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Anticancer sustained-release injection containing neovascularization inhibitor

A technology of slow-release injections and slow-release gel injections, which is applied in the field of slow-release gel preparations and slow-release gel injections, and can solve problems such as ineffective control of postoperative recurrence, complicated implantation process, and ineffective coverage

Inactive Publication Date: 2008-10-01
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

[0046] 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.

[0047] 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

[0049] 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

[0051] 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.

[0052] 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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Abstract

The invention relates to an anti-cancer sustained-release injection containing an angiogenesis inhibitor, which comprises the angiogenesis inhibitor, an amphiphilic block copolymer, a solvent and a certain amount of drug release regulator; wherein, the mixture of the amphiphilic block copolymer and a solvent without organic solvent has the temperature-sensitive gelatinization feature, which is flowable liquid in the environment that is lower than the body temperature and can be automatically converted to the water-insoluble gel that can not flow and be biodegradable for absorption in an endotherm, and the water-insoluble gel can allow the contained angiogenesis inhibitor to have the local sustained release in a tumor and maintain the effective drug concentration for a plurality of weeks to a plurality of months. The sustained-release gel injection can be injected in the tumor or the tumor periphery or be arranged in the postoperative tumor cavity, thus significantly reducing the systemic reaction of the drug and being used for the treatment of the tumors in different stages. The angiogenesis inhibitor is selected from tipifarnib, sirolimus, gefitinib, erlotinib, lapatinib, pelitinib, endostatin, simatinib, dasatinib, avastin, sorafenib, sunitinib, ostwald and so on.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release injection containing a new blood vessel inhibitor, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing angiogenesis inhibitors locally in solid tumors, mainly a slow-release gel injection. The slow-release gel preparation is an aqueous solution at room temperature, In animals, it can become a semi-solid or solid gel, so it can slowly release the contained neovascularization inhibitor in the local tumor, from several days to several weeks. (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. However, the current biodegradable sustained and controlled release preparations mostly use solid polymers such as polyglycolic acid, polylactic acid or their copolymers as su...

Claims

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Application Information

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