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Chondroitin Sulfate–Glycyl-Prednisolone Conjugate as Arthritis Targeting System: Localization and Drug Release in Inflammatory Joints
https://stella.repo.nii.ac.jp/records/577
https://stella.repo.nii.ac.jp/records/5773c708158-d3f4-451a-9d03-521f7fa0e8a4
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
BiolPharmBull_37‐10_p1641.pdf (780.8 kB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||
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| 公開日 | 2016-02-08 | |||||||||||
| タイトル | ||||||||||||
| タイトル | Chondroitin Sulfate–Glycyl-Prednisolone Conjugate as Arthritis Targeting System: Localization and Drug Release in Inflammatory Joints | |||||||||||
| 言語 | en | |||||||||||
| 言語 | ||||||||||||
| 言語 | eng | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | conjugate | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | drug distribution | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | inflammatory joint | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | chondroitin sulfate | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | prednisolone | |||||||||||
| キーワード | ||||||||||||
| 言語 | en | |||||||||||
| 主題Scheme | Other | |||||||||||
| 主題 | potential enhancement | |||||||||||
| 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 |
Onishi, Hiraku
× Onishi, Hiraku
× Yoshida, Ryuya
× Matsuyama, Mototaka
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| 抄録 | ||||||||||||
| 内容記述タイプ | Abstract | |||||||||||
| 内容記述 | Chondroitin sulfate–glycyl-prednisolone conjugate (CS–GP) was previously demonstrated to exhibit superior anti-arthritic effects compared to prednisolone (PD) alone. In this study, CS–GP was examined for its pharmacokinetic features and tropism for inflammatory joints using rats with adjuvant-induced arthritis in order to identify the mechanism of the potential enhancement. After intravenous injection (2.5 mg PD eq./kg), CS–GP yielded an area under the curve (AUC) of the total (free+conjugated) drug much higher than that of PD alone. After intravenous administration at the same dose, the drug distribution to the hind paw inflammatory joints was investigated. For PD alone, the PD concentration was 1.2–1.7 µg/g at 1 h and fell to 0.12–0.14 µg/g at 24 h. In contrast, CS–GP maintained the total concentration in the range of 0.55–0.97 µg/g for 1–24 h, and maintained the free PD concentration at 0.06–0.16 µg/g for 1–24 h. Furthermore, at 24 h after intravenous administration (2.5 mg PD eq./kg), CS–GP exhibited a higher total drug concentration in arthritic rats than in healthy rats. These findings suggested that CS–GP may have the ability to target inflammatory joints. As the apparent molecular weight of CS–GP became greater in plasma, it might interact with blood components and cause high plasma retention and good tropism to the inflammatory sites. Enhancement of the anti-inflammatory potential of CS–GP was found to be due to good maintenance of drug levels in the inflamed area. | |||||||||||
| 書誌情報 |
Biological and Pharmaceutical Bulletin 巻 37, 号 10, p. 1641-1649, 発行日 2014 |
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| 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 | 0918-6158 | |||||||||||
| 書誌レコードID | ||||||||||||
| 収録物識別子タイプ | NCID | |||||||||||
| 収録物識別子 | AA10885497 | |||||||||||
| 論文ID（NAID） | ||||||||||||
| 関連タイプ | isIdenticalTo | |||||||||||
| 識別子タイプ | NAID | |||||||||||
| 関連識別子 | 130004693796 | |||||||||||
| DOI | ||||||||||||
| 関連タイプ | isIdenticalTo | |||||||||||
| 識別子タイプ | DOI | |||||||||||
| 関連識別子 | info:10.1248/bpb.b14-00390 | |||||||||||
| 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 | |||||||||||
