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Method for preparing docetaxel/beta-cyclodextrin clathrates

A technology of cyclodextrin inclusion complex and docetaxel, which is applied in the directions of non-active components of polymer compounds, medical preparations containing active components, drug combinations, etc., to achieve the effects of improving inclusion rate and high solubility

Inactive Publication Date: 2014-01-15
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] This patent proposes a method using supercritical CO 2 Preparation of docetaxel / β-cyclodextrin inclusion compound by method, so far there is no relevant report

Method used

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  • Method for preparing docetaxel/beta-cyclodextrin clathrates
  • Method for preparing docetaxel/beta-cyclodextrin clathrates
  • Method for preparing docetaxel/beta-cyclodextrin clathrates

Examples

Experimental program
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Embodiment 1

[0019] 1) Preparation of docetaxel / β-cyclodextrin inclusion compound

[0020] Weigh 100mg β-cyclodextrin with an analytical balance and place it in a 25ml volumetric flask, add pure water to constant volume to prepare a 4mg / ml β-cyclodextrin aqueous solution, weigh 25mg docetaxel and dissolve it in 1ml anhydrous methanol to prepare 25mg / ml Methanol solution of docetaxel. Take 5ml β-cyclodextrin aqueous solution and 0.04ml methanol solution of docetaxel in the autoclave successively, add a magnet, put the autoclave in a water bath at 35°C, turn on the magnetic stirring, and introduce carbon dioxide gas, when When the pressure in the autoclave reaches a certain pressure, the inlet valve is closed, and the autoclave is stabilized at 35° C. and 15 MPa, and stirred for four hours.

[0021] After the inclusion process in the supercritical high-pressure reactor is over, lower the temperature of the constant temperature water bath to room temperature, and gradually unscrew the air va...

Embodiment 2

[0033] Substantially the same as example 1, but wherein the supercritical reaction pressure is changed to 21MPa.

Embodiment 3

[0035]Substantially the same as example 1, but wherein the supercritical reaction pressure is changed to 25MPa.

[0036] in conclusion:

[0037] 1. The present invention proposes a method for preparing docetaxel / β-cyclodextrin inclusion compound using supercritical carbon dioxide fluid. By regulating the temperature and pressure of supercritical carbon dioxide fluid, the docetaxel / β-cyclodextrin Inclusion rate of docetaxel in fine clathrate. The results are shown in Table 1. The inclusion rate of docetaxel in the β-cyclodextrin inclusion compound is as high as 17.9%, much higher than the 0.1% encapsulation rate of the β-cyclodextrin inclusion compound prepared by the traditional method.

[0038] 2. The solubility of docetaxel / β-cyclodextrin inclusion compound prepared by supercritical carbon dioxide method in water is higher than that of docetaxel / β-cyclodextrin inclusion compound obtained by conventional solution-stirring method , the results are shown in Table 1. The solub...

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Abstract

The invention discloses a method for preparing docetaxel / beta-cyclodextrin clathrates by a supercritical carbon dioxide fluid. The docetaxel / beta-cyclodextrin clathrates with different clathration rates can be synthesized by changing preparation pressure. Compared with the a general solution-stirring method for preparing the docetaxel / beta-cyclodextrin clathrates, the method prepared by the invention, by regulating and controlling the temperature and pressure of the supercritical carbon dioxide fluid, substantially raises the clathration rates of the docetaxel in the docetaxel / beta-cyclodextrin clathrates. Furthermore, the solubility of the docetaxel / beta-cyclodextrin clathrates prepared by the supercritical carbon dioxide method in water is higher than that of the docetaxel / beta-cyclodextrin clathrates prepared by the general solution-stirring method.

Description

technical field [0001] The invention relates to the field of drug carrier preparation, and more specifically, relates to a preparation method of inclusion compound of β-cyclodextrin and docetaxel. Background technique [0002] Docetaxel is a semi-synthetic taxane compound, which is obtained by structure modification from the needle leaf extract of Taxus berry. It is white powdery solid, molecular formula C 43 h 53 NO 14 , is an antineoplastic drug that acts on microtubules. At present, it is mainly used in the treatment of breast cancer, ovarian cancer, prostate cancer and non-alpha cell lung cancer. Since docetaxel is poorly soluble in water (solubility at room temperature is 2.903 μg / ml), the injection made of docetaxel Tween-80 solution, 13% ethanol and normal saline or glucose is used in clinical application. However, the stability of Tween solution is low, and the clinically used injections are prone to precipitate and precipitate, which may easily cause adverse re...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K31/337A61P35/00
Inventor 安学勤龚俊孔立纲
Owner EAST CHINA UNIV OF SCI & TECH
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