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Gel sustained-release injection containing camptothecin or derivatives thereof, and preparation method thereof

A technology for sustained-release injection and camptothecin, applied in the field of medicine, can solve the problems of limited medical use, no longer thermal gelation, loss of sol-gel transition, etc., and achieves the effect of improving the closed-loop rate

Inactive Publication Date: 2011-10-05
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] (1) Exceeding a certain composition and / or molecular weight, it can only be completely dissolved in water or partially or completely become precipitated, thus losing the sol-gel transition and no longer having the relevant heat-sensitive gelling performance;
[0007] (2) In addition, even if some polymers can have heat-sensitive properties, their gelation temperature is not suitable for human application;
[0008] (3) The adjustment range and kinetic process of its degradation rate have certain limitations, which also limit its medical use

Method used

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  • Gel sustained-release injection containing camptothecin or derivatives thereof, and preparation method thereof
  • Gel sustained-release injection containing camptothecin or derivatives thereof, and preparation method thereof
  • Gel sustained-release injection containing camptothecin or derivatives thereof, and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] Add PEG (1500) into a 250 ml three-necked flask, heat the oil bath to 150°C, and vacuum filter for three hours while stirring to remove the residual moisture in the PEG, and then add DL-lactide with a molar ratio of 4:1 And glycolide, after heating under vacuum to make it melt completely, add 120 μl stannous octoate, the oil bath is heated up to 160 ℃, continue to react under argon atmosphere for 24 hours. After the reaction was completed, vacuum filtration was performed for two hours to remove unreacted monomers and low-boiling products. The initial product was dissolved in dichloromethane solution and precipitated with ether, the yield was about 80%. The number-average and weight-average molecular weight ( M n , M w ) were 5510 and 6390, respectively, and the molecular weight distribution coefficient ( M w / M n ) is 1.16. The copolymer itself does not have thermosensitive gelling properties in water.

Embodiment 2

[0072] Add single-ended methoxypolyethylene glycol MPEG (550) into a 250 ml three-necked flask, heat the oil bath to 150°C, and vacuum filter for three hours while stirring to remove residual moisture in MPEG, and then add the molar ratio of 3:1 DL-lactide and glycolide, heated under vacuum to melt completely, then added 120 μl stannous octoate, heated the oil bath to 160°C, and continued the reaction for 24 hours under an argon atmosphere. After the reaction was completed, vacuum filtration was performed for two hours to remove unreacted monomers and low-boiling products. The initial product was dissolved in dichloromethane solution and precipitated with ether, the yield was about 85%. The number-average and weight-average molecular weight ( M n , M w ) were 3550 and 4620, respectively, and the molecular weight distribution coefficient ( M w / M n ) is 1.30. The copolymer itself does not have thermosensitive gelling properties in water.

Embodiment 3

[0074] Add polyethylene glycol (1000) and PLGA ( M n 4750, M w 6020, LA / GA=1 / 1), the mixture was heated under vacuum to make it completely melted, and the oil bath was heated to 160°C for condensation reaction for 18 hours. After the reaction is complete, the initial product is dissolved in dichloromethane solution and precipitated with a large amount of ether, and the yield is about 85%. Measure the number average and weight average molecular weight ( M n , M w ) are 6520 and 8340 (PLGA-PEG-PLGA, Copolymer-15), respectively, molecular weight distribution coefficient ( M w / M n ) is 1.28. The copolymer itself does not have thermosensitive gelling properties in water.

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Abstract

The invention belongs to the technical field of medicaments, and in particular relates to a gel sustained-release injection containing camptothecin or derivatives thereof, and a preparation method thereof. The gel sustained-release injection is composed of amphipathic segmented copolymers, an effective dose of anti-tumor drug and a solvent, wherein the gel material is a mixture composed of two or more polymers, the water system of the gel material is capable of generating thermosensitive gelation when the temperature rises, and the polymers are generally segmented copolymers formed by polyethylene glycol as a hydrophilic segment and degradable polyester as a hydrophobic segment; and the anti-tumor drug is selected from camptothecin or derivatives thereof. The preparation can be administered by injection, and after the preparation is gelated in situ in vivo, the encapsulated drug can be slowly released. The preparation can be injected into or around a tumor, also can be administered in a tumor cavity after an operation, has a passive targeting function, can effectively reduce the systemic toxicity of the drug, and can be used for treating tumors at different stages.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a gel sustained-release injection and a preparation method thereof. Background technique [0002] As we all know, cancer is a major disease that endangers the life and health of people in all countries, and surgery plus chemotherapy is the main means of treating cancer. Clinical practice has proved that in the process of traditional chemotherapy to treat tumors, the effective concentration of drugs actually reaching the tumor site is relatively low, and the toxic and side effects are large. Improving the enrichment of drugs in tumor sites to enhance the effect of chemotherapy is a current research hotspot. Among them, local tumor administration can be artificially and passively targeted to the tumor site, so that the local tumor can maintain a high concentration, thereby improving the therapeutic effect and reducing systemic toxicity. [0003] Camptothecin and its...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4745A61K47/34A61K47/36A61K47/42A61P35/00A61P35/04
Inventor 丁建东俞麟常广涛
Owner FUDAN UNIV
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