JP2004331651A - 外用剤 - Google Patents
外用剤 Download PDFInfo
- Publication number
- JP2004331651A JP2004331651A JP2004099024A JP2004099024A JP2004331651A JP 2004331651 A JP2004331651 A JP 2004331651A JP 2004099024 A JP2004099024 A JP 2004099024A JP 2004099024 A JP2004099024 A JP 2004099024A JP 2004331651 A JP2004331651 A JP 2004331651A
- Authority
- JP
- Japan
- Prior art keywords
- skin
- blood circulation
- external
- promoting
- vanillyl nonanoate
- 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.)
- Granted
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 11
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Landscapes
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Abstract
【解決する手段】外用血行促進剤又は外用脂肪分解促進剤については、有効成分としてノナン酸バニリルを用いる。また外用組成物としてはノナン酸バニリルを血行促進効果又は外用脂肪分解促進剤を発揮する態様で用いる。
【選択図】なし
Description
項1.ノナン酸バニリルを有効成分とする外用血行促進剤。
項2.ノナン酸バニリルを有効成分とする外用脂肪分解促進剤。
項3.項1記載の外用血行促進剤を含有する外用組成物。
項4.項2記載の外用脂肪分解促進剤を含有する外用組成物。
項5.皮膚化粧料、頭皮化粧料、入浴剤、医薬外用剤または点眼剤である項3又は項4に記載する外用組成物。
本発明の外用血行促進剤は、下式:
上記ノナン酸バニリルはまた、皮膚や粘膜等に経皮適用ないし経粘膜適用した場合に良好な脂肪分解促進効果を発揮し、しかも皮膚等に対して刺激性が抑制されて、刺激性を感じないか若しくは微弱な外用脂肪分解促進剤として適した特性を備えている。
上記ノナン酸バニリルは、血行促進を目的もしくは作用とする外用組成物の成分として使用することもできる。ここでいう外用組成物の例としては、例えば末梢血行障害に起因する例えばしもやけ、冷え性、手足のしびれ、むくみ、レイノー症、肩や首のこり、及び抜け毛(頭髪)等の各種疾患や病態(症状)に対する予防及び治療用の皮膚外用剤、血行を促進することで病態の改善を促進するための皮膚外用剤〔例えば、筋肉痛等のように血行不全が少なからず病態の改善の妨げになっているような疾患や病態(症状)の改善のための皮膚外用剤〕、または血行を促進して有効成分の経皮吸収性や薬効を促す作用を有する皮膚外用剤などの外用医薬組成物;眼の充血や疲れ目の抑制または改善作用を有する点眼剤、または眼の血行を促進して有効成分の経皮吸収性や薬効促進を促す作用を有する点眼剤;頭皮の血行を促進する作用を有する頭皮化粧料、または頭皮の血行を促進して有効成分の頭皮吸収性を促す作用を有する頭皮化粧料;血行を促進して温感作用または代謝を促す作用を有する皮膚化粧料、血行を促進して有効成分の経皮吸収性を促す作用を有する皮膚化粧料等を例示することができる。
また、ノナン酸バニリルは、脂肪分解促進を目的もしくは作用とする外用組成物の成分として使用することもできる。ここでいう外用組成物としては、新陳代謝を促進し、肥満の改善、高脂血症の予防又は改善、体の全体又は部分を細くする、セルライトを除去するための外用医薬組成物、皮膚化粧料、入浴剤等を例示することができる。
文献Journal of Medicinal Chemistry 1993, Vol. 36, No. 16 p.2337の記載に従って、下記の方法によりノナン酸バニリルを製造した。
1H NMR(300MHz CDCl3):δ0.9(3H, t, alkyl CH3), 1.25(12H, env, alkyl CH2), 2.35(2H, t, CH2CO), 3.85(3H, s, ArOCH3), 5.02(2H, s, ArCH2OCO), 5.9(1H, brs, ArOH), 6.85(3H, m, ArH)
上記で調製したノナン酸バニリル(99%以上)を用いて下記の試験(試験例1)を行った。
ノナン酸バニリルを皮膚に適用した場合の血行促進効果を、下記に記載するようにラットを用いて評価した。なお、被験サンプルは実施例として参考例1で調製したノナン酸バニリル(実施例1)を用い、比較例としてノニル酸ワニリルアミド(東洋ファルマー社製・99%以上)の0.1重量%溶液(比較例1)、コントロールとしてエタノール/水混合溶液(1:1(w/w)の等量混合液)(コントロール1)を用いた。ここでノニル酸ワニリルアミドは、皮膚に対する血行促進作用が知られた化合物であり、陽性コントロールとして用いた。上記においてノニル酸ワニリルアミドの0.1重量%溶液はエタノール/水の等量混合液(1:1(w/w))で調製した溶液である。
ノナン酸バニリルを皮膚に適用した場合の脂肪分解促進効果を、下記に記載するようにラットを用いて評価した。なお、被験サンプルは実施例として参考例1で調製したノナン酸バニリル(実施例1)を用い、比較例としてアミノフィリン(ICN社製 Cat. No. 190144)の2重量%溶液(比較例2)、コントロールとしてエタノール/水混合溶液(1:1(W/W)の等量混合液)(コントロール1)を用いた。ここでアミノフィリンは、皮膚適用で脂肪分解作用が知られた化合物であり、陽性コントロールとして用いた。上記においてアミノフィリンの2重量%溶液はエタノール/水の等量混合液(1:1(W/W))で調製した溶液である。
ノナン酸バニリルの皮膚に対する刺激性を、下記に記載するようにラットを用いて評価した。なお、被験サンプルは実施例として参考例1で調製したノナン酸バニリル(実施例1)を用い、比較例としてノニル酸ワニリルアミド(東洋ファルマー社製・99%以上)の0.1重量%溶液(比較例1)、コントロールとしてエタノール/水混合溶液(1:1(w/w)の等量混合液)(コントロール1)を用いた。
下記の処方に従って、軟膏状の皮膚外用医薬組成物(軟膏剤)を調製した。この軟膏剤は、皮膚に塗布することにより、血行促進剤としても脂肪分解促進剤としても使用することができる。
ステアリルアルコール 220.00g
プロピレングリコール 120.00g
ラウリル硫酸ナトリウム 15.00g
パラオキシ安息香酸メチル 0.25g
パラオキシ安息香酸プロピル 0.15g
ノナン酸バニリル 10.00g
精製水 残 部
合 計 1000.00g。
下記の処方に従って、クリーム状の皮膚化粧料を調製した。この皮膚化粧料は、皮膚に塗布することにより、血行促進剤としても脂肪分解促進剤としても使用することができる。
ステアリルアルコール 70g
還元ラノリン 20g
スクワラン 50g
オクチルドデカノール 60g
ポリオキシエチレンセチルエーテル(25E.O.) 30g
親油型モノステアリン酸グリセリン 20g
ノナン酸バニリル 10g
香料 3g
防腐剤 適 量
酸化防止剤 適 量
プロピレングリコール 50g
精製水 残 部
合 計 1000g。
下記の処方に従って、液状の消炎鎮痛剤(皮膚外用組成物:液剤)を調製した。この液剤は、皮膚に塗布することにより、より効果の高い消炎鎮痛剤として、また、脂肪分解促進作用を有する消炎鎮痛剤として使用することができる。
アジピン酸ジイソプロピル 50g
プロピレングリコール 100g
ラウロマクロゴール 30g
精製水 270g
ノナン酸バニリル 10g
イソプロパノール 残 部
合 計 1000g。
Claims (4)
- ノナン酸バニリルを有効成分とする外用血行促進剤。
- ノナン酸バニリルを有効成分とする外用脂肪分解促進剤。
- 請求項1記載の外用血行促進剤又は請求項2記載の外用脂肪分解促進剤を含有する外用組成物。
- 皮膚化粧料、頭皮化粧料、入浴剤、医薬外用剤または点眼剤である請求項3に記載する外用組成物。
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2007145793A (ja) * | 2005-02-01 | 2007-06-14 | Ajinomoto Co Inc | 血行促進外用剤及びこれを含有してなる皮膚毛髪用化粧料及び入浴剤 |
US9399030B2 (en) | 2005-02-01 | 2016-07-26 | Ajinomoto Co., Inc. | Topically applied circulation enhancing agent and skin and hair cosmetic and bath agent containing the same |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2007145793A (ja) * | 2005-02-01 | 2007-06-14 | Ajinomoto Co Inc | 血行促進外用剤及びこれを含有してなる皮膚毛髪用化粧料及び入浴剤 |
US9399030B2 (en) | 2005-02-01 | 2016-07-26 | Ajinomoto Co., Inc. | Topically applied circulation enhancing agent and skin and hair cosmetic and bath agent containing the same |
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