Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Liquid preparation for increasing active closed-loop rate of camptothecin compounds as well as preparation method and applications of liquid preparation

A liquid preparation, camptothecin technology, applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of changing the proportion of active ingredients in drug molecules

Inactive Publication Date: 2013-03-13
FUDAN UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Polyethylene glycol is a pharmaceutical excipient that has been approved by the FDA. It has been widely used as a solubilizer and modifier in pharmaceutical preparations. Some insoluble drugs are compatibilized by PEG, but PEG is used to change drug molecules (philic Aqueous drugs and hydrophobic drugs) the proportion of active ingredients has not been reported

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
  • Liquid preparation for increasing active closed-loop rate of camptothecin compounds as well as preparation method and applications of liquid preparation
  • Liquid preparation for increasing active closed-loop rate of camptothecin compounds as well as preparation method and applications of liquid preparation
  • Liquid preparation for increasing active closed-loop rate of camptothecin compounds as well as preparation method and applications of liquid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-9

[0039] Examples 1-9: Different end groups of polyethylene glycol

Embodiment 1

[0041] Take 15 g of polyethylene glycol 1500 (PEG1500), add 5 g of succinic anhydride, 2 ml of pyridine, dissolve in 200 ml of dichloromethane, and reflux for 48 hours. After removing part of the organic solvent and pyridine by suspension evaporation, unreacted succinic anhydride was precipitated by cooling, and the filtrate was filtered off. Rotary evaporation again to remove most of the organic solvent, precipitation with 10 times excess diethyl ether, filtration to obtain the product, vacuum drying to obtain a carrier material with carboxyl groups at both ends.

Embodiment 2

[0043] Take 20 g of monomethoxypolyethylene glycol 2000 (PEG2000), add 5 g of succinic anhydride, 2 ml of pyridine, dissolve in 200 ml of dichloromethane, and reflux for 48 hours. After removing part of the organic solvent and pyridine by suspension evaporation, unreacted succinic anhydride was precipitated by cooling, and the filtrate was filtered off. Rotary evaporation again to remove most of the organic solvent, precipitation with 10 times excess ether, filtration to obtain the product, and vacuum drying to obtain a carrier material with a single terminal group of carboxyl group.

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 preparation for increasing the active closed-loop rate of camptothecin compounds through simply adding polyethylene glycol. The liquid preparation is prepared from polyethylene glycol, camptothecin derivatives and a dispersion medium, wherein the polyethylene glycol is taken as an additive, the camptothecin derivatives are taken as medicament molecules, the dispersion medium is taken as a solvent, and the main body of the dispersion medium is water. The main additive is polyethylene glycol, and the medicament molecules are one or more of camptothecin, 10-hydroxycamptothecine, 9-nitrocamptothecin, 9-aminocamptothecin, 7-ethyl-10-hydroxycamptothecine, Topotecan, Irinotecan, Rubitecan, Exatecan, Belotecan, Karenitecin, Chimmitecan, Gimatecan, and the like. Through simply adding polyethylene glycol, the preparation can significantly improve the active closed-loop rate of camptothecin drugs, enhances the medicament effect, and can effectively reduce the general reaction of medicament, and therefore, the preparation is expected to be used in the cancer treatment of different stages.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a liquid preparation for increasing the active ring-closing rate of camptothecin compounds and its preparation method and application. Background technique [0002] Camptothecin is an active molecule of anticancer drugs, which was isolated from camptotheca in our country in the 1960s, hence the name. Due to its poor water solubility and high toxicity and side effects, some functional groups are usually modified on active non-sensitive sites to improve drug efficacy and water solubility. At present, two camptothecin derivatives, irinotecan (CPT-11) and topotecan (Topotecan) have been approved by the State Food and Drug Administration for clinical use, and have been widely used in gastric cancer, esophageal cancer, and pancreatic cancer. and colon cancer treatment. But almost all camptothecin drugs are faced with the problem of instability of their own structure, su...

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
IPC IPC(8): A61K9/00A61K31/4745A61K47/34A61P35/00A61K47/10
Inventor 丁建东慈天元李婷俞麟
Owner FUDAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com