Anticancer implantation agent

A technology of implants and anti-cancer drugs, applied in the field of anti-cancer implants, can solve the problems of treatment failure, enhanced tolerance of anti-cancer drugs, etc.

Inactive Publication Date: 2006-02-22
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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

[0077] Put 80 mg of polylactic acid (PLGA) with a peak molecular weight of 15000-25000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 10 mg of 7-amino-indazole (nitric oxide synthase inhibitor) and 10 mg of thiazolin (vasoinhibitor), re-shake and vacuum-dry to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer implant containing 10% 7-amino-indazole and 10% thiamine. All are percentages by weight. The drug release time of the anticancer implant in the physiological saline in vitro is 15-20 days, and the drug release time in the mouse subcutaneous is 30-40 days.

Embodiment 2

[0079] The method step of processing into an anticancer implant is the same as in Example 1, but the difference is that the contained anticancer active ingredient is one of the following:

[0080] (A) Carboxyaminotriazole, thalidomide, ranolaramine, enkistetin, endosterides, vascular endothelial growth factor receptor inhibitors, imatinib mesylate, 5-[5-fluoro- 2-Oxo-1,2-dihydroindoline-(3Z)-methylene]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, 3 , 3-dichloro-5-(4-methylsulfonylpyridine)-2-indolinone (DCM), 3-[1-(3H-imidazole-4-yl)-methyl-(Z)- Nylon-5-methoxy-1,3-dihydro-indole-2-indolinone, 1H-pyrrole-3-propionic acid, 2-[(1,2-dihydro-2-oxo-3H -indol-3-ylidene)methyl]-4-methyl, 2H-indol-2-one, 3-((4,5-dimethyl-1H-pyrrol-2-yl)methylene )-1,3-dihydro-[CAS], gefitinib, erlotinib, phenol, 4-(4-(((1R)-1-phenylethyl)amino)-1H-pyrrolo( 2,3-d) Pyrimidin-6-yl, lapatinib, vortalanib or peritinib and glutathione disulfide, tetramethylthiuram disulfide, amin...

Embodiment 3

[0084] Put 80 mg of polyglycolic acid and glycolic acid copolymer (PLGA) with a peak molecular weight of 20,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix, add 10 mg of imatinib (vascular inhibitor) and 10 mg of butylthionine thioxime (glutathione synthase inhibitor), re-shake and dry in vacuum to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to prepare an anticancer implant containing 10% imatinib and 10% butylthionine thioxime. All are percentages by weight. The drug release time of the anticancer implant in the physiological saline in vitro is 15-20 days, and the drug release time in the mouse subcutaneous is 30-40 days.

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PUM

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Abstract

Disclosed is an anti-cancer implant which comprises anti-cancer active constituent and medicinal adjuvant, wherein the active anti-cancer constituents mainly include blood vessel inhibitor and anti-cancer medicament, the anti-cancer medicament is selected from glutathione synthetic enzyme inhibitor or nitrogen oxide synthetic enzyme inhibitor or their combination, The medicinal subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, which can slowly release the anti-cancer medicament onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. when locally dispensed on the tumor, the composition can lower down the whole body toxicity reaction of the anti-cancer medicament, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

Description

(1) Technical field [0001] The invention relates to an anticancer implant and belongs to the technical field of medicines. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment not only cannot clear 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 concentration or therapeutic dose in the tumor, resulting in poor efficacy and high toxicity. However, simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82, 1998 (Kong Q et al., J Surg Oncol.1998 Oct; 69 (2): 76-82). [0003] Local placement of antitumor drugs can better overcome the ...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/00A61P35/00
Inventor 孔庆忠孙娟孙忠厚
Owner 孔庆忠
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