Development of Sarpogrelate External Preparation for Intractable Pain Control. I. Pre-formulation Study on Application of Modified β-Cyclodextrins
スポンサーリンク
概要
- 論文の詳細を見る
To optimize the formulation of in-hospital sarpogrelate (SPG) preparation for external use, various cyclodextrins (CDs) were investigated for their ability to improve the aqueous solubility and chemical stability of SPG. Although hydrolysis of SPG was markedly accelerated at above pH 7.0 in aqueous solution, the addition of modified β-CD resulted in suppressed SPG hydrolysis. Addition of sulfobutylether-β-CD (SBE-β-CD, Captisol®) had the most significant stabilization effect. Phase solubility diagram and 1H-NMR analyses indicated that dimethyl-β-CD and SBE-β-CD formed significantly stable inclusion complexes with SPG in aqueous solution, thereby contributing to both the increased solubility and chemical stabilization of SPG. In terms of the clinical safety of CD derivatives, SBE-β-CD was determined to be the most suitable solubilizing agent for external SPG preparation.
著者
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Higashi Kenjirou
Graduate School of Pharmaceutical Sciences, Chiba University
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Hanawa Takehisa
Department of Pharmacy, Yamanashi Medical University
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Oguchi Toshio
Department Of Pharmacy University Hospital University Of Yamanashi
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Moribe Kunikazu
Graduate School Of Pharmaceutical Sciences Chiba University
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Yamamoto Keiji
Graduate School Of Pharmaceutical Sciences Chiba University
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Hanawa T
Graduate School Of Pharmaceutical Sciences Chiba University
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HANAWA KAZUMI
Department of Pharmacy, Yamanashi Medical University
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TSUCHIYA Chikako
Department of Pharmacy, University Hospital, University of Yamanashi
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Suzuki Masahiko
Department Of Orthopedic Surgery Graduate School Of Medicine Chiba University
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Suzuki Masahiko
Department Of Applied Chemistry Faculty Of Science Science University Of Tokyo
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Higashi Kenjirou
Graduate School Of Pharmaceutical Sciences Chiba University
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Moribe Kunikazu
Graduate School Of Pharmaceutical Sciences Chiba Univ.
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Hanawa Takehisa
Department of Pharmacy, University Hospital, University of Yamanashi
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HANAWA Kazumi
Department of Pharmacy, University Hospital, University of Yamanashi
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Suzuki Masahiko
Department of Pharmacy, University Hospital, University of Yamanashi
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