JPWO2018147409A1 - 水性点眼点鼻用組成物 - Google Patents
水性点眼点鼻用組成物 Download PDFInfo
- Publication number
- JPWO2018147409A1 JPWO2018147409A1 JP2018567510A JP2018567510A JPWO2018147409A1 JP WO2018147409 A1 JPWO2018147409 A1 JP WO2018147409A1 JP 2018567510 A JP2018567510 A JP 2018567510A JP 2018567510 A JP2018567510 A JP 2018567510A JP WO2018147409 A1 JPWO2018147409 A1 JP WO2018147409A1
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- Prior art keywords
- levocetirizine
- composition
- salt
- composition according
- concentration
- 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
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Abstract
Description
安定性試験
レボセチリジン塩酸塩1%を含む点眼液に添加剤を無配合のもの、エデト酸ナトリウム水和物あるいはクエン酸ナトリウム水和物を配合したものを使用して、室温4週間後のレボセチリジン塩酸塩の析出の有無をマイクロスコープにて確認した。
結果を表3に示す。
安定性試験
レボセチリジン0.2%に相当するレボセチリジン塩酸塩を含む点眼液に表4に示す種々の添加剤を配合し、HPLCでレボセチリジン含量とその不純物総量を測定した。なお、不純物総量とはレボセチリジンの分解生成物含量と添加剤由来の不純物を合算した総量とする。
レボセチリジン塩酸塩を1.19mg、2.38mgあるいは5.94mgに変更する以外は処方例1と同じ処方にて、点眼・点鼻液を3種類調製した。
薬効評価試験
モルモット結膜にヒスタミンを投与することにより、疑似的なアレルギー性結膜炎モデルを作製し、実施例4の点眼液のうちレボセチリジン0.05%、0.1%及び0.2%に相当するレボセチリジン塩酸塩を含む点眼液の作用について検討した。また、陰性対照としてレボセチリジン塩酸塩を含まないプラセボ、陽性対照としてアレジオン(登録商標)点眼液0.05%(参天製薬)を用いた。各試験検体をヒスタミン投与の6時間前に点眼投与し、100 μg/mLのヒスタミン50 μLを結膜に、10mg/mLの色素(エバンスブルー)1 mL/kgを静脈内に投与した。ヒスタミン投与の30分後において結膜中のエバンスブルー量を測定した。結果を図1に示す。
Claims (12)
- レボセチリジンまたはその塩類を有効成分として含む水性点眼点鼻用組成物。
- レボセチリジンまたはその塩類の濃度が、レボセチリジンとして0.05〜0.5%(w/v)である、請求項1に記載の組成物。
- 界面活性剤および/または有機酸塩をさらに含む、請求項1または2に記載の組成物。
- 界面活性剤としてポリソルベート80を含む、請求項3に記載の組成物。
- 界面活性剤が0.1〜2.0%(w/v)の濃度である、請求項3または4に記載の組成物。
- 有機酸塩としてクエン酸塩を含む、請求項3〜5いずれかに記載の組成物。
- 有機酸塩が0.4〜2.5%(w/v)の濃度である、請求項3〜6いずれかに記載の組成物。
- 塩酸ポリヘキサニドを防腐剤としてさらに含む、請求項1〜7いずれかに記載の組成物。
- レボセチリジンまたはその塩類をレボセチリジンとして0.05〜0.5%(w/v)、ポリソルベート80を0.1〜2.0%(w/v)、クエン酸塩を0.4〜2.5%(w/v)、エデト酸二ナトリウムを0.001〜0.3%(w/v)および塩酸ポリヘキサニドを含む、請求項1に記載の組成物。
- レボセチリジン塩酸塩をレボセチリジンとして0.05〜0.5%(w/v)、ポリソルベート80を約0.2%(w/v)、クエン酸ナトリウムを約0.75%(w/v)、エデト酸二ナトリウムを約0.018%(w/v)および塩酸ポリヘキサニドを0.00005〜0.0005%(w/v)含む、請求項9に記載の組成物。
- 点眼用の請求項1〜10いずれかに記載の組成物。
- アレルギー疾患の処置のための、請求項1〜11いずれかに記載の組成物。
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