JP7570174B2 - Emulsion stabilization method - Google Patents
Emulsion stabilization method Download PDFInfo
- Publication number
- JP7570174B2 JP7570174B2 JP2019221140A JP2019221140A JP7570174B2 JP 7570174 B2 JP7570174 B2 JP 7570174B2 JP 2019221140 A JP2019221140 A JP 2019221140A JP 2019221140 A JP2019221140 A JP 2019221140A JP 7570174 B2 JP7570174 B2 JP 7570174B2
- Authority
- JP
- Japan
- Prior art keywords
- emulsion
- weight
- water
- emulsion composition
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000839 emulsion Substances 0.000 title claims description 177
- 238000000034 method Methods 0.000 title claims description 52
- 230000006641 stabilisation Effects 0.000 title claims description 48
- 238000011105 stabilization Methods 0.000 title claims description 48
- 239000000203 mixture Substances 0.000 claims description 84
- 150000003839 salts Chemical class 0.000 claims description 42
- JDLSRXWHEBFHNC-UHFFFAOYSA-N Ufenamate Chemical compound CCCCOC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 JDLSRXWHEBFHNC-UHFFFAOYSA-N 0.000 claims description 19
- 229950010121 ufenamate Drugs 0.000 claims description 19
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims description 8
- 229940079889 pyrrolidonecarboxylic acid Drugs 0.000 claims description 8
- 238000002156 mixing Methods 0.000 claims description 4
- -1 alkyl methacrylate Chemical compound 0.000 description 41
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 29
- 239000003921 oil Substances 0.000 description 29
- 235000019198 oils Nutrition 0.000 description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 14
- 239000008346 aqueous phase Substances 0.000 description 12
- 235000014113 dietary fatty acids Nutrition 0.000 description 12
- 239000000194 fatty acid Substances 0.000 description 12
- 229930195729 fatty acid Natural products 0.000 description 12
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
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- 229940045920 sodium pyrrolidone carboxylate Drugs 0.000 description 4
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- 230000000087 stabilizing effect Effects 0.000 description 4
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- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 3
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- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
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Description
本発明は、ウフェナマートの新たな用途に関し、具体的には、水溶性カルボン酸及び/又はその塩を含有する乳化組成物の乳化安定化のためのウフェナマートの用途に関する。 The present invention relates to a new use of ufenamate, specifically, to the use of ufenamate for emulsion stabilization of an emulsion composition containing a water-soluble carboxylic acid and/or its salt.
乳化組成物は、水性成分と油性成分を配合でき、様々な製剤処方に対応できると共に、皮膚に適用した際の使用感も優れている。このため、乳化組成物は、外用医薬品や化粧料の分野において汎用されている。 Emulsion compositions can be used to blend aqueous and oily ingredients, can be used in a variety of formulations, and have an excellent feel when applied to the skin. For this reason, emulsion compositions are widely used in the fields of topical medicines and cosmetics.
乳化組成物の水相には、美白効果、保湿効果、消炎効果、収斂効果、紫外線吸収効果等を期待して様々な機能性成分が配合される。このような機能性成分には、カルボキシル基を有する化合物が数多く知られており、例えば、アスコルビン酸、グリチルリチン酸ジカリウム、コンドロイチン硫酸ナトリウム、クエン酸、グルコン酸、コハク酸、乳酸、リンゴ酸、アミノ酸(特許文献1)、ピロリドンカルボン酸ナトリウム(特許文献1~4)等が挙げられる。 Various functional ingredients are blended into the aqueous phase of the emulsion composition in the hope of providing whitening, moisturizing, anti-inflammatory, astringent, UV absorbing, etc. Many compounds having a carboxyl group are known as such functional ingredients, and examples of such compounds include ascorbic acid, dipotassium glycyrrhizinate, sodium chondroitin sulfate, citric acid, gluconic acid, succinic acid, lactic acid, malic acid, amino acids (Patent Document 1), and sodium pyrrolidone carboxylate (Patent Documents 1 to 4).
特許文献1に記載の乳化組成物は、レシチン及び2-メタクリロイルオキシエチルホスホリルコリンと所定のモル分率のアルキルメタクリレートとの共重合体を必須とすることから、処方上の制約が大きく近年の多様化する乳化製剤の処方に対応できないケースがある。また、特許文献1に記載の乳化組成物のうち、実際に乳化安定性が確認された処方は上記のカルボキシル基を有する化合物の配合量が少ないことから、期待する効果が得られるほどに充分量の機能性成分を配合できないケースがある。 The emulsion composition described in Patent Document 1 requires lecithin and a copolymer of 2-methacryloyloxyethyl phosphorylcholine and a specified molar fraction of alkyl methacrylate, and therefore has significant formulation restrictions and may not be able to accommodate the increasingly diverse emulsion formulations of recent years. In addition, among the emulsion compositions described in Patent Document 1, the formulations for which emulsion stability has actually been confirmed contain a small amount of the above-mentioned compound having a carboxyl group, and therefore may not contain a sufficient amount of functional ingredients to achieve the expected effect.
また、特許文献2~4に記載の乳化組成物ピロリドンカルボン酸又はその塩が配合されてよいことが記載されているものの、実際に、ピロリドンカルボン酸又はその塩が配合された場合の乳化組成物の性状安定性については検討されていない。 In addition, although it is described in Patent Documents 2 to 4 that pyrrolidone carboxylic acid or a salt thereof may be blended in the emulsion compositions, the stability of the properties of the emulsion compositions when pyrrolidone carboxylic acid or a salt thereof is blended has not actually been examined.
発明は、水溶性カルボン酸及び/又はその塩を含む乳化組成物の乳化状態を安定化させるための新たな方法を提供することを目的とする。 The object of the invention is to provide a new method for stabilizing the emulsified state of an emulsion composition containing a water-soluble carboxylic acid and/or its salt.
本発明者は、水溶性カルボン酸及び/又はその塩を含む乳化組成物について鋭意検討を行ったところ、これまで乳化安定化効果が知られていなかったウフェナマートを配合することで、優れた乳化安定性が備わることを予期せずして見出した。本発明は、この知見に基づいて更に検討を重ねることにより完成したものである。 The inventors conducted extensive research into emulsion compositions containing water-soluble carboxylic acids and/or their salts, and unexpectedly discovered that excellent emulsion stability was achieved by incorporating ufenamate, which was not previously known to have an emulsion stabilizing effect. The present invention was completed through further research based on this finding.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項1. 水溶性カルボン酸及び/又はその塩を含む乳化組成物中に、前記水溶性カルボン酸及び/又はその塩と共に、ウフェナマートを配合する、乳化安定化方法。
項2. 前記乳化組成物が、前記水溶性カルボン酸及び/又はその塩を総量で0.001~10重量%含む、項1に記載の乳化安定化方法。
項3. 前記水溶性カルボン酸及び/又はその塩の総量1重量部当たり、前記ウフェナマートを1.5重量部以上配合する、項1又は2に記載の乳化安定化方法。
That is, the present invention provides the following aspects.
Item 1. A method for emulsion stabilization, comprising blending ufenamate together with a water-soluble carboxylic acid and/or a salt thereof in an emulsion composition containing the water-soluble carboxylic acid and/or a salt thereof.
Item 2. The method for stabilizing an emulsion according to Item 1, wherein the emulsion composition contains the water-soluble carboxylic acid and/or a salt thereof in a total amount of 0.001 to 10% by weight.
Item 3. The method for emulsion stabilization according to Item 1 or 2, wherein 1.5 parts by weight or more of the ufenamate are blended per 1 part by weight of the total amount of the water-soluble carboxylic acid and/or salt thereof.
本発明によると、水溶性カルボン酸及び/又はその塩を含む乳化組成物に、優れた乳化安定性を備えさせることができる。 According to the present invention, it is possible to provide an emulsion composition containing a water-soluble carboxylic acid and/or its salt with excellent emulsion stability.
本発明の乳化安定化方法は、水溶性カルボン酸及び/又はその塩を含む乳化組成物中に、前記水溶性カルボン酸及び/又はその塩と共に、ウフェナマートを配合することを特徴とする。以下、本発明の乳化安定化方法について詳述する。 The emulsion stabilization method of the present invention is characterized in that ufenamate is blended into an emulsion composition containing a water-soluble carboxylic acid and/or a salt thereof together with the water-soluble carboxylic acid and/or a salt thereof. The emulsion stabilization method of the present invention is described in detail below.
本発明の乳化安定化方法において、乳化安定化とは、保存後において乳化組成物の分離を抑制することをいう。分離とは、乳化組成物から、水相及び/又は油相が分離することをいう。乳化安定化のより好ましい態様としては、保存後において乳化組成物からの水相の分離を抑制することが挙げられ、より好ましい態様としては、保存後において乳化組成物の乳化状態が均一であること、つまりエマルジョン中の液滴が分散媒中に均一に分散した状態が保たれることが挙げられる。 In the emulsion stabilization method of the present invention, emulsion stabilization refers to suppressing separation of the emulsion composition after storage. Separation refers to separation of the aqueous phase and/or oil phase from the emulsion composition. A more preferred aspect of emulsion stabilization is suppressing separation of the aqueous phase from the emulsion composition after storage, and a more preferred aspect is maintaining the emulsion state of the emulsion composition uniform after storage, that is, maintaining a state in which the droplets in the emulsion are uniformly dispersed in the dispersion medium.
水溶性カルボン酸及び/又はその塩
本発明の乳化安定化方法における乳化組成物には、水溶性カルボン酸及び/又はその塩が含まれる。水溶性カルボン酸及び/又はその塩は、水相中でCOO-基を生じ、COO-基がエマルジョン粒子を不安定化させるが、本発明の乳化安定化方法によって、水溶性カルボン酸及び/又はその塩を含みながらも優れた乳化安定性を備えさせることができる。
Water-soluble carboxylic acid and/or salt thereof The emulsion composition in the emulsion stabilization method of the present invention contains a water-soluble carboxylic acid and/or a salt thereof. The water-soluble carboxylic acid and/or a salt thereof generates a COO 2 -group in the aqueous phase, and the COO 2 -group destabilizes emulsion particles. However, the emulsion stabilization method of the present invention can provide excellent emulsion stability even when the emulsion composition contains a water-soluble carboxylic acid and/or a salt thereof.
水溶性カルボン酸及び/又はその塩としては、美白効果、保湿効果、消炎効果、収斂効果、紫外線吸収効果等が知られている機能性成分を特に制限なく用いることができる。このような機能性成分には、カルボキシル基を有する化合物が数多く知られており、例えば、アスコルビン酸、グリチルリチン酸、コンドロイチン硫酸、クエン酸、グルコン酸、コハク酸、乳酸、リンゴ酸、アミノ酸及びその誘導体、並びにこれらの塩が挙げられる。本発明においては、水溶性カルボン酸及び/又はその塩として、これらの化合物から1種を単独で用いてもよいし、複数種を組み合わせて用いてもよい。 As the water-soluble carboxylic acid and/or its salt, any functional ingredient known to have a whitening effect, a moisturizing effect, an anti-inflammatory effect, an astringent effect, an ultraviolet absorbing effect, etc. can be used without any particular restrictions. Many compounds having a carboxyl group are known as such functional ingredients, and examples of such compounds include ascorbic acid, glycyrrhizic acid, chondroitin sulfate, citric acid, gluconic acid, succinic acid, lactic acid, malic acid, amino acids and their derivatives, and salts thereof. In the present invention, one of these compounds may be used alone as the water-soluble carboxylic acid and/or its salt, or a combination of two or more of them may be used.
アミノ酸としては、グリシン、アラニン、バリン、ロイシン、イソロイシン、セリン、トレオニン、アスパラギン酸、アスパラギン、グルタミン酸、グルタミン、ピロリドンカルボン酸、リシン,アルギニン、メチオニン、フェニルアラニン、チロシン、ヒスチジン、プロリン等が挙げられ、アミノ酸の誘導体としては、グルタミン酸代謝物であるピロリドンカルボン酸等が挙げられる。これらのアミノ酸は、1種を単独で用いてもよいし、複数種を組み合わせて用いてもよい。また、アミノ酸の立体構造については特に限定されず、D-アミノ酸、L-アミノ酸、及びDL-アミノ酸のいずれであってもよい。 Examples of amino acids include glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, pyrrolidone carboxylic acid, lysine, arginine, methionine, phenylalanine, tyrosine, histidine, and proline, and examples of amino acid derivatives include pyrrolidone carboxylic acid, which is a metabolite of glutamic acid. These amino acids may be used alone or in combination. There are no particular limitations on the three-dimensional structure of the amino acids, and they may be any of D-amino acids, L-amino acids, and DL-amino acids.
上記化合物の塩としては、薬学的又は香粧学的に許容されるものである限り特に制限されないが、ナトリウム塩、カリウム塩、リチウム塩等のアルカリ金属塩;カルシウム塩、マグネシウム塩等のアルカリ土類金属塩;マグネシウム塩;亜鉛塩;アンモニウム塩、アルカノールアミン塩等が挙げられる。これらの塩は、1種を単独で用いてもよいし、複数種を組み合わせて用いてもよい。 The salts of the above compounds are not particularly limited as long as they are pharma- ceutically or cosmetically acceptable, and examples thereof include alkali metal salts such as sodium salts, potassium salts, and lithium salts; alkaline earth metal salts such as calcium salts and magnesium salts; magnesium salts; zinc salts; ammonium salts, alkanolamine salts, and the like. These salts may be used alone or in combination.
本発明の乳化安定化方法は、乳化組成物の保存後において優れた乳化安定性を奏するため、乳化組成物に乳化粒子の凝集を引き起こしやすい電解質がより多く共存していても効果的に乳化安定性を得ることができる。このような観点から、本発明の乳化安定化方法における乳化組成物は、水溶性カルボン酸及び/又はその塩の中でも、完全電離によってより多くの電解質を生じる水溶性カルボン酸の塩を含んでいることがより一層好ましい。 The emulsion stabilization method of the present invention provides excellent emulsion stability after storage of the emulsion composition, and therefore can effectively obtain emulsion stability even when the emulsion composition contains a larger amount of electrolytes that tend to cause aggregation of emulsion particles. From this perspective, it is even more preferable that the emulsion composition in the emulsion stabilization method of the present invention contains, among water-soluble carboxylic acids and/or salts thereof, a salt of a water-soluble carboxylic acid that generates a larger amount of electrolytes upon complete ionization.
本発明の乳化安定化方法ににおいて、乳化組成物中の水溶性カルボン酸及び/又はその塩の含有量としては特に限定されず、付与すべき特性に応じて適宜決定することができるが、水溶性カルボン酸及び/又はその塩の総量で、例えば0.001~10重量%が挙げられる。より一層好ましい乳化安定性を得る観点から、水溶性カルボン酸及び/又はその塩の含有量の好ましい例として、0.001~5重量%が挙げられる。また、本発明の乳化安定化方法は、乳化組成物の保存後において優れた乳化安定性を奏するため、乳化組成物に水溶性カルボン酸及び/又はその塩が比較的多く含まれていても、効果的に乳化安定性を奏することができる。このような観点から、本発明の乳化安定化方法においては、乳化組成物中の水溶性カルボン酸及び/又はその塩の含有量の好適な例として、0.1~10重量%、好ましくは1~10重量%、より好ましくは2~10重量%が挙げられる。 In the emulsion stabilization method of the present invention, the content of the water-soluble carboxylic acid and/or its salt in the emulsion composition is not particularly limited and can be appropriately determined depending on the properties to be imparted, but the total amount of the water-soluble carboxylic acid and/or its salt is, for example, 0.001 to 10% by weight. From the viewpoint of obtaining even more favorable emulsion stability, a preferred example of the content of the water-soluble carboxylic acid and/or its salt is 0.001 to 5% by weight. In addition, since the emulsion stabilization method of the present invention exhibits excellent emulsion stability after storage of the emulsion composition, even if the emulsion composition contains a relatively large amount of water-soluble carboxylic acid and/or its salt, it can effectively exhibit emulsion stability. From this viewpoint, in the emulsion stabilization method of the present invention, a preferred example of the content of the water-soluble carboxylic acid and/or its salt in the emulsion composition is 0.1 to 10% by weight, preferably 1 to 10% by weight, more preferably 2 to 10% by weight.
ウフェナマート
本発明の乳化安定化方法において、乳化組成物に含まれるウフェナマートは、フルフェナム酸ブチルとも称され、水難溶性の非ステロイド性抗炎症薬として公知の成分である。水溶性カルボン酸及び/又はその塩を含む乳化組成物は保存後における性状が不安定であるが、本発明の乳化安定化方法における乳化組成物は、ウフェナマートを配合することで、優れた乳化安定性を奏する。このような本発明の効果が得られるメカニズムとしては定かではないが、ウフェナマートが有するトリフルオロメチル基の極めて高い疎水性が、界面活性剤が油相へ過度に分配されることを妨げることで界面構造を安定化し、これによってCOO-基によるエマルジョン粒子の不安定化が抑制されるものと考えられる。
Ufenamate In the emulsion stabilization method of the present invention, ufenamate contained in the emulsion composition is also called butyl flufenamate, and is a known component as a poorly water-soluble nonsteroidal anti-inflammatory drug. Although the emulsion composition containing water-soluble carboxylic acid and/or its salt has unstable properties after storage, the emulsion composition in the emulsion stabilization method of the present invention exhibits excellent emulsion stability by blending ufenamate. Although the mechanism by which the effect of the present invention is obtained is not clear, it is considered that the extremely high hydrophobicity of the trifluoromethyl group of ufenamate prevents the surfactant from being excessively distributed into the oil phase, thereby stabilizing the interface structure, thereby suppressing the destabilization of emulsion particles caused by COO- groups.
本発明の乳化安定化方法において、乳化組成物におけるウフェナマートの含有量については特に限定されず、奏すべき乳化安定性に応じて適宜設定されるが、例えば1~20重量%、好ましくは2~10重量%、更に好ましくは3~7重量%が挙げられる。 In the emulsion stabilization method of the present invention, the content of ufenamate in the emulsion composition is not particularly limited and is appropriately set depending on the emulsion stability to be achieved, but may be, for example, 1 to 20% by weight, preferably 2 to 10% by weight, and more preferably 3 to 7% by weight.
本発明の乳化安定化方法において、水溶性カルボン酸及び/又はその塩に対するウフェナマートの比率については、上記の各成分の各含有量に応じて定まるが、より一層優れた乳化安定性を得る観点から、例えば、水溶性カルボン酸及び/又はその塩の総量1重量部当たりのウフェナマートの含有量として、例えば1.5重量部以上、好ましくは1.8重量部以上、より好ましくは2重量部以上が挙げられる。水溶性カルボン酸及び/又はその塩の総量1重量部当たりのウフェナマートの含有量の範囲の上限としては特に限定されないが、例えば40重量部以下、好ましくは20重量部以下、より好ましくは10重量部以下、更に好ましくは5重量部以下が挙げられる。 In the emulsion stabilization method of the present invention, the ratio of ufenamate to the water-soluble carboxylic acid and/or its salt is determined according to the content of each of the above-mentioned components, but from the viewpoint of obtaining even better emulsion stability, the content of ufenamate per part by weight of the total amount of water-soluble carboxylic acid and/or its salt is, for example, 1.5 parts by weight or more, preferably 1.8 parts by weight or more, and more preferably 2 parts by weight or more. The upper limit of the range of the content of ufenamate per part by weight of the total amount of water-soluble carboxylic acid and/or its salt is not particularly limited, but may be, for example, 40 parts by weight or less, preferably 20 parts by weight or less, more preferably 10 parts by weight or less, and even more preferably 5 parts by weight or less.
油分
本発明の乳化安定化方法において、乳化組成物は、油相の基剤成分として油分を含む。油分としては薬学的又は香粧学的に許容されることを限度として特に制限されないが、例えば、液状油、固形油、高級アルコール等が挙げられる。これらの油分は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。
In the emulsion stabilization method of the present invention, the emulsion composition contains an oil as a base component of the oil phase. The oil is not particularly limited as long as it is pharma- ceutical or cosmetically acceptable, and examples of the oil include liquid oil, solid oil, and higher alcohol. These oils may be used alone or in combination of two or more.
本発明の乳化安定化方法において、乳化組成物における油分の含有量については、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、2~60重量%、好ましくは4~30重量%、より好ましくは4~15重量%、さらに好ましくは6~8重量%が挙げられる。 In the emulsion stabilization method of the present invention, the oil content in the emulsion composition may be appropriately set depending on the emulsion type, form, and application of the emulsion composition, and may be, for example, 2 to 60% by weight, preferably 4 to 30% by weight, more preferably 4 to 15% by weight, and even more preferably 6 to 8% by weight.
本発明の乳化安定化方法において、乳化組成物には、上記の油分の中でも、液状油を含有することが好ましい。液状油とは、25℃において液状の形態を保つ油である。液状油としては、化粧料や外用医薬品等に通常用いられるものであればよく、例えば、;オレイン酸、インステアリン酸等の脂肪酸;エチルヘキサン酸セチル、パルミチン酸エチルヘキシル、ミリスチン酸オクチルドデシル、ミリスチン酸イソプロピル、ジエチルヘキサン酸ネオペンチルグリコール、トリ2-エチルへキサン酸グリセリル、オレイン酸オクチルドデシル、ミリスチン酸イソプロピル、トリイソステアリン酸グリセリル、ジバラメトキシケイヒ酸-モノエチルへキサン酸グリセリル等のエステル油;ジメチルポリシロキサン、メチルハイドロジエンポリシロキサン、メチルフェニルポリシロキサン、オクタメチルシクロテトラシロキサン等のシリコーン油;流動パラフィン、スクワレン、スクワラン等の液状炭化水素油等が挙げられる。 In the emulsion stabilization method of the present invention, it is preferable that the emulsion composition contains a liquid oil among the above oils. A liquid oil is an oil that maintains a liquid form at 25°C. The liquid oil may be any oil that is commonly used in cosmetics and topical medicines, and examples of such oils include fatty acids such as oleic acid and isostearic acid; ester oils such as cetyl ethylhexanoate, ethylhexyl palmitate, octyldodecyl myristate, isopropyl myristate, neopentyl glycol diethylhexanoate, glyceryl tri-2-ethylhexanoate, octyldodecyl oleate, isopropyl myristate, glyceryl triisostearate, and glyceryl di-methylmethoxycinnamate-monoethylhexanoate; silicone oils such as dimethylpolysiloxane, methylhydrogenpolysiloxane, methylphenylpolysiloxane, and octamethylcyclotetrasiloxane; and liquid hydrocarbon oils such as liquid paraffin, squalene, and squalane.
これらの液状油は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 These liquid oils may be used alone or in combination of two or more.
これらの液状油の中でも、好ましくは、エステル油、シリコーン油、液状炭化水素油が挙げられ、より好ましくはミリスチン酸オクチルドデシル、ミリスチン酸イソプロピル、ジメチルポリシロキサン、流動パラフィンが挙げられる。また、これらの液状油の中でも、より一層好ましい乳化安定性を得る観点から、好ましくは液状炭化水素油が挙げられ、より好ましくは流動パラフィンが挙げられる。 Among these liquid oils, preferably, ester oil, silicone oil, and liquid hydrocarbon oil are used, and more preferably, octyldodecyl myristate, isopropyl myristate, dimethylpolysiloxane, and liquid paraffin are used. Furthermore, among these liquid oils, from the viewpoint of obtaining even more preferable emulsion stability, preferably, liquid hydrocarbon oil is used, and more preferably, liquid paraffin is used.
本発明の乳化安定化方法において、乳化安定化剤に液状油を含有させる場合、その含有量については、特に制限されず、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、0.5~30重量%、好ましくは1~20重量%、より好ましくは3~10重量%、さらに好ましくは5~8重量%が挙げられる。 In the emulsion stabilization method of the present invention, when the emulsion stabilizer contains a liquid oil, the content is not particularly limited and may be appropriately set depending on the emulsion type, form, and application of the emulsion composition, but may be, for example, 0.5 to 30% by weight, preferably 1 to 20% by weight, more preferably 3 to 10% by weight, and even more preferably 5 to 8% by weight.
水
本発明の乳化安定化方法において、乳化組成物は、水相の基剤成分として水を含む。本発明の乳化組成物における水の含有量について、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、30~95重量%、好ましくは30~90重量%、より好ましくは30~80重量%、更に好ましくは30~75重量%が挙げられる。
In the emulsion stabilization method of the present invention, the emulsion composition contains water as a base component of the aqueous phase. The content of water in the emulsion composition of the present invention may be appropriately set depending on the emulsion type, form, application, etc. of the emulsion composition, and may be, for example, 30 to 95% by weight, preferably 30 to 90% by weight, more preferably 30 to 80% by weight, and even more preferably 30 to 75% by weight.
また、本発明の乳化安定化方法は、乳化組成物に、保存後の水相分離を抑制する優れた乳化安定性を付与することができるため、乳化組成物が、本来的に水相分離がより一層生じやすい、水を多く含む場合であっても、優れた乳化安定性を奏することが可能になる。このような本発明の効果を鑑みれば、本発明の乳化安定化方法における乳化組成物の好適な態様として、水の含有量が比較的多い乳化組成物が挙げられる。より具体的には、本発明の乳化安定化方法における乳化組成物中の水の含有量の好適な例として、例えば、40~95重量%、好ましくは45~95重量%、より好ましくは50~95重量%、さらに好ましくは55~95重量%、一層好ましくは60~95重量%が挙げられる。 The emulsion stabilization method of the present invention can impart excellent emulsion stability to the emulsion composition, suppressing aqueous phase separation after storage, and therefore can provide excellent emulsion stability even when the emulsion composition contains a large amount of water, which is inherently more prone to aqueous phase separation. In view of the effects of the present invention, a suitable embodiment of the emulsion composition in the emulsion stabilization method of the present invention is an emulsion composition having a relatively high water content. More specifically, suitable examples of the water content in the emulsion composition in the emulsion stabilization method of the present invention include, for example, 40 to 95% by weight, preferably 45 to 95% by weight, more preferably 50 to 95% by weight, even more preferably 55 to 95% by weight, and even more preferably 60 to 95% by weight.
界面活性剤
本発明の乳化安定化方法において、乳化組成物は、油相及び水相を乳化させる成分として界面活性剤を含む。界面活性剤としては、薬学的又は香粧学的に許容されることを限度として特に制限されないが、例えば、ノニオン性界面活性剤、アニオン性界面活性剤、カチオン性界面活性剤、両性界面活性剤等が挙げられる。
In the emulsion stabilization method of the present invention, the emulsion composition contains a surfactant as a component that emulsifies the oil phase and the aqueous phase. The surfactant is not particularly limited as long as it is medicamentally or cosmetically acceptable, and examples thereof include nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants, etc.
界面活性剤のHLB値としては、より一層優れた乳化安定性を得る観点から、例えば10~19、好ましくは13~17.5、より好ましくは13.5~15.5が挙げられる。HLB値は、川上法(HLB値=7+11.7log(親水部の式量の総和/親油部の式量の総和))に従って算出される値である。 From the viewpoint of obtaining even better emulsion stability, the HLB value of the surfactant may be, for example, 10 to 19, preferably 13 to 17.5, and more preferably 13.5 to 15.5. The HLB value is a value calculated according to the Kawakami method (HLB value = 7 + 11.7 log (sum of formula weights of hydrophilic parts/sum of formula weights of lipophilic parts)).
これらの界面活性剤の中でも、より優れた乳化安定性を得る観点から、好ましくはノニオン性界面活性剤が挙げられる。 Among these surfactants, nonionic surfactants are preferred from the viewpoint of obtaining better emulsion stability.
ノニオン性界面活性剤としては、具体的には、ポリオキシエチレン硬化ヒマシ油類(例えば、PEG-40水添ヒマシ油、PEG-50水添ヒマシ油、PEG-60水添ヒマシ油、PEG-80水添ヒマシ油、PEG-100水添ヒマシ油、);ソルビタン脂肪酸エステル類(例えば、ソルビタンモノオレエート、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ソルビタンセスキオレエート、ソルビタントリオレエート、ペンタ-2-エチルヘキシル酸ジグリセロールソルビタン、テトラ-2-エチルヘキシル酸ジグリセロールソルビタン等);グリセリン脂肪酸エステル類(例えば、モノ綿実油脂肪酸グリセリル、モノエルカ酸グリセリル、セスキオレイン酸グリセリル、モノステアリン酸グリセリル(ステアリン酸グリセリン)、α,α’-オレイン酸ピログルタミン酸グリセリル、モノステアリン酸グリセリンリンゴ酸等);プロピレングリコール脂肪酸エステル類(例えば、モノステアリン酸プロピレングリコール等);グリセリンアルキルエーテル;ステアレス-2;ポリオキシエチレンソルビタン脂肪酸エステル類(例えば、ポリオキシエチレンソルビタンモノオレエート、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンソルビタンテトラオレエート等);ポリオキシエチレンソルビット脂肪酸エステル類(例えば、ポリオキシエチレンソルビットモノラウレート、ポリオキシエチレンソルビットモノオレエート、ポリオキシエチレンソルビットペンタオレエート、ポリオキシエチレンソルビットモノステアレート等);ポリオキシエチレングリセリン脂肪酸エステル類(例えば、ポリオキシエチレングリセリンモノステアレート、ポリオキシエチレングリセリンモノイソステアレート、ポリオキシエチレングリセリントリイソステアレート等);ポリオキシエチレン脂肪酸エステル類(例えば、ポリオキシエチレンモノオレエート、ポリオキシエチレンモノステアレート、ポリオキシエチレンジステアレート、ポリオキシエチレンモノジオレエート、ジステアリン酸エチレングリコール等);ポリオキシエチレンアルキルエーテル類(例えば、ポリオキシエチレンラウリルエーテル、ポリオキシエチレンオレイルエーテル、ポリオキシエチレンステアリルエーテル、ポリオキシエチレンベヘニルエーテル、ポリオキシエチレン2-オクチルドデシルエーテル、ポリオキシエチレンコレスタノールエーテル等);プルロニック型類(例えば、プルロニック等);ポリオキシエチレン・ポリオキシプロピレンアルキルエーテル類(例えば、ポリオキシエチレン・ポリオキシプロピレン-セチルエーテル、ポリオキシエチレン・ポリオキシプロピレン-2-デシルテトラデシルエーテル、ポリオキシエチレン・ポリオキシプロピレンモノブチルエーテル、ポリオキシエチレン・ポリオキシプロピレン水添ラノリン、ポリオキシエチレン・ポリオキシプロピレングリセリンエーテル等);ステアレス-21等が挙げられる。 Specific examples of nonionic surfactants include polyoxyethylene hydrogenated castor oils (e.g., PEG-40 hydrogenated castor oil, PEG-50 hydrogenated castor oil, PEG-60 hydrogenated castor oil, PEG-80 hydrogenated castor oil, PEG-100 hydrogenated castor oil); sorbitan fatty acid esters (e.g., sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan sesquioleate, sorbitan trioleate, diglycerol sorbitan penta-2-ethylhexyl acid, diglycerol sorbitan tetra-2-ethylhexyl acid, etc.); glycerin fatty acid esters (e.g., monoglyceryl cottonseed oil fatty acid, monoerucic acid, etc.); glyceryl, glyceryl sesquioleate, glyceryl monostearate (glycerin stearate), α,α'-oleic acid pyroglutamate glyceryl, monostearate glycerin malate, etc.); propylene glycol fatty acid esters (e.g., propylene glycol monostearate, etc.); glycerin alkyl ether; steareth-2; polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan tetraoleate, etc.); polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan mono oleate, polyoxyethylene sorbitol pentaoleate, polyoxyethylene sorbitol monostearate, etc.); polyoxyethylene glycerin fatty acid esters (e.g., polyoxyethylene glycerin monostearate, polyoxyethylene glycerin monoisostearate, polyoxyethylene glycerin triisostearate, etc.); polyoxyethylene fatty acid esters (e.g., polyoxyethylene monooleate, polyoxyethylene monostearate, polyoxyethylene distearate, polyoxyethylene monodioleate, ethylene glycol distearate, etc.); polyoxyethylene alkyl ethers (e.g., polyoxyethylene lauryl ether, polyoxyethylene oleate, yl ether, polyoxyethylene stearyl ether, polyoxyethylene behenyl ether, polyoxyethylene 2-octyldodecyl ether, polyoxyethylene cholestanol ether, etc.); Pluronic types (e.g., Pluronic, etc.); polyoxyethylene-polyoxypropylene alkyl ethers (e.g., polyoxyethylene-polyoxypropylene-cetyl ether, polyoxyethylene-polyoxypropylene-2-decyltetradecyl ether, polyoxyethylene-polyoxypropylene monobutyl ether, polyoxyethylene-polyoxypropylene hydrogenated lanolin, polyoxyethylene-polyoxypropylene glycerin ether, etc.); steareth-21, etc.
これらの界面活性剤は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 These surfactants may be used alone or in combination of two or more.
これらのノニオン性界面活性剤の中でも、より優れた乳化安定性を得る観点から、好ましくはポリオキシエチレン硬化ヒマシ油類、ポリオキシエチレンソルビタン脂肪酸エステル類、ポリオキシエチレン脂肪酸エステル類が挙げられ、より好ましくは、PEG-60水添ヒマシ油、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンモノステアレートが挙げられる。また、これらのノニオン性界面活性剤の中でも、より一層優れた乳化安定性を得る観点から、ポリオキシエチレンソルビタン脂肪酸エステル類が挙げられ、より好ましくは、ポリオキシエチレンソルビタンモノステアレートが挙げられる。 Among these nonionic surfactants, from the viewpoint of obtaining better emulsion stability, polyoxyethylene hydrogenated castor oils, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene fatty acid esters are preferred, and more preferred are PEG-60 hydrogenated castor oil, polyoxyethylene sorbitan monostearate, and polyoxyethylene monostearate. Furthermore, among these nonionic surfactants, from the viewpoint of obtaining even better emulsion stability, polyoxyethylene sorbitan fatty acid esters are preferred, and more preferred is polyoxyethylene sorbitan monostearate.
本発明の乳化安定化方法において、乳化組成物中の界面活性剤の含有量については、使用する界面活性剤の種類等に応じて適宜設定すればよいが、例えば0.5~7重量%、好ましくは1~5重量%、より好ましくは2~5重量%、更に好ましくは3~5重量%が挙げられる。 In the emulsion stabilization method of the present invention, the content of the surfactant in the emulsion composition may be appropriately set depending on the type of surfactant used, etc., but may be, for example, 0.5 to 7% by weight, preferably 1 to 5% by weight, more preferably 2 to 5% by weight, and even more preferably 3 to 5% by weight.
その他の成分
本発明の乳化安定化方法において、乳化組成物は、前述する成分の他に、必要に応じて、通常使用される他の添加剤が含まれていてもよい。このような添加剤としては、例えば、多価アルコール、増粘剤、pH調節剤、緩衝剤、可溶化剤、キレート剤、防腐剤、保存剤、酸化防止剤、安定化剤、香料、着色料等が挙げられる。
In the emulsion stabilization method of the present invention, the emulsion composition may contain, in addition to the above-mentioned components, other commonly used additives as necessary. Examples of such additives include polyhydric alcohols, thickeners, pH regulators, buffers, solubilizers, chelating agents, preservatives, antioxidants, stabilizers, fragrances, colorants, etc.
多価アルコールとしては、薬学的又は香粧学的に許容されることを限度として特に制限されないが、例えば、プロピレングリコール、1,3-ブチレングリコール、エチレングリコール、イソプレングリコール、ジエチレングリコール、ジプロピレングリコール等の2価アルコール;グリセリン等の3価アルコール、マクロゴール4000、マクロゴール6000等のポリエチレングリコール等が挙げられる。これらの多価アルコールは、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。これらの多価アルコールの中でも、より優れた乳化安定性を得る観点から、好ましくは2価アルコール、3価アルコールが挙げられ、より好ましくは1,3-ブチレングリコール、グリセリンが挙げられる。 The polyhydric alcohol is not particularly limited as long as it is pharma- ceutically or cosmetically acceptable, and examples thereof include dihydric alcohols such as propylene glycol, 1,3-butylene glycol, ethylene glycol, isoprene glycol, diethylene glycol, and dipropylene glycol; trihydric alcohols such as glycerin; and polyethylene glycols such as Macrogol 4000 and Macrogol 6000. These polyhydric alcohols may be used alone or in combination of two or more. Among these polyhydric alcohols, from the viewpoint of obtaining better emulsion stability, dihydric alcohols and trihydric alcohols are preferred, and 1,3-butylene glycol and glycerin are more preferred.
本発明の乳化安定化方法において、乳化組成物中に多価アルコールを含有させる場合、その含有量については、使用する多価アルコールの種類等に応じて適宜設定すればよいが、例えば1~20重量%、好ましくは5~18重量%、より好ましくは10~16重量%が挙げられる。 When a polyhydric alcohol is contained in the emulsion composition in the emulsion stabilization method of the present invention, the content may be appropriately set depending on the type of polyhydric alcohol used, and may be, for example, 1 to 20% by weight, preferably 5 to 18% by weight, and more preferably 10 to 16% by weight.
増粘剤としては、薬学的又は香粧学的に許容されることを限度として特に制限されないが、例えば、カルボキシビニルポリマー、ヒプロメロース、ポリビニルピロリドン、アルギン酸ナトリウム、エチルセルロース、カルボキシメチルセルロースナトリウム、キサンタンガム、カラギーナン等が挙げられる。これらの増粘剤の中でも、より優れた乳化安定性を得る観点から、好ましくはキサンタンガムが挙げられる。また、これらの増粘剤のうち、カルボキシビニルポリマーは、水溶性カルボン酸及び/又はその塩との共存下で極端な粘度低下を受けるため、水溶性カルボン酸及び/又はその塩を含む通常の乳化組成物に配合すると保存安定性の顕著な低下を招来するが、本発明の乳化安定化方法は、乳化組成物に保存後における優れた乳化安定性を付与することができるため、カルボキシビニルポリマーが含まれていても効果的に乳化安定性を奏することができる。このような本発明の効果に鑑みれば、本発明の乳化安定化方法における乳化組成物には増粘剤として少なくともカルボキシビニルポリマーを含んでいることが好ましい。 The thickener is not particularly limited as long as it is pharma- ceutically or cosmetically acceptable, and examples thereof include carboxyvinyl polymer, hypromellose, polyvinylpyrrolidone, sodium alginate, ethyl cellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, and the like. Among these thickeners, xanthan gum is preferred from the viewpoint of obtaining better emulsion stability. Among these thickeners, carboxyvinyl polymer undergoes an extreme viscosity reduction in the presence of water-soluble carboxylic acid and/or its salt, and therefore, when incorporated into a normal emulsion composition containing water-soluble carboxylic acid and/or its salt, it leads to a significant reduction in storage stability. However, the emulsion stabilization method of the present invention can impart excellent emulsion stability after storage to the emulsion composition, and therefore, even if the emulsion contains carboxyvinyl polymer, it can effectively achieve emulsion stability. In view of such effects of the present invention, it is preferable that the emulsion composition in the emulsion stabilization method of the present invention contains at least carboxyvinyl polymer as a thickener.
本発明の乳化安定化方法において、乳化組成物に増粘剤を含有させる場合、その含有量については、使用する増粘剤の種類等に応じて適宜設定すればよいが、より優れた乳化安定性を得る観点から、例えば0.1~2重量%、好ましくは0.1~1.8重量%、より好ましくは0.2~1.5重量%、更に好ましくは0.3~1重量%、一層好ましくは0.3~0.6重量%が挙げられる。また、本発明の乳化安定化方法において、乳化組成物にカルボキシビニルポリマーを含有させる場合、カルボキシビニルポリマーの含有量としては、例えば0.1~1重量%、好ましくは0.3~0.5重量%、より好ましくは0.35~0.45重量%が挙げられる。また、水溶性カルボン酸及び/又はその塩に対するカルボキシビニルポリマーの比率については、上記の各成分の各含有量に応じて定まるが、例えば、水溶性カルボン酸及び/又はその塩の総量1重量部当たりのカルボキシビニルポリマーの含有量として、例えば0.01~0.5重量部、好ましくは0.03~0.3重量部、より好ましくは0.06~0.2重量部が挙げられる。 In the emulsion stabilization method of the present invention, when a thickener is contained in the emulsion composition, the content of the thickener may be appropriately set depending on the type of thickener used, but from the viewpoint of obtaining better emulsion stability, the content is, for example, 0.1 to 2% by weight, preferably 0.1 to 1.8% by weight, more preferably 0.2 to 1.5% by weight, even more preferably 0.3 to 1% by weight, and even more preferably 0.3 to 0.6% by weight. In the emulsion stabilization method of the present invention, when a carboxyvinyl polymer is contained in the emulsion composition, the content of the carboxyvinyl polymer is, for example, 0.1 to 1% by weight, preferably 0.3 to 0.5% by weight, and more preferably 0.35 to 0.45% by weight. The ratio of the carboxyvinyl polymer to the water-soluble carboxylic acid and/or its salt is determined according to the content of each of the above components, but for example, the content of the carboxyvinyl polymer per 1 part by weight of the total amount of the water-soluble carboxylic acid and/or its salt is, for example, 0.01 to 0.5 parts by weight, preferably 0.03 to 0.3 parts by weight, and more preferably 0.06 to 0.2 parts by weight.
更に、本発明の乳化安定化方法において、乳化組成物は、前述する成分の他に、薬学的又は香粧学的な生理機能を発揮できる薬効成分が、必要に応じて含まれていてもよい。このような薬効成分としては、例えば、ステロイド剤(デキサメタゾン、塩酸デキサメタゾン、酢酸デキサメタゾン、塩酸ヒドロコルチゾン、吉草酸プレドニゾロン、酢酸プレドニゾロン等)、抗ヒスタミン剤(ジフェンヒドラミン、塩酸ジフェンヒドラミン、マレイン酸クロルフェニラミン等)、局所麻酔剤(リドカイン、ジブカイン、プロカイン、テトラカイン、ブピバカイン、メピバカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩)、安息香酸アルキルエステル(例えばアミノ安息香酸エチル、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル)、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチン等)、抗炎症剤(アラントイン、サリチル酸、サリチル酸グリコール、サリチル酸メチル、インドメタシン、フェルビナク、ジクロフェナクナトリウム、ロキソプロフェンナトリウム等)、殺菌剤(塩化ベンザルコニウム、塩化デカリニウム、塩化ベンゼトニウム、塩化セチルピリジニウム、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、アンモニア水、スルファジアジン、乳酸、フェノール等)、鎮痒剤(クロタミトン、チアントール等)、皮膚保護剤(コロジオン、ヒマシ油等)、血行促進成分(ノニル酸ワニリルアミド、ニコチン酸ベンジルエステル、カプサイシン、トウガラシエキス等)、ビタミン類(ビタミンA,B,C,D,E等)、ムコ多糖類(コンドロイチン硫酸ナトリウム、グルコサミン、ヒアルロン酸等)等が挙げられる。これらの薬効成分は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。また、本発明の乳化安定化方法において、乳化組成物にこれらの薬効成分を含有させる場合、その含有量については、使用する薬効成分の種類、期待する効果等に応じて適宜設定すればよい。 Furthermore, in the emulsion stabilization method of the present invention, the emulsion composition may contain, in addition to the components described above, medicinal ingredients capable of exerting pharmaceutical or cosmetic physiological functions, as necessary. Examples of such medicinal ingredients include steroids (dexamethasone, dexamethasone hydrochloride, dexamethasone acetate, hydrocortisone hydrochloride, prednisolone valerate, prednisolone acetate, etc.), antihistamines (diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, etc.), local anesthetics (lidocaine, dibucaine, procaine, tetracaine, bupivacaine, mepivacaine, chloroprocaine, proparacaine, meprylcaine, or salts thereof), alkyl benzoates (e.g., ethyl aminobenzoate, diethylaminoethyl p-butylaminobenzoate hydrochloride), orthocaine, oxethazaine, oxypolyethyleneoxydecane, scopolamine extract, percaminepase, tesit decitin, etc.), anti-inflammatory agents (arabinose, anthoin, salicylic acid, glycol salicylate, methyl salicylate, indomethacin, felbinac, diclofenac sodium, loxoprofen sodium, etc.), bactericides (benzalkonium chloride, dequalinium chloride, benzethonium chloride, cetylpyridinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, aqueous ammonia, sulfadiazine, lactic acid, phenol, etc.), antipruritic agents (crotamiton, thianthol, etc.), skin protectants (collodion, castor oil, etc.), blood circulation promoting components (vanillylamide nonylate, benzyl nicotinate, capsaicin, chili pepper extract, etc.), vitamins (vitamins A, B, C, D, E, etc.), mucopolysaccharides (sodium chondroitin sulfate, glucosamine, hyaluronic acid, etc.), etc. These medicinal components may be used alone or in combination of two or more. Furthermore, in the emulsion stabilization method of the present invention, when these medicinal ingredients are contained in the emulsion composition, the content may be appropriately set depending on the type of medicinal ingredient used, the expected effect, etc.
製剤形態・用途
本発明の乳化安定化方法において、乳化組成物の乳化タイプは、油中水型又は水中油型のいずれであってもよい。本発明の乳化安定化方法は、乳化組成物に、保存後における分離を抑制する優れた乳化安定性を備えさせることができるため、本来的に水相分離がより一層生じやすい、水中油型のような水を多く含む乳化組成物に対しても、優れた乳化安定性を備えさせることが可能になる。このような本発明の効果に鑑みれば、本発明の乳化安定化方法における乳化組成物の好ましい乳化タイプは、水の含有量が比較的多い水中油型である。
Formulation and Use In the emulsion stabilization method of the present invention, the emulsion type of the emulsion composition may be either water-in-oil type or oil-in-water type. The emulsion stabilization method of the present invention can provide the emulsion composition with excellent emulsion stability that suppresses separation after storage, so that it is possible to provide excellent emulsion stability even for emulsion compositions that contain a lot of water, such as oil-in-water type, which is inherently more prone to aqueous phase separation. In view of the effects of the present invention, the preferred emulsion type of the emulsion composition in the emulsion stabilization method of the present invention is oil-in-water type, which has a relatively high water content.
本発明の乳化安定化方法において、乳化組成物は、化粧料、外用医薬部外品、外用医薬品等の外用剤として使用することができる。本発明の乳化安定化方法におけり乳化組成物の製品形態については、特に制限されないが、例えば、クリーム剤、軟膏剤、乳液剤、ゲル剤、油剤、ローション剤、リニメント剤、エアゾール剤等が挙げられる。これらの中でも、好ましくは、クリーム剤、軟膏剤、乳液剤、ローション剤が挙げられ、より好ましくは、クリーム剤、乳液剤、ローション剤が挙げられる。 In the emulsion stabilization method of the present invention, the emulsion composition can be used as an external preparation such as a cosmetic, an external quasi-drug, or an external medicine. The product form of the emulsion composition in the emulsion stabilization method of the present invention is not particularly limited, and examples thereof include creams, ointments, emulsions, gels, oils, lotions, liniments, and aerosols. Of these, creams, ointments, emulsions, and lotions are preferred, and creams, emulsions, and lotions are more preferred.
製造方法
本発明の乳化安定化方法において、乳化組成物は、乳化タイプに応じて、公知の乳化製剤の製剤化手法に従って製造することができる。例えば、本発明の乳化安定化方法における乳化組成物の製造方法としては、含有させる成分を水溶性成分と油性成分に分けて、水溶性成分を含む水相と、油性成分を含む油相とを調製し、これらを公知の手法に従って乳化させる方法が挙げられる。
In the emulsion stabilization method of the present invention, the emulsion composition can be manufactured according to the formulation method of known emulsion preparations depending on the emulsion type.For example, the method of manufacturing the emulsion composition in the emulsion stabilization method of the present invention includes a method of dividing the components to be contained into water-soluble components and oily components, preparing an aqueous phase containing the water-soluble components and an oily phase containing the oily components, and emulsifying them according to a known method.
以下に実施例を示して本発明をより具体的に説明するが、本発明はこれらに限定されるものではない。 The present invention will be explained in more detail below with reference to examples, but the present invention is not limited to these.
試験例
表1及び2に示すに示す乳化組成物を調製した。具体的には、(B)成分を(I)の各成分の混合物に加え、70~80℃で溶解させ、油相を調製した。一方、(II)の各成分の混合物を75~85℃で溶解させ、更に(A)成分の50重量%水溶液を加え、水相を調製した。70~80℃に加温した油相に、70~80℃に加温した水相を加え、ホモミキサーを用いて撹拌して乳化し、35℃まで冷却した。これによって、乳化組成物(乳液剤;水中油型)を製造した。
Test Examples The emulsion compositions shown in Tables 1 and 2 were prepared. Specifically, component (B) was added to a mixture of each component (I) and dissolved at 70 to 80°C to prepare an oil phase. Meanwhile, a mixture of each component (II) was dissolved at 75 to 85°C, and a 50% by weight aqueous solution of component (A) was added to prepare an aqueous phase. A water phase heated to 70 to 80°C was added to an oil phase heated to 70 to 80°C, emulsified by stirring using a homomixer, and cooled to 35°C. In this way, an emulsion composition (emulsion; oil-in-water type) was produced.
得られた各乳化組成物10gを、15mLの透明プラスチックチューブに充填し、密封して、遠心分離機により3,000rpmで10分遠心した。遠心後の各乳化組成物を目視にて観察し、以下の基準に基づいて乳化安定性を評価した。結果を表1及び2に示す。
--:相分離が明確に認められ、水相の濁りの程度が少ない。
-:相分離が明確に認められ、水相の濁りの程度が大きい。
+:相分離が認められず、クリーミング傾向のみ認められる。
++:相分離が認められず、チューブの底先端部にのみ僅かなクリーミング傾向が認められる。
+++:相分離が認められず、乳化状態も均一である。
なお、クリーミング傾向とは、乳化状態の不均一状態をいい、具体的には、生成したエマルジョン中の液滴が、分散媒との比重差によって浮上又は沈降する過程にある状態をいう。
10 g of each of the obtained emulsion compositions was filled into a 15 mL transparent plastic tube, sealed, and centrifuged at 3,000 rpm for 10 minutes using a centrifuge. After centrifugation, each emulsion composition was visually observed and evaluated for emulsion stability based on the following criteria. The results are shown in Tables 1 and 2.
--: Phase separation was clearly observed, and the degree of turbidity of the aqueous phase was low.
-: Phase separation was clearly observed, and the water phase was significantly turbid.
+: No phase separation was observed, and only a creaming tendency was observed.
++: No phase separation observed, slight creaming tendency observed only at the bottom tip of the tube.
+++: No phase separation was observed and the emulsion was uniform.
The creaming tendency refers to a non-uniform emulsified state, specifically, a state in which droplets in the generated emulsion are in the process of floating up or sinking down due to the difference in specific gravity with the dispersion medium.
表2から明らかなように、ピロリドンカルボン酸ナトリウムを含まない乳化組成物では乳化状態は安定である(参考例)が、ピロリドンカルボン酸ナトリウムを含む乳化組成物では乳化状態が不安定になる(比較例1、2)ことが認められた。これに対し、表1から明らかなように、ピロリドンカルボン酸ナトリウムを含む乳化組成物に更にウフェナマートを配合することで、乳化状態が安定化した(実施例1~7)。この乳化安定性の向上効果は、特に、実施例1、4~7において顕著であった。 As is clear from Table 2, the emulsion state was stable in the emulsion composition not containing sodium pyrrolidone carboxylate (Reference Example), but the emulsion state was found to be unstable in the emulsion composition containing sodium pyrrolidone carboxylate (Comparative Examples 1 and 2). In contrast, as is clear from Table 1, the emulsion state was stabilized by further blending ufenamate with the emulsion composition containing sodium pyrrolidone carboxylate (Examples 1 to 7). This effect of improving emulsion stability was particularly noticeable in Examples 1 and 4 to 7.
処方例
表3及び4に示す処方の乳化組成物(水中油型)を調製した。いずれの乳化組成物も、ウフェナマートによって優れた乳化安定性を獲得した。
Formulation Examples Emulsion compositions (oil-in-water type) were prepared according to the formulations shown in Tables 3 and 4. All of the emulsion compositions achieved excellent emulsion stability due to the ufenamate.
Claims (3)
3. The method for emulsion stabilization according to claim 1, wherein 1.5 parts by weight or more of said ufenamate are blended per 1 part by weight of the total amount of said pyrrolidone carboxylic acid and/or its salt.
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