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Compound anticarcinogen slow-release preparation containing vasoinhibitor

A technology of vascular inhibitors and slow-release agents, which is applied in the field of anti-cancer slow-release agents, can solve the problems of increased resistance to anti-cancer drugs, restrictions on the effective diffusion of drugs, and obstacles to chemotherapy for tumors, so as to facilitate drug injection, reduce costs, The effect of reducing complications

Inactive Publication Date: 2007-07-18
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] Put 80 mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 10,000-25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of tipifarnib and 10 mg of gemcitabine, re-shake and vacuum Dry to remove organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer slow-release agent containing 10% tipifarnib and 10% gemcitabine. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 14-21 days, and the drug release time in mouse subcutaneous is 20-25 days.

Embodiment 2

[0128] As described in Example 1, the difference is that the auxiliary material is polylactic acid (PLGA, 75:25) with a peak molecular weight of 25000-45000, and the anticancer active ingredients and weight percentage are:

[0129] (a) 0.1%-40% vandetanib, tipifarnib, sirolimus, sirolimus, tacrolimus, lenalidomide or isatecan and 0.1%-40% rapamycin, bleomycin daunomycin, nogamycin, puromycin, arubicin, idarubicin, clarithromycin, adazol, doxorubicin, epirubicin, valrubicin, a combination of pirarubicin, loxantrone, loxoxantrone, mitoxantrone, piroxantrone, tiloxantrone, or clozocin; or

[0130] (b) 0.1%-40% vandetanib, tipifarnib, sirolimus, sirolimus, tacrolimus, lenalidomide, or exatecan with 2%-40% pemetrexed, pemetrexed Sediba, Lumitrexed, Carmofur, Tegafur, Temozolomide, Zalcitabine, Emtricitabine, Gallocitabine, Ibacitabine, Ancitabine, Decitabine, Fluoxetine Tabine, Enoxitabine, Mizotabine, Capecitabine, Gemcitabine, Fazarabine, Fludarabine, Cladribine, Pentasylate, R...

Embodiment 3

[0132] Put 70mg of polyphenylene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of vanilla Detanib and 20 mg of doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% vandetanib and 20% doxorubicin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 20-25 days, and the drug release time in mouse subcutaneous is 20-30 days.

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Abstract

A slow-releasing composite anticancer injection containing angiostatin is composed of the slow-release microballs containing active anticancer component chosen from angiostatin, anticancer antibiotic and antimetabolitic medicine and slow-release auxiliary, and the special solvent containing suspending aid.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release agent containing angiostatin, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing a blood vessel inhibitor. The anti-cancer slow-release agent can effectively inhibit or destroy the solid tumor stroma and tumor blood vessels, and can inhibit the neovascularization of the tumor, which is conducive to the effective diffusion of drugs into the solid tumor and in the tumor, and increases drug sensitivity. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00A61K47/10A61K47/26A61K47/36A61K47/38A61K47/42
Inventor 孙娟刘玉燕孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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