Anti-cancer medicine composition

An anti-cancer drug and composition technology, which can be applied in drug combinations, anti-tumor drugs, pharmaceutical formulations, etc., can solve problems such as difficulty in forming effective drug concentrations

Inactive Publication Date: 2005-06-22
南京天一药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor (see Kong Qingzhong "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Qet al., J Surg Oncol.1998 Oct; 69 (2 ):76-82), simply increasing the dosage is limited by systemic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0318] Put 90 mg of PLGA (a copolymer of lactic acid and glycolic acid) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of wortmannin (WM), re-shake, and vacuum dry to remove organic matter. solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer drug composition containing 10% wortmannin by weight. The drug release time of the anticancer drug composition in the physiological saline in vitro is 15-20 days, and the drug release time in the mouse subcutaneous is about 30-40 days.

Embodiment 2

[0320] The method step of being processed into anticancer drug composition is identical with embodiment 1, but contained active ingredient is:

[0321] a) 1-40% by weight of benzopyran, 6-aryl-2-morphol-4-yl-pyran-4-yl, 6-aryl-2-morphol-4-yl-4H -thiopyran-4-yl, 2-(4-morpholinyl)-8-phenylchromone, 1-(2-hydroxy-4-morpholin-4-yl-phenyl)-ethylidene), Kinase inhibitors, vanillin, 2-aminopurine, 7-ethyl-10-hydroxycamptothecin, 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyridine-[1H] -2-1. Phenylbutyrate; or

[0322] b) 1-40% by weight of 3-aminobenzamide, benzamide, 3,4-dihydromethoxyisoquinoline-1(2H)-benzamide, polymerase inhibitor, polymerase Inhibitors, amino-substituted 2-arylbenzimidazole-4-carboxamides, benzimidazole-4-carboxamides, tricyclic lactam hydrogen sulfide, tricyclic benzimidazole carboxamides; or

[0323] c) 1-40% by weight of benzimidazole, 1H-tricyclic benzimidazole carboxamide, 2-aryl-1H-benzimidazole-4-carboxamide, 2-phenyl-1H-benzimidazole- 4-carboxamide, 2-(4...

Embodiment 3

[0325] Put 80mg of pharmaceutical excipients (EVAc) into a container, add 100ml of dichloromethane to dissolve and mix well, then add 20mg of 2-(4-morpholinyl)-8-phenylchromone, shake well and then vacuum dry to remove the organic solvent . The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer drug composition containing 20% ​​by weight of 2-(4-morpholinyl)-8-phenylchromone. The drug release time of the anticancer drug composition in the physiological saline in vitro is 14-24 days, and the drug release time in the mouse subcutaneous is about 20-35 days.

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PUM

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Abstract

The invention provides an anti-cancer medicine composition, with comprises medicinal adjuvant and DNA restoring enzyme inhibitor containing effective anticancer constituents, wherein the DNA restoring enzyme inhibitor is selected from poly (ADP-ribose) poly enzyme inhibitor and / or DNA-dependent protein kinase inhibitor, which can effectively destroy the DNA restoring function in the tumor cells, and lower the survivability of tumor cell to Nitrosoureas anti-cancer drugs and their analogues, and the medicinal adjuvant mainly comprises biological compactable, degradable and absorbing macromolecular polymers, which can slowly release the DNA restoring enzyme inhibitor 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. The anti-cancer medicinal composition also contain Nitrosoureas anti-cancer drugs and their analogues, by dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and / or DNA restoring enzyme inhibitor can be lowered, 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 drug composition, which belongs to the technical field of drugs. (2) Background technology [0002] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, nitrosourea anticancer drugs have obvious effects and have been widely used in various malignant tumors. However, further research found that the DNA repair function in many tumor cells increased significantly after the treatment. The latter often leads to enhanced resistance of tumor cells to nitrosourea anticancer drugs, resulting in treatment failure. [0003] It has recently been found that inactivation or inhibition of intracellular DNA repair proteins can enhance the sensitivity of some tumor cells to chemotherapy (see Dolan et al. ""Cancer Research" 51 pp. 3367-3372 (1991) (Dolan et al., Cancer Res., 51, 3367-3372, 1991)). However, blood vessels, connective tissue, matri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P35/00
Inventor 孔庆忠
Owner 南京天一药业有限公司
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