Gel sustained-release preparation capable of improving ring-close rates of camptothecin and derivative lactone ring thereof

A slow-release preparation, camptothecin technology, applied in the field of medicine, can solve the problems of loss of anti-cancer activity, insufficient closed-loop rate, and it is difficult to load hydrophobic drugs into it, so as to enhance the activity, reduce the drug dosage, and improve the closed-loop rate. Effect

Inactive Publication Date: 2011-10-12
FUDAN UNIV
View PDF2 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Under neutral and alkaline conditions, the lactone ring opens, resulting in the loss of anticancer activity; under the physiological conditions of pH 7.4 and 37°C, the ring closure rate of most camptothecin and its derivatives is less than 10%.
However, traditional hydrogels such as PEG hydrogels are difficult to control the release of small-molecule hydrophilic drugs, and the drugs are released quickly and completely; it is also difficult to load hydrophobic drugs into them.

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
  • Gel sustained-release preparation capable of improving ring-close rates of camptothecin and derivative lactone ring thereof
  • Gel sustained-release preparation capable of improving ring-close rates of camptothecin and derivative lactone ring thereof
  • Gel sustained-release preparation capable of improving ring-close rates of camptothecin and derivative lactone ring thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 In a 500 ml three-necked flask, add 30 g of dihydroxy polyethylene glycol (1500), remove water under vacuum at 130 °C for 4 hours, cool to 70 °C with argon, add 60 g of lactide, 15 g of glycolide, and 26 mg of octanoic acid Stannous (containing a small amount of toluene), evacuated at 100 °C for 30 minutes, passed argon, heated to 130 °C and reacted for 12 hours. After the reaction was completed, the product was poured out while hot, and after cooling, the product was dissolved in dichloromethane, and ether was precipitated to obtain the desired gel material.

Embodiment 2

[0061] Example 2 In a 500 ml three-necked flask, add 30 g of dihydroxy polyethylene glycol (1500), remove water under vacuum at 130 °C for 4 hours, cool to 70 °C with argon, add 48 g of lactide, 26 mg of stannous octoate (containing a small amount of water) Toluene), evacuated at 100 °C for 30 minutes, passed argon, heated to 130 °C and reacted for 12 hours. After the reaction was completed, the product was poured out while hot, and after cooling, the product was dissolved in dichloromethane, and ether was precipitated.

[0062] Take 15 g of the above materials, add 4 g of succinic anhydride, and 2 mL of pyridine, dissolve them in 100 mL of dichloromethane, and reflux for 48 hours. Most of the dichloromethane and pyridine were removed by suspension, washed with 80°C hot water (add a few drops of hydrochloric acid), pyridine and dichloromethane were removed, and freeze-dried to obtain a gel material with a carboxyl end group.

Embodiment 3

[0063] Example 3 In a 500 ml three-necked flask, add 30 g of dihydroxy polyethylene glycol (1500), dewater at 130 °C for 4 hours, cool to 70 °C with argon, add 34 g of lactide, 34 g of caprolactone, and 26 mg of octanoic acid Stannous (containing a small amount of toluene), evacuated at 100 °C for 30 minutes, passed argon, heated to 130 °C and reacted for 12 hours. After the reaction was completed, the product was poured out while hot, and after cooling, the product was dissolved in dichloromethane, and ether was precipitated to obtain the desired gel material.

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 belongs to the technical field of medicine and in particular relates to a gel sustained-release preparation capable of improving ring-close rates of a camptothecin and a derivative lactone ring thereof. The gel sustained-release preparation is composed of a amphipathy block copolymer, an anti-tumor medicine in effective dose and a solvent, wherein the amphipathy block copolymer is constructed by taking a polyethylene glycol as a hydrophilic block and a polyester as a lyophobic block, and the tail end of the block polymer is connected with a functional end group; the anti-tumor medicine is selected from the camptothecin and the derivative thereof. The gel preparation can be used for effectively improving the ring-close rates of the born camptothecin and derivative lactone ring thereof. The preparation can be administrated through injection; and the encapsulated medicine can be slowly released after the preparation is gelled in situ in a body. The thermo-sensitive hydrogel preparation can be used for enhancing the activity of the medicine, and obviously reducing the required medicine dosage, and can be injected into a tumor or around the tumor, or administrated in a tumor cavity after the surgery; and the gel sustained-release preparation has a passive targeting function, can be used for effectively reducing the general reaction of the medicine and can be used for treating the tumor at different stages.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a temperature-sensitive hydrogel sustained-release preparation and a preparation method thereof. Background technique [0002] Clinical practice has proved that traditional chemotherapy methods for the treatment of tumors often have large side effects, and the effective concentration of drugs to reach the local tumor is low, so the chemotherapy effect is not good. Increasing the local concentration of drugs at the tumor site, thereby enhancing the effect of chemotherapy, is a current research hotspot. Among them, local tumor administration can be passively targeted to the tumor site, thereby increasing the effective therapeutic concentration. Because of its similarity with tissues, hydrogels have good biocompatibility and are excellent materials for constructing topical drug delivery systems. [0003] Camptothecin and its derivatives are topoisomerase I inhibitors....

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 Applications(China)
IPC IPC(8): A61K9/00A61K31/4745A61K47/34A61P35/00
Inventor 丁建东常广涛慈天元俞麟
Owner FUDAN UNIV
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