Water soluble anticancer medicine taxol composite and its prepn

A paclitaxel compound and anti-cancer drug technology, which is applied in the direction of drug combination, anti-tumor drug, pharmaceutical formula, etc., can solve the problem of not obtaining the solid powder of the compound, and achieve the effect of improving low solubility

Inactive Publication Date: 2003-09-10
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Moser et al. studied the inclusion of bridged bicyclodextrin and paclitaxel in aqueous solution, but did not obtain a solid powder of the complex (J.Incl.Phenom.Mol.Chem.39, 2001, 13-18)

Method used

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  • Water soluble anticancer medicine taxol composite and its prepn
  • Water soluble anticancer medicine taxol composite and its prepn
  • Water soluble anticancer medicine taxol composite and its prepn

Examples

Experimental program
Comparison scheme
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Embodiment

[0024] Tetraethylenepentamine bridged bicyclodextrin and paclitaxel compound involved in the present invention are synthesized as follows:

[0025] 1) Synthesis of tetraethylenepentamine-bridged bicyclodextrin 2

[0026] The synthesis route of tetraethylenepentamine bridged dicyclodextrin is shown in Image 6 .

[0027] Add 1.3 g tetraethylenepentamine monomodified β-cyclodextrin and 1.3 g mono(6-oxo-6-p-toluenesulfonyl)-β-cyclodextrin into a 100 ml dry round bottom flask, then add 50 ml treated DMF was used as a solvent, stirred until dissolved under the protection of nitrogen, then heated to 80°C, and reacted for three days under the protection of nitrogen, the reaction mixture was dropped into 300ml of acetone, and the precipitate was collected by Buchner funnel suction filtration. This operation was repeated twice to obtain the crude product. Dissolve it in water, use CM Sephadex C-25 ion column for separation, use 1M ammonia water as eluent; then use Sephadex G-25 gel ...

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Abstract

The present invention relates to soluble anticancer medicine taxol composite and its preparation. The present invention is prepared directly with tetravinyl pentamine bridged dicyclodextrin and taxol in the compounding ratio of 0.5. The soluble anticancer medicine taxol composite of the present invention has taxol slubilizing and slow releasing effect and thus prolonged medicine effect. The present invention provides a new way for the clinical application of taxol as anticancer medicine.

Description

Technical field [0001] The invention relates to a water-soluble anticancer drug paclitaxel compound and a preparation method thereof, in particular to preparing a water-soluble compound of the anticancer drug paclitaxel by tetraethylenepentamine bridged bicyclodextrin functional molecules. The water-soluble anticancer drug paclitaxel complex can solubilize and slow the release of paclitaxel, thereby prolonging the drug effect, thus providing a new and feasible way for the anticancer drug paclitaxel to be used clinically. Background technique [0002] Paclitaxel (1, English name Paclitaxel, Taxol), the structure shown below, is a natural compound isolated from the bark of Pacific Yew by American chemists Wani and Wall. product. Yew (taxus) is a rare plant, which is a tree or a large shrub, and its scientific name in Chinese Botany is "yew". Plant classification belongs to gymnosperm subphylum, pine spruce class, taxaceae, yew family, yew genus. [0003] Paclitaxel has go...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61P35/00
Inventor 刘育陈国颂李莉张衡益
Owner NANKAI UNIV
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