JP6467167B2 - ロキソプロフェン配合外用剤組成物 - Google Patents
ロキソプロフェン配合外用剤組成物 Download PDFInfo
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- JP6467167B2 JP6467167B2 JP2014168992A JP2014168992A JP6467167B2 JP 6467167 B2 JP6467167 B2 JP 6467167B2 JP 2014168992 A JP2014168992 A JP 2014168992A JP 2014168992 A JP2014168992 A JP 2014168992A JP 6467167 B2 JP6467167 B2 JP 6467167B2
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- Prior art keywords
- loxoprofen
- external preparation
- preparation composition
- inflammatory
- sodium
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Description
また、カンゾウ(甘草)の成分でもあるグリチルリチン酸やグリチルレチン酸は、外用剤では抗炎症成分としてよく知られており(例えば、非特許文献4参照)、カンゾウ末のみを配合したパップ剤に鎮痛・消炎効果があることも開示されている(非特許文献3参照)。
(1)ロキソプロフェンと、オウバク又はその抽出物、及び/又は、グリチルレチン酸とを含有する外用剤組成物であり、好適には、
(2)皮膚に適用するための、請求項1に記載の外用剤組成物、
(3)鎮痛消炎剤である、請求項1又は2に記載の外用剤組成物、又は
(4)消炎剤である、請求項1又は2に記載の外用剤組成物
である。
(表1)
100g中(g) a b c
―――――――――――――――――――――――――――――――
ロキソプロフェンナトリウム 1 1 1
オウバク乾燥エキス 1 0 1
グリチルレチン酸 0 1 1
エタノール 5 10 20
精製水 残部 残部 残部
―――――――――――――――――――――――――――――――
(表2)
100g中(g) a b c
―――――――――――――――――――――――――――――――
ロキソプロフェンナトリウム 1 1 1
オウバク乾燥エキス 1 0 1
グリチルレチン酸 0 1 1
カルボキシビニルポリマー 2 2 2
ヒプロメロース 1.5 1.5 1.5
エタノール 5 5 5
精製水 残部 残部 残部
―――――――――――――――――――――――――――――――
(1)被検物質
ロキソプロフェンナトリウム・2水和物は第一三共製のものを、オウバク乾燥エキスは日本粉末薬品製のものを、グリチルレチン酸は和光純薬工業製のものをそれぞれ使用した。各被験物質は、溶媒として5%エタノールを用い、1%濃度となるように調製し、2剤併用の場合には各薬剤がそれぞれ1%となるように調製した。
(2)使用動物
Wistar今道雄性ラット5週齢(動物繁殖研究所)を5日間の検疫及び2日間の馴化後に使用した。動物は温度20−26℃、湿度30−80%、照明時間8−20時に制御されたラット飼育室内で5匹/ケージにて飼育した。マウス・ラット用固形試料(フナバシファーム製、F-2)およびフィルターを通した水道水を自由に摂取させ、1週間予備飼育した後、毛並、体重増加などの一般症状の良好な動物を選別して供試した。
(3)試験方法
試験前日夕刻より絶食(飲水は自由)させ、試験当日の朝より絶水し試験終了まで継続した。試験当日、動物の個体識別のための標識を行った後、動物用天秤を用いて体重を測定後、ラットの右後肢体積を、足容積測定装置(Volume Meter TK-105、室町機械製)を用いて測定して投与前値とした。
溶媒として5%エタノールを用いて1%濃度のカラゲニン(シグマアルドリッチジャパン製)溶液に調製したものを、被験物質塗布直前にラットの右後肢皮下に0.1mL投与して炎症浮腫を惹起させた。
カラゲニン皮下投与(起炎)直後に、各被験物質をラットの右後肢に0.1mL塗布した。塗布後、動物を速やかに補綴器具で補綴し、塗布部分を動物が舐めることを回避した。
カラゲニン皮下投与3時間および5時間後に右後肢容積を測定し、各固体の浮腫強度を次式により算出した(N=5)。
得られた、カラゲニン投与3時間および5時間後における各被験物質群の浮腫抑制率の結果を表3に示す(N=5)。ここで、ロキソプロフェンはロキソプロフェンナトリウム、オウバクはオウバク乾燥エキス、GRAはグリチルレチン酸である。
浮腫抑制率(%)
被験物質(濃度%) 3時間後 5時間後
―――――――――――――――――――――――――――――――――――
ロキソプロフェン(1) 37.8 20.8
オウバク(1) 38.1 4.0
ロキソプロフェン(1)+オウバク(1) 48.3 35.9
―――――――――――――――――――――――――――――――――――
GRA(1) 30.1 −8.1
ロキソプロフェン(1)+GRA(1) 56.0 35.2
一方、ロキソプロフェンにオウバクを併用すると、ロキソプロフェンの抗浮腫効果の増加のみならず、相乗的な持続時間の延長がもたらされる。さらに、ロキソプロフェンにグリチルレチン酸を併用した場合には、ロキソプロフェンの抗浮腫効果の増加のみならず、顕著な持続時間の延長が発現するという意外な事実が判明した。
Claims (4)
- ロキソプロフェン、オウバク又はその抽出物、及び、グリチルレチン酸を含有する外用剤組成物。
- 皮膚に適用するための、請求項1に記載の外用剤組成物。
- 鎮痛消炎剤である、請求項1又は2に記載の外用剤組成物。
- 消炎剤である、請求項1又は2に記載の外用剤組成物。
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