JP6058604B2 - Core shell structure and S / O type suspension containing the same - Google Patents
Core shell structure and S / O type suspension containing the same Download PDFInfo
- Publication number
- JP6058604B2 JP6058604B2 JP2014191274A JP2014191274A JP6058604B2 JP 6058604 B2 JP6058604 B2 JP 6058604B2 JP 2014191274 A JP2014191274 A JP 2014191274A JP 2014191274 A JP2014191274 A JP 2014191274A JP 6058604 B2 JP6058604 B2 JP 6058604B2
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- Prior art keywords
- core
- shell structure
- acid
- sucrose
- surfactant
- 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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Landscapes
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Edible Oils And Fats (AREA)
Description
本発明は、コアシェル構造体及びそれを含有するS/O型サスペンションに関する。 The present invention relates to a core-shell structure and an S / O type suspension containing the same.
コア部及びシェル部を含むコアシェル構造体、及びそれを含有するS/O型サスペンションが、例えば医薬、食品及び化粧品等の幅広い用途に用いられている。 A core-shell structure including a core part and a shell part, and an S / O suspension containing the core-shell structure are used in a wide range of applications such as medicine, food, and cosmetics.
医薬、食品及び化粧品等の用途に用いられる例として、薬物を含むコア部をシェル部が包み込む構造となっており、シェル部の作用により薬物の体内動態が制御されるもの等が挙げられる。例えば、封入物の漏洩が抑制された微細なS/O粒子が分散したS/O/Wエマルション等が提案されている(特許文献1)。また、親水性薬剤の皮膚透過性を向上させたS/O型外用剤等も提案されている(特許文献2)。 As an example used for uses such as pharmaceuticals, foods, and cosmetics, there is a structure in which a core part containing a drug is wrapped in a shell part, and the pharmacokinetics of the drug is controlled by the action of the shell part. For example, an S / O / W emulsion in which fine S / O particles with suppressed leakage of inclusions are dispersed has been proposed (Patent Document 1). In addition, an S / O-type external preparation that improves the skin permeability of a hydrophilic drug has been proposed (Patent Document 2).
本発明者らは、独自の研究により、親水性基及び疎水性基を有する化合物を含有するコア部とシェル部からなるコアシェル構造体を設計し、これを実際に製造しようとしても、従来広く使用されているシェル部の構成を採用すると、コアシェル構造体を製造することができないという問題があることを見出した。 The inventors of the present invention designed a core-shell structure composed of a core part and a shell part containing a compound having a hydrophilic group and a hydrophobic group by original research, and even when trying to actually manufacture this structure, it has been widely used in the past. It has been found that there is a problem that a core-shell structure cannot be manufactured if the configuration of the shell portion is adopted.
そこで、本発明は、親水性基及び疎水性基を有する化合物をコア部に含むコアシェル構造体を提供することを課題とする。 Then, this invention makes it a subject to provide the core-shell structure which contains the compound which has a hydrophilic group and a hydrophobic group in a core part.
本発明者らは、上記課題を解決するべく鋭意検討を重ね、融点30℃以上の界面活性剤を含有するシェル部を用いることにより、上記課題を解決できることを見出した。本発明は、かかる知見に基づいてさらなる試行錯誤を経て完成されたものであり、以下の態様を含む。
項1.
コア部及びシェル部を含むコアシェル構造体であって、
コア部が、親水性基及び疎水性基を有する化合物を、かつ
シェル部が、融点30℃以上の界面活性剤を
それぞれ含有するコアシェル構造体。
項2.
前記界面活性剤が、ショ糖脂肪酸エステルである、項1に記載のコアシェル構造体。
項3.
前記ショ糖脂肪酸エステルが、ショ糖と、炭素数8〜30の飽和又は不飽和の一価の脂肪酸とのエステルである、項2に記載のコアシェル構造体。
項4.
前記ショ糖脂肪酸エステルが、ショ糖パルミチン酸エステル、ショ糖オレイン酸エステル及びショ糖ベヘニン酸エステルからなる群より選択される少なくとも一種のショ糖脂肪酸エステルである、項2に記載のコアシェル構造体。
項5.
項1〜4のいずれか一項に記載のコアシェル構造体、及び
基剤相を含有し、
前記基剤相が前記コアシェル構造体を含有する、
S/O型サスペンション。
The inventors of the present invention have made extensive studies to solve the above problems, and have found that the above problems can be solved by using a shell portion containing a surfactant having a melting point of 30 ° C. or higher. The present invention has been completed through further trial and error based on this finding, and includes the following aspects.
Item 1.
A core shell structure including a core portion and a shell portion,
A core-shell structure in which the core part contains a compound having a hydrophilic group and a hydrophobic group, and the shell part contains a surfactant having a melting point of 30 ° C. or higher.
Item 2.
Item 2. The core-shell structure according to Item 1, wherein the surfactant is a sucrose fatty acid ester.
Item 3.
Item 3. The core-shell structure according to Item 2, wherein the sucrose fatty acid ester is an ester of sucrose and a saturated or unsaturated monovalent fatty acid having 8 to 30 carbon atoms.
Item 4.
Item 3. The core-shell structure according to Item 2, wherein the sucrose fatty acid ester is at least one sucrose fatty acid ester selected from the group consisting of sucrose palmitate, sucrose oleate, and sucrose behenate.
Item 5.
The core-shell structure according to any one of Items 1 to 4, and a base phase,
The base phase contains the core-shell structure;
S / O type suspension.
本発明によれば、親水性基及び疎水性基を有する化合物をコア部に含むコアシェル構造体を提供できる。 ADVANTAGE OF THE INVENTION According to this invention, the core shell structure which contains the compound which has a hydrophilic group and a hydrophobic group in a core part can be provided.
1. 本発明のコアシェル構造体
本発明のコアシェル構造体は、コア部が、親水性基及び疎水性基を有する化合物を、かつシェル部が、融点30℃以上の界面活性剤をそれぞれ含有する。
1. Core-shell structure of the present invention In the core- shell structure of the present invention, the core part contains a compound having a hydrophilic group and a hydrophobic group, and the shell part contains a surfactant having a melting point of 30 ° C. or higher.
本発明のコアシェル構造体は、より具体的には、シェル部の界面活性剤がコア部の一部又は全面を被覆しているコアシェル構造を有する。 More specifically, the core-shell structure of the present invention has a core-shell structure in which the surfactant in the shell part covers a part or the entire surface of the core part.
コアシェル構造体の形状やサイズは、特に限定されないが、好ましくは平均サイズが、2nm〜10μmである。 The shape and size of the core-shell structure are not particularly limited, but the average size is preferably 2 nm to 10 μm.
なお、本発明において、コアシェル構造体の平均サイズとは、溶媒分散時の動的光散乱法により、数平均径を算出したものとする。
1.1 コア部
親水性基及び疎水性基を有する化合物は、特に限定されない。
In the present invention, the average size of the core-shell structure is a number average diameter calculated by a dynamic light scattering method during solvent dispersion.
1.1 The compound having a core part hydrophilic group and a hydrophobic group is not particularly limited.
特に理論に束縛されないが、親水性基及び疎水性基を有する化合物は、界面活性剤としての作用を発揮しうる。コアシェル構造体の製造過程において、親水性基及び疎水性基を有する化合物は本来、コア部に配置されるべきところ、その界面活性剤としての特性に起因してシェル部の界面活性剤と同様の挙動を示す場合があり、この際にはコア部への配置がうまくいかず、結果的にコアシェル構造体の製造が困難になると考えられる。 Although not particularly bound by theory, a compound having a hydrophilic group and a hydrophobic group can exhibit an action as a surfactant. In the production process of the core-shell structure, the compound having a hydrophilic group and a hydrophobic group should be placed in the core part, and it is the same as the surfactant in the shell part due to its properties as a surfactant. In this case, the arrangement in the core portion may not be successful, and as a result, it may be difficult to manufacture the core-shell structure.
親水性基及び疎水性基を有する化合物は、典型的には、以下の特性(1)〜(3)の少なくとも一つを有する化合物である:
(1)分子量が、100〜10000である。
(2)水溶解度が、1%〜100%である。
(3)HLB値が、0〜7又は10〜20である。
The compound having a hydrophilic group and a hydrophobic group is typically a compound having at least one of the following characteristics (1) to (3):
(1) The molecular weight is 100 to 10,000.
(2) Water solubility is 1% to 100%.
(3) HLB value is 0-7 or 10-20.
上記において、分子量は、好ましくは、100〜5000であり、より好ましくは100〜1000である。 In the above, molecular weight becomes like this. Preferably it is 100-5000, More preferably, it is 100-1000.
上記において、水溶解度は、好ましくは、5%〜50%であり、より好ましくは10%〜50%である。 In the above, the water solubility is preferably 5% to 50%, more preferably 10% to 50%.
上記において、HLB値は、好ましくは、0〜5であり、より好ましくは0〜3である。 In the above, the HLB value is preferably 0 to 5, and more preferably 0 to 3.
なお、本発明において、水溶解度は、EPA法(EPA Chemical Fate testing Guidline CG−1500 “Water Solubility”)に基づく値とする。 In the present invention, the water solubility is a value based on the EPA method (EPA Chemical Fate Testing Guideline CG-1500 “Water Solubility”).
親水性基及び疎水性基を有する化合物の具体例としては、特に限定されないが、例えば、薬物である場合には、モンテルカスト、塩化ベンザルコニウム、デヒドロコール酸及びポリドカノール等が挙げられる。 Specific examples of the compound having a hydrophilic group and a hydrophobic group are not particularly limited, and examples thereof include montelukast, benzalkonium chloride, dehydrocholic acid, polidocanol and the like in the case of a drug.
なお、親水性基及び疎水性基を有する化合物が薬物である場合、上記の薬理学的に許容される塩も、該化合物として用いることができる。 In addition, when the compound having a hydrophilic group and a hydrophobic group is a drug, the above-described pharmacologically acceptable salt can also be used as the compound.
親水性基及び疎水性基を有する化合物の別の具体例としては、他にも、例えば、硬化剤及び/又は硬化促進剤、発泡剤、接着剤、インク、化粧料、香料等が挙げられる。 Other specific examples of the compound having a hydrophilic group and a hydrophobic group include, for example, curing agents and / or curing accelerators, foaming agents, adhesives, inks, cosmetics, and fragrances.
コアシェル構造体に含まれる、親水性基及び疎水性基を有する化合物の量は、化合物の特性にもよるが、例えば、1〜30重量%とすることができる。 The amount of the compound having a hydrophilic group and a hydrophobic group contained in the core-shell structure can be, for example, 1 to 30% by weight, depending on the characteristics of the compound.
コア部は、必要に応じて、親水性基及び疎水性基を有する化合物を二種以上含有していてもよい。 The core portion may contain two or more compounds having a hydrophilic group and a hydrophobic group as necessary.
特に限定されないが、コア部は、典型的には、親水性基及び疎水性基を有する化合物を有効成分として含むものである。この場合において、コア部は、必要に応じて、親水性基及び疎水性基の一方のみ有する化合物及び/又はこれらをいずれも有さない化合物を、別の有効成分としてさらに含有していてもよい。 Although not particularly limited, the core part typically contains a compound having a hydrophilic group and a hydrophobic group as an active ingredient. In this case, the core part may further contain a compound having only one of a hydrophilic group and a hydrophobic group and / or a compound having neither of these as another active ingredient, if necessary. .
コア部は、親水性基及び疎水性基を有する化合物に加えてさらに他の成分を少なくとも一種さらに含有していてもよい。他の成分としては、特に限定されないが、使用目的に応じて、例えば、安定化剤、防腐剤、経皮吸収促進剤、皮膚刺激低減剤、硬化剤、硬化促進剤及び発泡剤等が挙げられる。 The core part may further contain at least one other component in addition to the compound having a hydrophilic group and a hydrophobic group. Examples of other components include, but are not limited to, stabilizers, preservatives, transdermal absorption accelerators, skin irritation reducing agents, curing agents, curing accelerators, and foaming agents, depending on the purpose of use. .
安定化剤は、コアシェル構造を安定化させる作用を有し、コアシェル構造の意図せぬ早期の崩壊を防止し、親水性基及び疎水性基を有する化合物の徐放効果を担保する役割を有する。 The stabilizer has a function of stabilizing the core-shell structure, prevents unintended early collapse of the core-shell structure, and ensures the sustained release effect of the compound having a hydrophilic group and a hydrophobic group.
安定化剤としては、特に限定されないが、具体的には、多糖類、タンパク質、及び親水性高分子材料等が挙げられる。安定化剤のコア部における含有量は、その種類にもより、適宜設定できるが、例えば、親水性基及び疎水性基を有する化合物と安定化剤の重量比が、1:0.1〜1:10となるように配合することもできる。 The stabilizer is not particularly limited, and specific examples include polysaccharides, proteins, and hydrophilic polymer materials. The content of the stabilizer in the core portion can be appropriately set depending on the type of the stabilizer. For example, the weight ratio of the compound having a hydrophilic group and a hydrophobic group to the stabilizer is from 1: 0.1 to 1. : It can also mix | blend so that it may be set to 10.
防腐剤としては、特に限定されないが、具体的には、パラオキシ安息香酸メチル、パラオキシ安息香酸プロピル、フェノキシエタノール及びチモール等が挙げられる。防腐剤のコア部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.01%〜10%となるように配合することもできる。防腐剤は、1種又は2種以上を含有してもよい。 The preservative is not particularly limited, and specific examples include methyl paraoxybenzoate, propyl paraoxybenzoate, phenoxyethanol and thymol. Although the content rate in the core part of an antiseptic | preservative can be set suitably also with the kind, For example, it can also mix | blend so that it may become 0.01%-10%. An antiseptic | preservative may contain 1 type (s) or 2 or more types.
経皮吸収促進剤としては、特に限定されないが、具体的には、高級アルコール、N−アシルサルコシン及びその塩、高級モノカルボン酸、高級モノカルボン酸エステル、芳香族モノテルペン脂肪酸エステル、炭素数2〜10の2価カルボン酸及びその塩、ポリオキシエチレンアルキルエーテルリン酸エステル及びその塩、乳酸、乳酸エステル、並びにクエン酸等が挙げられる。経皮吸収促進剤は、1種又は2種以上を含有してもよい。経皮吸収促進剤のコア部における含有量は、その種類にもより、適宜設定できるが、例えば、親水性基及び疎水性基を有する化合物と経皮吸収促進剤の重量比が、1:0.01〜1:50となるように配合することもできる。 Although it does not specifically limit as a percutaneous absorption enhancer, Specifically, higher alcohol, N-acyl sarcosine and its salt, higher monocarboxylic acid, higher monocarboxylic acid ester, aromatic monoterpene fatty acid ester, carbon number 2 To 10 divalent carboxylic acids and salts thereof, polyoxyethylene alkyl ether phosphates and salts thereof, lactic acid, lactic acid esters, and citric acid. The percutaneous absorption enhancer may contain one kind or two or more kinds. The content of the percutaneous absorption enhancer in the core can be appropriately set depending on the type of the percutaneous absorption enhancer. For example, the weight ratio of the compound having a hydrophilic group and a hydrophobic group to the transdermal absorption enhancer is 1: 0. .01 to 1:50 can also be blended.
皮膚刺激低減剤としては、特に限定されないが、具体的には、ハイドロキノン配糖体、パンテチン、トラネキサム酸、レシチン、酸化チタン、水酸化アルミニウム、亜硝酸ナトリウム、亜硝酸水素ナトリウム、大豆レシチン、メチオニン、グリチルレチン酸、BHT、BHA、ビタミンE及びその誘導体、ビタミンC及びその誘導体、ベンゾトリアゾール、没食子酸プロピル、並びにメルカプトベンズイミダゾール等が挙げられる。皮膚刺激低減剤は、1種又は2種以上を含有してもよい。皮膚刺激低減剤のコア部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.1%〜50%となるように配合することもできる。 The skin irritation reducing agent is not particularly limited. Specifically, hydroquinone glycoside, pantethine, tranexamic acid, lecithin, titanium oxide, aluminum hydroxide, sodium nitrite, sodium hydrogen nitrite, soybean lecithin, methionine, Examples include glycyrrhetinic acid, BHT, BHA, vitamin E and derivatives thereof, vitamin C and derivatives thereof, benzotriazole, propyl gallate, and mercaptobenzimidazole. The skin irritation reducing agent may contain one kind or two or more kinds. Although the content rate in the core part of a skin irritation reducing agent can be suitably set according to the kind, it can also mix | blend, for example so that it may be 0.1%-50%.
1.2 シェル部
シェル部は、融点30℃以上の界面活性剤を含有する。
1.2 Shell Part The shell part contains a surfactant having a melting point of 30 ° C. or higher.
上記界面活性剤は、コアシェル構造のシェル部を形成できるものであればよく、特に限定されない。 The surfactant is not particularly limited as long as it can form a shell part having a core-shell structure.
シェル部は、複数種の界面活性剤を併用してもよい。このとき、シェル部は、界面活性剤として、融点30℃以上の界面活性剤のみを複数種含んでいてもよいし、融点30℃以上の界面活性剤に加えてさらに融点が30℃未満の界面活性剤を一種又は二種以上含んでいてもよい。 The shell portion may use a plurality of types of surfactants in combination. At this time, the shell portion may contain only a plurality of surfactants having a melting point of 30 ° C. or higher as the surfactant, or an interface having a melting point of less than 30 ° C. in addition to the surfactant having a melting point of 30 ° C. or higher. One or more activators may be included.
シェル部が、融点30℃以上の界面活性剤に加えてさらに融点が30℃未満の界面活性剤を含む場合、前者の比率が、界面活性剤の総量に対して0.5重量%〜20重量%、好ましくは1重量%〜10重量%となるようにすることができる。 When the shell portion contains a surfactant having a melting point of 30 ° C. or higher and a surfactant having a melting point of less than 30 ° C., the former ratio is 0.5 wt% to 20 wt% with respect to the total amount of the surfactant. %, Preferably 1 to 10% by weight.
特に限定されないが、コアシェル構造体を製造する際、後述のように、界面活性剤を含むシェル部成分を、シクロヘキサン、ヘキサン又はトルエン等の溶剤に溶解した溶液を使用する場合には、シェル部成分が、融点30℃以上の界面活性剤に加えてさらに融点が30℃未満の界面活性剤を含んでいると、界面活性剤が溶剤に溶解しやすくなるので、有利である。 Although not particularly limited, when producing a core-shell structure, as described later, when using a solution in which a shell part component containing a surfactant is dissolved in a solvent such as cyclohexane, hexane, or toluene, the shell part component is used. However, if a surfactant having a melting point of less than 30 ° C. is further contained in addition to the surfactant having a melting point of 30 ° C. or higher, it is advantageous because the surfactant is easily dissolved in the solvent.
融点30℃以上の界面活性剤としては、特に限定されないが、具体例として、ショ糖脂肪酸エステル等が挙げられる。 The surfactant having a melting point of 30 ° C. or higher is not particularly limited, and specific examples include sucrose fatty acid esters.
上記ショ糖脂肪酸エステルとしては、特に限定されないが、好ましくはショ糖と、炭素数8〜30の飽和又は不飽和の一価の脂肪酸とのエステルが挙げられる。 Although it does not specifically limit as said sucrose fatty acid ester, Preferably ester with sucrose and a C8-C30 saturated or unsaturated monovalent fatty acid is mentioned.
上記ショ糖脂肪酸エステルの具体例として、特に限定されないが、好ましくはショ糖パルミチン酸エステル、ショ糖オレイン酸エステル及びショ糖ベヘニン酸エステル等が挙げられる。 Although it does not specifically limit as a specific example of the said sucrose fatty acid ester, Preferably sucrose palmitic acid ester, sucrose oleic acid ester, sucrose behenic acid ester, etc. are mentioned.
ショ糖脂肪酸エステルとして、複数種のショ糖脂肪酸エステルを併用してもよい。 A plurality of sucrose fatty acid esters may be used in combination as the sucrose fatty acid ester.
融点30℃以上の界面活性剤として、特に限定されないが、好ましくはHLB値が7以下、さらに好ましくは5以下のものを用いることができる。 The surfactant having a melting point of 30 ° C. or higher is not particularly limited, but those having an HLB value of preferably 7 or less, more preferably 5 or less can be used.
界面活性剤総量の配合量は、本発明の効果が奏される範囲内において適宜設定することができるが、例えば、コア部に含まれる、親水性基及び疎水性基を有する化合物との重量比を1:5〜1:100とすることができる。 The blending amount of the total amount of the surfactant can be appropriately set within the range in which the effect of the present invention is exerted. For example, the weight ratio with the compound having a hydrophilic group and a hydrophobic group contained in the core part Can be 1: 5 to 1: 100.
シェル部は、界面活性剤に加えてさらに他の成分を少なくとも一種さらに含有していてもよい。他の成分としては、特に限定されないが、使用目的に応じて、例えば、安定化剤、防腐剤、皮膚刺激低減剤、鎮痛剤、経皮吸収促進剤、分散剤及び粘度調製剤等が挙げられる。 The shell portion may further contain at least one other component in addition to the surfactant. Examples of other components include, but are not limited to, stabilizers, preservatives, skin irritation reducing agents, analgesics, percutaneous absorption enhancers, dispersants, viscosity adjusting agents, and the like, depending on the purpose of use. .
安定化剤は、コアシェル構造を安定化させる作用を有し、コアシェル構造の意図せぬ早期の崩壊を防止し、さらに必要に応じて、コア部に含まれる成分の徐放効果を担保する役割を有する。 The stabilizer acts to stabilize the core-shell structure, prevents unintended early collapse of the core-shell structure, and further ensures the sustained release effect of the components contained in the core part as necessary. Have.
安定化剤としては、特に限定されないが、具体的には、脂肪酸及びその塩、メチルパラベン,プロピルパラペン等のパラヒドロキシ安息香酸エステル類、クロロブタノール、ペンジルアルコール,フェニルエチルアルコール等のアルコール類、チメロサール、無水酢酸、ソルビン酸、亜硫酸水素ナトリウム、L−アスコルビン酸、アスコルビン酸ナトリウム、ブチルヒドロキシアニソール、プチルヒドロキシトルエン、没食子酸プロピル、酢酸トコフェロール、dl−α−トコフェロール、タンパク質及び多糖類等が挙げられる。安定化剤は、1種又は2種以上を含有してもよい。安定化剤のシェル部における含有量は、その種類にもより、適宜設定できるが、例えば、界面活性剤の総量と安定化剤の重量比が、1:0.01〜1:50となるように配合することもできる。 The stabilizer is not particularly limited, and specifically, fatty acids and salts thereof, parahydroxybenzoates such as methylparaben and propylparapen, alcohols such as chlorobutanol, pendyl alcohol, and phenylethyl alcohol, thimerosal , Acetic anhydride, sorbic acid, sodium bisulfite, L-ascorbic acid, sodium ascorbate, butylhydroxyanisole, butylhydroxytoluene, propyl gallate, tocopherol acetate, dl-α-tocopherol, protein and polysaccharides. A stabilizer may contain 1 type, or 2 or more types. The content of the stabilizer in the shell portion can be appropriately set depending on the type of the stabilizer, but for example, the weight ratio of the total amount of the surfactant and the stabilizer is 1: 0.01 to 1:50. It can also be blended.
防腐剤としては、特に限定されないが、具体的には、パラオキシ安息香酸メチル、パラオキシ安息香酸プロピル、フェノキシエタノール及びチモール等が挙げられる。防腐剤は、1種又は2種以上を含有してもよい。防腐剤のシェル部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.01%〜10%となるように配合することもできる。 The preservative is not particularly limited, and specific examples include methyl paraoxybenzoate, propyl paraoxybenzoate, phenoxyethanol and thymol. An antiseptic | preservative may contain 1 type (s) or 2 or more types. Although the content rate in the shell part of an antiseptic | preservative can be suitably set according to the kind, it can also mix | blend, for example so that it may become 0.01%-10%.
皮膚刺激低減剤としては、特に限定されないが、具体的には、ハイドロキノン配糖体、パンテチン、トラネキサム酸、レシチン、酸化チタン、水酸化アルミニウム、亜硝酸ナトリウム、亜硝酸水素ナトリウム、大豆レシチン、メチオニン、グリチルレチン酸、BHT、BHA、ビタミンE及びその誘導体、ビタミンC及びその誘導体、ベンゾトリアゾール、没食子酸プロピル、並びにメルカプトベンズイミダゾール等が挙げられる。皮膚刺激低減剤は、1種又は2種以上を含有してもよい。皮膚刺激低減剤のシェル部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.1%〜50%となるように配合することもできる。 The skin irritation reducing agent is not particularly limited. Specifically, hydroquinone glycoside, pantethine, tranexamic acid, lecithin, titanium oxide, aluminum hydroxide, sodium nitrite, sodium hydrogen nitrite, soybean lecithin, methionine, Examples include glycyrrhetinic acid, BHT, BHA, vitamin E and derivatives thereof, vitamin C and derivatives thereof, benzotriazole, propyl gallate, and mercaptobenzimidazole. The skin irritation reducing agent may contain one kind or two or more kinds. Although the content rate in the shell part of a skin irritation reducing agent can be suitably set according to the kind, it can also mix | blend, for example so that it may be 0.1%-50%.
鎮痛剤としては、特に限定されないが、具体的には、プロカイン、テトラカイン、リドカイン、ジブカイン及びプリロカイン等の局所麻酔薬及びその塩等が挙げられる。鎮痛剤は、1種又は2種以上を含有してもよい。鎮痛剤のシェル部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.1%〜30%となるように配合することもできる。 Although it does not specifically limit as an analgesic, Specifically, local anesthetics, such as procaine, tetracaine, lidocaine, dibucaine, and prilocaine, its salt, etc. are mentioned. An analgesic may contain 1 type (s) or 2 or more types. Although the content rate in the shell part of an analgesic can be suitably set according to the kind, it can also mix | blend so that it may be 0.1%-30%, for example.
経皮吸収促進剤としては、特に限定されないが、具体的には、高級アルコール、N−アシルサルコシン及びその塩、高級モノカルボン酸、高級モノカルボン酸エステル、芳香族モノテルペン脂肪酸エステル、炭素数2〜10の2価カルボン酸及びその塩、ポリオキシエチレンアルキルエーテルリン酸エステル及びその塩、乳酸、乳酸エステル、並びにクエン酸等が挙げられる。経皮吸収促進剤は、1種又は2種以上を含有してもよい。経皮吸収促進剤のシェル部における含有割合は、その種類にもより、適宜設定できるが、例えば、0.1%〜30%となるように配合することもできる。 Although it does not specifically limit as a percutaneous absorption enhancer, Specifically, higher alcohol, N-acyl sarcosine and its salt, higher monocarboxylic acid, higher monocarboxylic acid ester, aromatic monoterpene fatty acid ester, carbon number 2 To 10 divalent carboxylic acids and salts thereof, polyoxyethylene alkyl ether phosphates and salts thereof, lactic acid, lactic acid esters, and citric acid. The percutaneous absorption enhancer may contain one kind or two or more kinds. Although the content rate in the shell part of a percutaneous absorption enhancer can be suitably set according to the kind, it can also mix | blend so that it may be set to 0.1%-30%, for example.
2. 本発明のS/O型サスペンション
本発明のS/O型サスペンションは、基剤相を含有し、
該基剤相が前記コアシェル構造体を含有する、
S/O型サスペンションである。
2. S / O type suspension of the present invention The S / O type suspension of the present invention contains a base phase,
The base phase contains the core-shell structure;
This is an S / O type suspension.
2.1 基剤相
基剤相とは、基剤を含有する相であり、該S/O型サスペンションにおいて、前記コアシェル構造体は、前記基剤相中に分散又は溶解している。
2.1 Base Phase The base phase is a phase containing a base, and in the S / O suspension, the core shell structure is dispersed or dissolved in the base phase.
基剤は、コアシェル構造体を分散又は溶解させるのに適切なものの中から使用目的等に応じて適宜選択することができ、特に限定されない。 The base can be appropriately selected from those suitable for dispersing or dissolving the core-shell structure according to the purpose of use and the like, and is not particularly limited.
また、複数種の基剤を併用してもよい。 A plurality of types of bases may be used in combination.
基剤としては、特に限定されないが、例えば、植物油、動物油、中性脂質、合成油脂、ステロール誘導体、ワックス類、炭化水素類、モノアルコールカルボン酸エステル類、オキシ酸エステル類、多価アルコール脂肪酸エステル類、シリコーン類、高級(多価)アルコール類、高級脂肪酸類及びフッ素系油剤類等が挙げられる。 The base is not particularly limited. For example, vegetable oils, animal oils, neutral lipids, synthetic fats and oils, sterol derivatives, waxes, hydrocarbons, monoalcohol carboxylates, oxyacid esters, polyhydric alcohol fatty acid esters , Silicones, higher (polyhydric) alcohols, higher fatty acids and fluorinated oils.
植物油としては、特に限定されないが、例えば、大豆油、ゴマ油、オリーブ油、やし油、バーム油、こめ油、綿実油、ひまわり油、コメヌカ油、カカオ脂、コーン油、べに花油及びなたね油等が挙げられる。 The vegetable oil is not particularly limited, and examples thereof include soybean oil, sesame oil, olive oil, palm oil, balm oil, rice bran oil, cottonseed oil, sunflower oil, rice bran oil, cacao butter, corn oil, bean flower oil and rapeseed oil. .
動物油としては、特に限定されないが、例えば、ミンク油、タートル油、魚油、牛油、馬油、豚油及び鮫スクワラン等が挙げられる。 Although it does not specifically limit as animal oil, For example, mink oil, turtle oil, fish oil, cow oil, horse oil, pig oil, shark squalane, etc. are mentioned.
中性脂質としては、特に限定されないが、例えば、トリオレイン、トリリノレイン、トリミリスチン、トリステアリン及びトリアラキドニン等が挙げられる。 The neutral lipid is not particularly limited, and examples thereof include triolein, trilinolein, trimyristin, tristearin, and triarachidonin.
合成油脂としては、特に限定されないが、例えば、リン脂質及びアゾン等が挙げられる。 Although it does not specifically limit as synthetic fats and oils, For example, a phospholipid, an azone, etc. are mentioned.
ステロール誘導体としては、としては、特に限定されないが、例えば、ジヒドロコレステロール、ラノステロール、ジヒドロラノステロール、フィトステロール、コール酸及びコレステリルリノレート等が挙げられる。 The sterol derivative is not particularly limited, and examples thereof include dihydrocholesterol, lanosterol, dihydrolanosterol, phytosterol, cholic acid, and cholesteryl linoleate.
ワックス類としては、キャンデリラワックス、カルナウバワックス、ライスワックス、木ろう、みつろう、モンタンワックス、オゾケライト、セレシン、パラフィンワックス、マイクロクリスタリンワックス、ペトロラタム、フィッシャートロプシュワックス、ポリエチレンワックス及びエチレン・プロピレンコポリマー等が挙げられる。 Examples of waxes include candelilla wax, carnauba wax, rice wax, beeswax, beeswax, montan wax, ozokerite, ceresin, paraffin wax, microcrystalline wax, petrolatum, Fischer-Tropsch wax, polyethylene wax, and ethylene / propylene copolymer. Can be mentioned.
炭化水素類としては、流動パラフィン(ミネラルオイル)、重質流動イソパラフィン、軽質流動イソパラフィン、α−オレフィンオリゴマー、ポリイソブテン、水添ポリイソブテン、ポリブテン、スクワラン、オリーブ由来スクワラン、スクワレン、ワセリン及び固形パラフィン等が挙げられる。 Examples of hydrocarbons include liquid paraffin (mineral oil), heavy liquid isoparaffin, light liquid isoparaffin, α-olefin oligomer, polyisobutene, hydrogenated polyisobutene, polybutene, squalane, olive-derived squalane, squalene, petrolatum and solid paraffin. It is done.
モノアルコールカルボン酸エステル類としては、ミリスチン酸オクチルドデシル、ミリスチン酸ヘキシルデシル、イソステアリン酸オクチルドデシル、パリミチン酸セチル、パルミチン酸オクチルドデシル、オクタン酸セチル、オクタン酸ヘキシルデシル、イソノナン酸イソトリデシル、イソノナン酸イソノニル、イソノナン酸オクチル、イソノナン酸イソトリデシル、ネオペンタン酸イソデシル、ネオペンタン酸イソトリデシル、ネオペンタン酸イソステアリル、ネオデカン酸オクチルドデシル、オレイン酸オレイル、オレイン酸オクチルドデシル、リシノレイン酸オクチルドデシル、ラノリン脂肪酸オクチルドデシル、ジメチルオクタン酸ヘキシルデシル、エルカ酸オクチルドデシル、イソステアリン酸硬化ヒマシ油、オレイン酸エチル、アボカド油脂肪酸エチル、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、パルミチン酸オクチル、イソステアリン酸イソプロピル、ラノリン脂肪酸イソプロピル、セバチン酸ジエチル、セバチン酸ジイソプロピル、セバチン酸ジオクチル、アジピン酸ジイソプロピル、セバチン酸ジブチルオクチル、アジピン酸ジイソブチル、コハク酸ジオクチル及びクエン酸トリエチル等が挙げられる。 Examples of monoalcohol carboxylic acid esters include octyldodecyl myristate, hexyldecyl myristate, octyldodecyl isostearate, cetyl palmitate, octyldodecyl palmitate, cetyl octoate, hexyldecyl octoate, isotridecyl isononanoate, isononanoyl isononanoate, Octyl isononanoate, isotridecyl isononanoate, isodecyl neopentanoate, isotridecyl neopentanoate, isostearyl neopentanoate, octyldodecyl neodecanoate, oleyl oleate, octyl dodecyl oleate, octyldodecyl ricinoleate, octyldodecyl lanolinate, hexyldecyl dimethyloctanoate , Octyldodecyl erucate, isostearic acid hydrogenated castor oil, ethyl oleate Avocado oil fatty acid ethyl, isopropyl myristate, isopropyl palmitate, octyl palmitate, isopropyl isostearate, isopropyl lanolin fatty acid, diethyl sebacate, diisopropyl sebacate, dioctyl sebacate, diisopropyl adipate, dibutyloctyl sebacate, diisobutyl adipate, Examples include dioctyl succinate and triethyl citrate.
オキシ酸エステル類としては、乳酸セチル、リンゴ酸ジイソステアリル及びモノイソステアリン酸水添ヒマシ油等が挙げられる。 Examples of oxyesters include cetyl lactate, diisostearyl malate, and hydrogenated castor oil monoisostearate.
多価アルコール脂肪酸エステル類としては、トリオクタン酸グリセリル、トリオレイン酸グリセリル、トリイソステアリン酸グリセリル、ジイソステアリン酸グリセリル、トリ(カプリル酸/カプリン酸)グリセリル、トリ(カプリル酸/カプリン酸/ミリスチン酸/ステアリン酸)グリセリル、水添ロジントリグリセリド(水素添加エステルガム)、ロジントリグリセリド(エステルガム)、ベヘン酸エイコサン二酸グリセリル、トリオクタン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、ジオクタン酸ネオペンチルグリコール、ジカプリン酸ネオペンチルグリコール、ジオクタン酸2−ブチル−2−エチル−1,3−プロパンジオール、ジオレイン酸プロピレングリコール、テトラオクタン酸ペンタエリスリチル、水素添加ロジンペンタエリスリチル、トリエチルヘキサン酸ジトリメチロールプロパン、(イソステアリン酸/セバシン酸)ジトリメチロールプロパン、トリエチルヘキサン酸ペンタエリスリチル、(ヒドロキシステアリン酸/ステアリン酸/ロジン酸)ジペンタエリスリチル、ジイソステアリン酸ジグリセリル、テトライソステアリン酸ポリグリセリル、ノナイソステアリン酸ポリグリセリル−10、デカ(エルカ酸/イソステアリン酸/リシノレイン酸)ポリグリセリル−8、(ヘキシルデカン酸/セバシン酸)ジグリセリルオリゴエステル、ジステアリン酸グリコール(ジステアリン酸エチレングリコール)、ジネオペンタン酸3−メチル−1,5−ペンタンジオール及びジネオペンタン酸2,4−ジエチル−1,5−ペンタンジオール等が挙げられる。 Polyhydric alcohol fatty acid esters include glyceryl trioctanoate, glyceryl trioleate, glyceryl triisostearate, glyceryl diisostearate, glyceryl tri (caprylic acid / capric acid), tri (caprylic acid / capric acid / myristic acid / stearic acid) ) Glyceryl, hydrogenated rosin triglyceride (hydrogenated ester gum), rosin triglyceride (ester gum), glyceryl behenate, trimethylolpropane trioctanoate, trimethylolpropane triisostearate, neopentylglycol dioctanoate, neopentyl glycol dicaprate Pentyl glycol, 2-butyl-2-ethyl-1,3-propanediol dioctanoate, propylene glycol dioleate, pentaerythrtetraoctanoate Chill, hydrogenated rosin pentaerythrityl, triethylhexanoic acid ditrimethylolpropane, (isostearic acid / sebacic acid) ditrimethylolpropane, triethylhexanoic acid pentaerythrityl, (hydroxystearic acid / stearic acid / rosinic acid) dipentaerythrityl, diisostearic acid di Glyceryl, polyglyceryl tetraisostearate, polyglyceryl-10 nonaisostearate, deca (erucic acid / isostearic acid / ricinoleic acid) polyglyceryl-8, (hexyldecanoic acid / sebacic acid) diglyceryl oligoester, glycol distearate (ethylene glycol distearate) Dineopentanoic acid 3-methyl-1,5-pentanediol and dineopentanoic acid 2,4-diethyl-1,5-penta Diol, and the like.
シリコーン類としては、ジメチコン(ジメチルポリシロキサン)、高重合ジメチコン(高重合ジメチルポリシロキサン)、シクロメチコン(環状ジメチルシロキサン、デカメチルシクロペンタシロキサン)、フェニルトリメチコン、ジフェニルジメチコン、フェニルジメチコン、ステアロキシプロピルジメチルアミン、(アミノエチルアミノプロピルメチコン/ジメチコン)コポリマー、ジメチコノール、ジメチコノールクロスポリマー、シリコーン樹脂、シリコーンゴム、アミノプロピルジメチコン又はアモジメチコン等のアミノ変性シリコーン、カチオン変性シリコーン、ジメチコンコポリオール等のポリエーテル変性シリコーン、ポリグリセリン変性シリコーン、糖変性シリコーン、カルボン酸変性シリコーン、リン酸変性シリコーン、硫酸変性シリコーン、アルキル変性シリコーン、脂肪酸変性シリコーン、アルキルエーテル変性シリコーン、アミノ酸変性シリコーン、ペプチド変性シリコーン、フッ素変性シリコーン、カチオン変性又はポリエーテル変性シリコーン、アミノ変性又はポリエーテル変性シリコーン、アルキル変性又はポリエーテル変性シリコーン及びポリシロキサン・オキシアルキレン共重合体等が挙げられる。 Silicones include dimethicone (dimethylpolysiloxane), highly polymerized dimethicone (highly polymerized dimethylpolysiloxane), cyclomethicone (cyclic dimethylsiloxane, decamethylcyclopentasiloxane), phenyltrimethicone, diphenyldimethicone, phenyldimethicone, stearoxypropyl. Dimethylamine, (aminoethylaminopropylmethicone / dimethicone) copolymer, dimethiconol, dimethiconol crosspolymer, silicone resin, silicone rubber, amino-modified silicone such as aminopropyldimethicone or amodimethicone, cation-modified silicone, polyether modified such as dimethicone copolyol Silicone, polyglycerin modified silicone, sugar modified silicone, carboxylic acid modified silicone, phosphoric acid modified silicone Sulfuric acid modified silicone, alkyl modified silicone, fatty acid modified silicone, alkyl ether modified silicone, amino acid modified silicone, peptide modified silicone, fluorine modified silicone, cationic modified or polyether modified silicone, amino modified or polyether modified silicone, alkyl modified or polyether Examples thereof include modified silicones and polysiloxane / oxyalkylene copolymers.
高級(多価)アルコール類としては、セタノール、ミリスチルアルコール、オレイルアルコール、ラウリルアルコール、セトステアリルアルコール、ステアリルアルコール、アラキルアルコール、ベヘニルアルコール、ホホバアルコール、キミルアルコール、セラキルアルコール、バチルアルコール、ヘキシルデカノール、イソステアリルアルコール、2−オクチルドデカノール及びダイマージオール等が挙げられる。 Higher (polyhydric) alcohols include cetanol, myristyl alcohol, oleyl alcohol, lauryl alcohol, cetostearyl alcohol, stearyl alcohol, aralkyl alcohol, behenyl alcohol, jojoba alcohol, chimyl alcohol, seraalkyl alcohol, batyl alcohol, hexyl decanol, Examples include isostearyl alcohol, 2-octyldodecanol, and dimer diol.
高級脂肪酸類としては、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、ベヘン酸、ウンデシレン酸、12−ヒドロキシステアリン酸、パルミトレイン酸、オレイン酸、リノール酸、リノレイン酸、エルカ酸、ドコサヘキサエン酸、エイコサペンタエン酸、イソヘキサデカン酸、アンテイソヘンイコサン酸、長鎖分岐脂肪酸、ダイマー酸及び水素添加ダイマー酸等が挙げられる。 Higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, behenic acid, undecylenic acid, 12-hydroxystearic acid, palmitoleic acid, oleic acid, linoleic acid, linolenic acid, erucic acid, docosahexaenoic acid Eicosapentaenoic acid, isohexadecanoic acid, anteisohenicosanoic acid, long-chain branched fatty acid, dimer acid and hydrogenated dimer acid.
フッ素系油剤類としては、パーフルオロデカン、パーフルオロオクタン及びパーフルオロポリエーテル等が挙げられる。 Examples of the fluorinated oils include perfluorodecane, perfluorooctane and perfluoropolyether.
また、その他の基剤としては、特に限定されないが、軟膏剤、クリーム剤、エアゾール剤、テープ剤、パッチ剤、パップ剤、ゲル剤又はマイクロニードル等に使用される基剤等が挙げられる。 Other bases are not particularly limited, and examples include bases used in ointments, creams, aerosols, tapes, patches, poultices, gels, microneedles, and the like.
2.2 その他の添加成分
本発明のS/O型サスペンションは、その剤形や使用目的等に応じて、その他の添加成分を含有していてもよい。
2.2 Other Additive Components The S / O suspension of the present invention may contain other additive components depending on the dosage form, purpose of use, and the like.
添加成分としては、特に限定されないが、使用目的に応じて、賦形剤、着色剤、滑沢剤、結合剤、乳化剤、増粘剤、湿潤剤、安定剤、保存剤、溶剤、溶解補助剤、懸濁化剤、緩衝剤、pH調整剤、ゲル化剤、粘着剤、酸化防止剤、経皮吸収促進剤、刺激緩和剤、防腐剤、キレート剤及び分散剤等の中から適宜選択することができる。 The additive component is not particularly limited, but depending on the purpose of use, excipient, colorant, lubricant, binder, emulsifier, thickener, wetting agent, stabilizer, preservative, solvent, solubilizer , Suspending agent, buffering agent, pH adjusting agent, gelling agent, pressure-sensitive adhesive, antioxidant, transdermal absorption enhancer, irritation relaxation agent, preservative, chelating agent, dispersing agent, etc. Can do.
2.3 本発明のコアシェル構造及び本発明のS/O型サスペンションの製造方法
本発明のコアシェル構造及び本発明のS/O型サスペンションは、特に限定されないが、例えば以下のようにして製造することができる。
2.3 Manufacturing method of the core-shell structure of the present invention and the S / O type suspension of the present invention The core-shell structure of the present invention and the S / O type suspension of the present invention are not particularly limited. For example, they are manufactured as follows. Can do.
まず、特に限定されないが、本発明のコアシェル構造体を、例えば以下のようにして製造することができる。親水性基及び疎水性基を有する化合物並びに所望により添加成分を純水又はリン酸緩衝液等の溶媒に溶解する。これに、界面活性剤並びに所望により添加成分を、シクロヘキサン、ヘキサン又はトルエン等の溶剤に溶解した溶液を加え、ホモジナイザー撹拌する。その後に凍結乾燥することによって本発明のコアシェル構造体を調製できる。 First, although not particularly limited, the core-shell structure of the present invention can be produced, for example, as follows. The compound having a hydrophilic group and a hydrophobic group and, if desired, the additive component are dissolved in a solvent such as pure water or a phosphate buffer. To this, a solution in which the surfactant and optionally added components are dissolved in a solvent such as cyclohexane, hexane, or toluene is added and stirred with a homogenizer. Thereafter, the core-shell structure of the present invention can be prepared by lyophilization.
2.4 本発明のS/O型サスペンションの用途
本発明のS/O型サスペンションは、特に限定されないが、例えば、外用剤、接着剤、塗料、化粧料及び香料等の用途に使用できる。
2.4 Application of the S / O Type Suspension of the Present Invention The S / O type suspension of the present invention is not particularly limited, but can be used for applications such as external preparations, adhesives, paints, cosmetics and fragrances.
外用剤としては、特に限定されないが、例えば、テープ剤、軟膏剤、ローション剤、エアゾール剤、硬膏剤、水性バップ剤、クリーム剤、テープ剤、ゲル剤、エアゾール剤、パッチ剤及びマイクロニードル等として使用できる。 Although it does not specifically limit as an external preparation, For example, as a tape agent, an ointment, a lotion agent, an aerosol agent, a plaster agent, an aqueous batting agent, a cream agent, a tape agent, a gel agent, an aerosol agent, a patch agent, a microneedle, etc. Can be used.
接着剤としては、特に限定されないが、例えば、熱硬化型接着剤及びシール剤等として使用できる。 Although it does not specifically limit as an adhesive agent, For example, it can use as a thermosetting type adhesive agent, a sealing agent, etc.
以下、本発明を実施例及び試験例を例に挙げて詳しく説明するが、本発明がこれらの例に限定されるものではない。 Hereinafter, the present invention will be described in detail by way of examples and test examples, but the present invention is not limited to these examples.
実施例1
モンテルカストナトリウム0.1gを40gの純水に溶解し、これに、ショ糖エルカ酸エステル(三菱化学フーズ社製、ER−290、融点4.0℃、HLB2、主成分はジエステル及びトリエステル)1.0g及びショ糖ステアリン酸エステル(三菱化学フーズ社製、S−070、融点61.5℃、HLB1以下、主成分はジエステル及びトリエステル)1.0gをシクロヘキサン80gに溶解した溶液を加え、ホモジナイザー(ポリトロン社製、PT3100型)を用いて25℃でホモジナイザー攪拌(10000rpm、2分)した。この後に凍結乾燥装置(東京理化器械社製、FDU1100型)で2日間凍結乾燥することによって、コアシェル構造体を調製した。当該生成物3.0gを17.0gのミリスチン酸イソプロピルに加え、サスペンションを得た。
Example 1
Montelukast sodium (0.1 g) is dissolved in 40 g of pure water, and sucrose erucic acid ester (manufactured by Mitsubishi Chemical Foods, ER-290, melting point: 4.0 ° C., HLB2, main components are diester and triester) 1 0.0 g and sucrose stearate (S-070, manufactured by Mitsubishi Chemical Foods Co., Ltd., melting point 61.5 ° C., HLB1 or less, main components are diester and triester) are added to a solution of 80 g of cyclohexane and a homogenizer is added. A homogenizer was stirred (10000 rpm, 2 minutes) at 25 ° C. using a Polytron Corp. PT3100 type. Thereafter, the core-shell structure was prepared by freeze-drying for 2 days using a freeze-drying apparatus (FDU1100, manufactured by Tokyo Rika Kikai Co., Ltd.). 3.0 g of the product was added to 17.0 g of isopropyl myristate to obtain a suspension.
実施例2
ショ糖エルカ酸エステルの量を2.0gにしたこと以外は実施例1と同様にして、サスペンションを得た。
Example 2
A suspension was obtained in the same manner as in Example 1 except that the amount of sucrose erucic acid ester was 2.0 g.
実施例3
ショ糖エルカ酸エステルの量を2.5gに、ショ糖ステアリン酸エステルの量を0.5gにしたこと以外は実施例1と同様にして、サスペンションを得た。
Example 3
A suspension was obtained in the same manner as in Example 1 except that the amount of sucrose erucic acid ester was 2.5 g and the amount of sucrose stearate was 0.5 g.
実施例4
ショ糖エルカ酸エステルの量を2.75gに、ショ糖ステアリン酸エステルの量を0.25gにしたこと以外は実施例1と同様にして、サスペンションを得た。
Example 4
A suspension was obtained in the same manner as in Example 1 except that the amount of sucrose erucic acid ester was 2.75 g and the amount of sucrose stearate was 0.25 g.
実施例5
ショ糖エルカ酸エステルの量を2.9gに、ショ糖ステアリン酸エステルの量を0.1gにしたこと以外は実施例1と同様にして、サスペンションを得た。
Example 5
A suspension was obtained in the same manner as in Example 1 except that the amount of sucrose erucic acid ester was 2.9 g and the amount of sucrose stearate was 0.1 g.
実施例6
ショ糖ステアリン酸エステルをS−170(三菱化学フーズ社製、融点65.2℃、HLB1、主成分はジエステル及びトリエステル)にしたこと以外は実施例5を同様にして、サスペンションを得た。
Example 6
A suspension was obtained in the same manner as in Example 5 except that sucrose stearate was changed to S-170 (Mitsubishi Chemical Foods, melting point 65.2 ° C., HLB1, main components were diester and triester).
比較例1
モンテルカストナトリウム0.1gを40gの純水に溶解し、これに、ショ糖エルカ酸エステル(三菱化学フーズ社製、ER−290、融点4.0℃、HLB2、主成分はジエステル及びトリエステル)3.0gをシクロヘキサン80gに溶解した溶液を加え、ホモジナイザー(ポリトロン社製、PT3100型)を用いて25℃でホモジナイザー攪拌(10000rpm、2分)した。この後に凍結乾燥装置(東京理化器械社製、FDU1100型)で凍結乾燥した。当該生成物3.0gを17.0gのミリスチン酸イソプロピルに加えたが、生成物は溶解し、サスペンションは得られなかった。
Comparative Example 1
Montelukast sodium (0.1 g) is dissolved in 40 g of pure water, and sucrose erucic acid ester (manufactured by Mitsubishi Chemical Foods, ER-290, melting point: 4.0 ° C., HLB2, main components are diester and triester) 3 A solution prepared by dissolving 0.0 g in 80 g of cyclohexane was added, and homogenizer stirring (10000 rpm, 2 minutes) was performed at 25 ° C. using a homogenizer (manufactured by Polytron, PT3100 type). Thereafter, it was freeze-dried with a freeze-drying apparatus (FDU1100, manufactured by Tokyo Rika Kikai Co., Ltd.). 3.0 g of the product was added to 17.0 g of isopropyl myristate, but the product dissolved and no suspension was obtained.
比較例2
ショ糖エルカ酸エステルをショ糖ラウリン酸エステル(三菱化学フーズ社製、L−195、融点23.9℃、HLB2、主成分はジエステル及びトリエステル)5.0gにしたこと以外は比較例1と同様にして、同様の結果を得た。
Comparative Example 2
Comparative Example 1 except that sucrose erucic acid ester was changed to 5.0 g of sucrose lauric acid ester (manufactured by Mitsubishi Chemical Foods, L-195, melting point 23.9 ° C., HLB2, main components are diester and triester) Similarly, similar results were obtained.
Claims (5)
コア部が、親水性基及び疎水性基を有する化合物を、かつ
シェル部が、融点30℃以上の界面活性剤及び融点30℃未満の界面活性剤を
それぞれ含有するコアシェル構造体。 A core shell structure including a core portion and a shell portion,
A core-shell structure in which the core part contains a compound having a hydrophilic group and a hydrophobic group, and the shell part contains a surfactant having a melting point of 30 ° C. or higher and a surfactant having a melting point of less than 30 ° C. , respectively.
基剤相を含有し、
前記基剤相が前記コアシェル構造体を含有する、
S/O型サスペンション。
The core-shell structure according to any one of claims 1 to 4, and a base phase,
The base phase contains the core-shell structure;
S / O type suspension.
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