JP2013151486A - 感冒薬組成物 - Google Patents
感冒薬組成物 Download PDFInfo
- Publication number
- JP2013151486A JP2013151486A JP2012281952A JP2012281952A JP2013151486A JP 2013151486 A JP2013151486 A JP 2013151486A JP 2012281952 A JP2012281952 A JP 2012281952A JP 2012281952 A JP2012281952 A JP 2012281952A JP 2013151486 A JP2013151486 A JP 2013151486A
- Authority
- JP
- Japan
- Prior art keywords
- loxoprofen
- caffeine
- mequitazine
- medicine composition
- fexofenadine
- 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
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Abstract
【解決手段】(a)ロキソプロフェン、(b)カフェイン、及び、(c)メキタジン、エピナスチン及び/又はフェキソフェナジンから選ばれる1種以上、を含有する、ロキソプロフェンによる胃粘膜障害を軽減することを特徴とする感冒薬組成物。
【選択図】なし
Description
1)ロキソプロフェンに、クレマスチン、クロルフェニラミン、カルビノキサミン、エフェドリン、コデイン、フェニルプロパノールアミン、セラペプターゼ、リゾチーム及びブロムヘキシンより選択される1種又は2種以上からなる医薬組成物(特許文献8参照)。
2)ロキソプロフェンに、ケトチフェンを含有したロキソプロフェンの解熱効果を高めた組成物(特許文献9参照)。
3)ロキソプロフェンとクレマスチンフマル酸塩を混合しただけの製剤より、無水カフェインを更に混合すると、製剤の安定性が改善される(特許文献10参照)。
4)ロキソプロフェンと、カルビノキサミン、クロルフェニラミン、ケトチフェン、メキタジン、エピナスチンから選ばれる1種以上の抗ヒスタミン薬乃至抗アレルギー薬を配合すると鼻閉症状が改善される(特許文献11参照)。更に、同文献の実施例1には、ロキソプロフェン、無水カフェイン、ケトチフェン、他9種の有効成分を含有した製剤、実施例4にはロキソプロフェン、無水カフェイン、エピナスチン、他5種の有効成分を含有した製剤が開示されている。
すなわち、本発明の課題はロキソプロフェンとカフェインを含有した場合の胃粘膜障害を軽減する技術を提供することである。
(1)(a)ロキソプロフェン、(b)カフェイン、及び、(c)メキタジン及び/又はフェキソフェナジンから選ばれる1種以上、を含有する感冒薬組成物、
(2)(c)がメキタジンである、請求項1に記載された感冒薬組成物、
(3)(c)がフェキソフェナジンである、請求項1に記載された感冒薬組成物。
(4)ロキソプロフェンによる胃粘膜障害を軽減することを特徴とする、請求項1乃至3から選択されるいずれか1項に記載の感冒薬組成物、
(5)(a)ロキソプロフェン、(b)カフェイン、及び(c)エピナスチンを含有する、胃粘膜障害が軽減された感冒薬組成物、
(6)メキタジン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤、
(7)フェキソフェナジン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤、又は
(8)エピナスチン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤。
例えば、本発明の組成物が1日1回100mL服用する液剤であれば、その液剤におけるロキソプロフェンの含有量は、好ましくは20〜120mg/100mLであり、好ましくは、40〜80mg/100mLである。また、カフェイン及びフェキソフェナジンの含有量は、いずれも、好ましくは5〜500mg/100mL、より好ましくは10〜200mg/100mLである。更に、メキタジン及びエピナスチンの含有量は、いずれも、好ましくは0.5〜50mg/100mL、より好ましくは1〜30mg/100mLである。
(表1)
1カプセル中(mg) a b c
――――――――――――――――――――――――――――――
ロキソプロフェンナトリウム 60 60 60
カフェイン 20 20 20
フェキソフェナジン塩酸塩 40 − −
エピナスチン塩酸塩 − 7 −
メキタジン − − 2
ステアリン酸マグネシウム 5 5 5
結晶セルロース 15 15 15
乳糖 適量 適量 適量
――――――――――――――――――――――――――――――
(表2)
1錠中(mg) d e f
――――――――――――――――――――――――――――――
ロキソプロフェンナトリウム 60 60 60
カフェイン 20 20 20
フェキソフェナジン塩酸塩 40 − −
エピナスチン塩酸塩 − 7 −
メキタジン − − 2
ステアリン酸マグネシウム 5 5 5
結晶セルロース 10 10 10
ヒドロキシプロピルセルロース 適量 適量 適量
――――――――――――――――――――――――――――――
(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、無水カフェインは東京化成工業製のものを、クロルフェニラミンマレイン酸塩は金剛化学製のものを、メキタジンは和光純薬工業製のものを、エピナスチン塩酸塩は東京化成工業製のものを、フェキソフェナジン塩酸塩はアミノケミカル製のものをそれぞれ使用した。
被験物質はトガラント(SIGMA製)を注射用水(大塚製薬製)に溶解した0.5%トガラント溶液中に懸濁させて調整した。
(2)使用動物
Slc:Wistar/ST雄性ラット7週齢(日本エスエルシー)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40−70%、照明時間6−18時に制御されたラット飼育室内で個別飼育した。固形試料(オリエンタル酵母工業ラット用固形飼料、CRF-1)および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
18時間以上絶食したラットに、ディスポーザブルラット用経口ゾンデ(フチガミ器械製)を取り付けたポリプロピレン製ディスポーザブル注射筒(テルモ製)を用いて、被験物質を経口投与した。なお、被験物質はマグネチックスターラーを用いて攪拌しながら使用した。
被験物質投与後5時間に、20%イソフルラン軽麻酔下での頚椎脱臼により動物を安楽死させ、速やかに胃を摘出し、内部に生理食塩液を10mL充填後、1%ホルマリンに浸して翌日まで固定する。
固定した胃を大湾に沿って切開し、デジタルノギスを用いて胃粘膜傷害の長さを測定する。個体の胃粘膜傷害の長さは、長径を計測しそれらの総和(傷害総長)を算出した。
(4)試験結果
上述の課題を解決したものが以下の結果である。
ロキソプロフェン(L)及び無水カフェイン(C)に、抗ヒスタミン薬乃至抗アレルギー薬のクロルフェニラミンマレイン酸塩(CP)、メキタジン(MQ)、エピナスチン塩酸塩(EP)、フェキソフェナジン塩酸塩(FX)をそれぞれ併用した場合の結果を表4に示す。なお、いずれの投与群も1群6匹の平均値であり、胃粘膜障害抑制率(%)は、ロキソプロフェンとカフェインを併用した場合を基準に、次式により求めた。
被験薬(mg/Kg) 胃粘膜障害抑制率%
――――――――――――――――――――――――――――――
L(80)+C(27) 0
L(80)+C(27)+MQ(10) 41
L(80)+C(27)+EP(20) 39
L(80)+C(27)+FX(80) 38
L(80)+C(27)+CP(10) −1
――――――――――――――――――――――――――――――
Claims (8)
- (a)ロキソプロフェン、(b)カフェイン、及び、(c)メキタジン及び/又はフェキソフェナジンから選ばれる1種以上、を含有する感冒薬組成物。
- (c)がメキタジンである、請求項1に記載された感冒薬組成物。
- (c)がフェキソフェナジンである、請求項1に記載された感冒薬組成物。
- ロキソプロフェンによる胃粘膜障害を軽減することを特徴とする、請求項1乃至3から選択されるいずれか1項に記載の感冒薬組成物。
- (a)ロキソプロフェン、(b)カフェイン、及び(c)エピナスチンを含有する、胃粘膜障害が軽減された感冒薬組成物。
- メキタジン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤。
- フェキソフェナジン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤。
- エピナスチン及びカフェインを含有する、胃粘膜障害が軽減されたロキソプロフェン製剤。
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JP2016088853A (ja) * | 2014-10-31 | 2016-05-23 | 興和株式会社 | フェキソフェナジンとnsaid含有医薬組成物 |
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