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Anti entity tumour medicinal composition containing tetrazine kind compound

A technology of tumor drugs and compositions, which is applied in the direction of drug combinations, anti-tumor drugs, active ingredients of heterocyclic compounds, etc., and can solve the problems of difficult local formation of effective drug concentrations and limitations in tumors

Inactive Publication Date: 2005-10-26
DASEN BIOLOGICAL PHARMA CO LTD
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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

[0089] Put 80 mg of polyglycolic acid and glycolic acid copolymer (PLGA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of procarbazine and 10 mg of mitomycin C, and re- Shake well and dry under vacuum to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anti-solid tumor pharmaceutical composition containing 10% procarbazine and 10% mitomycin C. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition is 15-20 days in physiological saline in vitro, and 30-40 days in mice subcutaneously.

Embodiment 2

[0090] Embodiment 2. As described in embodiment 1, the difference is that the contained anticancer active ingredients are:

[0091](A) 1-50% procarbazine, mitozolomide, dacarbazine, temozolomide, imidazotetrazine, imidazopiperazine, 1H-imidazo[b]piperazine, imidazopyridine, 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-methyltriazol-1-yl)-imidazo-4-carboxamide, 8-nitro-3-methyl-benzo-1,2,3,5-tetraazepine-4-temozolomide, 3,5-dimethyl-pyrido-1,2,3,5-tetra Azepine-4-temozolomide or 3-(2-chloroethane)-N,N-dimethyl-4-oxo-3,4-dihydroimidazol[5,1-d]-1,2,3, 5-tetrazine-8-carboxamide, 5-(triazenyl)imidazole-4-carboxamide, 3-aminobenzamide or 6-aminonicotinamide with 1-50% paclitaxel, docetaxel, 2 '-Hydroxytaxol, 10-deacetylbaccatin III, 14β-hydroxy-10-deacetylbaccatin III, 9-dihydroxy-13-baccatin III, 10-deacetyltaxane A combination of phenol, 7-epi-ta...

Embodiment 3

[0095] Put 80 mg of polyglycolic acid and glycolic acid copolymer (PLGA) with a molecular weight of 20,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of mitozolomide and 10 mg of doxorubicin, and re-shake Then dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anti-solid tumor pharmaceutical composition containing 10% mitozolomide and 10% doxorubicin. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition is 15-20 days in physiological saline in vitro, and 30-40 days in mice subcutaneously.

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Abstract

A composite medicine for treating solid tumor by locally putting it in the tumor is composed of the active anticancer component (tetraazine compound and its synergist chosen from taxol-type anticancer medicine, antineoplastic antibiotic and antibetabolitic medicine), and the medicinal auxiliary (biocompatible and biodegradable high-molecular polymer).

Description

(1) Technical field [0001] The invention relates to an anti-solid tumor pharmaceutical composition, which belongs to the technical field of medicines. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, tetrazine compounds have obvious effects and have been widely used in various malignant tumors. Since topoase inhibitors exert their anti-tumor effect by inhibiting RNA synthesis, and the DNA repair function in many tumor cells is significantly increased after treatment, so effectively reducing or inhibiting the DNA repair function in tumor cells has become the current research topic. focus. [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)). Howeve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/08
Inventor 孔庆忠孙娟赵云峰张楠
Owner DASEN BIOLOGICAL PHARMA CO LTD
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