而適宜設定。就緩和菸鹼醯胺可能產生之乾燥、黏膩、或刺激之觀點而言,相對於油中水型乳化組成物的總量,(A)成分的含量較佳為20質量%以下,更佳為10質量%以下,進而較佳為8質量%以下。另外,就用以充分賦予美白、抗衰老等有效性所必需之含量而言,相對於油中水型乳化組成物的總量,(A)成分的總含量為3質量%以上。(A)成分較佳可設為4質量%以上,更佳可設為5質量%以上。相對於油中水型乳化組成物的總量,(A)成分的總含量較佳為3質量%至20質量%,更佳為3質量%至15質量%,進而較佳為3質量%至10質量%,進而更佳為3質量%至8質量%。In the water-in-oil emulsion composition of the present invention, the content of the component (A) relative to the total amount of the water-in-oil emulsion composition can be appropriately set according to the balance with other components. From the viewpoint of alleviating dryness, stickiness, or irritation that may be caused by nicotine amide, the content of component (A) is preferably 20% by mass or less, more preferably, relative to the total amount of water-based emulsified composition in oil It is 10% by mass or less, and more preferably 8% by mass or less. In addition, in terms of the content necessary to sufficiently impart whitening and anti-aging effects, the total content of the (A) component is 3% by mass or more relative to the total amount of the water-type emulsion composition in the oil. The component (A) can be preferably 4% by mass or more, and more preferably 5% by mass or more. The total content of component (A) is preferably 3% by mass to 20% by mass, more preferably 3% by mass to 15% by mass, and still more preferably 3% by mass to 15% by mass, relative to the total amount of the water-in-oil emulsion composition. 10% by mass, more preferably 3% to 8% by mass.

[(B)界面活性劑,選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上] 作為本發明的油中水型乳化組成物中所含之界面活性劑,可列舉選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上。此種界面活性劑的HLB值並無限定,較佳為15以下、更佳為10以下、進而較佳為9以下,進而更佳為8以下、最佳為2至6。[(B) Surfactant, one or more selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerol ester surfactants, and glyceride surfactants] The surfactant contained in the water-in-oil emulsion composition of the present invention may be selected from the group consisting of silicone surfactants, sorbitan ester surfactants, polyglycerol ester surfactants, and glyceride surfactants. One or more of the group consisting of agents. The HLB value of such a surfactant is not limited, and is preferably 15 or less, more preferably 10 or less, still more preferably 9 or less, still more preferably 8 or less, and most preferably 2-6.

此處,本發明中的HLB(Hydphile-Lipophile Balance;親水親油平衡值)係表示親水性-親油性之平衡之指標,由基於小田、寺村等人之下述(式1)計算。 HLB=(Σ無機性值/Σ有機性)×10・・・(式1) 此處,Σ無機性值/Σ有機性被稱為IOB(Inorganic-Organic balance;無機有機平衡值),可藉由下述方式算出:基於各種原子及各官能基所設定之「無機性值」、「有機性值」,累計構成界面活性劑等有機化合物之原子及官能基的「無機性值」、「有機性值」(參照甲田善生著作「有機概念圖-基礎與應用-」,第11頁至第17頁,三共出版,1984年發行)。Here, HLB (Hydphile-Lipophile Balance; Hydrophile-Lipophile Balance) in the present invention is an index representing the balance of hydrophilicity-lipophile, and is calculated by the following (Equation 1) based on Oda, Teramura and others. HLB=(Σ Inorganic Value/Σ Organic)×10...(Equation 1) Here, the Σ inorganic value/Σ organic is called IOB (Inorganic-Organic balance; inorganic-organic balance), which can be calculated by the following method: based on the "inorganic value" set by various atoms and functional groups , "Organic value", which accumulates the "inorganic value" and "organic value" of the atoms and functional groups that constitute organic compounds such as surfactants (refer to Koda Yoshio's book "Organic Concept Map-Basics and Applications -", 11 Pages to 17, published by Sankyo, issued in 1984).

[矽酮系界面活性劑] 作為本發明的油中水型乳化組成物中所含之矽酮系界面活性劑,只要為於醫藥品、準藥品或化妝品領域中,例如用作皮膚外用劑之成分之化合物,則無特別限定。[Silicone Surfactant] The silicone-based surfactant contained in the water-in-oil emulsion composition of the present invention is not particularly limited as long as it is a compound used as a component of an external preparation for skin in the fields of pharmaceuticals, quasi-drugs, or cosmetics. .

矽酮系界面活性劑可較佳地例示:聚醚改性矽酮系界面活性劑、聚醚-烷基共改性矽酮系界面活性劑、聚甘油改性矽酮系界面活性劑、或聚甘油-烷基共改性矽酮系界面活性劑。詳細而言,可列舉:作為聚氧乙烯-甲基聚矽氧烷共聚物之PEG-10二甲基矽酮、PEG-3二甲基矽酮、PEG-12二甲基矽酮、PEG/PPG-19/19二甲基矽酮、聚矽酮13、以及PEG-9聚二甲基矽烷氧基乙基二甲基矽酮等聚醚改性矽酮系界面活性劑;甲基聚矽氧烷-鯨蠟基甲基聚矽氧烷-聚(氧乙烯-氧丙烯)甲基聚矽氧烷共聚物、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮等聚醚-烷基共改性矽酮系界面活性劑;雙丁基二甲基矽酮聚甘油-3、聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-3二矽氧烷二甲基矽酮等聚甘油改性矽酮系界面活性劑;月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮等聚甘油-烷基共改性矽酮系界面活性劑。Silicone-based surfactants can be preferably exemplified: polyether-modified silicone-based surfactants, polyether-alkyl co-modified silicone-based surfactants, polyglycerol-modified silicone-based surfactants, or Polyglycerol-alkyl co-modified silicone surfactant. In detail, it can be listed: PEG-10 dimethyl silicone, PEG-3 dimethyl silicone, PEG-12 dimethyl silicone, PEG/ Polyether-modified silicone surfactants such as PPG-19/19 dimethyl silicone, polysilicon 13, and PEG-9 polydimethylsiloxyethyl dimethyl silicone; methyl polysilicon Oxyane-cetyl methyl polysiloxane-poly(oxyethylene-oxypropylene) methyl polysiloxane copolymer, lauryl PEG-9 polydimethylsiloxane oxyethyl dimethyl silicone, etc. Polyether-alkyl co-modified silicone surfactants; dibutyl dimethyl silicone polyglycerol-3, polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone, polyglycerol- 3 Polyglycerol-modified silicone-based surfactants such as disiloxane dimethyl silicone; Lauryl polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone and other polyglycerol-alkyl co-modified Silicone-based surfactants.

本發明中,並無限定,較佳為PEG-10二甲基矽酮、PEG-3二甲基矽酮、PEG-12二甲基矽酮、PEG/PPG-19/19二甲基矽酮、聚矽酮13、PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、甲基聚矽氧烷-鯨蠟基甲基聚矽氧烷-聚(氧乙烯-氧丙烯)甲基聚矽氧烷共聚物、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、雙丁基二甲基矽酮聚甘油-3、聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-3二矽氧烷二甲基矽酮、或月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮,這些之中,更佳為PEG-10二甲基矽酮、PEG-3二甲基矽酮、PEG-12二甲基矽酮、PEG/PPG-19/19二甲基矽酮、聚矽酮13、以及PEG-9聚二甲基矽烷氧基乙基二甲基矽酮甲基聚矽氧烷-鯨蠟基甲基聚矽氧烷-聚(氧乙烯-氧丙烯)甲基聚矽氧烷共聚物、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、或月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮。這些之中,就穩定性等觀點而言,進而更佳為PEG-10二甲基矽酮、PEG/PPG-19/19二甲基矽酮、PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、或月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮,尤佳為PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮。In the present invention, there is no limitation, preferably PEG-10 dimethyl silicone, PEG-3 dimethyl silicone, PEG-12 dimethyl silicone, PEG/PPG-19/19 dimethyl silicone , Polysiloxane 13, PEG-9 polydimethylsiloxane oxyethyl dimethyl siloxane, methyl polysiloxane-cetyl methyl polysiloxane-poly (oxyethylene-oxypropylene) methyl -Based polysiloxane copolymer, lauryl PEG-9 polydimethylsiloxy ethyl dimethyl silicone, dibutyl dimethyl silicone polyglycerol-3, polyglycerol-3 polydimethylsiloxane Oxyethyl dimethyl silicone, polyglyceryl-3 disiloxane dimethyl silicone, or lauryl polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone, among these, More preferably PEG-10 dimethyl silicone, PEG-3 dimethyl silicone, PEG-12 dimethyl silicone, PEG/PPG-19/19 dimethyl silicone, polysilicon 13, and PEG -9 polydimethylsiloxane oxyethyl dimethyl silicone methyl polysiloxane-cetyl methyl polysiloxane-poly(oxyethylene-oxypropylene) methyl polysiloxane copolymer, Lauryl PEG-9 polydimethylsiloxy ethyl dimethyl silicone, or lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone. Among these, from the viewpoint of stability and the like, PEG-10 dimethyl silicone, PEG/PPG-19/19 dimethyl silicone, and PEG-9 polydimethylsiloxyethyl are more preferred. Dimethicone, lauryl PEG-9 polydimethylsiloxy ethyl dimethyl silicone, or lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, especially preferred It is PEG-9 dimethicone oxyethyl dimethyl silicone, PEG-10 dimethyl siloxane, PEG-9 dimethicone oxyethyl dimethyl silicone, lauryl PEG- 9 Polydimethylsiloxy ethyl dimethyl silicone, lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone.

矽酮系界面活性劑可使用市售之製品或合成而使用。Silicone-based surfactants can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉:KF-6017(HLB4.5,信越化學工業公司)、KF-6019(HLB4.5,信越化學工業公司)、KF-6015(HLB4.5,信越化學工業公司)、SH3772M(HLB6,東麗道康寧公司)、SH3775M(HLB5,東麗道康寧公司)、BY-11-030(HLB6,東麗道康寧公司)、KF-6004(HLB9,信越化學工業公司)、KF-6011(HLB14.5,信越化學工業公司)、FZ-2222、FZ-2233、KF-6028(HLB4,信越化學工業公司)、ABIL EM90(Goldschmidt公司製造)、KF-6048(HLB3.5,信越化學工業公司)、KF-6038(HLB4.5,信越化學工業公司)、KF-6104、KF6106(HLB低,信越化學工業公司)、KF-6100(HLB中,信越化學工業公司)、KF-6105(HLB低,信越化學工業公司)等。The commercially available products are not limited, and examples include KF-6017 (HLB4.5, Shin-Etsu Chemical Co., Ltd.), KF-6019 (HLB4.5, Shin-Etsu Chemical Co., Ltd.), and KF-6015 (HLB4.5, Shin-Etsu Chemical Co., Ltd.) Chemical Industry Corporation), SH3772M (HLB6, Toray Dow Corning Corporation), SH3775M (HLB5, Toray Dow Corning Corporation), BY-11-030 (HLB6, Toray Dow Corning Corporation), KF-6004 (HLB9, Shin-Etsu Chemical Industry Corporation) , KF-6011 (HLB14.5, Shin-Etsu Chemical Co., Ltd.), FZ-2222, FZ-2233, KF-6028 (HLB4, Shin-Etsu Chemical Co., Ltd.), ABIL EM90 (manufactured by Goldschmidt), KF-6048 (HLB3.5 , Shin-Etsu Chemical Industry Co.), KF-6038 (HLB4.5, Shin-Etsu Chemical Industry Co.), KF-6104, KF6106 (Low HLB, Shin-Etsu Chemical Co., Ltd.), KF-6100 (HLB, Shin-Etsu Chemical Co., Ltd.), KF -6105 (low HLB, Shin-Etsu Chemical Industry Co.), etc.

本發明中,矽酮系界面活性劑可使用1種或組合使用2種以上。In the present invention, a silicone-based surfactant can be used singly or in combination of two or more.

[酯系界面活性劑] 作為本發明的油中水型乳化組成物中可含有之酯系界面活性劑,只要為於醫藥品、準藥品或化妝品領域中,例如用作皮膚外用劑之成分之化合物,則無特別限定。[Ester Surfactant] The ester-based surfactant that can be contained in the water-in-oil emulsion composition of the present invention is not particularly limited as long as it is a compound used as a component of an external preparation for skin in the fields of pharmaceuticals, quasi-drugs, or cosmetics.

酯系界面活性劑可較佳地例示:山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、甘油酯界面活性劑。詳細而言,並無限定,可列舉:山梨醇酐油酸酯、山梨醇酐倍半油酸酯、山梨醇酐三油酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐三異硬脂酸酯、山梨醇酐硬脂酸酯、山梨醇酐三硬脂酸酯、山梨醇酐倍半硬脂酸酯等山梨醇酐酯界面活性劑;聚甘油-2三異硬脂酸酯、聚甘油-2異硬脂酸酯、聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-6縮合蓖麻醇酸酯、聚甘油-6五異硬脂酸酯、聚甘油-6五油酸酯、聚甘油-6五羥基硬脂酸酯等聚甘油酯界面活性劑;油酸甘油酯、倍半油酸甘油酯、三油酸甘油酯、倍半異硬脂酸甘油酯、異硬脂酸甘油酯、三異硬脂酸甘油酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、三硬脂酸甘油酯等甘油酯界面活性劑等。Ester surfactants can be preferably exemplified: sorbitan ester surfactants, polyglycerol ester surfactants, and glycerol ester surfactants. The details are not limited, and examples include sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, sorbitan sesquiisostearate, and sorbitan iso Sorbitan ester surfactants such as stearate, sorbitan triisostearate, sorbitan stearate, sorbitan tristearate, and sorbitan sesquistearate; Polyglycerol-2 triisostearate, polyglycerol-2 isostearate, polyglycerol-10 condensed ricinoleate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentaoleic acid Ester, polyglycerol-10 pentastearate, polyglycerol-10 pentahydroxystearate, polyglycerol-6 condensed ricinoleate, polyglycerol-6 pentastearate, polyglycerol-6 penta Polyglyceryl ester surfactants such as oleate and polyglycerol-6 pentahydroxystearate; glyceryl oleate, glyceryl sesquioleate, glyceryl trioleate, glyceryl sesquiisostearate, iso Glyceride surfactants such as glyceryl stearate, glyceryl triisostearate, glyceryl stearate, glyceryl sesquistearate, glyceryl tristearate, etc.

本發明中,並無限定,較佳為山梨醇酐油酸酯、山梨醇酐倍半油酸酯、山梨醇酐三油酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐三異硬脂酸酯、山梨醇酐硬脂酸酯、山梨醇酐倍半硬脂酸酯、山梨醇酐三硬脂酸酯、聚甘油-2三異硬脂酸酯、聚甘油-2異硬脂酸酯、聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-6縮合蓖麻醇酸酯、聚甘油-6五異硬脂酸酯、聚甘油-6五油酸酯、聚甘油-6五羥基硬脂酸酯油酸甘油酯、倍半油酸甘油酯、三油酸甘油酯、倍半異硬脂酸甘油酯、異硬脂酸甘油酯、三異硬脂酸甘油酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、三硬脂酸甘油酯,這些之中,更佳為山梨醇酐油酸酯、山梨醇酐倍半油酸酯、山梨醇酐三油酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐硬脂酸酯、聚甘油-2三異硬脂酸酯、聚甘油-2異硬脂酸酯、聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-6縮合蓖麻醇酸酯、聚甘油-6五異硬脂酸酯、聚甘油-6五油酸酯、聚甘油-6五羥基硬脂酸酯、油酸甘油酯、倍半油酸甘油酯、三油酸甘油酯、倍半異硬脂酸甘油酯、異硬脂酸甘油酯、三異硬脂酸甘油酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、或三硬脂酸甘油酯。這些之中,就穩定性之觀點而言,進而更佳為聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、或聚甘油-10五羥基硬脂酸酯。In the present invention, it is not limited, but sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, sorbitan sesquiisostearate, sorbitan iso Stearate, sorbitan triisostearate, sorbitan stearate, sorbitan sesquistearate, sorbitan tristearate, polyglycerol-2 triisostearate Acid ester, polyglycerol-2 isostearate, polyglycerol-10 condensed ricinoleate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentaoleate, polyglycerol-10 five hardened Fatty acid ester, polyglycerol-10 pentahydroxystearate, polyglycerol-6 condensed ricinoleate, polyglycerol-6 pentaisostearate, polyglycerol-6 pentaoleate, polyglycerol-6 Pentahydroxy stearate glyceryl oleate, glyceryl sesquioleate, glyceryl trioleate, glyceryl sesquiisostearate, glyceryl isostearate, glyceryl triisostearate, stearin Among these, sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, and glyceryl tristearate are more preferred. Sorbitan sesquiisostearate, sorbitan isostearate, sorbitan stearate, polyglyceryl-2 triisostearate, polyglyceryl-2 isostearate, poly Glycerol-10 condensed ricinoleate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentaoleate, polyglycerol-10 pentastearate, polyglycerol-10 pentahydroxystearate , Polyglycerol-6 condensed ricinoleate, polyglycerol-6 pentaisostearate, polyglycerol-6 pentaoleate, polyglycerol-6 pentahydroxystearate, glyceryl oleate, sesquis Glyceryl oleate, glyceryl trioleate, glyceryl sesquistearate, glyceryl isostearate, glyceryl triisostearate, glyceryl stearate, glyceryl sesquistearate, or Glyceryl tristearate. Among these, from the viewpoint of stability, polyglycerol-10 condensed ricinoleate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentaoleate, and polyglycerol- 10 Pentastearate, or polyglycerol-10 pentahydroxystearate.

酯系界面活性劑可使用市售之製品或合成而使用。Ester-based surfactants can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉:NIKKOL SO-10V(日光化學公司製造)、NIKKOL SO-15V(日光化學公司製造)、NIKKOL SO-30V(日光化學公司製造)、NIKKOL SI-15RV(日光化學公司製造)、NIKKOL SI-10RV(日光化學公司製造)、NIKKOL SS-10MV(日光化學公司製造)、NIKKOL SS-15V(日光化學公司製造)、NIKKOL DGTIS(日光化學公司製造)、NIKKOL DGMIS(日光化學公司製造)、NIKKOL DECAGLYN-PR20(日光化學公司製造)、NIKKOL DECAGLYN-5ISV(日光化學公司製造)、NIKKOL DECAGLYN-5OV(日光化學公司製造)、NIKKOL DECAGLYN-5SV(日光化學公司製造)、NIKKOL DECAGLYN-5HS(日光化學公司製造)、NIKKOL MGS-BMV(日光化學公司製造)、NIKKOL MGS-AMV(日光化學公司製造)、NIKKOL MGIS(日光化學公司製造)、NIKKOL MGO(日光化學公司製造)等。The commercially available products are not limited, and include: NIKKOL SO-10V (manufactured by Nikko Chemical Co., Ltd.), NIKKOL SO-15V (manufactured by Nikko Chemical Co., Ltd.), NIKKOL SO-30V (manufactured by Nikko Chemical Co., Ltd.), and NIKKOL SI-15RV (Manufactured by Nikko Chemical Company), NIKKOL SI-10RV (manufactured by Nikko Chemical Company), NIKKOL SS-10MV (manufactured by Nikko Chemical Company), NIKKOL SS-15V (manufactured by Nikko Chemical Company), NIKKOL DGTIS (manufactured by Nikko Chemical Company), NIKKOL DGMIS (manufactured by Nikko Chemical Company), NIKKOL DECAGLYN-PR20 (manufactured by Nikko Chemical Company), NIKKOL DECAGLYN-5ISV (manufactured by Nikko Chemical Company), NIKKOL DECAGLYN-5OV (manufactured by Nikko Chemical Company), NIKKOL DECAGLYN-5SV (manufactured by Nikko Chemical Company) ), NIKKOL DECAGLYN-5HS (manufactured by Nikko Chemical Company), NIKKOL MGS-BMV (manufactured by Nikko Chemical Company), NIKKOL MGS-AMV (manufactured by Nikko Chemical Company), NIKKOL MGIS (manufactured by Nikko Chemical Company), NIKKOL MGO (manufactured by Nikko Chemical Company) Manufacturing) etc.

即便於高濃度含有(A)成分之菸鹼醯胺之情形時,此種(B)成分可有助於兼顧製劑的穩定性及使用感。Even when the nicotine amide of the component (A) is contained in a high concentration, the component (B) can contribute to the stability of the preparation and the feeling of use.

本發明的油中水型乳化組成物中,相對於油中水型乳化組成物的總量,(B)成分的總含量較佳為0.5質量%以上,更佳為1質量%以上,進而較佳為1.5質量%以上,進而更佳為2質量%以上,最佳為3質量%以上。相對於油中水型乳化組成物的總量,(B)成分的總含量較佳為20質量%以下,更佳為10質量%以下,進而較佳為8質量%以下,進而更佳為6質量%以下,最佳為4質量%以下。若(B)成分的總含量為上述範圍,則作為界面活性劑充分地發揮功能,能夠獲得良好的穩定性。另外,黏膩等使用感之惡化得到緩和。In the water-in-oil emulsion composition of the present invention, the total content of component (B) is preferably 0.5% by mass or more, more preferably 1% by mass or more, relative to the total amount of the water-in-oil emulsion composition. It is preferably 1.5% by mass or more, more preferably 2% by mass or more, and most preferably 3% by mass or more. The total content of component (B) is preferably 20% by mass or less, more preferably 10% by mass or less, still more preferably 8% by mass or less, and still more preferably 6 with respect to the total amount of the water-type emulsion composition in the oil. Mass% or less, preferably 4 mass% or less. If the total content of the component (B) is in the above range, it will fully function as a surfactant and good stability can be obtained. In addition, the deterioration of feeling in use such as stickiness is alleviated.

相對於油中水型乳化組成物的總量,(B)成分的總含量較佳為0.5質量%至8質量%,更佳為0.5質量%至5質量%,進而較佳為1質量%至5質量%,進而更佳為2質量%至5質量%,最佳為2質量%至4質量%。The total content of the component (B) is preferably 0.5% by mass to 8% by mass, more preferably 0.5% by mass to 5% by mass, and still more preferably 1% by mass to 5% by mass, more preferably 2% to 5% by mass, most preferably 2% to 4% by mass.

本發明的油中水型乳化組成物中,(B)成分之總含量相對於(A)成分之比率並無特別限定,相對於(A)成分的總含量1質量份,較佳為0.2質量份至1質量份,更佳為0.4質量份至1.0質量份,進而較佳為0.4質量份至0.8質量份。In the water-in-oil emulsion composition of the present invention, the ratio of the total content of the component (B) to the component (A) is not particularly limited, and it is preferably 0.2 mass relative to 1 part by mass of the total content of the component (A) Part to 1 part by mass, more preferably 0.4 part by mass to 1.0 part by mass, and still more preferably 0.4 part by mass to 0.8 part by mass.

本發明的油中水型乳化組成物中所使用之(B)成分較佳為選自矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、甘油酯界面活性劑中的1種以上之界面活性劑,更佳為選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、山梨醇酐硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、異硬脂酸甘油酯、倍半異硬脂酸甘油酯、油酸甘油酯、倍半油酸甘油酯、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-10五油酸酯所組成之群組中的1種以上之界面活性劑,進而較佳為選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-10五油酸酯所組成之群組中的1種以上之界面活性劑,進而較佳為選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、及月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的1種以上之界面活性劑。The component (B) used in the water-in-oil emulsion composition of the present invention is preferably selected from silicone surfactants, sorbitan ester surfactants, polyglyceryl ester surfactants, and glyceride surfactants One or more surfactants in the group, more preferably selected from PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG-10 dimethyl silicone, and lauryl PEG-9 polydimethylsiloxane Base silyloxy ethyl dimethyl silicone, lauryl polyglycerol-3 poly dimethyl silalkoxy ethyl dimethyl silicone, sorbitan stearate, sorbitan isostearate, Sorbitan sesquistearate, sorbitan oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate, sesquis Glyceryl isostearate, glyceryl oleate, glyceryl sesquioleate, polyglyceryl-10 pentastearate, polyglyceryl-10 pentaisostearate, polyglyceryl-10 pentahydroxystearate , One or more surfactants in the group consisting of polyglycerol-10 pentaoleate, and more preferably selected from PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG- 10 Dimethicone Lauryl PEG-9 Polydimethylsiloxyethyl Dimethicone, Lauryl Polyglycerol-3 Polydimethylsiloxyethyl Dimethicone, Polyglycerol- 10 Pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, polyglycerol-10 pentaoleate, more than one of the group consisting of interfacial activity The agent is more preferably selected from the group consisting of PEG-9 polydimethylsiloxane oxyethyl dimethyl silicone, PEG-10 dimethyl siloxane, lauryl PEG-9 polydimethyl siloxane oxyethyl two One or more surfactants in the group consisting of methyl silicone and lauryl polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone.

本發明的油中水型乳化組成物中所使用之(B)成分較佳為選自矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、甘油酯界面活性劑中的2種以上之界面活性劑,更佳為至少1種係選自PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、山梨醇酐硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、異硬脂酸甘油酯、倍半異硬脂酸甘油酯、油酸甘油酯、倍半油酸甘油酯、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-10五油酸酯,進而較佳為至少1種係選自PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-10五油酸酯,進而更佳為至少1種係選自PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮。The component (B) used in the water-in-oil emulsion composition of the present invention is preferably selected from silicone surfactants, sorbitan ester surfactants, polyglyceryl ester surfactants, and glyceride surfactants More than two kinds of surfactants, more preferably at least one kind is selected from PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG-10 dimethyl silicone, lauryl PEG- 9 Polydimethylsiloxy ethyl dimethyl silicone, lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, sorbitol anhydride stearate, sorbitol anhydride is hard Fatty acid ester, sorbitan sesquiisostearate, sorbitan oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate Ester, glyceryl sesquiisostearate, glyceryl oleate, glyceryl sesquioleate, polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxy Stearate, polyglycerol-10 pentaoleate, more preferably at least one type selected from PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG-10 dimethyl silicone , Lauryl PEG-9 polydimethylsiloxy ethyl dimethyl silicone, lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, polyglycerol-10 pentastearic acid Ester, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, polyglycerol-10 pentaoleate, and more preferably at least one species selected from PEG-9 polydimethyl Silanoxy ethyl dimethyl silicone, PEG-10 dimethyl silicone, lauryl PEG-9 polydimethyl silyloxy ethyl dimethyl silicone, lauryl polyglycerol-3 polydimethyl silicone Silanoxy ethyl dimethyl silicone.

作為本發明的油中水型乳化組成物中所使用之(B)成分之2種以上之組合的具體的一態樣,較佳為以至少選自矽酮系界面活性劑中的2種以上之界面活性劑之組合作為(B)成分的構成要素。並無限定,例如可為選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、及月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的2種之組合。As a specific aspect of the combination of two or more of the (B) components used in the water-in-oil emulsion composition of the present invention, it is preferable to use at least two or more selected from silicone surfactants The combination of surfactants is the constituent element of component (B). It is not limited, for example, it can be selected from PEG-9 polydimethylsiloxyethyl dimethylsilicone, PEG-10 dimethylsilicone, lauryl PEG-9 polydimethylsilyloxyethyl A combination of two types in the group consisting of dimethyl silicone and lauryl polyglycerol-3 polydimethylsiloxyethyl dimethyl silicone.

另外,作為本發明的油中水型乳化組成物中所使用之(B)成分之2種以上之組合的具體的另一態樣,較佳為含有(B)-1成分 選自矽酮系界面活性劑中的1種以上之界面活性劑、及(B)-2成分 選自由山梨醇酐硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、異硬脂酸甘油酯、倍半異硬脂酸甘油酯、油酸甘油酯、倍半油酸甘油酯、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、及聚甘油-10五油酸酯所組成之群組中的1種以上之界面活性劑,進而更佳為至少含有(B)-1成分 選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的1種以上之界面活性劑、及(B)-2成分 選自由山梨醇酐硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐油酸酯、山梨醇酐倍半油酸酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、異硬脂酸甘油酯、倍半異硬脂酸甘油酯、油酸甘油酯、倍半油酸甘油酯、聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-10五油酸酯所組成之群組中的界面活性劑。In addition, as another specific aspect of the combination of two or more components of (B) used in the water-in-oil emulsion composition of the present invention, it is preferable to contain (B)-1 component selected from silicone series One or more surfactants in the surfactant, and (B)-2 component are selected from sorbitan stearate, sorbitan isostearate, sorbitan sesquiisostearate, Sorbitan oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate, glyceryl sesquistearate, glyceryl oleate , Glyceryl sesquioleate, polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol-10 pentaoleate One or more surfactants in the composition group, more preferably at least containing (B)-1 component selected from PEG-9 polydimethylsilyloxyethyl dimethyl silicone, PEG-10 two The group consisting of methyl silicone, lauryl PEG-9 polydimethylsiloxy ethyl dimethyl silicone, and lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone One or more surfactants and (B)-2 component are selected from sorbitan stearate, sorbitan isostearate, sorbitan sesquiisostearate, and sorbitan Oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate, glyceryl sesquiisostearate, glyceryl oleate, sesquis The group consisting of glyceryl oleate, polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol-10 pentaoleate Surfactant in.

其中,進而更佳為含有作為(B)-1成分之選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的1種以上之界面活性劑、及作為(B)-2成分之選自聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、及聚甘油-10五油酸酯中的1種以上之界面活性劑。Among them, it is more preferable to contain PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG-10 dimethyl silicone, and lauryl PEG-9 as the component (B)-1. One or more surfactants in the group consisting of dimethylsiloxy ethyl dimethyl silicone, lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, and (B)-2 component selected from polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol-10 pentaoleic acid One or more surfactants in esters.

另外,根據目標製劑的使用感等,亦可將選自(B)-1、(B)-2成分中的界面活性劑3種以上適宜組合而使用。例如可例示:將作為B-1成分之選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、及月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的1種以上之界面活性劑、作為B-2成分之選自聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、及聚甘油-10五油酸酯中的2種以上之界面活性劑加以組合;將作為B-1成分之選自由PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、PEG-10二甲基矽酮、月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮所組成之群組中的2種以上之界面活性劑、作為B-2成分之選自聚甘油-10五硬脂酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五羥基硬脂酸酯、及聚甘油-10五油酸酯中的1種以上之界面活性劑加以組合等。In addition, depending on the usability of the target formulation, etc., three or more surfactants selected from the components (B)-1 and (B)-2 may be appropriately combined and used. For example, the B-1 component can be selected from PEG-9 dimethicone, PEG-10 dimethicone, and lauryl PEG-9 dimethicone. One or more surfactants in the group consisting of oxyethyl dimethyl silicone, and lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, as B-2 The ingredients are selected from more than 2 kinds of polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol-10 pentaoleate Combination of surfactants; the B-1 component is selected from PEG-9 polydimethylsiloxyethyl dimethyl silicone, PEG-10 dimethyl silicone, lauryl PEG-9 polydimethicone Two or more surfactants in the group consisting of methylsiloxyethyl dimethyl silicone and lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, as B -2 Ingredients selected from polyglycerol-10 pentastearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentahydroxystearate, and polyglycerol-10 pentaoleate Combination of more than one kind of surfactants.

[(C)油溶性增黏劑,選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上] 作為本發明的油中水型乳化組成物中所含之油溶性增黏劑,只要為於醫藥品、準藥品或化妝品領域中,例如用作皮膚外用劑之成分之化合物,則無特別限定。[(C) Oil-soluble thickener, one or more selected from the group consisting of clay thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid oil gelling agents ] The oil-soluble thickener contained in the water-in-oil emulsion composition of the present invention is not particularly limited as long as it is a compound used as a component of an external preparation for skin in the fields of pharmaceuticals, quasi-drugs, or cosmetics.

作為本發明的油中水型乳化組成物中所含之油溶性增黏劑,可列舉選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上。較佳為選自由黏土系增黏劑、糊精脂肪酸酯、及菊糖脂肪酸酯所組成之群組中的1種以上。The oil-soluble thickener contained in the water-in-oil emulsion composition of the present invention may be selected from clay based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid based oil gels. One or more of the group of gelling agents. Preferably, it is one or more selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, and inulin fatty acid esters.

[黏土系增黏劑] 本說明書中,「黏土系增黏劑」意指有機改性黏土礦物,可例示四級銨鹽型陽離子改性黏土礦物等。具體而言,可例示:二甲基二硬脂基銨鋰膨潤石、二甲基烷基銨鋰膨潤石、二甲基二硬脂基銨膨潤土、苄基二甲基硬脂基銨鋰膨潤石、經氯化二硬脂基二甲基銨處理之矽酸鋁鎂等。[Clay Series Tackifier] In this specification, "clay-based thickener" means organically modified clay minerals, and quaternary ammonium salt type cationic modified clay minerals can be exemplified. Specifically, exemplified are: dimethyl distearyl ammonium lithium bentonite, dimethyl alkyl ammonium lithium bentonite, dimethyl distearyl ammonium bentonite, and benzyl dimethyl stearyl ammonium lithium bentonite Stone, magnesium aluminum silicate treated with distearyl dimethyl ammonium chloride, etc.

本發明中,此種有機改性黏土礦物並無限定,較佳為二甲基二硬脂基銨鋰膨潤石、二甲基烷基銨鋰膨潤石、二甲基二硬脂基銨膨潤土、或苄基二甲基硬脂基銨鋰膨潤石,這些之中,更佳為二甲基二硬脂基銨鋰膨潤石、或苄基二甲基硬脂基銨鋰膨潤石,進而更佳為二甲基二硬脂基銨鋰膨潤石。In the present invention, the organically modified clay mineral is not limited, preferably dimethyl distearyl ammonium lithium bentonite, dimethyl alkyl ammonium lithium bentonite, dimethyl distearyl ammonium bentonite, Or benzyl dimethyl stearyl ammonium lithium bentonite, among these, more preferred is dimethyl distearyl ammonium lithium bentonite, or benzyl dimethyl stearyl ammonium lithium bentonite, and even more preferred It is dimethyl distearyl ammonium lithium bentonite.

黏土系增黏劑可使用市售之製品或合成而使用。The clay-based tackifier can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉:BENTONE 38V、BENTONE 38VCG(Elementis Japan股份有限公司製造)、BENTONE 27(Elementis Japan股份有限公司製造)等。The commercially available products are not limited, and include BENTONE 38V, BENTONE 38VCG (manufactured by Elementis Japan Co., Ltd.), BENTONE 27 (manufactured by Elementis Japan Co., Ltd.), and the like.

[糊精脂肪酸酯] 本說明書中,作為糊精脂肪酸酯,可例示:糊精棕櫚酸酯、糊精油酸酯、糊精硬脂酸酯、糊精肉豆蔻酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精(棕櫚酸/己基癸酸)酯等糊精衍生物。[Dextrin Fatty Acid Ester] In this specification, examples of dextrin fatty acid esters include dextrin palmitate, dextrin oleate, dextrin stearate, dextrin myristate, and dextrin (palmitic acid/ethylhexanoic acid) ester , Dextrin (palmitic acid/hexyl decanoic acid) ester and other dextrin derivatives.

本發明中,此種糊精脂肪酸酯並無限定,較佳為糊精棕櫚酸酯、糊精肉豆蔻酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精(棕櫚酸/己基癸酸)酯等糊精衍生物,更佳為糊精棕櫚酸酯、糊精肉豆蔻酸酯、糊精(棕櫚酸/己基癸酸)酯。In the present invention, such dextrin fatty acid esters are not limited, and dextrin palmitate, dextrin myristate, dextrin (palmitic acid/ethylhexanoic acid) ester, dextrin (palmitic acid/hexyl Dextrin derivatives such as capric acid) ester are more preferably dextrin palmitate, dextrin myristate, and dextrin (palmitic acid/hexyl decanoic acid) ester.

糊精脂肪酸酯可使用市售之製品或合成而使用。The dextrin fatty acid ester can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉:Rheopearl KL2(千葉製粉公司製造)、Rheopearl TL2(千葉製粉公司製造)、Rheopearl MKL2(千葉製粉公司製造)、Rheopearl TT2(千葉製粉公司製造)、Rheopearl WX(千葉製粉公司製造)、Rheopearl ISK2(千葉製粉公司製造)、Rheopearl ISL2(千葉製粉公司製造)等。The commercially available products are not limited, and examples include Rheopearl KL2 (manufactured by Chiba Flour Mills), Rheopearl TL2 (manufactured by Chiba Flour Mills), Rheopearl MKL2 (manufactured by Chiba Flour Mills), Rheopearl TT2 (manufactured by Chiba Flour Mills), Rheopearl WX (manufactured by Chiba Flour Mills), Rheopearl ISK2 (manufactured by Chiba Flour Mills), Rheopearl ISL2 (manufactured by Chiba Flour Mills), and the like.

[菊糖脂肪酸酯] 本發明中,作為菊糖脂肪酸酯並無限定,可列舉菊糖硬脂酸酯、菊糖棕櫚酸酯、菊糖肉豆蔻酸酯,尤佳為菊糖硬脂酸酯。[Inulin fatty acid ester] In the present invention, the fatty acid ester of inulin is not limited, and inulin stearate, inulin palmitate, and inulin myristate are exemplified, and inulin stearate is particularly preferred.

脂肪酸菊糖可使用市售之製品或合成而使用。The fatty acid inulin can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉Rheopearl ISK2(千葉製粉公司製造)、Rheopearl ISL2(千葉製粉公司製造)等。The commercially available products are not limited, and Rheopearl ISK2 (manufactured by Chiba Flour Mills), Rheopearl ISL2 (manufactured by Chiba Flour Mills), and the like are mentioned.

[胺基酸系油凝膠化劑] 本說明書中,作為胺基酸系油凝膠化劑並無限定,可例示二丁基月桂醯麩胺醯胺或二丁基乙基己醯基麩胺醯胺等。[Amino acid oil gelling agent] In this specification, the amino acid oil gelling agent is not limited, and dibutyl lauric glutamine, dibutyl ethyl hexyl glutamine, etc. can be exemplified.

胺基酸系油凝膠化劑可使用市售之製品或合成而使用。The amino acid-based oil gelling agent can be used commercially or synthesized.

作為市售之製品,並無限定,可列舉GB-21(味之素公司製造)、EB-21(味之素公司製造)。The commercially available products are not limited, and GB-21 (manufactured by Ajinomoto) and EB-21 (manufactured by Ajinomoto) can be mentioned.

於高濃度含有(A)成分之菸鹼醯胺之情形時,此種(C)成分亦可有助於兼顧製劑的穩定性及使用感。When the nicotine amide of the component (A) is contained in a high concentration, the component (C) can also help to balance the stability of the formulation and the feeling of use.

本發明的油溶性增黏劑為選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上之油溶性增黏劑,尤佳為含有選自由苄基二甲基硬脂基銨鋰膨潤石、二甲基二硬脂基銨鋰膨潤石、菊糖硬脂酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精棕櫚酸酯、糊精肉豆蔻酸酯、二丁基月桂醯麩胺醯胺、及二丁基乙基己醯基麩胺醯胺所組成之群組中的1種以上之油溶性增黏劑,更佳為含有選自由二甲基二硬脂基銨鋰膨潤石、菊糖硬脂酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精棕櫚酸酯、及糊精肉豆蔻酸酯所組成之群組中的1種以上之油溶性增黏劑,進而更佳為含有選自由二甲基二硬脂基銨鋰膨潤石、菊糖硬脂酸酯、糊精(棕櫚酸/乙基己酸)酯、及糊精棕櫚酸酯所組成之群組中的1種以上之油溶性增黏劑,尤佳為含有選自由二甲基二硬脂基銨鋰膨潤石及菊糖硬脂酸酯所組成之群組中的1種以上之油溶性增黏劑。The oil-soluble tackifier of the present invention is one or more selected from the group consisting of clay-based tackifiers, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents Oil-soluble thickener, particularly preferably containing benzyl dimethyl stearyl ammonium lithium bentonite, dimethyl distearyl ammonium lithium bentonite, inulin stearate, dextrin (palmitic acid/ Ethylhexanoic acid) ester, dextrin palmitate, dextrin myristate, dibutyl lauryl glutamine amide, and dibutyl ethyl hexanyl glutamine amide in the group consisting of 1 More than three kinds of oil-soluble thickeners, more preferably containing dimethyl distearyl ammonium lithium bentonite, inulin stearate, dextrin (palmitic acid/ethylhexanoic acid) ester, dextrin palm One or more oil-soluble tackifiers in the group consisting of acid esters and dextrin myristate, and more preferably containing dimethyl distearyl ammonium lithium swelling stone, inulin stearic acid One or more oil-soluble tackifiers in the group consisting of dextrin, dextrin (palmitic acid/ethylhexanoic acid) ester, and dextrin palmitate, particularly preferably containing dimethyl distearate One or more oil-soluble thickeners in the group consisting of Lithium Ammonium Bentonite and Inulin Stearate.

本發明的油中水型乳化組成物中,相對於油中水型乳化組成物的總量,(C)成分的總含量根據所使用之(C)成分的種類或組合而適宜調整即可,就抑制黏膩之方面而言,較佳為5質量%以下,更佳為3質量%以下,進而更佳為2質量%以下。就能夠賦予更良好的穩定性之方面而言,相對於油中水型乳化組成物的總量,(C)成分的總含量較佳為0.1質量%以上,更佳為0.2質量%以上,進而更佳為0.5質量%以上,尤其進而較佳為1質量%以上。In the water-in-oil emulsion composition of the present invention, the total content of the (C) component relative to the total amount of the water-in-oil emulsion composition may be appropriately adjusted according to the type or combination of the (C) component used. In terms of suppressing stickiness, it is preferably 5% by mass or less, more preferably 3% by mass or less, and still more preferably 2% by mass or less. In terms of imparting better stability, the total content of component (C) is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, relative to the total amount of the water-in-oil emulsion composition. More preferably, it is 0.5% by mass or more, and even more preferably 1% by mass or more.

就能夠賦予更良好的熱穩定性之觀點而言,相對於油中水型乳化組成物的總量,(C)成分的總含量較佳為0.5質量%至5質量%,更佳為0.5質量%至3質量%,進而較佳為0.5質量%至2質量%。From the viewpoint of being able to impart better thermal stability, the total content of component (C) is preferably 0.5% by mass to 5% by mass, more preferably 0.5% by mass relative to the total amount of the water-in-oil emulsion composition % To 3% by mass, and more preferably 0.5% to 2% by mass.

本發明的油中水型乳化組成物中,(C)成分之含量相對於(A)成分之比率並無特別限定,相對於(A)成分的總含量1質量份,較佳為0.05質量份至1.0質量份,更佳為0.1質量份至0.8質量份,進而較佳為0.1質量份至0.6質量份,進而更佳為0.1質量份至0.5質量份,最佳為0.1質量份至0.4質量份。In the water-in-oil emulsion composition of the present invention, the ratio of the content of the component (C) to the component (A) is not particularly limited, and it is preferably 0.05 part by mass relative to 1 part by mass of the total content of the component (A) To 1.0 part by mass, more preferably 0.1 part by mass to 0.8 part by mass, still more preferably 0.1 part by mass to 0.6 part by mass, still more preferably 0.1 part by mass to 0.5 part by mass, most preferably 0.1 part by mass to 0.4 part by mass .

[紫外線吸收劑] 本發明的油中水型乳化組成物中,就使用感之提升、穩定性等觀點而言,只要不妨礙本發明的效果,則除上述(A)成分、(B)成分、及(C)成分以外,亦可含有(D)紫外線吸收劑。作為本發明中所使用之紫外線吸收劑,只要為於醫藥品、準藥品或化妝品領域中,例如用作皮膚外用劑之成分之化合物,則無特別限定。紫外線吸收劑並無限定,較佳可為水楊酸系紫外線吸收劑、肉桂酸系紫外線吸收劑、苯甲醯甲烷系紫外線吸收劑、苯甲酸酯衍生物紫外線吸收劑、三嗪衍生物紫外線吸收劑、亞苄基丙二酸酯衍生物紫外線吸收劑、奧克立林(Octocrylene)系紫外線吸收劑、咪唑磺酸衍生物紫外線吸收劑、二苯甲酮衍生物紫外線吸收劑等。[Ultraviolet absorber] In the water-in-oil emulsion composition of the present invention, from the viewpoints of improvement in usability, stability, etc., as long as the effects of the present invention are not hindered, the aforementioned (A) component, (B) component, and (C) are excluded In addition to the components, (D) ultraviolet absorbers may be contained. The ultraviolet absorber used in the present invention is not particularly limited as long as it is a compound used as a component of an external preparation for skin in the field of pharmaceuticals, quasi-drugs, or cosmetics. The ultraviolet absorber is not limited, but preferably may be a salicylic acid-based ultraviolet absorber, a cinnamic acid-based ultraviolet absorber, a benzyl methane-based ultraviolet absorber, a benzoate derivative ultraviolet absorber, and a triazine derivative ultraviolet Absorbent, benzylidene malonate derivative ultraviolet absorber, Octocrylene-based ultraviolet absorber, imidazole sulfonic acid derivative ultraviolet absorber, benzophenone derivative ultraviolet absorber, etc.

詳細而言,作為紫外線吸收劑,可列舉:水楊酸-2-乙基己酯、水楊酸3,3,5-三甲基環己酯、或乙二醇水楊酸酯等水楊酸系紫外線吸收劑;二對甲氧基肉桂酸單-2-乙基己酸甘油酯;對二羥基丙基苯甲酸乙酯、或對甲氧基肉桂酸2-乙基己酯等肉桂酸系紫外線吸收劑;4-第三丁基-4'-甲氧基二苯甲醯甲烷等苯甲醯甲烷系紫外線吸收劑;2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯等苯甲酸酯衍生物紫外線吸收劑;二甲氧基亞苄基二側氧咪唑啶丙酸2-乙基己酯;2,2'-亞甲基雙[6-(2H-苯并三唑-2基)-4-(1,1,3,3-四甲基丁基)苯酚];2,4-雙-[{4-(2-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪、二乙基己基丁醯胺基三嗪酮、2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪等三嗪衍生物;二甲基矽酮二乙基亞苄基丙二酸酯等亞苄基丙二酸酯衍生物紫外線吸收劑;2-氰基-3,3-二苯基丙-2-烯酸2-乙基己酯等奧克立林紫外線吸收劑;2-苯基苯并咪唑-5-磺酸、苯基二苯并咪唑四磺酸二鈉等咪唑磺酸衍生物紫外線吸收劑;2-羥基-4-甲氧基二苯甲酮、2-羥基-4-甲氧基二苯甲酮-5-磺酸及其鹽、二羥基二甲氧基二苯甲酮、二羥基二苯甲酮、或四羥基二苯甲酮等二苯甲酮衍生物紫外線吸收劑。Specifically, as the ultraviolet absorber, salicylic acid such as 2-ethylhexyl salicylate, 3,3,5-trimethylcyclohexyl salicylate, or ethylene glycol salicylate can be cited Acid-based ultraviolet absorber; di-p-methoxycinnamic acid mono-2-ethylhexanoic acid glyceride; p-dihydroxypropyl benzoate ethyl, or p-methoxycinnamic acid 2-ethylhexyl and other cinnamic acids UV absorbers; 4-tertiary butyl-4'-methoxydibenzoyl methane and other benzyl methane UV absorbers; 2-[4-(diethylamino)-2-hydroxybenzene Formaldehyde] benzoate derivative ultraviolet absorber such as hexyl benzoate; 2-ethylhexyl dimethoxybenzylidene dioximidazolidinium propionate; 2,2'-methylene bis[6 -(2H-benzotriazol-2yl)-4-(1,1,3,3-tetramethylbutyl)phenol]; 2,4-bis-[{4-(2-ethylhexyloxy) Yl)-2-hydroxy)-phenyl)-6-(4-methoxyphenyl)-1,3,5-triazine, diethylhexylbutyramidotriazinone, 2,4,6 -Tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine and other triazine derivatives; dimethyl silicone diethylbenzylidene malonate and other sub Benzylmalonate derivatives ultraviolet absorbers; 2-cyano-3,3-diphenylprop-2-enoic acid 2-ethylhexyl and other octocrelin ultraviolet absorbers; 2-phenylbenzene Imidazole sulfonic acid derivative ultraviolet absorbers such as bisimidazole-5-sulfonic acid, disodium phenyldibenzimidazole tetrasulfonic acid; 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methyl UV absorbers for benzophenone derivatives such as oxybenzophenone-5-sulfonic acid and its salts, dihydroxydimethoxybenzophenone, dihydroxybenzophenone, or tetrahydroxybenzophenone .

本發明中,作為此種紫外線吸收劑並無限定,較佳為對甲氧基肉桂酸2-乙基己酯、4-第三丁基-4'-甲氧基二苯甲醯甲烷、2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯、二甲氧基亞苄基二側氧咪唑啶丙酸2-乙基己酯、2,2'-亞甲基雙[6-(2H-苯并三唑-2基)-4-(1,1,3,3-四甲基丁基)苯酚]、2,4-雙-[{4-(2-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪、2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪、二甲基矽酮二乙基亞苄基丙二酸酯、2-氰基-3,3-二苯基丙-2-烯酸2-乙基己酯、2-苯基苯并咪唑-5-磺酸,更佳為對甲氧基肉桂酸2-乙基己酯、4-第三丁基-4'-甲氧基二苯甲醯甲烷、2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯、2,4-雙-[{4-(2-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪、2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪、2-苯基苯并咪唑-5-磺酸,進而更佳為對甲氧基肉桂酸2-乙基己酯、2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯、2,4-雙-[{4-(2-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪、2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪。In the present invention, the ultraviolet absorber is not limited, but 2-ethylhexyl p-methoxycinnamic acid, 4-tert-butyl-4'-methoxydiphenylmethyl methane, 2 -[4-(Diethylamino)-2-hydroxybenzoyl]hexyl benzoate, 2-ethylhexyl dimethoxybenzylidene dioximidazolidinium propionate, 2,2'- Methylenebis[6-(2H-benzotriazol-2yl)-4-(1,1,3,3-tetramethylbutyl)phenol], 2,4-bis-[{4-( 2-Ethylhexyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[4-( 2-Ethylhexyloxycarbonyl)anilino)-1,3,5-triazine, dimethyl silicone diethylbenzylidene malonate, 2-cyano-3,3-diphenyl 2-ethylhexyl prop-2-enoate, 2-phenylbenzimidazole-5-sulfonic acid, more preferably 2-ethylhexyl p-methoxycinnamic acid, 4-tert-butyl-4 '-Methoxy dibenzyl methane, 2-[4-(diethylamino)-2-hydroxybenzyl]hexyl benzoate, 2,4-bis-[{4-(2-ethyl Hexyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[4-(2-ethyl Hexyloxycarbonyl)anilino]-1,3,5-triazine, 2-phenylbenzimidazole-5-sulfonic acid, more preferably 2-ethylhexyl p-methoxycinnamic acid, 2 -[4-(Diethylamino)-2-hydroxybenzoyl]hexyl benzoate, 2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}-benzene Group]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl)anilino]-1, 3,5-Triazine.

紫外線吸收劑可使用市售之製品或合成而使用。The ultraviolet absorber can be used commercially or synthesized.

作為市售之製品,並無限定,可將Uvinul MC80(BASF公司製造)、Parsol 1789(DSM Nutrition Japan公司製造)等適宜組合而使用。As a commercially available product, it is not limited, and Uvinul MC80 (manufactured by BASF Corporation), Parsol 1789 (manufactured by DSM Nutrition Japan), etc. can be suitably used in combination.

本發明的油中水型乳化組成物中,相對於油中水型乳化組成物的總量,紫外線吸收劑的總含量較佳為20質量%以下,更佳為15質量%以下,進而較佳為10質量%以下。In the water-in-oil emulsion composition of the present invention, the total content of the ultraviolet absorber is preferably 20% by mass or less, more preferably 15% by mass or less, and still more preferably, relative to the total amount of the water-in-oil emulsion composition It is 10% by mass or less.

相對於油中水型乳化組成物的總量,紫外線吸收劑的總含量較佳為1質量%以上,更佳為3質量%以上,進而較佳為6質量%以上,進而更佳為7質量%以上。With respect to the total amount of the water-in-oil emulsion composition, the total content of the ultraviolet absorber is preferably 1% by mass or more, more preferably 3% by mass or more, still more preferably 6% by mass or more, and still more preferably 7% by mass %the above.

相對於油中水型乳化組成物的總量,紫外線吸收劑的總含量較佳為1質量%至20質量%,更佳為3質量%至20質量%,進而更佳為5質量%至20質量%,尤其更佳為6質量%至20質量%,最佳為7質量%至15質量%。Relative to the total amount of the water-in-oil emulsion composition, the total content of the ultraviolet absorber is preferably 1% to 20% by mass, more preferably 3% to 20% by mass, and even more preferably 5% to 20% by mass. The mass% is more preferably 6 mass% to 20 mass %, most preferably 7 mass% to 15 mass %.

本發明的油中水型乳化組成物中,紫外線吸收劑之含量相對於(A)成分之比率並無特別限定,相對於(A)成分的總含量1質量份,較佳為0.6質量份至2質量份,更佳為1質量份至2質量份,進而較佳為1.4質量份至2質量份。In the water-in-oil emulsion composition of the present invention, the ratio of the content of the ultraviolet absorber to the component (A) is not particularly limited, and it is preferably from 0.6 part by mass to 1 part by mass relative to the total content of the component (A) 2 parts by mass, more preferably 1 part by mass to 2 parts by mass, and still more preferably 1.4 parts by mass to 2 parts by mass.

[紫外線防禦劑] 本發明的油中水型乳化組成物中,就使用感之提升、穩定性等觀點而言,只要不妨礙本發明的效果,則除上述(A)成分、(B)成分、及(C)成分以外,亦可進而含有(E)紫外線防禦劑。具體而言,可列舉:微粒子氧化鈦、微粒子氧化鋅、氧化鐵、氧化鈰等,但並不限定於這些。本發明中,作為(E)紫外線防禦劑並無限定,可較佳地列舉微粒子氧化鈦、或微粒子氧化鋅等。這些(E)紫外線防禦劑亦可經表面處理。[Ultraviolet protection agent] In the water-in-oil emulsion composition of the present invention, from the viewpoints of improvement in usability, stability, etc., as long as the effects of the present invention are not hindered, the aforementioned (A) component, (B) component, and (C) are excluded In addition to the components, (E) ultraviolet protection agent may be further contained. Specific examples include fine particle titanium oxide, fine particle zinc oxide, iron oxide, cerium oxide, etc., but are not limited to these. In the present invention, the (E) ultraviolet protection agent is not limited, and preferably, fine particle titanium oxide, fine particle zinc oxide, and the like are mentioned. These (E) ultraviolet protection agents can also be surface-treated.

作為前述表面處理中所使用之表面處理劑的種類,可列舉:兩親媒性成分、矽酮成分、矽烷化合物、脂肪酸成分、烷基鈦酸酯等,但並不特別限定於這些,這些表面處理劑可使用1種或2種以上。作為前述表面處理劑之兩親媒性成分,例如可列舉:金屬皂、全氟烷基乙基磷酸酯二乙醇胺鹽、丙烯酸氟烷基酯/聚伸烷基二醇丙烯酸酯聚合物、全氟聚醚磷酸酯、具有全氟聚醚鏈之陰離子性或陽離子性高分子(聚胺基甲酸酯-27、或聚胺基甲酸酯-26)、氫化卵磷脂、醯化胺基酸、α-生育酚磷酸酯鹽等,只要為具有親水部及疏水部,且對粉體顯示吸附特性之化合物即可,另外,可為單體型或聚合物型之任一種。作為前述表面處理劑之矽酮成分,例如可列舉:二甲基聚矽氧烷、甲基氫聚矽氧烷、α-單烷氧基聚二甲基矽氧烷、α-二烷氧基聚二甲基矽氧烷及α-三烷氧基聚二甲基矽氧烷、三乙氧基矽烷基乙基聚二甲基矽烷氧基乙基二甲基矽酮、三乙氧基矽烷基乙基聚二甲基矽烷氧基乙基己基二甲基矽酮、胺基二甲基矽酮等。作為前述表面處理劑之矽烷化合物,例如可列舉:三乙氧基辛醯基矽烷、胺基丙基三乙氧基矽烷、全氟辛基乙基三乙氧基矽烷、全氟辛基三乙氧基矽烷等。作為前述表面處理劑之脂肪酸成分,例如可列舉:硬脂酸、異硬脂酸、油酸、羥基硬脂酸、肉豆蔻酸等。作為前述表面處理劑之烷基鈦酸酯,例如可列舉:焦磷酸型烷基鈦酸酯、亞磷酸型烷基鈦酸酯、胺基酸型烷基鈦酸酯、或長鏈羧酸型之烷基鈦酸酯等。作為前述烷基鈦酸酯,具體而言,可列舉三異硬脂醯基鈦酸異丙酯。The types of surface treatment agents used in the aforementioned surface treatment include: amphiphilic components, silicone components, silane compounds, fatty acid components, alkyl titanates, etc., but they are not particularly limited to these. One kind or two or more kinds of treatment agents can be used. As the amphiphilic component of the aforementioned surface treatment agent, for example, metal soap, perfluoroalkyl ethyl phosphate diethanolamine salt, fluoroalkyl acrylate/polyalkylene glycol acrylate polymer, perfluoro Polyether phosphate, anionic or cationic polymer (polyurethane-27 or polyurethane-26) with perfluoropolyether chain, hydrogenated lecithin, acylated amino acid, The α-tocopherol phosphate salt and the like may be any compound that has a hydrophilic part and a hydrophobic part and shows adsorption properties to powder, and may be either a monomer type or a polymer type. Examples of the silicone component of the aforementioned surface treatment agent include: dimethyl polysiloxane, methyl hydrogen polysiloxane, α-monoalkoxy polydimethylsiloxane, α-dialkoxy Polydimethylsiloxane and α-trialkoxy polydimethylsiloxane, triethoxysilylethyl polydimethylsilyloxyethyl dimethylsiloxane, triethoxysilane Ethyl polydimethylsilyloxyethylhexyl dimethyl silicone, amino dimethyl silicone, etc. As the silane compound of the aforementioned surface treatment agent, for example, triethoxy octyl silane, aminopropyl triethoxy silane, perfluorooctyl ethyl triethoxy silane, perfluorooctyl triethoxy Silane etc. Examples of the fatty acid component of the surface treatment agent include stearic acid, isostearic acid, oleic acid, hydroxystearic acid, and myristic acid. Examples of the alkyl titanate of the aforementioned surface treatment agent include: pyrophosphate type alkyl titanate, phosphorous acid type alkyl titanate, amino acid type alkyl titanate, or long-chain carboxylic acid type The alkyl titanate and so on. As said alkyl titanate, the isopropyl triisostearyl titanate is mentioned specifically,.

相對於油中水型乳化組成物的總量,紫外線防禦劑的總含量較佳為3質量%至10質量%。藉由以該範圍進行調配,亦能夠兼顧使用感及穩定性,並且提高紫外線防禦效果。The total content of the ultraviolet protection agent is preferably 3% by mass to 10% by mass relative to the total amount of the water-in-oil emulsion composition. By blending in this range, it is possible to balance the feeling of use and stability, and to improve the UV protection effect.

另外,本發明中雖無限定,但(D)紫外線吸收劑及(E)紫外線防禦劑亦可與其他成分複合化、擔載、膠囊化,這些的組合並無特別限定。In addition, although there is no limitation in the present invention, the (D) ultraviolet absorber and (E) ultraviolet protection agent may be combined, supported, and encapsulated with other components, and the combination of these is not particularly limited.

[基劑或載體] 本發明的油中水型乳化組成物中,就使用感之提升、穩定性等觀點而言,只要不妨礙本發明的效果,則除上述(A)成分、(B)成分、及(C)成分以外,亦可含有基劑或載體。作為基劑或載體,例如可列舉:纖維素衍生物;聚乙烯吡咯啶酮;角叉菜膠;聚乙烯醇縮丁醛;聚乙二醇;二醇醚;乙醇、異丙醇之類的低級醇等,但並不限定於這些,可使用調配於化妝品類、醫藥品類等皮膚外用劑中的公知的成分。[Base or Carrier] In the water-in-oil emulsion composition of the present invention, from the viewpoints of improvement in usability, stability, etc., as long as the effects of the present invention are not hindered, the aforementioned (A) component, (B) component, and (C) are excluded In addition to the ingredients, a base or carrier may also be contained. As the base or carrier, for example, cellulose derivatives; polyvinylpyrrolidone; carrageenan; polyvinyl butyral; polyethylene glycol; glycol ethers; ethanol, isopropanol, etc. Lower alcohols, etc., but are not limited to these, and well-known ingredients formulated in external skin preparations such as cosmetics and pharmaceuticals can be used.

本發明的油中水型乳化組成物中,亦可使用作為基劑或載體發揮功能之油分。作為此種基劑或載體,例如可列舉:石蠟、凡士林之類的烴;肉豆蔻酸異丙酯等酯油;月見草油等源自動植物之油脂類;蜂蠟之類的蠟類;甲基聚矽氧烷等矽氧烷、辛醯基甲聚矽氧烷等烷基改性矽酮、交聯型甲基聚矽氧烷、交聯型烷基改性矽酮、丙烯酸矽酮、及矽酮樹脂等矽酮類等,但並不限定於這些,可使用調配於化妝品類、醫藥品類等皮膚外用劑中的公知的成分。In the water-in-oil emulsion composition of the present invention, an oil that functions as a base or carrier may also be used. Examples of such a base or carrier include: hydrocarbons such as paraffin wax and petrolatum; ester oils such as isopropyl myristate; oils and fats derived from plants such as evening primrose oil; waxes such as beeswax; Silicone such as silicone, alkyl-modified silicone such as octylmethicone, cross-linked methyl polysiloxane, cross-linked alkyl-modified silicone, acrylic silicone, and silicone resin However, it is not limited to silicones, etc., and well-known ingredients formulated for external skin preparations such as cosmetics and pharmaceuticals can be used.

基劑或載體可單獨使用1種或組合使用2種以上。A base or carrier can be used individually by 1 type or in combination of 2 or more types.

[添加劑] 本發明的油中水型乳化組成物中,在無損本發明的效果之範圍內,可添加醫藥品、準藥品、或化妝品中所添加之公知的添加劑,例如抗氧化劑、增黏劑、保存劑、pH調整劑、穩定劑、刺激減輕劑、防腐劑、著色劑、香料、粉體及/或珍珠光澤賦予劑等。[additive] In the water-in-oil emulsion composition of the present invention, well-known additives added to pharmaceuticals, quasi-drugs, or cosmetics, such as antioxidants, thickeners, and preservatives, can be added to the extent that the effects of the present invention are not impaired. , PH adjuster, stabilizer, irritation reducing agent, preservative, coloring agent, fragrance, powder and/or pearl luster imparting agent, etc.

作為抗氧化劑,例如可列舉:二丁基羥基甲苯、丁基羥基甲氧苯、己二烯酸、亞硫酸鈉、抗壞血酸、抗壞血酸衍生物、生育酚、生育酚衍生物、異抗壞血酸、及L-半胱胺酸鹽酸鹽等。Examples of antioxidants include dibutylhydroxytoluene, butylhydroxymethoxybenzene, hexadienoic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives, tocopherol, tocopherol derivatives, erythorbic acid, and L-cysteine Acid salt etc.

作為增黏劑,例如可列舉:瓜爾膠、刺槐豆膠、角叉菜膠、三仙膠、聚乙烯醇、聚乙烯吡咯啶酮、羧基乙烯基聚合物、丙烯酸甲基丙烯酸烷基酯共聚物、(丙烯酸羥基乙酯/丙烯醯基二甲基牛磺酸鈉)共聚物、(丙烯酸鈉/丙烯醯基二甲基牛磺酸鈉)共聚物、聚丙烯酸醯胺、聚乙二醇、海藻酸、Macrogol(聚乙二醇)、軟骨素硫酸鈉、以及羥基乙基纖維素之類的纖維素系增黏劑等。As the thickener, for example, guar gum, locust bean gum, carrageenan, trixian gum, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, acrylic acid alkyl methacrylate copolymer Compound, (Hydroxyethyl Acrylate/Sodium Acrylate Dimethyl Taurate) Copolymer, (Sodium Acrylate/Sodium Acrylate Dimethyl Taurate) Copolymer, Polyacrylamide, Polyethylene Glycol, Alginic acid, Macrogol (polyethylene glycol), sodium chondroitin sulfate, and cellulose-based thickeners such as hydroxyethyl cellulose.

作為防腐劑、保存劑,例如可列舉:苯甲酸、苯甲酸鈉、脫氫乙酸、脫氫乙酸鈉、對羥基苯甲酸異丁酯、對羥基苯甲酸異丙酯、對羥基苯甲酸丁酯、對羥基苯甲酸乙酯、對羥基苯甲酸丙酯、對羥基苯甲酸苄酯、對羥基苯甲酸甲酯、苯氧基乙醇、苄醇、氯丁醇、己二烯酸及其鹽、葡萄糖酸洛赫西定、辛基羥肟酸、丁基胺基甲酸碘化丙炔酯及1,2-戊二醇、2,4-己二醇、1,2-己二醇、1,2-辛二醇等。Examples of preservatives and preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl p-hydroxybenzoate, isopropyl p-hydroxybenzoate, butyl p-hydroxybenzoate, and Ethyl hydroxybenzoate, propyl p-hydroxybenzoate, benzyl p-hydroxybenzoate, methyl p-hydroxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, hexadienoic acid and its salts, loxidine gluconate , Octyl hydroxamic acid, butylcarbamate propynyl iodide and 1,2-pentanediol, 2,4-hexanediol, 1,2-hexanediol, 1,2-octanediol, etc. .

作為pH調整劑,例如可列舉無機酸、有機酸、以及有機鹼等。As a pH adjuster, an inorganic acid, an organic acid, an organic base, etc. are mentioned, for example.

作為穩定劑,例如可列舉聚丙烯酸鈉、二丁基羥基甲苯、及丁基羥基甲氧苯等。 作為刺激降低劑,例如可列舉甘草萃取物、及海藻酸鈉等。Examples of stabilizers include sodium polyacrylate, dibutylhydroxytoluene, and butylhydroxymethoxybenzene. As the irritation reducing agent, for example, a licorice extract, sodium alginate, and the like can be cited.

作為著色劑,可列舉:顏料級氧化鈦、氧化鋅、氧化鐵、有機顏料、滑石、絹雲母、雲母、合成雲母、氧化鉻、群青等。Examples of colorants include pigment-grade titanium oxide, zinc oxide, iron oxide, organic pigments, talc, sericite, mica, synthetic mica, chromium oxide, ultramarine blue, and the like.

另外,亦可為了改良觸感或賦予化妝效果等而調配粉體,具體而言,可列舉:氮化硼、二氧化矽、氧化鋁、氫氧化鋁、金屬皂、矽酮粉體、胺基酸、聚甲基甲基丙烯酸甲酯等。In addition, powders can also be formulated for the purpose of improving the touch or imparting cosmetic effects. Specifically, examples include boron nitride, silica, alumina, aluminum hydroxide, metal soaps, silicone powders, and amino groups. Acid, polymethyl methacrylate, etc.

添加劑可單獨使用1種或組合使用2種以上。另外,並不限定於這些,可適宜使用調配於化妝品類、醫藥品類等皮膚外用劑中的公知的成分。Additives can be used individually by 1 type or in combination of 2 or more types. In addition, it is not limited to these, and well-known ingredients formulated in external skin preparations such as cosmetics and pharmaceuticals can be suitably used.

[其他有效成分] 本發明的油中水型乳化組成物可在無損本發明的效果之範圍內含有其他有效成分。作為有效成分的具體例,例如可列舉:清涼成分、保濕成分、抗發炎成分、抗菌或殺菌成分、維生素類、胺基酸或其衍生物、細胞活化成分、抗老化成分、血液循環促進成分、角質軟化成分、美白成分、及收斂成分等。[Other active ingredients] The water-in-oil emulsion composition of the present invention may contain other active ingredients within a range that does not impair the effects of the present invention. Specific examples of active ingredients include, for example, refreshing ingredients, moisturizing ingredients, anti-inflammatory ingredients, antibacterial or bactericidal ingredients, vitamins, amino acids or their derivatives, cell activation ingredients, anti-aging ingredients, blood circulation promoting ingredients, Cutin softening ingredients, whitening ingredients, and astringent ingredients.

作為清涼成分,例如可列舉:樟腦、薄荷腦、龍腦、丁香酚、桉樹腦、瑞香草酚、甜沒藥醇、α-蒎烯、或檸檬烯等單萜烯等倍半萜烯、二萜烯、桉樹油、日本薄荷油、丁香油、桂皮油、胡椒薄荷油、薄荷油、茶樹油、黃金菊油、迷迭香油、檸檬油、柳橙油、百里香油、鼠尾草油、丁香油等精油等。Examples of refreshing ingredients include sesquiterpenes and diterpenes such as camphor, menthol, borneol, eugenol, cineole, revanol, bisabolol, α-pinene, or monoterpenes such as limonene. Ene, eucalyptus oil, Japanese peppermint oil, clove oil, cinnamon oil, peppermint oil, peppermint oil, tea tree oil, rudbeckia oil, rosemary oil, lemon oil, orange oil, thyme oil, sage oil, clove oil And other essential oils.

作為保濕成分,例如可列舉:玻尿酸鈉、肝素類似物質、軟骨素硫酸鈉、膠原蛋白、彈力蛋白、角蛋白、甲殼素、及殼聚糖之類的高分子化合物或其水解物;甘胺酸、天冬胺酸、精胺酸之類的胺基酸;乳酸鈉、脲、及吡咯啶酮羧酸鈉之類的天然保濕因子;腦醯胺、及磷脂質之類的脂質;MPC(2-Methacryloyloxy ethyl phosphorylcholine;2-甲基丙烯醯氧基乙基磷醯膽鹼)聚合物等具有磷脂質極性基之高分子;聚氧丙烯甲基葡萄糖苷;PPG-10甲基葡萄糖、PEG/PPG/聚丁二醇8/5/3甘油;三甲基甘胺酸(甜菜鹼);羥基乙基脲;丙烯酸-丙烯酸醯胺-氯化二甲基二烯丙基銨共聚物;以及薏苡種子萃取物、艾草葉萃取物、洋甘菊萃取物、金縷梅萃取物、白樺樹液、海蓬子萃取物、紫丁香萃取物、茶萃取物、薰衣草油、及紫蘇萃取物之類的植物萃取萃取物;胎盤萃取物等動物性萃取物等。Examples of moisturizing ingredients include: sodium hyaluronate, heparin-like substances, sodium chondroitin sulfate, collagen, elastin, keratin, chitin, and chitosan and other polymer compounds or their hydrolysates; glycine , Aspartic acid, arginine and other amino acids; natural moisturizing factors such as sodium lactate, urea, and sodium pyrrolidone carboxylate; cerebroamide, and lipids such as phospholipids; MPC(2- Methacryloyloxy ethyl phosphorylcholine; 2-methacryloyloxy ethyl phosphorylcholine) polymer and other polymers with phospholipid polar groups; polyoxypropylene methyl glucoside; PPG-10 methyl glucose, PEG/PPG/ Polybutylene glycol 8/5/3 glycerin; trimethylglycine (betaine); hydroxyethyl urea; acrylic acid-acrylamide-dimethyl diallylammonium chloride copolymer; and coix seed extraction Plant extracts such as wormwood leaf extract, chamomile extract, witch hazel extract, birch sap, saphiridia extract, lilac extract, tea extract, lavender oil, and perilla extract; Animal extracts such as placental extracts, etc.

作為抗發炎成分,例如可列舉:源自植物(例如康福利草)之成分、尿囊素、甘草酸或其衍生物、甘草次酸或其衍生物、氧化鋅、吡哆醇鹽酸酯、生育酚乙酸酯、水楊酸或其衍生物、薁、類固醇類及ε-胺基己酸等。Examples of anti-inflammatory ingredients include: plant-derived ingredients (for example, Comfollicle), allantoin, glycyrrhizic acid or its derivatives, glycyrrhetinic acid or its derivatives, zinc oxide, pyridoxine hydrochloride, Tocopherol acetate, salicylic acid or its derivatives, azulene, steroids and ε-aminocaproic acid, etc.

作為抗菌或殺菌成分,例如可列舉:洛赫西定、水楊酸、氯化苄烷銨、利凡諾、硫、間苯二酚、乙醇、苄索氯銨、阿達巴林、過氧化苯甲醯、克林達黴素、甲酚、葡萄糖酸及其衍生物、聚維酮碘、碘化鉀、碘、異丙基甲基苯酚、三氯卡班、三氯沙、感光素101號、感光素201號、對羥基苯甲酸酯、苯氧基乙醇、1,2-戊二醇、鹽酸烷基二胺基甘胺酸、葡萄糖酸洛赫西定、及對苯酚磺酸鋅、吡羅克酮乙醇胺、及咪康唑等。Examples of antibacterial or bactericidal ingredients include loxidine, salicylic acid, benzalkonium chloride, rivanol, sulfur, resorcinol, ethanol, benzethonium chloride, adabalin, and benzyl peroxide Li, clindamycin, cresol, gluconic acid and its derivatives, povidone iodine, potassium iodide, iodine, isopropyl methylphenol, triclocarban, triclosan, sensitizer 101, sensitizer No. 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride, lohexidine gluconate, zinc p-phenolsulfonate, piroc Ketoethanolamine, miconazole, etc.

作為維生素類,例如可列舉:視黃醇衍生物(視黃醇、視黃醇乙酸酯、視黃醇棕櫚酸酯等)視黃酸、生育酚視黃酸酯等維生素A類;生育酚、生育酚乙酸酯等維生素E類;核黃素等維生素B2類;菸鹼醯胺以外的菸鹼酸類;抗壞血酸、抗壞血酸鹽、抗壞血酸衍生物等維生素C類;維生素D類;維生素K類、γ-榖維素、維生素B1類;吡哆醇鹽酸酯等維生素B6類;維生素B12類;葉酸類;泛醇等泛酸類;生物素類;以及肉鹼、吡咯喹啉醌等類維生素作用因子等。Examples of vitamins include: retinol derivatives (retinol, retinol acetate, retinol palmitate, etc.), vitamin A such as retinoic acid and tocopherol retinoate; tocopherol , Tocopherol acetate and other vitamin E; riboflavin and other vitamin B2; nicotinic acid other than nicotinic acid; vitamin C such as ascorbic acid, ascorbate, and ascorbic acid derivatives; vitamin D; vitamin K, γ-Colin, vitamin B1; vitamin B6 such as pyridoxine hydrochloride; vitamin B12; folic acid; pantothenic acid such as panthenol; biotin; and vitamins such as carnitine and pyrroloquinoline quinone Factor etc.

作為胺基酸或其衍生物,例如可列舉:甜菜鹼(三甲基甘胺酸)、脯胺酸、羥基脯胺酸、精胺酸、離胺酸、絲胺酸、甘胺酸、丙胺酸、苯基丙胺酸、β-丙胺酸、蘇胺酸、麩胺酸、麩醯胺、天冬醯胺、天冬胺酸、半胱胺酸、胱胺酸、甲硫胺酸、白胺酸、異白胺酸、纈胺酸、組胺酸、牛磺酸、γ-胺基丁酸、γ-胺基-β-羥基丁酸、肉鹼、肌肽、及肌酸等。Examples of amino acids or derivatives thereof include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, and propylamine Acid, phenylalanine, β-alanine, threonine, glutamine, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine, leucamine Acid, isoleucine, valine, histidine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, and creatine.

作為細胞活化成分,例如可列舉:胺基酸類;維生素類;乙醇酸、及乳酸等α-羥基酸類;單寧;類黃酮;皂苷;尿囊素;以及感光素301號等。 作為抗老化成分,例如可列舉:水解大豆蛋白、視黃醇類(視黃醇及其衍生物、視黃酸、視黃醛等)、平葡酸、激動素、熊果酸、薑黃萃取物、神經鞘胺醇衍生物、矽、矽酸、N-甲基-L-絲胺酸、及甲瓦龍酸內酯等。Examples of cell activation components include amino acids; vitamins; α-hydroxy acids such as glycolic acid and lactic acid; tannins; flavonoids; saponin; allantoin; and photoreceptor 301. Examples of anti-aging ingredients include hydrolyzed soy protein, retinols (retinol and its derivatives, retinoic acid, retinal, etc.), pyrogluconic acid, kinetin, ursolic acid, and turmeric extract , Sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, and mevalonolactone, etc.

作為血液循環促進作用成分,例如可列舉:源自植物(例如,朝鮮人參、明日葉、山金車、銀杏、茴香、延命草、西洋菜、洋甘菊、羅馬洋甘菊、胡蘿蔔、龍膽、牛蒡、稻米、山楂、香菇、歐洲山楂、歐洲杜松、川芎、當藥、百里香、丁香、陳皮、當歸、桃仁、雲杉、人參、大蒜、假葉樹(Butcher's Broom)、葡萄、牡丹、七葉樹、蜜蜂花、柚子、薏苡仁、迷迭香、玫瑰果、桃、杏、核桃、及玉米)之成分;以及葡糖基橙皮苷等。As the blood circulation promotion component, for example, there can be mentioned: plant-derived (for example, Korean ginseng, Ashitaba, arnica, ginkgo, fennel, longbirth, watercress, chamomile, Roman chamomile, carrot, gentian, burdock, rice , Hawthorn, Shiitake, European Hawthorn, European Juniper, Chuanxiong, Dang Medicine, Thyme, Clove, Tangerine Peel, Angelica, Peach Kernel, Spruce, Ginseng, Garlic, Butcher's Broom, Grape, Peony, Horse Chestnut, Melissa, grapefruit, coix seed, rosemary, rose hips, peach, apricot, walnut, and corn) ingredients; and glucosyl hesperidin, etc.

作為角質軟化成分,例如可列舉:羊毛脂、脲、α羥基酸及硫等。 作為美白成分,例如可列舉:抗壞血酸及其衍生物、熊果苷、及生育酚、傳明酸、對苯二酚、曲酸、水楊酸衍生物、胎盤萃取物、亞麻油酸及具有美白作用之植物成分(例如,虎耳草、蘆薈等之萃取物)等。 作為收斂成分,例如可列舉:對苯酚磺酸鋅、氧化鋅、薄荷腦、及乙醇等。Examples of keratin softening components include lanolin, urea, α-hydroxy acid, sulfur, and the like. Examples of whitening ingredients include ascorbic acid and its derivatives, arbutin, and tocopherol, tranexamic acid, hydroquinone, kojic acid, salicylic acid derivatives, placental extracts, linoleic acid, and whitening agents. Effective plant ingredients (for example, extracts of saxifrage and aloe) etc. As an astringent component, zinc p-phenolsulfonate, zinc oxide, menthol, ethanol, etc. are mentioned, for example.

其他有效成分可單獨使用1種或組合使用2種以上。另外,並不限定於這些,可適宜使用調配於化妝品類、醫藥品類等皮膚外用劑中的公知的成分。Other active ingredients can be used alone or in combination of two or more. In addition, it is not limited to these, and well-known ingredients formulated in external skin preparations such as cosmetics and pharmaceuticals can be suitably used.

[製造方法] 本發明的油中水型乳化組成物的製造方法並無特別限定,乳化時的攪拌方法或乳化溫度、油相與水相之投入順序、投入速度等適宜設定即可。[Manufacturing method] The manufacturing method of the water-in-oil emulsion composition of the present invention is not particularly limited, and the stirring method during emulsification, the emulsification temperature, the order of the oil phase and the water phase, the injection speed, etc. may be appropriately set.

具體而言,可列舉以下之方法等:分別準備根據需要加熱溶解後混合之油相與水相,於室溫下於油相中緩慢地添加水,藉由均質機等機械攪拌力進行乳化。但並不特別限定於這些方法。Specifically, the following methods can be cited: separately preparing an oil phase and a water phase mixed after heating and dissolving as needed, slowly adding water to the oil phase at room temperature, and emulsifying by mechanical stirring force such as a homogenizer. However, it is not particularly limited to these methods.

另外,亦可於製造步驟中加入使油溶性增黏劑膨潤之步驟,例如可列舉:加熱分散、機械碎解、油相中的預攪拌等,但並不特別限定於這些。In addition, a step of swelling the oil-soluble tackifier may be added to the production step. Examples include heating dispersion, mechanical disintegration, pre-stirring in the oil phase, etc., but are not particularly limited to these.

[製劑形態] 本發明的油中水型乳化組成物可與醫藥品、準藥品、或化妝品中通常所使用之基劑或載體、及根據需要所使用之添加劑一起混合,製成醫藥品、準藥品、或化妝品用之油中水型乳化組成物。[Formulation of preparation] The water-in-oil emulsion composition of the present invention can be mixed with bases or carriers commonly used in pharmaceuticals, quasi-drugs, or cosmetics, and additives used as needed, to produce pharmaceuticals, quasi-drugs, or cosmetics It is an oil-in-water emulsion composition.

醫藥品用之油中水型乳化組成物之形態並無特別限定,例如可列舉:液劑、懸浮劑、乳劑、乳霜劑、軟膏劑、凝膠劑、擦劑(liniment agent)、洗劑、貼附劑及氣溶膠劑等。這些製劑可依據日本藥典第17次修訂版之製劑總則中所記載之方法等進行製造。其中,較佳為液劑、懸浮劑、乳劑、乳霜劑、軟膏劑、凝膠劑、洗劑、貼附劑,更佳為乳霜劑、乳劑、軟膏劑、洗劑及凝膠劑。The form of the water-in-oil emulsion composition for pharmaceuticals is not particularly limited, and examples include liquids, suspensions, emulsions, creams, ointments, gels, liniment agents, and lotions. , Adhesives and aerosols, etc. These preparations can be manufactured in accordance with the methods described in the General Rules of Preparations of the 17th Revision of the Japanese Pharmacopoeia. Among them, preferred are liquids, suspensions, emulsions, creams, ointments, gels, lotions, and patches, and more preferred are creams, emulsions, ointments, lotions and gels.

於製成準藥品或化妝品用之油中水型乳化組成物之情形時,亦可設為與上述醫藥品相同的形態。另外,除此以外,可列舉:棒劑、及使藥液含浸於不織布而成之片劑等。其中,較佳為液劑、懸浮劑、乳劑、乳霜劑、軟膏劑、凝膠劑、洗劑、棒劑及片劑,更佳為乳霜劑、乳劑、軟膏劑、凝膠劑或洗劑。In the case of preparing a water-in-oil emulsion composition for quasi-drugs or cosmetics, it can also be in the same form as the above-mentioned pharmaceuticals. In addition, other examples include sticks, and tablets obtained by impregnating a drug solution in a nonwoven fabric. Among them, preferred are liquids, suspensions, emulsions, creams, ointments, gels, lotions, sticks and tablets, and more preferred are creams, emulsions, ointments, gels or lotions. Agent.

本發明的油中水型乳化組成物包含油性基劑及水性基劑,典型而言,可採取乳霜劑或乳液等形態。The water-in-oil emulsion composition of the present invention includes an oily base and an aqueous base, and typically, it can take the form of a cream or an emulsion.

作為製成準藥品或化妝品用之油中水型乳化組成物之情形時的用途,具體而言,例如可列舉:化妝水、乳液、凝膠、乳霜、美容液、防曬用化妝料、敷劑、面膜、護手霜、多合一凝膠及體霜之類的基礎化妝料;以及BB(Blemish Balm;無瑕修護)霜、粉餅、化妝基底等面部化妝用化妝料、口紅、唇膏、唇彩、唇線等嘴唇化妝料;造型劑之類的毛髪用化妝料等。這些之中,尤佳為皮膚用之油中水型乳化組成物。亦即,本發明的油中水型乳化組成物可製成醫藥品、準藥品、或化妝品用之皮膚油中水型乳化組成物。皮膚油中水型乳化組成物的製劑形態與本發明的油中水型乳化組成物之情形相同。另外,可使用之基劑或載體、添加劑、及有效成分、以及這些中較佳的成分係與本發明的油中水型乳化組成物之情形相同。As the application in the case of preparing a water-in-oil emulsion composition for quasi-drugs or cosmetics, specific examples include: lotions, emulsions, gels, creams, beauty lotions, sunscreen cosmetics, dressings Basic cosmetics such as balm, facial mask, hand cream, all-in-one gel and body cream; and BB (Blemish Balm; flawless repair) cream, pressed powder, makeup base and other facial cosmetics, lipstick, lipstick, Lip cosmetics such as lip gloss and lip liner; hair cosmetics such as styling agents, etc. Among these, the oil-in-water emulsion composition for skin is particularly preferred. That is, the water-in-oil emulsion composition of the present invention can be made into a skin oil-in-water emulsion composition for pharmaceuticals, quasi-drugs, or cosmetics. The formulation form of the water-in-oil emulsion composition for skin is the same as that of the water-in-oil emulsion composition of the present invention. In addition, the usable bases or carriers, additives, and effective ingredients, as well as the preferred components among these, are the same as those of the water-in-oil emulsion composition of the present invention.

本發明中的油相與水相的質量比適宜設定即可,並無限定,就獲得更良好的穩定性及使用感之方面而言,較佳為油相:水相=3:7至7:3,尤佳為油相:水相=4:6至6:4之比例。The mass ratio of the oil phase to the water phase in the present invention may be appropriately set and is not limited. In terms of obtaining better stability and usability, the oil phase: water phase=3:7 to 7 : 3, especially oil phase: water phase = 4:6 to 6:4 ratio.

[容器] 本發明的油中水型乳化組成物可根據使用目的及用途而收容於適宜選擇過之形狀、材質之容器而使用。作為具體的容器,例如可例示:噴霧型、瓶型、管型、罐型、滴管型、分注器型、棒型、小袋、及包裝袋(cheer pack)等。就容易自容器取出之觀點而言,本發明的油中水型乳化組成物由於能夠以較佳的狀態使用,故而能夠提高含有高濃度的菸鹼醯胺之製劑設計的自由度。亦即,即便為含有高濃度的菸鹼醯胺之製劑,亦可容易地用於罐或棒、以及噴霧、瓶、管或分注器等多種容器,能夠確保商品設計的自由度,尤其可極有用地應用於管型或分注器型、瓶型之容器。[container] The water-in-oil emulsion composition of the present invention can be stored in a container of appropriately selected shape and material according to the purpose of use and use. Examples of specific containers include spray type, bottle type, tube type, can type, dropper type, dispenser type, stick type, pouch, and cheer pack. From the standpoint of being easy to take out from the container, the water-in-oil emulsion composition of the present invention can be used in a better state, and therefore, the degree of freedom in the design of formulations containing high concentrations of nicotine amide can be increased. In other words, even if it is a formulation containing a high concentration of nicotine amide, it can be easily used in a variety of containers such as cans or rods, as well as sprays, bottles, tubes, or dispensers, ensuring the freedom of product design, especially It is very useful for tube type, dispenser type, bottle type container.

另外,作為容器的材質,可例示:聚對苯二甲酸乙二酯、聚丙烯、聚乙烯(HDPE(High Density Polyethylene;高密度聚乙烯)、LDPE(Low Density Polyethylene;低密度聚乙烯)、LLDPE(Linear Low Density Polyethylene;線性低密度聚乙烯)等)、ABS(Acrylonitrile Butadiene Styrene;丙烯腈-丁二烯-苯乙烯)樹脂、乙烯乙烯醇樹脂、聚苯乙烯、玻璃、及金屬(鋁等)等。另外,這些材料可考慮強度、柔軟性、耐候性、或成分的穩定性等,進行各種塗佈處理,或者將這些材料例如混合等而組合,或者進行積層而用作容器材料。其中,較佳為使用聚丙烯、聚乙烯(HDPE、LDPE、LLDPE等)、乙烯乙烯醇樹脂、金屬(鋁等)。In addition, examples of the material of the container include polyethylene terephthalate, polypropylene, polyethylene (HDPE (High Density Polyethylene), LDPE (Low Density Polyethylene), LLDPE) (Linear Low Density Polyethylene; Linear Low Density Polyethylene), etc.), ABS (Acrylonitrile Butadiene Styrene; acrylonitrile-butadiene-styrene) resin, ethylene vinyl alcohol resin, polystyrene, glass, and metal (aluminum, etc.) Wait. In addition, these materials may be subjected to various coating treatments in consideration of strength, flexibility, weather resistance, stability of components, etc., or these materials may be combined for example by mixing or the like, or may be laminated and used as a container material. Among them, it is preferable to use polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ethylene vinyl alcohol resin, and metal (aluminum, etc.).

[使用方法等] 本發明的油中水型乳化組成物可期待菸鹼醯胺的生理活性,以血液循環促進、抗發炎、腦醯胺合成促進為目的而較佳地使用。進而,亦可期待美白、抗皺、抗衰老之效果,而作為包括美白劑、防曬劑等之多功能的製劑有用。[How to use etc.] The water-in-oil emulsion composition of the present invention can be expected to have physiological activity of nicotine amide, and is preferably used for the purpose of promoting blood circulation, anti-inflammatory, and promoting ceramide synthesis. Furthermore, whitening, anti-wrinkle, and anti-aging effects can also be expected, and it is useful as a multifunctional formulation including whitening agents, sunscreen agents, and the like.

另外,收容組成物之容器及組成物的使用方法與本發明的油中水型乳化組成物之情形相同。In addition, the container containing the composition and the method of using the composition are the same as those of the water-in-oil emulsion composition of the present invention.

[使用感提升方法] 另外,本發明亦包含含有(A)菸鹼醯胺之油中水型乳化組成物的使用感提升方法。根據本發明,藉由製成含有(A)菸鹼醯胺、(B)選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上、以及(C)油溶性增黏劑之油中水型乳化組成物,能夠達成油中水型乳化組成物的使用感提升。此處,所謂使用感提升,於例如乳霜劑等情形時,係指應用於肌膚時的延展性良好、親和性良好、不黏膩、濕潤水嫩、保持適度的柔和性。[How to improve usability] In addition, the present invention also includes a method for improving the feeling of use of the water-in-oil emulsion composition containing (A) nicotine amide. According to the present invention, it is prepared by containing (A) nicotine amide, (B) selected from silicone surfactants, sorbitan ester surfactants, polyglycerol ester surfactants, and glyceride surfactants One or more of the group consisting of and (C) the water-in-oil emulsion composition of the oil-soluble tackifier can improve the feeling of use of the water-in-oil emulsion composition. Here, the improvement in the feeling of use, in the case of creams, etc., means that when applied to the skin, it has good extensibility, good affinity, non-sticky, moist and tender, and maintains moderate softness.

[其他] 另外,本發明的油中水型乳化組成物的穩定性優異。此處,所謂穩定性優異,並無限定,係指例如即便於高溫下或低溫下亦確保穩定性。具體而言,係指至少於保存油中水型乳化組成物之情形時,分離等亦得到抑制等。[other] In addition, the water-in-oil emulsion composition of the present invention has excellent stability. Here, the term "excellent in stability" is not limited, and means that, for example, stability is ensured even at high or low temperatures. Specifically, it means that at least when the water-in-oil emulsion composition is preserved, separation etc. are also suppressed.

本發明的方法中,關於含有(A)菸鹼醯胺、(B)選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、甘油酯界面活性劑所組成之群組中的1種以上、以及(C)油溶性增黏劑之油中水型乳化組成物的條件等,與前述油中水型乳化組成物中所使用之條件相同。進而,利用本方法所獲得之組成物可根據用途等每天1次至分為數次,以公知或慣用之用法、用量使用。 [實施例]In the method of the present invention, it contains (A) nicotinic amide, (B) selected from silicone-based surfactants, sorbitan ester surfactants, polyglycerol ester surfactants, and glyceride surfactants. The conditions of one or more types in the group and (C) the oil-soluble tackifier of the water-in-oil emulsion composition are the same as those used in the aforementioned water-in-oil emulsion composition. Furthermore, the composition obtained by this method can be used from once to several times a day according to the purpose, etc., in a known or customary usage and dosage. [Example]

其次,藉由實施例具體地說明本發明,但本發明並不限定於以下之實施例。Next, the present invention will be specifically explained with examples, but the present invention is not limited to the following examples.

[試驗例1]穩定化評價 製備表中所記載之實施例及比較例的組成物,觀察製造後1小時的製劑的狀態、及保存後的狀態。 可藉由下述方式製備實施例及比較例的組成物:藉由加熱溶解、混合來分別製備油相、水相,使兩相成為室溫後,一邊使油相中緩慢地含有水相,一邊使用均質攪拌機充分地進行攪拌,從而獲得目標之油中水型乳化組成物。[Test Example 1] Stabilization evaluation The compositions of the examples and comparative examples described in the preparation table were prepared, and the state of the preparations 1 hour after the production and the state after storage were observed. The compositions of Examples and Comparative Examples can be prepared by the following method: the oil phase and the water phase are prepared separately by heating and dissolving and mixing, and after the two phases are brought to room temperature, the oil phase is slowly contained in the water phase, While fully mixing with a homomixer, the target water-in-oil emulsion composition is obtained.

[穩定性] 針對剛製造後及製造後於室溫下保管24小時後的製劑,進行利用目視之外觀評價,判定是否具有充分的穩定性。[stability] For the formulations stored at room temperature for 24 hours immediately after production and after production, visual appearance evaluation was performed to determine whether they had sufficient stability.

[評價基準] ×         無法乳化,於剛製造後分離或於表面產生離漿。 ○        於剛製造後整體維持均一的乳化狀態。 ◎        於保管24小時後亦整體維持均一的乳化狀態。[Evaluation criteria] × Unable to emulsify, it separates immediately after manufacture or produces de-sizing on the surface. ○ Maintain a uniform emulsification state as a whole immediately after manufacturing. ◎ The overall emulsification state is maintained even after 24 hours of storage.

[熱負荷試驗(熱穩定性)] 為了評價熱負荷試驗下的穩定性,將各實施例及比較例的組成物填充至30mL玻璃瓶中,於50℃之恆溫槽中加以保管。 於經過3天後及經過2週後將試驗製劑自恆溫槽中取出,恢復至室溫後,進行利用目視之外觀評價,判定各實施例及比較例的組成物是否具有長期穩定性。[Heat load test (thermal stability)] In order to evaluate the stability under the heat load test, the compositions of the respective examples and comparative examples were filled into 30 mL glass bottles and stored in a thermostat at 50°C. After 3 days and 2 weeks, the test formulation was taken out of the thermostat, and after returning to room temperature, visual appearance evaluation was performed to determine whether the composition of each example and comparative example had long-term stability.

[評價基準] ×         於經過3天後大幅產生分離,性狀大幅變化,對使用感有影響。 △        於經過3天後稍微分離或於表面產生離漿,但為對使用感無影響,以性狀而言落在無特別問題之範圍。 ○        於經過3天後亦整體維持均一的乳化狀態。 ◎        於2週後亦整體維持均一的乳化狀態。 此外,此處△之製劑於25℃保存時,於2周後亦整體維持均一的乳化狀態。[Evaluation criteria] × After 3 days, a large separation occurred, and the properties changed significantly, which affected the feeling of use. △ After 3 days, it is slightly separated or has a dissociation on the surface, but it does not affect the feeling of use and falls within the range of no special problems in terms of properties. ○ The overall emulsification state was maintained even after 3 days. ◎ After 2 weeks, it also maintained a uniform emulsification state. In addition, when the △ preparation is stored at 25°C, the overall uniform emulsification state is maintained even after 2 weeks.

首先,根據有無菸鹼醯胺,驗證組成物的穩定性。 [表1] 參考例1 參考例2 參考例3 比較例1 (A) 菸鹼醯胺 0.5 5 純化水 50 50 45 45 1,3-丁二醇 10 10 10 10 (B) 月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 3 3 3 3 山梨醇酐倍半油酸酯 1 1 1 1 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 十甲基環五矽氧烷 27 28 28 28 (C) 二甲基二硬脂基銨鋰膨潤石 1   合計 100 100 100 100 剛製造後 × 穩定性(25℃) × First, the stability of the composition was verified based on the presence or absence of nicotine amide. [Table 1] Reference example 1 Reference example 2 Reference example 3 Comparative example 1 (A) Nicotinamide 0.5 5 purified water 50 50 45 45 1,3-Butanediol 10 10 10 10 (B) Lauryl PEG-9 Polydimethylsilyloxyethyl Dimethicone 3 3 3 3 Sorbitan sesquioleate 1 1 1 1 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 Decamethylcyclopentasiloxane 27 28 28 28 (C) Dimethyl distearyl ammonium lithium bentonite 1 total 100 100 100 100 Just after manufacture × Stability (25℃) ×

根據表1的結果可知,若不含有菸鹼醯胺,則即便不將(B)成分與(C)成分組合,亦能夠成為充分良好的乳化狀態。另外,於菸鹼醯胺為低濃度之情形時,穩定性未見問題。但是,藉由如比較例1的組成物般高濃度含有菸鹼醯胺,乳化狀態會變得不穩定,難以製作穩定的製劑。From the results of Table 1, it can be seen that if nicotine amide is not contained, even if the component (B) and the component (C) are not combined, a sufficiently good emulsified state can be achieved. In addition, when the concentration of nicotine amide is low, there is no problem with stability. However, by containing nicotine amide in a high concentration like the composition of Comparative Example 1, the emulsified state becomes unstable and it is difficult to produce a stable formulation.

其次,製備表2至表7所示之實施例及比較例的組成物並進行評價。 [表2] 實施例1 實施例2 實施例3 比較例1 比較例2 比較例3 比較例4 (A) 菸鹼醯胺 5 5 5 5 5 5 5 純化水 45 45 45 45 45 45 45 1,3-丁二醇 10 10 10 10 10 10 10 (B) PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 3 3       月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮   3     3     山梨醇酐倍半油酸酯 1 1 4 1 1 4   (B)' 聚乙二醇二聚羥基硬脂酸酯             4 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 5 5 5 十甲基環五矽氧烷 27 27 27 28 28 28 27 (C) 二甲基二硬脂基銨鋰膨潤石 1 1 1       1 合計 100 100 100 100 100 100 100 穩定性(室溫) × × × × 熱穩定性(50℃) × × × × Next, the compositions of the Examples and Comparative Examples shown in Tables 2 to 7 were prepared and evaluated. [Table 2] Example 1 Example 2 Example 3 Comparative example 1 Comparative example 2 Comparative example 3 Comparative example 4 (A) Nicotinamide 5 5 5 5 5 5 5 purified water 45 45 45 45 45 45 45 1,3-Butanediol 10 10 10 10 10 10 10 (B) PEG-9 Polydimethylsilyloxyethyl Dimethicone 3 3 Lauryl PEG-9 Polydimethylsilyloxyethyl Dimethicone 3 3 Sorbitan sesquioleate 1 1 4 1 1 4 (B)' Polyethylene glycol dipolyhydroxystearate 4 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 5 5 5 Decamethylcyclopentasiloxane 27 27 27 28 28 28 27 (C) Dimethyl distearyl ammonium lithium bentonite 1 1 1 1 total 100 100 100 100 100 100 100 Stability (room temperature) X X X X Thermal stability (50℃) X X X X

於實施例1至實施例3中,即便於高濃度含有(A)菸鹼醯胺之情形時,藉由組合(B)及(C)成分,剛製造後的狀態及穩定性亦良好而獲得了油中水型乳化組成物,相對於此,於不含有油溶性增黏劑之比較例1至比較例3中,自剛製造後便產生分離。含有作為醚系界面活性劑之聚乙二醇二聚羥基硬脂酸酯之比較例4中,自剛製造後便產生分離。 另外,將實施例1至實施例3及比較例1至比較例3的油中水型乳化組成物分別用於皮膚而評價使用感,結果確認到:實施例的油中水型乳化組成物與比較例的油中水型乳化組成物相比,為未見析出、延展良好、無黏膩之製劑。以下,實施例中亦同樣地進行使用感之評價。In Example 1 to Example 3, even when (A) nicotine amide is contained in a high concentration, by combining the components (B) and (C), the state and stability immediately after production are also good. In contrast to the water-in-oil emulsion composition, in Comparative Examples 1 to 3 that did not contain an oil-soluble thickener, separation occurred immediately after production. In Comparative Example 4 containing polyethylene glycol dipolyhydroxystearate as an ether-based surfactant, separation occurred immediately after production. In addition, the water-in-oil emulsion compositions of Examples 1 to 3 and Comparative Examples 1 to 3 were applied to the skin to evaluate the feeling of use. As a result, it was confirmed that the water-in-oil emulsion compositions of the examples were compared with Compared with the water-in-oil emulsion composition of the comparative example, it is a formulation with no precipitation, good spread, and no stickiness. Hereinafter, the evaluation of the feeling in use was also performed in the same manner in the examples.

[表3] 實施例4 實施例5 實施例6 實施例7 實施例8 實施例9 實施 例10 (A) 菸鹼醯胺 5 5 5 5 5 5 5 純化水 45 45 45 45 45 45 45 1,3-丁二醇 10 10 10 10 10 10 10 (B) PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 2           PEG-10二甲基矽酮 2       聚甘油-10五異硬脂酸酯     2   山梨醇酐異硬脂酸酯 2 山梨醇酐硬脂酸酯 2 山梨醇酐倍半異硬脂酸酯 2 聚甘油-10異硬脂酸酯 2 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 5 5 5 十甲基環五矽氧烷 29 29 29 29 29 29 29 (C) 二甲基二硬脂基銨鋰膨潤石 1 1 1 1 1 1 1 合計 100 100 100 100 100 100 100 穩定性(室溫) 熱穩定性(50℃) [table 3] Example 4 Example 5 Example 6 Example 7 Example 8 Example 9 Example 10 (A) Nicotinamide 5 5 5 5 5 5 5 purified water 45 45 45 45 45 45 45 1,3-Butanediol 10 10 10 10 10 10 10 (B) PEG-9 Polydimethylsilyloxyethyl Dimethicone 2 PEG-10 Dimethicone 2 Polyglycerol-10 Pentaisostearate 2 Sorbitan Isostearate 2 Sorbitan Stearate 2 Sorbitan sesquiisostearate 2 Polyglycerol-10 Isostearate 2 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 5 5 5 Decamethylcyclopentasiloxane 29 29 29 29 29 29 29 (C) Dimethyl distearyl ammonium lithium bentonite 1 1 1 1 1 1 1 total 100 100 100 100 100 100 100 Stability (room temperature) Thermal stability (50℃)

於實施例4至實施例10中,於剛製造後得到了穩定性及熱穩定性良好而使用感良好之油中水型乳化組成物。尤其是藉由使用矽酮系界面活性劑、HLB為2至6之聚甘油酯界面活性劑,能夠確認到熱穩定性更良好之穩定性。In Example 4 to Example 10, an oil-in-water emulsion composition with good stability and thermal stability and a good feeling in use was obtained immediately after production. In particular, by using silicone-based surfactants and polyglycerol ester surfactants with HLB of 2 to 6, better thermal stability can be confirmed.

[表4] 實施例5 實施例11 實施例12 實施例13 比較例5 比較例6 比較例7 (A) 菸鹼醯胺 5 5 5 5 5 5 5 純化水 45 45 45 45 45 45 45 BG 10 10 10 10 10 10 10 (C)' 三仙膠         0.3     聚乙烯蠟           2 4 (B) PEG-10二甲基矽酮 2 2 2 2 2 2 2 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 5 5 5 十甲基環五矽氧烷 29 29 29 29 29.7 28 26 (C) 二甲基二硬脂基銨鋰膨潤石 1           菊糖硬脂酸酯   1             糊精棕櫚酸酯     1           糊精(棕櫚酸/乙基己酸)酯       1       合計 100 100 100 100 100 100 100 穩定性(室溫) × × × 熱穩定性(50℃) × × [Table 4] Example 5 Example 11 Example 12 Example 13 Comparative example 5 Comparative example 6 Comparative example 7 (A) Nicotinamide 5 5 5 5 5 5 5 purified water 45 45 45 45 45 45 45 BG 10 10 10 10 10 10 10 (C)' Sanxian Gum 0.3 Polyethylene wax 2 4 (B) PEG-10 Dimethicone 2 2 2 2 2 2 2 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 5 5 5 Decamethylcyclopentasiloxane 29 29 29 29 29.7 28 26 (C) Dimethyl distearyl ammonium lithium bentonite 1 Inulin Stearate 1 Dextrin palmitate 1 Dextrin (palmitic acid/ethylhexanoic acid) ester 1 total 100 100 100 100 100 100 100 Stability (room temperature) × × × Thermal stability (50℃) × ×

含有油溶性增黏劑之實施例5、實施例11至實施例13的組成物具有高的穩定性及熱穩定性。對於含有水溶性增黏劑而非油溶性增黏劑之比較例5的組成物,自剛製造後便確認到分離。 另外,確認到於熱穩定性方面實施例5、實施例11的組成物即便於50℃2週之相當嚴酷的條件下亦保持良好的穩定性,故而尤佳為含有選自菊糖硬脂酸酯或二甲基二硬脂基銨鋰膨潤石中的1種以上之油溶性增黏劑。The compositions of Example 5, Example 11 to Example 13 containing an oil-soluble tackifier have high stability and thermal stability. For the composition of Comparative Example 5 containing a water-soluble thickener instead of an oil-soluble thickener, separation was confirmed immediately after the production. In addition, it was confirmed that the compositions of Example 5 and Example 11 in terms of thermal stability maintained good stability even under very severe conditions at 50°C for 2 weeks, so it is particularly preferable to contain inulin stearic acid. One or more oil-soluble tackifiers in esters or dimethyl distearyl ammonium lithium bentonite.

[表5] 實施例1 實施例14 實施例15 實施例16 實施例17 實施例18 (A) 菸鹼醯胺 5 5 5 5 5 5 純化水 45 45 45 45 45 45 1,3-丁二醇 10 10 10 10 10 10 (B) PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 3 3 3 3 3 3 山梨醇酐倍半油酸酯 1 1 1 1 1 1 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 5 5 十甲基環五矽氧烷 27 27.7 27.5 26 25 23 (C) 二甲基二硬脂基銨鋰膨潤石 1 0.3 0.5 2       糊精(棕櫚酸/乙基己酸)酯         3 5 合計 100 100 100 100 100 100 穩定性(室溫) 熱穩定性(50℃) [table 5] Example 1 Example 14 Example 15 Example 16 Example 17 Example 18 (A) Nicotinamide 5 5 5 5 5 5 purified water 45 45 45 45 45 45 1,3-Butanediol 10 10 10 10 10 10 (B) PEG-9 Polydimethylsilyloxyethyl Dimethicone 3 3 3 3 3 3 Sorbitan sesquioleate 1 1 1 1 1 1 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 5 5 Decamethylcyclopentasiloxane 27 27.7 27.5 26 25 twenty three (C) Dimethyl distearyl ammonium lithium bentonite 1 0.3 0.5 2 Dextrin (palmitic acid/ethylhexanoic acid) ester 3 5 total 100 100 100 100 100 100 Stability (room temperature) Thermal stability (50℃)

對油溶性增黏劑的含量進行了研究,結果任一實施例的組成物均於剛製造後穩定性及熱穩定性良好而獲得了使用感良好之油中水型乳化組成物。The content of the oil-soluble tackifier was studied, and as a result, the composition of any of the examples had good stability and thermal stability immediately after manufacture, and a water-in-oil emulsion composition with a good feeling in use was obtained.

[表6] 實施例1 實施例19 實施例20 (A) 菸鹼醯胺 5 5 5 純化水 45 45 45 1,3-丁二醇 10 10 10 (B) PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 3 3 3 山梨醇酐倍半油酸酯 1 1 1 (D) 對甲氧基肉桂酸2-乙基己酯 3 10 20 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 十甲基環五矽氧烷 27 20 10 (C) 二甲基二硬脂基銨鋰膨潤石 1 1 1 合計 100 100 100 穩定性(室溫) 熱穩定性(50℃) [Table 6] Example 1 Example 19 Example 20 (A) Nicotinamide 5 5 5 purified water 45 45 45 1,3-Butanediol 10 10 10 (B) PEG-9 Polydimethylsilyloxyethyl Dimethicone 3 3 3 Sorbitan sesquioleate 1 1 1 (D) 2-ethylhexyl p-methoxycinnamic acid 3 10 20 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 Decamethylcyclopentasiloxane 27 20 10 (C) Dimethyl distearyl ammonium lithium bentonite 1 1 1 total 100 100 100 Stability (room temperature) Thermal stability (50℃)

對紫外線吸收劑的含量進行了研究,結果實施例中獲得了於剛製造後穩定性及熱穩定性良好之油中水型乳化組成物。The content of the ultraviolet absorber was studied, and as a result, in the examples, a water-in-oil emulsion composition with good stability and thermal stability immediately after manufacture was obtained.

[表7] 實施例21 實施例22 實施例23 實施例24 實施例25 實施例26 實施例27 (A) 菸鹼醯胺 5 5 5 5 5 5 5 純化水 45 45 45 45 45 45 45 1,3-丁二醇 10 10 10 10 10 10 10 (B) 聚甘油-10五異硬脂酸酯       1       PEG-10二甲基矽酮 2 2 2       1 PEG-9聚二甲基矽烷氧基乙基二甲基矽酮         2 2 月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮 2 2 硬脂酸甘油酯 1 1 山梨醇酐異硬脂酸酯 1 1 山梨醇酐硬脂酸酯 1 (D) 對甲氧基肉桂酸2-乙基己酯 3 3 3 3 3 3 3 二苯基矽烷氧基苯基三甲基矽酮 5 5 5 5 5 5 5 十甲基環五矽氧烷 28 28 28 28 28 28 28 (C) 二甲基二硬脂基銨鋰膨潤石 1 1 1 1 1 1 1 合計 100 100 100 100 100 100 100 穩定性(室溫) 熱穩定性(50℃) [Table 7] Example 21 Example 22 Example 23 Example 24 Example 25 Example 26 Example 27 (A) Nicotinamide 5 5 5 5 5 5 5 purified water 45 45 45 45 45 45 45 1,3-Butanediol 10 10 10 10 10 10 10 (B) Polyglycerol-10 Pentaisostearate 1 PEG-10 Dimethicone 2 2 2 1 PEG-9 Polydimethylsilyloxyethyl Dimethicone 2 2 Lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone 2 2 Glyceryl stearate 1 1 Sorbitan Isostearate 1 1 Sorbitan Stearate 1 (D) 2-ethylhexyl p-methoxycinnamic acid 3 3 3 3 3 3 3 Diphenylsilanoxy phenyl trimethyl silicone 5 5 5 5 5 5 5 Decamethylcyclopentasiloxane 28 28 28 28 28 28 28 (C) Dimethyl distearyl ammonium lithium bentonite 1 1 1 1 1 1 1 total 100 100 100 100 100 100 100 Stability (room temperature) Thermal stability (50℃)

任一實施例中均獲得了使用感良好且穩定性、熱穩定性尤其良好之油中水型乳化組成物。In any of the examples, a water-in-oil emulsion composition with good feeling in use and particularly good stability and thermal stability was obtained.

以下之表8至表9中表示配方例。 [表8]     配方例1 配方例 2 配方例 3 配方例 4 配方例5 配方例6 (A) 菸鹼醯胺 3 5 8 5 5 10   1,3-丁二醇 3   7 10 10 10 二丙二醇 3 10         1,3-丙二醇     0.1     0.5 1,2-己二醇         0.1   戊二醇 1 1   1 1   苯氧基乙醇 0.3 0.3 0.3   0.3 0.3 對羥基苯甲酸甲酯     0.1       辛基羥肟酸     0.05       苯甲酸鈉     0.05       EDTA-2Na 0.05       0.05   硫酸鎂 0.2 0.5         氯化鈉       0.2   0.5 三仙膠 0.1           羥基丙基甲基纖維素 0.1           玻尿酸鈉 0.001         0.01 乙醯化玻尿酸鈉   0.001     0.01   磷酸L-抗壞血酸鎂   0.001       0.005 傳明酸         1   甘草酸二鉀 0.1     0.05 0.01   雙乙氧基雙乙醇環己烷-1,4-二羧酸酯   1         水解膠原蛋白   0.001   0.01   0.01 水解大豆蛋白   0.01   0.01 0.01   大豆萃取物 0.01   0.01       氫氧化鈉 0.45           (B) 聚甘油-10五異硬脂酸酯 1           PEG-10二甲基矽酮 3   3   1   月桂基PEG-9聚二甲基矽烷氧基乙基二甲基矽酮     0.5       月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮   3   3 1 3 硬脂酸甘油酯   0.5         山梨醇酐異硬脂酸酯   0.5   2 1 1 山梨醇酐倍半油酸酯     1       (D) 對甲氧基肉桂酸2-乙基己酯 6 7 7 4   7 4-第三丁基-4'-甲氧基二苯甲醯甲烷         2 1 2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯   3 1 2   1 2,4-雙-[{4-(二-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪 1         1 2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪     2       奧克立林       3 5   水楊酸2-乙基己酯         1   二甲基矽酮二乙基亞苄基丙二酸酯         2   2-苯基苯并咪唑-5-磺酸 3             經疏水化處理之氧化鈦         5   經疏水化處理之氧化鋅           5   二苯基矽烷氧基苯基三甲基矽酮 4 7 5 8 8 5 十甲基環五矽氧烷 20.5 17.5 19 24 19 24   異壬酸異壬酯       5     三-2乙基己酸甘油酯         3   二丁基羥基甲苯 0.01 0.05         天然維生素E       0.01 0.05   (C) 糊精肉豆蔻酸酯       1   1 糊精(棕櫚酸/乙基己酸)酯         1   菊糖硬脂酸酯 1.5 0.5       1 二甲基二硬脂基銨鋰膨潤石   1 2 1 1     純化水 剩餘量 剩餘量 剩餘量 剩餘量 剩餘量 剩餘量   合計 100 100 100 100 100 100 [表9]     配方例7 配方例8 配方例9 配方例10 配方例11 (A) 菸鹼醯胺 6 3 6 5 5   乙醇       3 5   1,3-丁二醇 10   5 5 6 二丙二醇   7       1,3-丙二醇 0.5   1     1,2-己二醇           戊二醇 1 2 1 1 1 苯氧基乙醇 0.3         EDTA-2Na 0.05 0.05 0.05 0.05 0.05 硫酸鎂 0.1 0.05       三仙膠 0.1         羥基丙基甲基纖維素 0.1         玻尿酸鈉 0.001 0.001 0.001 0.001 0.001 傳明酸 1         磷酸L-抗壞血酸鎂 0.001 0.001 0.001 0.001 0.001 甘草酸二鉀         0.001 氫氧化鈉 0.45           氫化卵磷脂 0.01       0.01   雙乙氧基雙乙醇環己烷-1,4-二羧酸酯       0.1     聚甘油-10(二十烷二酸/十四烷二酸)酯 0.1           膽固醇 0.001 0.01     0.001   氫化大豆磷脂質   0.1         蝦紅素     0.1   0.01   月桃葉萃取物     0.01   0.005   玫瑰果萃取物     0.01   0.005   雪絨花萃取物       0.01 0.005   水解膠原蛋白 0.001 0.001   0.01 0.005   水解大豆蛋白 0.01     0.01     大豆萃取物 0.01   0.01       聚氧丙烯甲基葡萄糖苷       0.1     荷荷芭油 0.1 0.1 0.1 0.1 0.1   鯨蠟基PEG/PPG-10/1二甲基矽酮       2 2 PEG-9聚二甲基矽烷氧基乙基二甲基矽酮 2 2 2 1   硬脂酸甘油酯   1       山梨醇酐異硬脂酸酯 2   1   2 (D) 2-[4-(二乙基胺基)-2-羥基苯甲醯]苯甲酸己酯   0.4 0.4     2,4-雙-[{4-(二-乙基己氧基)-2-羥基}-苯基]-6-(4-甲氧基苯基)-1,3,5-三嗪   3 3 2   2,4,6-三[4-(2-乙基己氧基羰基)苯胺基]-1,3,5-三嗪   3 3 2   水楊酸2-乙基己酯       5   (E) 經疏水化處理之氧化鈦   3 2 5 7 經疏水化處理之氧化鋅   6 8 5 10   二苯基矽烷氧基苯基三甲基矽酮 5           二甲基矽酮(1.5CS)   5   3     二甲基矽酮(2CS)     5       二甲基矽酮(6CS)     3       辛醯基甲聚矽氧烷 3   3   3   甲基三甲基矽酮   5   5     異十二烷 5       7   異十六烷 3       3   角鯊烷 10           異壬酸異壬酯   8 8 10     三-2乙基己酸甘油酯 5       10   琥珀酸二乙基己酯 7 10   8     蘋果酸二異硬脂酯 2 2   4 2   偏苯三甲酸三乙基己酯     10       月桂醯麩胺酸二(辛基十二烷基/植物固醇/山萮基)酯       0.5     二聚物二亞麻油酸二(異硬脂基/植物固醇)酯     2       聚羥基硬脂酸   1 1 2 3   天然維生素E 0.01 0.01 0.01 0.01 0.01 (C) 糊精(棕櫚酸/乙基己酸)酯     1     菊糖硬脂酸酯       1   二甲基二硬脂基銨鋰膨潤石 1.5 1     1   純化水 剩餘量 剩餘量 剩餘量 剩餘量 剩餘量   合計 100 100 100 100 100 The following Table 8 to Table 9 show formulation examples. [Table 8] Formulation example 1 Formulation example 2 Formulation example 3 Formulation example 4 Formulation example 5 Formulation example 6 (A) Nicotinamide 3 5 8 5 5 10 1,3-Butanediol 3 7 10 10 10 Dipropylene glycol 3 10 1,3-propanediol 0.1 0.5 1,2-hexanediol 0.1 Pentylene Glycol 1 1 1 1 Phenoxyethanol 0.3 0.3 0.3 0.3 0.3 Methylparaben 0.1 Octyl Hydroxamic Acid 0.05 sodium benzoate 0.05 EDTA-2Na 0.05 0.05 Magnesium Sulfate 0.2 0.5 Sodium chloride 0.2 0.5 Sanxian Gum 0.1 Hydroxypropyl methylcellulose 0.1 Sodium Hyaluronate 0.001 0.01 Sodium Acetate Hyaluronate 0.001 0.01 Magnesium L-Ascorbate Phosphate 0.001 0.005 Tranexamic acid 1 Dipotassium Glycyrrhizinate 0.1 0.05 0.01 Bisethoxydiethanolcyclohexane-1,4-dicarboxylate 1 Hydrolyzed Collagen 0.001 0.01 0.01 Hydrolyzed soy protein 0.01 0.01 0.01 Soy extract 0.01 0.01 Sodium hydroxide 0.45 (B) Polyglycerol-10 Pentaisostearate 1 PEG-10 Dimethicone 3 3 1 Lauryl PEG-9 Polydimethylsilyloxyethyl Dimethicone 0.5 Lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone 3 3 1 3 Glyceryl stearate 0.5 Sorbitan Isostearate 0.5 2 1 1 Sorbitan sesquioleate 1 (D) 2-ethylhexyl p-methoxycinnamic acid 6 7 7 4 7 4-tert-butyl-4'-methoxydibenzoyl methane 2 1 2-[4-(Diethylamino)-2-hydroxybenzoyl]hexyl benzoate 3 1 2 1 2,4-Bis-[{4-(Di-ethylhexyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine 1 1 2,4,6-Tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine 2 Oakley Lin 3 5 2-ethylhexyl salicylate 1 Dimethyl silicone diethyl benzylidene malonate 2 2-phenylbenzimidazole-5-sulfonic acid 3 Hydrophobized titanium oxide 5 Hydrophobized zinc oxide 5 Diphenylsilanoxy phenyl trimethyl silicone 4 7 5 8 8 5 Decamethylcyclopentasiloxane 20.5 17.5 19 twenty four 19 twenty four Isononyl isononanoate 5 Glyceryl tri-2-ethylhexanoate 3 Dibutyl hydroxytoluene 0.01 0.05 Natural Vitamin E 0.01 0.05 (C) Dextrin myristate 1 1 Dextrin (palmitic acid/ethylhexanoic acid) ester 1 Inulin stearate 1.5 0.5 1 Dimethyl distearyl ammonium lithium bentonite 1 2 1 1 purified water remaining remaining remaining remaining remaining remaining total 100 100 100 100 100 100 [Table 9] Formulation example 7 Formulation example 8 Formulation example 9 Formulation example 10 Formulation example 11 (A) Nicotinamide 6 3 6 5 5 Ethanol 3 5 1,3-Butanediol 10 5 5 6 Dipropylene glycol 7 1,3-propanediol 0.5 1 1,2-hexanediol Pentylene Glycol 1 2 1 1 1 Phenoxyethanol 0.3 EDTA-2Na 0.05 0.05 0.05 0.05 0.05 Magnesium Sulfate 0.1 0.05 Sanxian Gum 0.1 Hydroxypropyl methylcellulose 0.1 Sodium Hyaluronate 0.001 0.001 0.001 0.001 0.001 Tranexamic acid 1 Magnesium L-Ascorbate Phosphate 0.001 0.001 0.001 0.001 0.001 Dipotassium Glycyrrhizinate 0.001 Sodium hydroxide 0.45 Hydrogenated Lecithin 0.01 0.01 Bisethoxydiethanolcyclohexane-1,4-dicarboxylate 0.1 Polyglycerol-10 (eicosandioic acid/tetradecanedioic acid) ester 0.1 cholesterol 0.001 0.01 0.001 Hydrogenated Soy Phospholipids 0.1 Astaxanthin 0.1 0.01 Moon Peach Leaf Extract 0.01 0.005 Rosehip extract 0.01 0.005 Edelweiss Extract 0.01 0.005 Hydrolyzed Collagen 0.001 0.001 0.01 0.005 Hydrolyzed soy protein 0.01 0.01 Soy extract 0.01 0.01 Polyoxypropylene methyl glucoside 0.1 Jojoba oil 0.1 0.1 0.1 0.1 0.1 Cetyl PEG/PPG-10/1 Dimethicone 2 2 PEG-9 Polydimethylsilyloxyethyl Dimethicone 2 2 2 1 Glyceryl stearate 1 Sorbitan Isostearate 2 1 2 (D) 2-[4-(Diethylamino)-2-hydroxybenzoyl]hexyl benzoate 0.4 0.4 2,4-Bis-[{4-(Di-ethylhexyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine 3 3 2 2,4,6-Tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine 3 3 2 2-ethylhexyl salicylate 5 (E) Hydrophobized titanium oxide 3 2 5 7 Hydrophobized zinc oxide 6 8 5 10 Diphenylsilanoxy phenyl trimethyl silicone 5 Dimethicone (1.5CS) 5 3 Dimethicone (2CS) 5 Dimethicone (6CS) 3 Octylmethicone 3 3 3 Methyl trimethicone 5 5 Isododecane 5 7 Isohexadecane 3 3 Squalane 10 Isononyl isononanoate 8 8 10 Glyceryl tri-2-ethylhexanoate 5 10 Diethylhexyl succinate 7 10 8 Diisostearyl malate 2 2 4 2 Triethylhexyl trimellitate 10 Lauryl Glutamate Di(octyldodecyl/phytosterol/behenyl) ester 0.5 Dimer dilinoleic acid di(isostearyl/phytosterol) ester 2 Polyhydroxystearic acid 1 1 2 3 Natural Vitamin E 0.01 0.01 0.01 0.01 0.01 (C) Dextrin (palmitic acid/ethylhexanoic acid) ester 1 Inulin stearate 1 Dimethyl distearyl ammonium lithium bentonite 1.5 1 1 purified water remaining remaining remaining remaining remaining total 100 100 100 100 100

Claims (7)

一種油中水型乳化組成物,含有: (A)菸鹼醯胺3質量%以上; (B)界面活性劑,係選自由矽酮系界面活性劑、山梨醇酐酯界面活性劑、聚甘油酯界面活性劑、及甘油酯界面活性劑所組成之群組中的1種以上;以及 (C)油溶性增黏劑,係選自由黏土系增黏劑、糊精脂肪酸酯、菊糖脂肪酸酯、及胺基酸系油凝膠化劑所組成之群組中的1種以上。An oil-in-water type emulsified composition containing: (A) Nicotinamide 3% by mass or more; (B) Surfactant, one or more selected from the group consisting of silicone surfactants, sorbitan ester surfactants, polyglycerol ester surfactants, and glyceride surfactants; and (C) Oil-soluble tackifier, one or more selected from the group consisting of clay-based tackifiers, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents . 如請求項1所記載之油中水型乳化組成物,其中前述(A)成分的含量為3質量%至10質量%。The water-in-oil emulsion composition according to claim 1, wherein the content of the aforementioned component (A) is 3% by mass to 10% by mass. 如請求項1或2所記載之油中水型乳化組成物,其中前述(B)成分為選自由聚乙二醇-10二甲基矽酮、聚乙二醇-3二甲基矽酮、聚乙二醇-12二甲基矽酮、聚乙二醇/聚丙二醇-19/19二甲基矽酮、聚矽酮13、聚乙二醇-9聚二甲基矽烷氧基乙基二甲基矽酮、甲基聚矽氧烷-鯨蠟基甲基聚矽氧烷-聚(氧乙烯-氧丙烯)甲基聚矽氧烷共聚物、月桂基聚乙二醇-9聚二甲基矽烷氧基乙基二甲基矽酮、雙丁基二甲基矽酮聚甘油-3、聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮、聚甘油-3二矽氧烷二甲基矽酮、月桂基聚甘油-3聚二甲基矽烷氧基乙基二甲基矽酮;山梨醇酐油酸酯、山梨醇酐倍半油酸酯、山梨醇酐三油酸酯、山梨醇酐倍半異硬脂酸酯、山梨醇酐異硬脂酸酯、山梨醇酐三異硬脂酸酯、山梨醇酐硬脂酸酯、山梨醇酐倍半硬脂酸酯、山梨醇酐三硬脂酸酯、聚甘油-2三異硬脂酸酯、聚甘油-2異硬脂酸酯、聚甘油-10縮合蓖麻醇酸酯、聚甘油-10五異硬脂酸酯、聚甘油-10五油酸酯、聚甘油-10五硬脂酸酯、聚甘油-10五羥基硬脂酸酯、聚甘油-6縮合蓖麻醇酸酯、聚甘油-6五異硬脂酸酯、聚甘油-6五油酸酯、聚甘油-6五羥基硬脂酸酯、油酸甘油酯、倍半油酸甘油酯、三油酸甘油酯、倍半異硬脂酸甘油酯、異硬脂酸甘油酯、三異硬脂酸甘油酯、硬脂酸甘油酯、倍半硬脂酸甘油酯、及三硬脂酸甘油酯所組成之群組中的1種以上。The water-in-oil emulsion composition described in claim 1 or 2, wherein the aforementioned component (B) is selected from polyethylene glycol-10 dimethyl silicone, polyethylene glycol-3 dimethyl silicone, Polyethylene Glycol-12 Dimethicone, Polyethylene Glycol/Polypropylene Glycol-19/19 Dimethicone, Polysiloxane 13, Polyethylene Glycol-9 Dimethicone Dimethicone Methyl silicone, methyl polysiloxane-cetyl methyl polysiloxane-poly(oxyethylene-oxypropylene) methyl polysiloxane copolymer, lauryl polyethylene glycol-9 polydimethyl Dimethyl silyloxyethyl dimethyl silicone, dibutyl dimethyl silicone polyglycerol-3, polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone, polyglycerol-3 disilicon Oxyane dimethyl silicone, lauryl polyglycerol-3 polydimethylsiloxy ethyl dimethyl silicone; sorbitan oleate, sorbitan sesquioleate, sorbitan three oils Acid esters, sorbitan sesquiisostearate, sorbitan isostearate, sorbitan triisostearate, sorbitan stearate, sorbitan sesquistearate , Sorbitan Tristearate, Polyglycerol-2 Triisostearate, Polyglycerol-2 Isostearate, Polyglycerol-10 Condensed Ricinoleate, Polyglycerol-10 Pentaisostearate Acid esters, polyglycerol-10 pentaoleate, polyglycerol-10 pentastearate, polyglycerol-10 pentahydroxystearate, polyglycerol-6 condensed ricinoleate, polyglycerol-6 pentaiso Stearate, polyglyceryl-6 pentaoleate, polyglycerol-6 pentahydroxystearate, glyceryl oleate, glyceryl sesquioleate, glyceryl trioleate, glyceryl sesquiisostearate One or more of esters, glyceryl isostearate, glyceryl triisostearate, glyceryl stearate, glyceryl sesquistearate, and glyceryl tristearate. 如請求項1或2所記載之油中水型乳化組成物,其中前述(C)成分為選自由二甲基二硬脂基銨鋰膨潤石、苄基二甲基硬脂基銨鋰膨潤石、經氯化二硬脂基二甲基銨處理之矽酸鋁鎂、糊精棕櫚酸酯、糊精油酸酯、糊精硬脂酸酯、糊精肉豆蔻酸酯、糊精(棕櫚酸/乙基己酸)酯、糊精(棕櫚酸/己基癸酸)酯、及菊糖硬脂酸酯、二丁基月桂醯麩胺醯胺、及二丁基乙基己醯基麩胺醯胺所組成之群組中的1種以上。The water-in-oil emulsion composition as described in claim 1 or 2, wherein the aforementioned component (C) is selected from dimethyl distearyl ammonium lithium bentonite, benzyl dimethyl stearyl ammonium lithium bentonite , Magnesium aluminum silicate treated with distearyl dimethyl ammonium chloride, dextrin palmitate, dextrin oleate, dextrin stearate, dextrin myristate, dextrin (palmitic acid/ethyl Hexanoic acid) ester, dextrin (palmitic acid/hexyl decanoic acid) ester, and inulin stearate, dibutyl lauryl glutamine amide, and dibutyl ethyl hexyl glutamine amide One or more types in the group. 如請求項1或2所記載之油中水型乳化組成物,其進而含有(D)紫外線吸收劑。The water-in-oil emulsion composition as described in claim 1 or 2, which further contains (D) an ultraviolet absorber. 如請求項5所記載之油中水型乳化組成物,其中前述(D)成分的總含量為20質量%以下。The water-in-oil emulsion composition described in claim 5, wherein the total content of the aforementioned (D) component is 20% by mass or less. 如請求項1或2所記載之油中水型乳化組成物,其進而含有(E)紫外線防禦劑。The water-in-oil emulsion composition as described in claim 1 or 2, which further contains (E) an ultraviolet protective agent.
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Publication number Priority date Publication date Assignee Title
TWI813460B (en) * 2021-09-30 2023-08-21 日商樂敦製藥股份有限公司 Water-in-oil composition for external use containing ascorbic acid and/or its salt

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