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

A technology of liquid glue and camptothecin, which is applied in the direction of drug combination, emulsion delivery, anti-tumor drugs, etc., can solve the problems of loss of anti-tumor activity, structural instability, toxic and side effects, etc., to improve the active closed-loop rate, enhance Drug efficacy, effect of reducing systemic reactions

Inactive Publication Date: 2013-03-13
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But almost all camptothecin drugs are facing a serious problem - the instability of their own structure
as attached figure 1 As shown in , there is a lactone ring in the structure of camptothecin drugs, and it is easy to undergo ring-opening hydrolysis under neutral and alkaline conditions. It has been clearly pointed out in the literature that camptothecin class anticancer drugs, Only the closed-loop form is effective, once the ring is opened, the original anti-tumor activity will be lost, and some unavoidable toxic side effects will be caused

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-10

[0053] Examples 1-10: Synthesis of different polymeric support materials

Embodiment 1

[0055] Add 30g of dihydroxypolyethylene glycol (1500) into a 500ml three-necked flask, heat the oil bath to 130°C to remove water under vacuum for 4 hours, cool to 70°C with argon, add 59g of lactide, 7g of glycolide, 26 mg of stannous octoate (containing a small amount of toluene), evacuated at 100°C for 30 minutes, blown with argon, and heated to 140°C for 12 hours. After the reaction was completed, the product was poured out while it was hot. After cooling, the product was dissolved in dichloromethane and ether precipitated. The PLGA-PEG-PLGA micellar carrier material is obtained. The material was tested by H 1 NMR detection molecular weight is 1670-1500-1670, GPC detection molecular weight distribution coefficient ( M w / M n ) is 1.23.

Embodiment 2

[0057] Add 30g of monomethoxy-capped PEG (MPEG, 1500) into a 500ml three-necked flask, remove water under vacuum at 130°C for 4 hours, cool to 70°C with argon, add 31g of lactide, 7.5g of glycolide, 13 mg of stannous octoate (containing a small amount of toluene), evacuated at 100 °C for 30 minutes, passed argon, and heated to 130 °C for 12 hours. After the reaction is completed, pour the product into hot water at 80°C while it is still hot, and discard the upper part of the water after fully settling to obtain an MPEG-PLGA carrier material. The molecular weight detected by NMR is 1500-1820, and the molecular weight distribution coefficient detected by GPC ( M w / M n ) is 1.28.

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Abstract

The invention belongs to the technical field of drugs, and in particular relates to a liquid micellar preparation for increasing the active closed-loop rate of camptothecin derivatives as well as a preparation method and applications of the preparation. The preparation disclosed by the invention is prepared from a amphiphilic copolymer, medicament molecules and an aqueous medium, wherein the amphiphilic copolymer is taken as a carrier material, the medicament molecules of active-dose camptothecin derivatives are physically loaded in a micellar form, and the aqueous medium is taken as a main dissolvent. The main body structure of the carrier material takes polyethylene glycol as a hydrophilic segment and takes polyester, poly-amino acid or polyether as a hydrophobic segment, 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. The micellar preparation can significantly improve the active closed-loop rate of the camptothecin medicament, enhances the medicament effect, and can effectively reduce the general reaction of the 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 micellar preparation capable of increasing the active ring-closing rate of camptothecin derivatives, a preparation method and application thereof. Background technique [0002] Camptothecin is an active molecule of anticancer drugs isolated from camptotheca in our country in the 1960s. 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 facing a serious problem - the instability of their own structure. as attach...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/4745A61P35/00
Inventor 丁建东慈天元常广涛俞麟
Owner FUDAN UNIV
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