| 論文名 |
A novel aqueous parenteral formulation of docetaxel using prodrugs. |
| 著者 |
Min-Ho Park
Chang-Gu Keum
Jae-Young Song
Daehee Kim
Cheong-Weon Cho
|
| キーワード |
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| 出版年月 |
1970年1月 |
| 発表先 |
Int J Pharm. 2014 Feb 28;462(1-2):1-7. doi: 10.1016/j.ijpharm.2013.12.027. Epub 2013 Dec 25. |
| WEBサイト |
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| 論文概要（和文） |
プロドラッグを使用したドセタキセルの新規水性非経口製剤 |
| 論文概要（英文） |
The aim of this study is to develop an aqueous parenteral solution of docetaxel using prodrugs. Docetaxel (DTX) is a highly lipophilic drug and practically insoluble in water. To overcome insolubility of docetaxel, three kinds of docetaxel prodrugs were synthesized using succinyl linker such as DTX-G, DTX-L or DTX-S and physicochemically characterized. The solubility of docetaxel prodrugs was determined by changing the concentration and type of surfactants, cosolvents or cyclodextrins. It was observed that the novel mixture of 15% PEG 400, 2.5% Tween 80 and 20% hydroxypropyl-β-cyclodextrin significantly increased the solubility of DTX-G up to 5.7 mg/mL. After subjected to the study of the hemolytic and cytotoxic activities, it was shown that the novel mixture did not show the hemolysis compared to Taxotere. It was suggested this novel mixture might have the potential to develop an aqueous parenteral formulation. |
