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Lidocaine self-sacrificially improves the skin permeation of the acidic and poorly water-soluble drug etodolac via its transformation into an ionic liquid
https://tokushima-u.repo.nii.ac.jp/records/2008042
https://tokushima-u.repo.nii.ac.jp/records/200804281d58ad7-3a04-4ea0-ac93-0e4419634e6c
| 名前 / ファイル | ライセンス | アクション |
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ejpb_102_92.pdf (1.19 MB)
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| Item type | 文献 / Documents(1) | |||||||||||||||||||||||
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| 公開日 | 2020-12-24 | |||||||||||||||||||||||
| アクセス権 | ||||||||||||||||||||||||
| アクセス権 | open access | |||||||||||||||||||||||
| 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 | |||||||||||||||||||||||
| 出版社版DOI | ||||||||||||||||||||||||
| 関連識別子 | https://doi.org/10.1016/j.ejpb.2016.03.003 | |||||||||||||||||||||||
| 関連名称 | 10.1016/j.ejpb.2016.03.003 | |||||||||||||||||||||||
| 出版タイプ | ||||||||||||||||||||||||
| 出版タイプ | VoR | |||||||||||||||||||||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||||||||||||||
| タイトル | ||||||||||||||||||||||||
| タイトル | Lidocaine self-sacrificially improves the skin permeation of the acidic and poorly water-soluble drug etodolac via its transformation into an ionic liquid | |||||||||||||||||||||||
| 著者 |
ミワ, ヤスシ
× ミワ, ヤスシ
× ハマモト, ヒデトシ
× 石田, 竜弘
WEKO
1145
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| 内容記述 | Poor transdermal penetration of active pharmaceutical ingredients (APIs) impairs both bioavailability and therapeutic benefits and is a major challenge in the development of transdermal drug delivery systems. Here, we transformed a poorly water-soluble drug, etodolac, into an ionic liquid in order to improve its hydrophobicity, hydrophilicity and skin permeability. The ionic liquid was prepared by mixing etodolac with lidocaine (1:1, mol/mol). Both the free drug and the transformed ionic liquid were characterized by differential scanning colorimetry (DSC), infrared spectroscopy (IR), and saturation concentration measurements. In addition, in vitro skin-permeation testing was carried out via an ionic liquid-containing patch (Etoreat patch). The lidocaine and etodolac in ionic liquid form led to a relatively lower melting point than either lidocaine or etodolac alone, and this improved the lipophilicity/hydrophilicity of etodolac. In vitro skin-permeation testing demonstrated that the Etoreat patch significantly increased the skin permeation of etodolac (9.3-fold) compared with an etodolac alone patch, although an Etoreat patch did not increase the skin permeation of lidocaine, which was consistent with the results when using a lidocaine alone patch. Lidocaine appeared to self-sacrificially improve the skin permeation of etodolac via its transformation into an ionic liquid. The data suggest that ionic liquids composed of approved drugs may substantially expand the formulation preparation method to meet the challenges of drugs which are characterized by poor rates of transdermal absorption. | |||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||
| 主題 | Ionic liquid | |||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||
| 主題 | Poorly water soluble drug | |||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||
| 主題 | Skin permeability | |||||||||||||||||||||||
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| 主題 | Topical delivery | |||||||||||||||||||||||
| キーワード | ||||||||||||||||||||||||
| 主題 | Etodolac | |||||||||||||||||||||||
| 書誌情報 |
en : European Journal of Pharmaceutics and Biopharmaceutics 巻 102, p. 92-100, 発行日 2016-03-02 |
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| 収録物識別子タイプ | ISSN | |||||||||||||||||||||||
| 収録物識別子 | 09396411 | |||||||||||||||||||||||
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| 収録物識別子タイプ | NCID | |||||||||||||||||||||||
| 収録物識別子 | AA10836618 | |||||||||||||||||||||||
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| 収録物識別子タイプ | NCID | |||||||||||||||||||||||
| 収録物識別子 | AA11527164 | |||||||||||||||||||||||
| 出版者 | ||||||||||||||||||||||||
| 出版者 | Elsevier | |||||||||||||||||||||||
| 権利情報 | ||||||||||||||||||||||||
| 権利情報 | This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/). | |||||||||||||||||||||||
| EID | ||||||||||||||||||||||||
| 識別子 | 310610 | |||||||||||||||||||||||
| 言語 | ||||||||||||||||||||||||
| 言語 | eng | |||||||||||||||||||||||
