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Anticancer sustained-release gel injection

A slow-release gel injection and slow-release microsphere technology, which is applied in the direction of anti-tumor drugs, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve the problem of tumor cell planting or dissemination, tissue trauma, and tumor cell ineffectiveness. Clear etc.

Inactive Publication Date: 2009-01-07
济南基福医药科技有限公司
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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
Solid implants cannot effectively cover the irregular tumor cavity after tumor resection, so the residual tumor cells cannot be effectively removed after surgery, and postoperative recurrence cannot be effectively controlled
In addition, organic solvents or high heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients
[0004] In addition, the existing sustained-release preparations have obvious burst release, and the release cycle is short, which is not ideal for slow-growing tumors, especially cells in the G0 phase

Method used

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  • Anticancer sustained-release gel injection
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  • Anticancer sustained-release gel injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] 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.

[0074] 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.

[0075] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in the sustained-release microspheres is polylactic acid / glycolic acid copolymer, wherein the blending ratio of lactic acid (LA) and glycolic acid (GA) can be 75 / 25 (W / W), the molecular weight of the copolymer of lactic acid and glycolic acid (PLGA) can be 15,000-38,000, and the weight ratio...

Embodiment 2

[0077] 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 31 ℃ (40%) and 35 ℃ (20%), and 10 The gelation temperatures of the % and 5% hydrogels were not determined at 10°C-38°C. After adding 5% slow-release microspheres (W / W) to the hydrogel, measure the gelation temperature of four kinds of hydrogels in Example 1, the results show that the gelation temperature of 40% and 20% hydrogels 33°C (40%) and 37.5°C (20%), respectively, while the gelation temperatures of 10% and 5% hydrogels were not detected at 10°C-39°C.

Embodiment 3

[0079] 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.

[0080] 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.

[0081] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in the sustained-release microspheres is polylactic acid / glycolic acid copolymer, wherein the blending ratio of lactic acid (LA) and glycolic acid (GA) can be 75 / 25 (W / W), the molecular weight of the copolymer of lactic acid and glycolic acid (PLGA) can be 25,000-35,000, and the weight rati...

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Abstract

The invention relates to an anticancer slow-release gel injection which contains slow-release microspheres containing an angiogenesis inhibitor, an amphiphilic block polymer, a solvent and a slow-release agent, wherein the composition of the amphiphilic block polymer and the non-organic solvent exhibit the property of temperature-sensitive gelation. After the in vivo injection, the injection turns into a stagnant and biodegradable water-insoluble gel and the gel slowly releases the drug contained therein for a plurality of weeks to a plurality of months. After the intratumoral or peritumoral injection, the anticancer slow-release gel injection can significantly reduce the general drug reactions and is used for treating tumors of different stages. The angiogenesis inhibitor is selected from SU5416, SU6668, bosutinib, sprycel, erlotinib, vandetanib, gefitnib, canertinib, lapatinib, lestaurtinib, masitinib, vatalanib, mubritinib, tandutinib, nilotinib, marimastat, nilotinib, pelitinib, telatinib, sunitinib, sorafenib, zarnestra, sirolimus, imatinfb, lenalidomide and thalidomide.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release gel injection, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing angiogenesis inhibitors and or slow-release microspheres in local solid tumors, mainly slow-release gel injections, and the slow-release gel preparation can be released at room temperature. The bottom is an aqueous solution, which can become a semi-solid or solid gel in the body of a warm-blooded animal, in which the angiogenesis inhibitor is partially or completely encapsulated in slow-release microspheres, and the angiogenesis inhibitor contained in the slow-release microspheres slowly spreads in the local tumor. The release time was further extended to several months. (2) Background technology [0002] Cancer has become the number one killer of human health. Although there are many ways to treat cancer, the living conditions of mo...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 毛海婷王明华
Owner 济南基福医药科技有限公司
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