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Anticancer sustained-release gel injection containing stines medicine

A slow-release gel injection and statin technology, applied in the field of medicine, can solve problems such as unsatisfactory cell action, degradation and denaturation of anti-cancer active ingredients, tissue trauma, etc.

Inactive Publication Date: 2008-09-17
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] 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.

[0076] 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.

[0077] The preparation of microspheres is prepared by the O / W method, and 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 of the copolymer ...

Embodiment 2

[0079] 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

[0081] 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.

[0082] 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.

[0083] The preparation of microspheres is prepared by the O / W method, and 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 (PLGA) of lactic acid and glycolic acid can be 25,000-35,000, and the weight ratio of copolymer and...

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Abstract

The invention relates to an anticancer sustained release gel injection with stine drugs, comprising sustained release microspheres with stine drugs, a amphiphilic block copolymer, solvent and releasing moderator; wherein, the mixture of the amphiphilic block copolymer and the solvent possesses sensitive gelation property; after in vivo injection, the injection can be transformed into nonflowing, biodegradable gel insoluble in water; the insoluble gel can release the contained drugs in local tumor for weeks, even months. Intra-tumor injection or local injection can be used to treat different tumors and unresectable tumors, control late complications and the postoperative residual tumor cell recurrent, reinforce the effect of radiotherapy and chemotherapy and the effect of radiotherapy particles; nimustine and carmustine and other stines; the amphiphilic block copolymer is a PLGA-PEG-PLGA copolymer with the molecular weight of PEG 1200-1600 accounting for 20% of the amphiphilic block copolymer weight; in the poly lactide coglycolide copolymer, the molar ratio of glycolide and lactide is 6:1.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release gel injection containing statins, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing statins and / or slow-release microspheres in local solid tumors, mainly a slow-release gel injection. It is an aqueous solution, which can become a semi-solid or solid gel in the body of a warm-blooded animal, wherein part or all of the statins are encapsulated in the sustained-release microspheres, and the statins contained in the sustained-release microspheres are slowly released locally in the tumor The time was further extended to several months. (2) Background technology [0002] Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. The fundamental problem is that traditional chemotherapy cannot achieve effective drug concentration at the tumor site and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/00A61K9/10A61P35/00
Inventor 张楠孙启明王启雨赵健
Owner 济南基福医药科技有限公司
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