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Dual sustained-release anticancer injection

A sustained-release injection and double-sustained-release technology, which is applied in the direction of antineoplastic drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the complex implantation process, the degradation and degeneration of anticancer active ingredients, and the inability to effectively remove tumor cells And other issues

Inactive Publication Date: 2008-11-12
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
In addition, organic solvents or high heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients
[0005] 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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] 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.

[0078] 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;

[0079] In the glycolide-lactide copolymer, the molar ratio of glycolide to lactide is 6:1.

[0080] 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 15000-38000, and the weight ratio of ...

Embodiment 2

[0082] 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 32 ℃ (40%) and 37 ℃ (20%), and 10 The gelation temperatures of the % and 5% hydrogels were not determined at 10°C-38°C.

Embodiment 3

[0084] 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.

[0085] 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.

[0086] 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 20,000-35,000, and the weight rati...

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Abstract

A double sustained release anticancer gel sustained release injection consists of anticancer medicine and amphiphilic block copolymer hydrogel, wherein the anticancer medicine comprises vincristine, vinorelbine, vinblastine, daunomycin, mitoxantrone, mitozolomide and temozolomide, etc., and exists in sustained release preparation injection in the forms of sustained release microsphere, microsphere or micropowder, i.e. the anticancer medicine in anticancer useful quantity is partly or completely wrapped inside the sustained release microsphere. Sustained release gel has temperature-sensitive gelling characteristics and is in the state of fluxible liquid in an environment with the temperature lower than body temperature; moreover, the sustained release gel can be automatically converted into non-flowing water-insoluble gel capable of biodegradation and absorption inside the body of a warm blood so as to slowly release medicine inside part of a tumor; the sustained release microsphere is propitious to release medicine smoothly and slowly, and double sustained release is propitious to control tumor cells entering a dormancy stage; moreover, the medicine which exists in the sustained release gel in the form of micropowder is propitious to release the medicine relatively faster and to control cells in faster proliferation. The double sustained release anticancer gel sustained release injection can used together with radiotherapeutic particle, etc.

Description

(1) Technical field [0001] The invention relates to a double slow-release anticancer gel injection, which belongs to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing anticancer drugs in local solid tumors, mainly a slow-release gel injection containing slow-release microspheres. It is an aqueous solution, which can become a semi-solid or solid gel in the body of a warm-blooded animal. The slow-release gel and slow-release microspheres can slowly release anticancer drugs locally on the tumor for several months. (2) Background technology [0002] Although there are many ways to treat cancer, the living conditions of most patients have not been significantly improved. Among the various treatments, chemotherapy remains one of the commonly used options. Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. The fundamental problem is...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 孙忠先张伟
Owner 济南基福医药科技有限公司
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