JP6047004B2 - 安全な医薬組成物 - Google Patents
安全な医薬組成物 Download PDFInfo
- Publication number
- JP6047004B2 JP6047004B2 JP2012276633A JP2012276633A JP6047004B2 JP 6047004 B2 JP6047004 B2 JP 6047004B2 JP 2012276633 A JP2012276633 A JP 2012276633A JP 2012276633 A JP2012276633 A JP 2012276633A JP 6047004 B2 JP6047004 B2 JP 6047004B2
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- JP
- Japan
- Prior art keywords
- dada
- antipyretic
- tranexamic acid
- pharmaceutical composition
- present
- 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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Description
(1)ジクロロ酢酸ジイソプロピルアミン、及び、トラネキサム酸を含有する、経口用医薬組成物。
(2)感冒時の発熱の解熱のために用いられることを特徴とする、(1)に記載の経口用医薬組成物。
また、上記製剤が吸水等により保存安定性や品質に課題が発生する場合には、乾燥剤入り包装、及び/又は、製剤や顆粒の防湿コーティング等により、適宜、対応すればよい。
表1に記載の成分及び分量をとり、日局製剤総則「錠剤」の項に準じて錠剤を製造する。
3錠中(mg) 錠剤1 錠剤2 錠剤3
――――――――――――――――――――――――――――――――――
ジクロロ酢酸ジイソプロピルアミン 60 60 90
トラネキサム酸 20 120 750
乳糖 90 90 90
ステアリン酸マグネシウム 2 2 2
ヒドロキシプロピルセルロース 適量 適量 適量
表2に記載の成分及び分量をとり、日局製剤総則「液剤」の項に準じて液剤を製造する。
50mL中(mg) 液剤1 液剤2 液剤3
――――――――――――――――――――――――――――――――――
ジクロロ酢酸ジイソプロピルアミン 60 60 90
トラネキサム酸 20 120 750
白糖 4000 4000 4000
安息香酸ナトリウム 5 5 5
pH調整剤 適量 適量 適量
精製水 残部 残部 残部
(1)被検物質
ジクロロ酢酸ジイソプロピルアミン(DADA)及びトラネキサム酸(以下、TRAと略す場合がある)は、いずれも第一三共(株)製のものを使用した。
DADA60mgを0.5%CMC(カルボキシメチルセルロース ナトリウム溶液)10mLに溶解して、DADA単剤の被験物質として使用した。DADAとTRAとの合剤については、DADA60mgとTRA60mgを0.5%CMC10mLに溶解して、合剤の被験物質として使用した。
7週齢のSlc:SD雄性ラットを日本チャールズリバー(株)から購入し、1週間予備飼育した後、一般状態に異常の認めない良好なものを実験に使用した。
馴化終了後、至近の体重をもとに1群3匹の3群に分けた。第1群は陽性対照群(擬似ウイルス接種かつ媒体投与;図1における「対照」)、第2群はDADA投与群(擬似ウイルス接種かつDADA投与;図1における「DADA単剤」)、第3群はDADAとTRAの併用群(擬似ウイルス接種かつDADA+TRA投与;図1における「DADA+TRA」)とした。
擬似ウイルスとしてpoly I:C(シグマ社製)を用いて、これを生理食塩水で5mg/mLの濃度に希釈してウイルス接種投与溶液を調製した。これを、各投与ラットの最新の体重を用い、1mL/kgとなるように腹腔内投与し、擬似ウイルス感染状態を誘発した。
擬似ウイルス接種4日前から11日間、ラット体重10g当り、上記の被験物質0.05mL(対照群は溶媒である0.5%CMCのみを投与)を1日1回(合計11回)、胃ゾンデ(フチガミ器械社製)と注射器(テルモ社製)を用いて強制経口投与した。
群分け終了翌日、すなわち擬似ウイルス接種3日前より、1日1回直腸温の測定を行った。擬似ウイルス摂取日は、直腸温を測定した後、poly I:Cを投与し、投与後2時間おきに直腸温を測定した。投与後の直腸温変化[Δ(デルタ,℃)]は次式により求めて評価した。
得られた結果を図1に示した。図1の横軸は擬似感染からの経過時間で、縦軸は直腸温の変化Δ(デルタ,℃)である。
媒体のみの投与群(対照)では、poly I:Cの投与により、時間とともに深部体温(直腸温度として)が上昇することが確認できた。DADA単剤(30mg/Kg)の投与でも解熱作用の傾向が認められたが、解熱作用を有しないトラネキサム酸(TRA、10mg/Kg)を併用した場合、顕著な解熱効果が発現することが判明した。
Claims (1)
- ジクロロ酢酸ジイソプロピルアミン、及び、トラネキサム酸を含有する、感冒時の発熱の解熱のために用いられることを特徴とする経口用医薬組成物。
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