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Water-soluble paclitaxel anticancer drug compound and its preparation method and use

An anticancer drug, paclitaxel technology, applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of low encapsulation rate, price restriction, drug leakage stability, etc., to achieve high anticancer activity, good The effect of water solubility

Active Publication Date: 2017-04-05
NANJING YOUYI MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are more or less defects in various drug delivery systems, such as low encapsulation efficiency, drug leakage and stability, etc., which need to be further resolved
However, the high price of nab-paclitaxel for injection limits its clinical use

Method used

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  • Water-soluble paclitaxel anticancer drug compound and its preparation method and use
  • Water-soluble paclitaxel anticancer drug compound and its preparation method and use
  • Water-soluble paclitaxel anticancer drug compound and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Synthesis of embodiment 1 polyethylene glycol monomethyl ether (Mn=1000) paclitaxel-2'-diglycolate

[0059] The synthesis of the water-soluble paclitaxel anticancer drug compound comprises the following steps:

[0060] 1) Synthesis of Polyethylene Glycol Monomethyl Ether (Mn=1000) Diglycolate

[0061] method one:

[0062] The reaction formula is as follows:

[0063]

[0064] Experimental steps:

[0065] In a 100mL round bottom flask, add 2.400g (2.4mmol) of dried polyethylene glycol monomethyl ether (Mn=1000), 0.557g (4mmol) of diglycolic anhydride and 200mg of 2-ethylhexanoic acid tin (II ), then add 30mL xylene, stir, and heat to reflux under nitrogen protection until the reaction is complete. After removing the xylene in the reaction solution with a rotary evaporator, add 20 mL of ethyl acetate, stir, then add 10 mL of diethyl ether, a white solid precipitates, filter to remove the solid matter, and use a rotary evaporator to concentrate the filtrate to 10 mL,...

Embodiment 2

[0075] The preparation of embodiment 2 water-soluble paclitaxel anticancer drug compound (XBB-021)

[0076] Include in the present embodiment the injection that water, physiological saline (0.9% sodium chloride) or glucose (5%) injection are made, contain the water-soluble paclitaxel anticancer drug compound of the present invention in the preparation formula, each component is in formula The content in is calculated by weight percentage.

[0077] A. Deionized water injection of water-soluble paclitaxel anticancer drug compound

[0078] Add 100mg of water-soluble paclitaxel anticancer drug compound (XBB-021) into a 10mL volumetric flask, dilute it to 10mL with deionized water, and shake the composition of the produced injection as follows:

[0079] XBB-021 1.0%

[0080] Deionized water 99.0%.

[0081] The prepared injection was filtered through a 0.2 micron filter and filled into sterile glass vials.

[0082] B. Saline Injection of Water-Soluble Paclitaxel Anticancer Drug ...

Embodiment 3

[0092] The mensuration of embodiment 3 water-soluble paclitaxel anticancer drug compound (XBB-021) micelle particle size

[0093] The water-soluble paclitaxel anticancer drug compound (XBB-021) forms micelles after being dissolved in water, and the particle size of the micelles is measured by a ZetaPlus laser scattering particle size analyzer from BROOKHAVEN, USA. The measurement method is: weigh the drug (XBB-021) Add 5mg and 10mg into 2mL distilled water respectively, stir to make it fully dissolve, let it stand for 10min, and add the liquid into the sample pool (cuvette) after the bubbles disappear, pay attention that no bubbles will be generated during the adding of the sample, and then put Put the cuvette into the corresponding groove of the base of the sample cell, start the measurement, and measure each sample three times in parallel to get the average value.

[0094] See the experimental results image 3 and 4 . The results showed that: when the concentration of XBB...

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Abstract

The invention discloses a water-soluble paclitaxel anticancer drug compound. The water-soluble paclitaxel anticancer drug compound has a structure shown in the formula I. Anticancer drug active ingredients of paclitaxel and polyethylene glycol monoalkyl ether are covalently bound by a linking group (carbonylmethoxyacetyl) to form the water-soluble paclitaxel anticancer drug compound. The invention also relates to a preparation method and a use of the drug compound.

Description

technical field [0001] The present invention relates to a new anticancer drug compound and its preparation method and application, in particular to a water-soluble paclitaxel anticancer drug compound, its preparation, preparation method and application as an anticancer drug. Background technique [0002] Many compounds with anticancer activity have been an obstacle to drug development due to insolubility or poor stability in water and / or other biocompatible solvents, often leading to delays in drug development time. It is estimated that as many as 40 percent of screened potentially valuable drug candidates are rejected from formulation research and development due to their poor water solubility, and 30 percent of existing drugs are poorly soluble. Several technologies are currently being researched and developed to address the poor solubility of pharmaceutical compounds, including complexing agent technology to increase solubility, nanoparticle technology, microemulsion tech...

Claims

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Application Information

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IPC IPC(8): C07D305/14A61K31/337A61K9/08A61P35/00
CPCC07D305/14
Inventor 张跃华
Owner NANJING YOUYI MEDICAL TECH CO LTD
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