JP2008184445A - アダパレン含有外用剤組成物 - Google Patents
アダパレン含有外用剤組成物 Download PDFInfo
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- JP2008184445A JP2008184445A JP2007020290A JP2007020290A JP2008184445A JP 2008184445 A JP2008184445 A JP 2008184445A JP 2007020290 A JP2007020290 A JP 2007020290A JP 2007020290 A JP2007020290 A JP 2007020290A JP 2008184445 A JP2008184445 A JP 2008184445A
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- adapalene
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- ascorbic acid
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- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 28
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- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 98
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Images
Abstract
【解決手段】(a)アダパレン、並びに(b)リボフラビン、ニコチン酸アミド、パンテノール、アスコルビン酸又はその塩、及びビオチンの少なくとも1種、を含有することを特徴とする外用剤組成物。
【選択図】なし
Description
前提:Tanakaらによれば、開放系でのシリコン膜を用いた移行性試験は局所投与製剤の経皮吸収性の評価に適しているとされている(S.Tanaka,et al.,International Journal of Pharmaceutics, 27:29-38(1985))ことから、角質への浸透性をシリコン膜移行性試験により評価した。また、シリコン膜にすることで、アダパレンが浸透しやすい毛穴の影響を排除することができるので、単純にアダパレンの角質への移行性を評価できると考えられる。
表1及び2に記載の各液剤中に溶解しているアダパレン量に依存してアダパレンのシリコン膜移行性が増大しているとも考えられることから、各液剤のアダパレンの溶解度とシリコン膜移行性との関係を調べるため、各液剤中のアダパレンの飽和溶解度を測定した。
比較例2(アダパレンの1質量部に対して2.5質量部のパントテニルエチルエーテル)では1.5倍、比較例4(アダパレンの1質量部に対して25質量部のパントテニルエチルエーテル)では約3倍と、アダパレンの溶解補助剤であるパントテニルエチルエーテルの濃度依存的にアダパレンの溶解度比率は増大した。また、実施例2(アダパレンの1質量部に対して2.5質量部のリボフラビン)では1.0倍、比較例5(アダパレンの1質量部に対して25質量部のリボフラビン)では1.2倍、実施例5(アダパレンの1質量部に対して2.5質量部のニコチン酸アミド)では1.0倍、実施例7(アダパレンの1質量部に対して25質量部のニコチン酸アミド)では1.4倍、実施例9(アダパレンの1質量部に対して2.5質量部のパンテノール)では1.3倍、実施例11(アダパレンの1質量部に対して25質量部のパンテノール)では2.7倍、実施例20(アダパレンの1質量部に対して2.5質量部のアスコルビン酸2-硫酸エステル二ナトリウム二水和物)では1.2倍、実施例21(アダパレンの1質量部に対して25質量部のアスコルビン酸2-硫酸エステル二ナトリウム二水和物)では2.1倍と、リボフラビン及びニコチン酸アミド及びパンテノール及びアスコルビン酸2-硫酸エステル二ナトリウム二水和物の濃度依存的に、またアスコルビン酸テトライソパルミテートの濃度非依存的にアダパレンの溶解度比率がやや増大した。これに対して、実施例12〜15(アダパレンの1質量部に対して0.5〜25質量部のアスコルビン酸)、実施例16〜18(アダパレンの1質量部に対して0.5〜25質量部のアスコルビン酸ナトリウム)、実施例22〜25アダパレンの1質量部に対して0.5〜25質量部のアスコルビン酸グルコシド)、実施例26〜29(アダパレンの1質量部に対して0.5〜25質量部のリン酸アスコルビルマグネシウム)、実施例34〜37(アダパレンの1質量部に対して0.5〜25質量部のビオチン)では、アスコルビン酸及びアスコルビン酸ナトリウム及びアスコルビン酸グルコシド及びリン酸アスコルビルマグネシウム及びビオチンの濃度が増大してもアダパレンの溶解度比率は増大しないか、または逆に濃度依存的に低下した。
Claims (5)
- (a)アダパレン、並びに(b)リボフラビン、ニコチン酸アミド、パンテノール、アスコルビン酸又はその塩、及びビオチンの少なくとも1種、を含有することを特徴とする外用剤組成物。
- アダパレンの含有量が外用剤組成物全体に対して0.01〜1.0質量%である請求項1記載の外用剤組成物。
- リボフラビンの含有量がアダパレンの1質量部に対して0.5〜5質量部である請求項1記載の外用剤組成物。
- ニコチン酸アミド、パンテノール、アスコルビン酸又はその塩、及びビオチンの少なくとも1種の含有量が、アダパレンの1質量部に対して0.5〜25質量部である請求項1記載の外用剤組成物。
- 液剤、ローション剤、ゲル剤、エアゾール剤、クリーム剤又は水性軟膏剤である請求項1〜4の何れか1項に記載の外用剤組成物。
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