Chlorambucil multi-targeting medicine carrying system and preparation method and application thereof

A technology of chlorambucil and drug-carrying system, which is applied in the field of pharmaceuticals, can solve the problems of high toxicity and side effects, poor cell selectivity, etc., achieve wide applicability, expand the scope of application, and improve the effect of drug invisibility

Inactive Publication Date: 2013-11-20
WUHAN UNIV OF TECH
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, aiming at and strengthening the basic research on common problems such as poor cell selectivity, large toxic and side effects, and serious adverse reactions, especially tumor cell MDR, which are common in this type of chemotherapeutic drug preparations, it is important to develop new drug delivery systems for chemotherapeutic drugs and improve the treatment of malignant tumors. The effect has important theoretical and practical significance

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Chlorambucil multi-targeting medicine carrying system and preparation method and application thereof
  • Chlorambucil multi-targeting medicine carrying system and preparation method and application thereof
  • Chlorambucil multi-targeting medicine carrying system and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 1. Preparation of PEG-HA-CHL Components

[0042] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0043] 10g (5mmol) PEG-2000 was placed in a 250ml three-necked flask with a condenser, a stirrer and a thermometer, and 100ml of chloroform (CaH 2 After the dissolution, add 2.5g (25mmol) of succinic anhydride, heat to dissolve, add 2ml of dry pyridine at the same time, reflux reaction under stirring for 6 hours, stop the reaction and cool to room temperature, and the reaction mixture is decompressed Evaporate until it becomes viscous, add a large amount of anhydrous ether to precipitate a white product, filter it with suction, dissolve the product with 30ml of dichloromethane, filter off the insoluble matter, add anhydrous ether to precipitate a white product, repeat several times, and filter with suction Then vacuum-dry to constant weight to obtain carboxyl-terminated polyethylene glycol, which is weighed;

[0044] (2) Preparation of PEG-HA

...

Embodiment 2

[0063] 1. Preparation of PEG-HA-CHL Components

[0064] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0065] Put 15g of PEG-2000 in a 250mL three-neck flask with a condenser, agitator and thermometer, add 150mL of chloroform (steamed out in the presence of CaH2) to dissolve, after the dissolution is complete, add 3.75g of succinic anhydride, heat to dissolve, and add 3mL of dry pyridine was stirred and refluxed for 6 hours. After the reaction was stopped, it was cooled to room temperature. Dissolve the product in methane, filter out the insoluble matter, add anhydrous ether to precipitate a white product, repeat several times, vacuum-dry to constant weight after suction filtration, obtain carboxyl-terminated polyethylene glycol, and weigh;

[0066] (2) Preparation of PEG-HA

[0067] Dissolve 0.75 g of carboxy-terminated polyethylene glycol obtained in step (1) in 3.75 g of hyaluronic acid hydrolyzate, pour it into a 500 mL three-necked flask equ...

Embodiment 3

[0086] 1. Preparation of PEG-HA-CHL Components

[0087] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0088] Put 20g (5mmol) PEG-2000 in a 500mL three-necked flask with a condenser, a stirrer and a thermometer, add 200mL chloroform (distilled out in the presence of CaH2) to dissolve, and add 5g (50mmol) succinic anhydride after the dissolution is complete, Heat to dissolve, add 4mL of dry pyridine at the same time, reflux reaction under stirring for 6 hours, stop the reaction and cool to room temperature, the reaction mixture is evaporated under reduced pressure until it becomes viscous, the residue is added with a large amount of anhydrous ether to precipitate a white product, suction filtered, Dissolve the product with 60ml of dichloromethane, filter out the insoluble matter, add anhydrous ether to precipitate a white product, repeat several times, vacuum-dry to constant weight after suction filtration, obtain carboxyl-terminated polyethylene gl...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a chlorambucil multi-targeting medicine carrying system and a preparation method and application thereof in the aspect of anti-tumor medicines. The chlorambucil multi-targeted medicine carrying system is prepared by mixing a PEG-HA-CHL (polyethylene glycol-hyaluronic acid-chlorambucil) component with an Fe3O4 magnetofluid component in weigh ratio of 1:(1-5), wherein the PEG-HA-CHL comprises the following components in parts by weight: 20-100 parts of chlorambucil, 500-1500 parts of PEG, 100-500 parts of HA, 10-50 parts of DCC (dicyclohexylcarbodiimide), 1-10 parts of DMAP (dimethylamino pyridine), 100-500 parts of butanedioic anhydride, 10-50 parts of EDC (dichloroethane) and 20-100 parts of sodium hydrogensulfite. The invention has the advantages of intelligent medicine release, multiple targeting and better reverse medicine resistance, controlled medicine release, better blood circulation stability, better invisibility and wide applicability.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a tumor cell multi-targeting drug-carrying system, a preparation method of the drug-carrying system and the application of the drug-carrying system in antitumor drugs. Background technique [0002] At present, the treatment of malignant tumors is mainly combined with surgery and chemotherapy. Chemotherapy is a necessary treatment method. However, the existing chemotherapeutic drugs have poor selectivity for normal cells and tumor cells, and are prone to serious adverse reactions and multidrugs. Drug resistance (Multi-drug resistance, MDR), resulting in unsatisfactory chemotherapy effect. At present, any method that can increase the effective concentration of chemotherapy drugs in tumor cells is a feasible method to overcome MDR, such as using new preparations such as liposomes and targeted drug delivery systems for treatment. Therefore, aiming at and strengthening the basic research on ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K9/19A61K31/196A61K47/02A61P35/00A61K47/61
Inventor 徐海星许沛虎黄志军郑化刘霞姜晓晔李冉王玲
Owner WUHAN UNIV OF TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap