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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 the problems of difficult tumor local formation of effective drug concentration and limitations

Inactive Publication Date: 2005-05-18
广州多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

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 Q et 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

[0244] Put 95 mg of polylactic acid (PLA) with a molecular weight of 20,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, add 5 mg of anticancer active ingredient (temozolomide), re-shake, 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 5%. Put the drug-containing compound under the skin of mice, take it out regularly to measure the drug content, and calculate the cumulative release percentage (%) according to the remaining drug amount. It was found that 80-95% of the drug was released uniformly within 30 days. All the above are percentages by weight.

Embodiment 2

[0246] The method steps of processing into an anticancer drug composition are the same as in Example 1, but the contained active ingredient is listed as one of:

[0247] (a) 2-25% of imidazotetrazine, imidazopiperazine, 1H-imidazo[b]piperazine, or imidazopyridine;

[0248] (b) 2-30% of 1H-imidazo[1,2-a]pyridine, 4-carboxy temozolomide, 3-N-methyl temozolomide, pyrrole[2,1-d][1,2,3,5 ]tetrazine-4(3H)-temozolomide, pyrrole[2,1-d][1,2,3,5]tetrazine 10a-o, 5-(3-N-methyltriazine-1-yl) - imidazo-4-carboxamide or 8-nitro-3-methyl-benzo-1,2,3,5-tetraazepine-4-temozolomide;

[0249] (c) 2-35% of 3,5-dimethyl-pyrido-1,2,3,5-tetraazepine-4-temozolomide or 3-(2-chloroethane)-N,N di Methyl-4-oxo-3,4-dihydroimidazol[5,1-d]-1,2,3,5-tetrazine-8-carboxamide or 5-(triazenyl)imidazole-4- carboxamide; or

[0250] (d) 2-35% procarbazine, topotecan, irinotecan, mitozolomide, dacarbazine, temozolomide, 3-aminobenzamide or 6-aminonicotinamide.

[0251] All the above are percentages by weight.

Embodiment 3

[0253] The method step of being processed into the anticancer pharmaceutical composition is the same as that of Example 1, but the pharmaceutical auxiliary materials used are respectively one of the following:

[0254] a) Polylactic acid (PLA) with a molecular weight of 5000-15000, 10000-20000, 25000-35000 or 30000-50000;

[0255] b) Copolymers of polyglycolic acid and glycolic acid (PLGA) having a molecular weight of 5000-15000, 10000-20000, 25000-35000 or 30000-50000;

[0256] c) ethylene vinyl acetate copolymer (EVAc);

[0257] d) 10:90, 20:80, 30:70, 40:60, 50:50, or 60:40 p-carboxyphenylpropane (p-CPP):sebacic acid (SA) copolymer (polyphenylpropane ), are percentages by weight.

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PUM

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Abstract

The present invention relates to an anticancer medicine composition and belongs to the field of medicine technology. The anticancer medicine composition contains tetrazine medicine and medicinal supplementary material. The tetrazine medicinecan inhibit intracellular DNA repair function and reduce the tolerance one tumor cell on anticancer nitrosourea medicine; and the medicine supplementary material is mainly degradable biocompatible polymer. During the degrading and absorption process of the supplementary material, the anticancer medicine is released slowly to the tumor part, and this can lower the systemic toxic reaction while maintaining local effective medicine concentration. The anticancer medicine composition contains also anticancer nitrosourea medicine, and is set to the tumor part locally to enhance the treatment effect.

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 inactivating or inhibiting 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 p...

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 广州多福医药科技有限公司
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