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Liquid preparation for improving active ring-closing rate of camptothecin compounds and its preparation method and application

A technology of liquid preparations and camptothecin, which is applied in the field of medicine and can solve problems such as changing the ratio of active ingredients of drug molecules

Inactive Publication Date: 2015-12-02
FUDAN UNIV
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  • 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

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  • Liquid preparation for improving active ring-closing rate of camptothecin compounds and its preparation method and application
  • Liquid preparation for improving active ring-closing rate of camptothecin compounds and its preparation method and application
  • Liquid preparation for improving active ring-closing rate of camptothecin compounds and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1-9

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

Embodiment 1

[0041] Take 15g of polyethylene glycol 1500 (PEG1500), add 5g of succinic anhydride, 2ml of pyridine, dissolve in 200ml 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 20g of monomethoxypolyethylene glycol 2000 (PEG2000), add 5g of succinic anhydride, 2ml of pyridine, dissolve in 200ml 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.

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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

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/4745A61K47/34A61P35/00A61K47/10
Inventor 丁建东慈天元李婷俞麟
Owner FUDAN UNIV
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