JP6859033B2 - 乳化組成物 - Google Patents
乳化組成物 Download PDFInfo
- Publication number
- JP6859033B2 JP6859033B2 JP2016135352A JP2016135352A JP6859033B2 JP 6859033 B2 JP6859033 B2 JP 6859033B2 JP 2016135352 A JP2016135352 A JP 2016135352A JP 2016135352 A JP2016135352 A JP 2016135352A JP 6859033 B2 JP6859033 B2 JP 6859033B2
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- JP
- Japan
- Prior art keywords
- oil
- emulsified composition
- present
- retinol
- water
- 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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- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 claims description 48
- 235000020944 retinol Nutrition 0.000 claims description 47
- 239000011607 retinol Substances 0.000 claims description 46
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- 239000011734 sodium Substances 0.000 claims description 42
- 229910052708 sodium Inorganic materials 0.000 claims description 42
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Description
項1. ポリエチレンスルホン酸ナトリウムを含有する、乳化組成物。
項2. ニコチン酸ベンジル、γ−オリザノール、レチノール、レチノールの誘導体、トコフェロール、及びトコフェロールの誘導体よりなる群から選択される少なくとも1種の油性成分を含む、項1に記載の乳化組成物。
項3. 液状油を含む、項1又は2に記載の乳化組成物。
項4. 固形油を含まない、項1〜3のいずれかに記載の乳化組成物。
項5. 油中水型である、項1〜4のいずれかに記載の乳化組成物。
項6. ポリエチレンスルホン酸ナトリウムを含む、乳化安定化剤。
項7. 乳化組成物にポリエチレンスルホン酸ナトリウムを添加する、乳化安定化方法。
本発明の乳化組成物は、ポリエチレンスルホン酸ナトリウムを含有することを特徴とする。以下、本発明の乳化組成物について詳述する。
本発明の乳化組成物は、乳化安定性を向上させる成分として、ポリエチレンスルホン酸ナトリウムを含有する。
本発明の乳化組成物は、ニコチン酸ベンジル、γ−オリザノール、レチノール、レチノールの誘導体、トコフェロール、及びトコフェロールの誘導体よりなる群から選択される少なくとも1種の油性成分を含んでいてもよい。これらの油性成分は、従来の乳化組成物において、乳化安定性を低下させたり、粘度を低下させたりする傾向があるが、本発明の乳化組成物によれば、これらの油性成分を含んでいても、乳化安定性の向上が図られ、特に油中水型の場合には粘度の低下を抑制することができる。
ニコチン酸ベンジルとは、血行促進作用、細胞賦活作用等が知られている公知の化合物である。本発明の乳化組成物が、ニコチン酸ベンジルを含む場合には、血行促進作用を発揮することができ、特にニコチン酸ベンジルを含み且つ油中水型である場合には、格段に優れた血行促進作用を発揮することが可能になる。
γ−オリザノールとは、フェルラ酸とトリテルペンアルコールとのエステル、又はフェルラ酸とステロールとのエステルである。
レチノールは、ビタミンAの1種であり、ビタミンAアルコールとも称されることがある成分である。
トコフェロールは、ビタミンEとしても知られている公知の成分である。本発明で使用されるトコフェロールは、d体又はdl体のいずれであってもよく、またα、β、γ、δの構造のいずれであってもよい。本発明で使用されるトコフェロールとして、具体的には、d−α−トコフェロール、d−β−トコフェロール、d−γ−トコフェロール、d−δ−トコフェロール、l−α−トコフェロール、l−β−トコフェロール、l−γ−トコフェロール、l−δ−トコフェロール、それらの混合物であるdl−α−トコフェロール、dl−β−トコフェロール、dl−γ−トコフェロール、dl−δ−トコフェロール等が挙げられる。
本発明の乳化組成物には、油相の基剤成分として、液状油、固形油、高級アルコール等の油性基剤が含まれる。
液状油とは、25℃において液状の形態を保つ油である。本発明で使用される液状油としては、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、アボガド油、ツバキ油、マカデミアナツツ油、オリーブ油、ホホバ油等の植物油;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、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。
固形油とは、25℃において固形の形態を保つ油である。本発明で使用される固形油としては、通常化粧料や外用医薬品等に用いられるものであればよく、例えば、キャンデリラロウ、コメヌカロウ、ミツロウ、綿ロウ、カルナウバロウ、ラノリン、セラックロウ、オゾケライト、セレシン、ポリエチレンワックス、マイクロクリスタリンワックス、パラフィン、ワセリン、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、ベヘニン酸、12−ヒドロキシステアリン酸、ウンデシレン酸、ミリスチン酸ミリスチル、ミリスチン酸セチル、ステアリン酸ステアリル、ステアリン酸セチル、パルミチン酸セチル、ステアリン酸コレステリル、オレイン酸コレステリル、パルミチン酸デキストリン、ステアリン酸イヌリン、水素添加ホホバ油、セレシンワックス、固形パラフィンワックス、ポリエチレンワックス、シリコーンワックス等の固形油が挙げられる。
高級アルコールとは、1分子中の炭素原子数が6個以上の1価アルコールである。本発明で使用される高級アルコールにおける1分子中の炭素原子数について、6以上であればよいが、好ましくは6〜34、更に好ましくは14〜22が挙げられる。
本発明の乳化組成物には、水相の基剤成分として水が含まれる。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、30〜90重量%、好ましくは40〜80重量%、更に好ましくは50〜70重量%が挙げられる。
本発明の乳化組成物は、乳化形態に調製するためにノニオン性界面活性剤が含まれていることが好ましい。本発明で使用されるノニオン性界面活性剤は、本発明の乳化組成物の乳化タイプに応じて適宜設定すればよい。
本発明の乳化組成物を油中水型にする場合に主に使用されるノニオン性界面活性剤(HLB値が2〜8程度)としては、例えば、ポリグリセリン脂肪酸エステル、グリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、プロピレングリコール脂肪酸エステル、ポリオキシエチレン硬化ヒマシ油、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等が挙げられる。
本発明の乳化組成物を水中油型にする場合に主に使用されるノニオン性界面活性剤(HLB値が8〜17程度)としては、例えば、グリセリン脂肪酸エステル、ポリグセリン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレンソルビット脂肪酸エステル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンアルキルエーテル、ポリエチレングリコール脂肪酸エステル、レシチン誘導体等が挙げられる。
本発明の乳化組成物には、保湿性の付与等のために、必要に応じて多価アルコールが含まれていてもよい。
本発明の乳化組成物は、前述する成分の他に、必要に応じて、他の薬理成分を含有していてもよい。このような薬理成分としては、例えば、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等)、局所麻酔剤(プロカイン、テトラカイン、ブピパカイン、メピパカイン、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、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(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)、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)、清涼化剤(メントール、カンフル、ボルネオール、ハッカ水、ハッカ油等)、ムコ多糖類(コンドロイチン硫酸ナトリウム、グルコサミン等)等が挙げられる。
本発明の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が、好ましくは油中水型が挙げられる。油中水型の場合であれば、より一層効果的に乳化安定性を向上させることができ、更に粘度を高めて、外用剤として良好な硬さを備えさせることができる。更に、本発明の乳化組成物が油中水型であって、液状油とニコチン酸ベンジルを含む場合には、格段に優れた血行促進作用を発揮させることも可能になる。
本発明の乳化組成物は、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。
本発明の乳化安定化剤は、乳化組成物の乳化安定性を向上させるために使用されるものであって、ポリエチレンスルホン酸ナトリウムを含むことを特徴する。また、本発明の乳化安定化方法は、乳化組成物にポリエチレンスルホン酸ナトリウムを添加することを特徴とする。
表1に示す組成の水中油型乳化組成物(クリーム剤)を調製した。具体的には、油性成分、界面活性剤、高級アルコール、及び液状油を混合し、80℃で加熱溶解することにより、油相原料を調製した。また、別途、水性成分、多価アルコール、及び水性基剤を混合し、80℃で加熱溶解することにより、水相原料を調製した。80℃に加熱した水相原料に、80℃に加熱した油相原料を徐々に添加しホモミキサーを用いて乳化させた。その後、撹拌しながら35度まで冷却することにより、水中油型乳化組成物を得た。
<乳化安定性の判定基準>
◎:油相と液相の分離が認められず、性状も変化していない。
○:油相と液相の分離は認められないが、性状がやや変化している。
△:油相と液相の分離がやや認められる。
×:油相と液相の分離が認められる。
表2に示す組成の油中水型乳化組成物(クリーム剤)を調製した。具体的には、油性成分、界面活性剤、高級アルコール、液状油、及び固形油を混合し、80℃で加熱溶解することにより、油相原料を調製した。また、別途、水性成分、多価アルコール、及び水性基剤を混合し、80℃で加熱溶解することにより、水相原料を調製した。80℃に加熱した油相原料に対して、80℃に加熱した油相原料をディスパーをかけながら徐々に添加して乳化を行った。その後、撹拌しながら35度まで冷却することにより、油中水型乳化組成物を得た。
前記試験例2で調製した油中水型乳化組成物(実施例3〜6及び比較例3〜6)の25℃における粘度の測定を行った。25℃における粘度の測定は、各油中水型乳化組成物45gをスクリュー管(50ml)に充填し、ブルックフィールド回転粘度計(B型粘度計、BROOK Field社製DV-II)にて、使用スピンドルT−E、回転数20rpm、回転開始から3分後の条件で測定することによって求めた。
前記試験例1で調製した水中油型乳化組成物(実施例1及び比較例1)、及び前記試験例2で調製した油中水型乳化組成物(実施例3、5及び比較例3、5)を用いて、血行促進作用の評価を行った。
表5に示す組成の油中水型乳化組成物(クリーム剤)製造した。具体的な製造方法は、前記試験例2の場合と同様である。得られた油中水型乳化組成物について、前記試験例2と同様の方法で乳化安定性の評価を行ったところ、いずれも優れた乳化安定性を有していた。得られた油中水型乳化組成物について、前記試験例3と同様の方法で粘度の評価を行ったところ、高い粘度を有していることも確認された。更に、得られた油中水型乳化組成物のうち、処方例1、3、5、7及び8について、前記試験例4と同様の方法で血行促進作用の評価を行ったところ、いずれも優れた血行促進作用が認められた。
Claims (3)
- ポリエチレンスルホン酸ナトリウム、ニコチン酸ベンジル、及び液状油を含有し、且つ固形油を含まない、乳化組成物(但し、アントラニル酸系、フェニル酢酸系、インドール系、プロピオン酸系、ピラゾロン系、ベンゾサイアジン系及びスルホンアミド系のいずれかの消炎鎮痛薬を含む場合を除く)。
- γ−オリザノール、レチノール、レチノールの誘導体、トコフェロール、及びトコフェロールの誘導体よりなる群から選択される少なくとも1種の油性成分を含む、請求項1に記載の乳化組成物。
- 油中水型である、請求項1又は2に記載の乳化組成物。
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