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  1. 学術雑誌論文
  2. Chemical & pharmaceutical bulletin

Quetiapine Free Base Complexed with Cyclodextrins to Improve Solubility for Parenteral Use

https://stella.repo.nii.ac.jp/records/459
https://stella.repo.nii.ac.jp/records/459
da778d41-d8ed-40c8-9c2f-47f0ba63002b
名前 / ファイル ライセンス アクション
ChemPharmBull_61‐8_p809.pdf ChemPharmBull_61‐8_p809.pdf (1.1 MB)
Item type 学術雑誌論文 / Journal Article(1)
公開日 2016-02-01
タイトル
タイトル Quetiapine Free Base Complexed with Cyclodextrins to Improve Solubility for Parenteral Use
言語 en
言語
言語 eng
キーワード
言語 en
主題Scheme Other
主題 quetiapine
キーワード
言語 en
主題Scheme Other
主題 cyclodextrin
キーワード
言語 en
主題Scheme Other
主題 parenteral administration
キーワード
言語 en
主題Scheme Other
主題 inclusion compound
キーワード
言語 en
主題Scheme Other
主題 solubility enhancement
キーワード
言語 en
主題Scheme Other
主題 antipsychotic drug
資源タイプ
資源タイプ識別子 http://purl.org/coar/resource_type/c_6501
資源タイプ journal article
著者 Ogawa, Noriko

× Ogawa, Noriko

en Ogawa, Noriko

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Kaga, Mayumi

× Kaga, Mayumi

en Kaga, Mayumi

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Endo, Tomohiro

× Endo, Tomohiro

en Endo, Tomohiro

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Nagase, Hiromasa

× Nagase, Hiromasa

en Nagase, Hiromasa

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Furuishi, Takayuki

× Furuishi, Takayuki

en Furuishi, Takayuki

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Yamamoto, Hiromitsu

× Yamamoto, Hiromitsu

en Yamamoto, Hiromitsu

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Kawashima, Yoshiaki

× Kawashima, Yoshiaki

en Kawashima, Yoshiaki

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Ueda, Haruhisa

× Ueda, Haruhisa

en Ueda, Haruhisa

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抄録
内容記述タイプ Abstract
内容記述 Quetiapine, an antipsychotic drug used for schizophrenia treatment, is poorly water soluble, and therefore, administration of the more water-soluble quetiapine fumarate is preferred. Absorption of quetiapine through biological membranes may be improved by enhancing the solubility of the quetiapine base, the non-ionic form. In this study, the currently used salt form was converted into the free base (oily material). We employed cyclodextrins (CDs) as pharmaceutical additives to improve the solubility of the quetiapine base. The formation of quetiapine–β-cyclodextrin (β-CD) complexes was studied by phase solubility studies, continuous variation method, NMR spectroscopy, and powder X-ray diffraction. The formation of a poorly water-soluble complex was confirmed by the phase solubility study, and the interaction between quetiapine and β-CD in water was confirmed by NMR spectroscopy. In addition, the effects of β-CD derivatives (glucosyl-β-CD, maltosyl-β-CD, 2-hydroxypropyl-β-CD, dimethyl-β-CD, and trimethyl-β-CD) on the solubility of the quetiapine base were studied. The findings indicated that the aforementioned hydrophilic β-CD derivatives could be used as pharmaceutical additives of quetiapine for parenteral formulations as a result of the improved solubility of the quetiapine base because of inclusion complexation. Therefore, converting the currently used salt form into the free base, investigating the free base as a candidate for CD inclusion, and converting the oily material such as the free base into a powder by forming an inclusion complex that is easy to deal with is considered a worthwhile approach that may lead to novel formulations of the drug in question.
書誌情報 Chemical and Pharmaceutical Bulletin

巻 61, 号 8, p. 809-815, 発行日 2013
出版者
出版者 日本薬学会
ISSN
収録物識別子タイプ ISSN
収録物識別子 0009-2363
書誌レコードID
収録物識別子タイプ NCID
収録物識別子 AA00602100
論文ID(NAID)
関連タイプ isIdenticalTo
識別子タイプ NAID
関連識別子 130003360812
DOI
関連タイプ isIdenticalTo
識別子タイプ DOI
関連識別子 info:10.1248/cpb.c13-00157
権利
権利情報 日本薬学会
フォーマット
内容記述タイプ Other
内容記述 application/pdf
著者版フラグ
出版タイプ VoR
出版タイプResource http://purl.org/coar/version/c_970fb48d4fbd8a85
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