Development of Sarpogrelate External Preparation for Intractable Pain Control. I. Pre-formulation Study on Application of Modified .BETA.-Cyclodextrins

DOI Web Site Web Site PubMed 1 Citations 13 References Open Access
  • Hanawa Kazumi
    Department of Pharmacy, University Hospital, University of Yamanashi Graduate School of Pharmaceutical Sciences, Chiba University
  • Hanawa Takehisa
    Department of Pharmacy, University Hospital, University of Yamanashi
  • Tsuchiya Chikako
    Department of Pharmacy, University Hospital, University of Yamanashi
  • Higashi Kenjirou
    Graduate School of Pharmaceutical Sciences, Chiba University
  • Suzuki Masahiko
    Department of Pharmacy, University Hospital, University of Yamanashi
  • Moribe Kunikazu
    Graduate School of Pharmaceutical Sciences, Chiba University
  • Yamamoto Keiji
    Graduate School of Pharmaceutical Sciences, Chiba University
  • Oguchi Toshio
    Department of Pharmacy, University Hospital, University of Yamanashi

Bibliographic Information

Other Title
  • Development of sarpogrelate external preparation for intractable pain control (1) Pre-formulation study on application of modified β-cyclodextrins
  • Development of sarpogrelate external preparation for intractable pain control 1 Pre formulation study on application of modified v cyclodextrins

Search this article

Description

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.

Journal

Citations (1)*help

See more

References(13)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top