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Method for preparing negative pressure anti-solvent of water-soluble nano-taxol powder

A kind of paclitaxel and nanotechnology, applied in the direction of organic chemistry and the like, can solve the problems of unsuitable implementation of large-scale production conditions, and achieve the effects of low production cost, low environmental pollution and high yield

Inactive Publication Date: 2012-09-05
NORTHEAST FORESTRY UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its technical feature is to use high-speed stirring and ultrasonic vibration crystallization under the action of surfactants. Stirring is the key to controlling the shape and size of crystallization. However, high-speed stirring and ultrasonic vibration are only suitable for small-scale production, and large-scale production conditions are not suitable for implementation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0022] First prepare the paclitaxel absolute ethanol solution with a concentration of 20mg / mL, in a vacuum of -0.06MPa and an air flow of 2m 3 Under the negative pressure cavitation stirring state of / h, inject this solution into the anti-solvent water of 5 times its volume, control the crystallization temperature to be 4 ℃, crystallize for 5 minutes, then plate and frame filter the mixed solution, and the obtained filter cake is at 80 The water-soluble paclitaxel powder is obtained after drying at ℃ for 24 hours, and the average particle size is lower than 1000nm.

example 2

[0024] First prepare a paclitaxel N-methyl-pyrrolidone solution with a concentration of 5mg / mL, and the vacuum degree is -0.06MPa and the ventilation rate is 5m 3 Under the negative pressure cavitation stirring state of / h, inject this solution into the anti-solvent water of 8 times its volume number, control the crystallization temperature to be 25 ℃, crystallize for 8 minutes, then plate and frame filter the mixed solution, and the obtained filter cake is at 80 After drying at ℃ for 24 hours, pulverize to obtain the water-soluble paclitaxel powder, the average particle size of which is lower than 600nm.

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Abstract

The invention discloses a method for preparing a negative pressure solvent of water-soluble nano-taxol powder. The method is characterized by comprising the following steps of: preparing the solution of 1 to 100 mg / ml taxol anhydrous alcohol or N-methyl-pyrrolidone; in a negative pressure cavitation stirring state, mixing the solution and anti-solvent water in an amount which is 3 to 8 times volume of the solution at the temperature of 4 to 40 DEG C and crystallizing; filtering mixed liquid by using a plate frame; drying an obtained filter cake at the temperature of 70 to 105 DEG C; crushing the dried filter cake to obtain the water-soluble nano-taxol powder; and recovering filtrate solvent for recycling. The taxol powder obtained by the method has uniform grain size distribution, high water solubility, high yield and low cost, and is easy to industrialize.

Description

technical field [0001] The invention relates to a method for preparing a drug water-soluble ultrafine powder, in particular to an anti-solvent preparation method for an anticancer drug paclitaxel water-soluble ultrafine powder. technical background [0002] Paclitaxel was isolated by American chemists Vanney and Wall in 1963 from the bark and wood of a Pacific fir growing in the large forests of the western United States. It is a complex secondary metabolite and the only one known so far. A drug that promotes microtubule polymerization and stabilizes polymerized microtubules. According to II-III clinical studies, paclitaxel is mainly suitable for the treatment of ovarian cancer and breast cancer, and also has a certain effect on lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma and brain tumor. [0003] Paclitaxel is insoluble in water, so it is not convenient for direct clinical use. It has high fat solubility and poor water solubility, and is often...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/14
Inventor 祖元刚赵修华祖柏实赵冬梅姜守刚王微陈小强祖纯林张晓楠孙志强
Owner NORTHEAST FORESTRY UNIVERSITY