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Development of Sarpogrelate External Preparation for Intractable Pain Control. I. Pre-formulation Study on Application of Modified .BETA.-Cyclodextrins
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- Hanawa Kazumi
- Department of Pharmacy, University Hospital, University of Yamanashi Graduate School of Pharmaceutical Sciences, Chiba University
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- Hanawa Takehisa
- Department of Pharmacy, University Hospital, University of Yamanashi
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- Tsuchiya Chikako
- Department of Pharmacy, University Hospital, University of Yamanashi
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- Higashi Kenjirou
- Graduate School of Pharmaceutical Sciences, Chiba University
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- Suzuki Masahiko
- 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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- Oguchi Toshio
- Department of Pharmacy, University Hospital, University of Yamanashi
Bibliographic Information
- Other Title
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- 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
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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
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 58 (1), 45-50, 2010
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390282679146488448
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- NII Article ID
- 130000140763
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 10497847
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- PubMed
- 20045965
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL Search
- Crossref
- CiNii Articles
- OpenAIRE
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- Abstract License Flag
- Disallowed