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Temperature control sustained-release injection containing resist metabolism series medicine

A technology of slow-release injections and slow-release gel injections, which is applied in the fields of temperature-controlled slow-release injections, slow-release gel injections, and slow-release gel preparations. It can solve the problems of ineffective coverage, complicated implantation process, and ineffective tumor cells Clear etc.

Inactive Publication Date: 2008-05-14
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or dissemination
In addition, organic solvents or high-heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients, and solid implants cannot effectively cover the irregular tumor cavity after tumor resection. relapse

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0048] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 800-1200, accounting for 20% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 6:1.

Embodiment 2

[0050] Measure the gelation temperature of four kinds of hydrogels in embodiment 1, the result shows that the gelation temperature of 40% and 20% hydrogel is respectively 28 ℃ (40%) and 35 ℃ (20%), and 10 The gelation temperatures of the % and 5% hydrogels were not determined at 10°C-38°C.

Embodiment 3

[0052] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0053] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 1200-1600, accounting for 15% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 4:1.

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PUM

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Abstract

The invention discloses a temperature control and sustained release injection containing anti-metabolism medicine, which comprises anticancer effective dose anti-metabolism medicine, amphiphilic block copolymer and certain amount of medicine releasing regulation agent; wherein, the amphiphilic block copolymer comprises polyethylene glycol and polyester; the mixture of the amphiphilic block copolymer and the solvent without organic solvent has the gelation property of the temperature sensitive, is the fluidity liquid in the environment below the body temperature, and can be automatically changed into the non-fluidity and biodegradation absorption water insoluble gel in the body of warm-blooded animal; the non-fluidity and biodegradation absorption water insoluble gel can release the anti-metabolism medicine slowly in the part of the tumor and maintain the effective medicine concentration of the effective medicine for a plurality of weeks or a plurality of months; the viscosity of the temperature control and sustained release injection is 10 cp to 3000 cp (5 DEG C to 30 DEG C), the temperature is 35 DEG C to 37 DEG C. The invention has the advantages of capability of injection inside or around the tumor or put inside the tumor cavity after the operation, obvious reduction of the systemic reaction of the medicine, and selective improvement of the therapeutic effect of the chemotherapy, the radiotherapy and other non-operation treatment method, and capability of curing the tumor in different stages.

Description

(1) Technical field [0001] The invention relates to a temperature-controlled sustained-release injection containing antimetabolites, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release gel preparation that can stably release antimetabolites to the local area of ​​solid tumors, mainly sustained-release gel injections. The sustained-release gel preparation is an aqueous solution at room temperature. Animals can be transformed into semi-solid or solid-state gels, so that the contained antimetabolites can be slowly released locally in the tumor, from several days to several weeks. (2) Background technology [0002] The local application of chemotherapy drugs, especially the local sustained release, has become the current research direction and hotspot of solid tumor chemotherapy. However, the current biodegradable sustained and controlled release preparations mostly use solid polymers such as polyglycolic acid, polylactic ac...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 孔庆忠杨健
Owner SHANDONG LANJIN PHARMA
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