Sustained-release injection containing octadecyl dimethyl-4-piperidine phosphate

A technology of sustained-release injection and sustained-release gel injection, applied in the field of anti-cancer sustained-release injection, can solve the problems of ineffective coverage of solid implants, ineffective removal of tumor cells, ineffective control of postoperative recurrence, etc. The drug resistance of tumor cells produces or stimulates tumor proliferation and metastasis, hemostasis and prevention of tumor cell proliferation, and the effect of hemostasis and tumor cell proliferation prevention

Inactive Publication Date: 2009-01-21
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

[0076] Put 4, 2, 1 and 0.5g amphiphilic block copolymer (PLGA-PEG-PLGA) into the four containers of A, B, C, and D respectively, and then transfer to the four containers of A, B, C and D. 6, 8, 9 and 9.5 milliliters of water for injection were added to the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0077] 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 combination of glycolide and lactide The molar ratio is 6:1.

[0078] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in sustained-release microspheres is polylactic acid / glycolic acid copolymer. Among them, 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 cop...

Embodiment 2

[0080] The gelation temperatures of the four hydrogels in Example 1 were measured, and the results showed that the gelation temperatures of 40% and 20% hydrogels were 32°C (40%) and 37.5°C (20%), and 10 The gelation temperature of 5% and 5% hydrogel is not measured at 12℃-38.5℃

Embodiment 3

[0082] Put 4, 2, 1 and 0.5g amphiphilic block copolymer (PLGA-PEG-PLGA) into the four containers of A, B, C, and D respectively, and then transfer to the four containers of A, B, C and D. 6, 8, 9 and 9.5 milliliters of water for injection were added to the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0083] 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; The molar ratio is 5:1.

[0084] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in sustained-release microspheres is polylactic acid / glycolic acid copolymer. Among them, 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 ratio of copolymer to edelfosine is 6:4.

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PUM

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Abstract

A sustained release anti-cancer injection with edelfosine consists of the edelfosine with effective anti-cancer amount and an amphiphilic block copolymer hydrogel, wherein, part or the whole of the edelfosine is encapsulated in sustained release microsphere and exists singly in the form of the sustained release microsphere or microsphere and micro-powder in the sustained release injection. The amphiphilic block copolymer hydrogel is selected from PLGA-polyethylene glycol-PLGA, sustained release gel has temperature-sensitive gelation property; and the sustained release gel is flowable fluid in an environment below body temperature, and can automatically change into biodegradable and absorbable non-flowable water-insoluble gel in bodies of warm blooded animals, thus causing the drug to be slowly released in the local part of tumor; the sustained release microsphere is favorable to the stable and sustained release of the drug, the dual sustained release is beneficial to controlling tumor cells in dormancy stage, the drug in the form of the micro-powder in the sustained release gel is favorable to the relatively quick release, thus being beneficial to controlling cells with quicker proliferation. The sustained release anti-cancer injection with edelfosine can be used together with radiotherapeutic particles, chemotherapeutic drugs, etc.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release injection, which belongs to the technical field of medicines. Specifically, the invention relates to a sustained-release gel formulation capable of stably releasing edelfosine to the local solid tumors, and it is mainly a sustained dual-release gel formulation containing sustained-release microspheres. Gel injection, the sustained-release gel preparation is an aqueous solution at room temperature, and can be transformed into a semi-solid or solid gel in warm-blooded animals. The sustained-release gel and sustained-release microspheres can slowly release edelfosine locally on the tumor for several months. (2) Background technology [0002] Phosphoinositide 3-kinase (PI3K) inhibitors have a significant inhibitory effect on the growth of a variety of tumor cells. However, the therapeutic effect of intravenous application on solid tumors is not obvious. The fundamental problem lies in traditional che...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/00A61K31/661A61K47/34A61P35/00
Inventor 陈颖孙忠厚
Owner 济南基福医药科技有限公司
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