Anti-cancer medicine composition

A technology of anti-cancer drugs and compositions, which is applied in drug combinations, anti-tumor drugs, and pharmaceutical formulations, and can solve problems such as difficulty in forming effective drug concentrations

Inactive Publication Date: 2008-11-12
SHANDONG LANJIN PHARMA
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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

[0109] Put 80mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into the container, add 100ml of methylene chloride to dissolve and mix well, then add 10mg of 2-(4-morpholinyl)-8-phenylchromone and 10mg of 5- Fluorouracil, shake again and dry in vacuo to remove organic solvents. Immediately shape the dried solid composition, subpackage it and sterilize it by radiation to obtain an anticancer drug composition containing 10% by weight of 2-(4-morpholinyl)-8-phenylchromone and 10% of 5-fluorouracil , In vivo implants. 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.

Embodiment 2

[0110] Embodiment 2. As described in embodiment 1, the difference is that the contained active ingredients are:

[0111](a) 1-50% of 6-mercaptopurine, 5-fluorouracil (5-FU), deoxyfluridine, floxuridine, mercaptopurine or thioguanine and 1-50% of wortmannin or benzopyridine Fran, 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-morphol-4-yl-phenyl)-ethylidene), kinase inhibitors, vanillin, 2-aminopurine, Combinations of 7-ethyl-10-hydroxycamptothecin, 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyridine-[1H]-2-1 or phenylbutyrate ;or

[0112] (b) 1-50% of 6-mercaptopurine, 5-fluorouracil (5-FU), deoxyfluridine, floxuridine, mercaptopurine or thioguanine and 1-50% of 3-aminobenzamide, Benzamide, 3,4-dihydromethoxyisoquinoline-1(2H)-benzamide, polymerase inhibitor, polymerase inhibitor, amino-substituted 2-arylbenzimidazole-4- Combinations of carboxamides, benzimidazole-4-carboxamides, tricyclic lactam h...

Embodiment 3

[0116] Put 80 mg of PLGA (copolymer of glycolic 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 wortmannin and 10 mg methotrexate, and re-shake Dry in vacuo 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 10% by weight of methotrexate and 10% wortmannin, which is an implant in the body. 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 4. As described in embodiment 3, the difference is that the contained active ingredients are:

[0117] a) 1-50% methotrexate, carmofur, tegafur, galocitabine, ibacitabine, enoxitabine, ancitabine, decitabine, flucitabine, Nortabine or imidazotabine with 1-50% of 2-(4-morpholinyl)-8-ph...

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PUM

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Abstract

An anticancer pharmaceutical composition composed of pharmaceutic adjuvant and anticancer effective constituent is disclosed. The main anticancer constituents are anti-metabolism drug and DNA repair enzyme, wherein, the DNA repair enzyme inhibitor is chosen from poly(ADP ribose) polymerase inhibitor and / or DNA dependant protein kinase inhibitor, the DNA repair enzyme inhibitor can effectively destroy the DNA repairing function inside the tumor cell so as to lowers the tolerance of tumor cell to anti metabolism drug, while the main pharmaceutic adjuvant is biological compatible, degradable and absorbable macromolecule polymer, which can make the DNA repairing enzyme inhibitor release to the local region of tumor in the degradation and absorption process, therefore, it can both considerably lower the whole body toxic reaction and maintain the effective drug level of local region of tumor.

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, anti-metabolite 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 increased resistance of tumor cells to antimetabolic 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, matrix proteins, fib...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61P35/00
Inventor 孔庆忠
Owner SHANDONG LANJIN PHARMA
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