Antientity tumour medicinal composition containing topoenzyme inhibitor

A technology of topoase inhibitors and tumor drugs, which is applied in the field of anti-solid tumor drug compositions containing topoase inhibitors, 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 concentr

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] 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 teniposide 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% teniposide and 10% mitomycin C. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-20 days, and the drug release time in mouse subcutaneous is 30-40 days.

Embodiment 2

[0092] As described in Example 1, the difference is that the contained anticancer active ingredients are:

[0093](A) 1-50% methylenedioxycamptothecin, (RS)-methylenedioxycamptothecin, (S)-methylenedioxycamptothecin glycinate, 9-amino-( S)-methylenedioxycamptothecin glycinate, letotecan, topotecan, irinotecan, 9-nitrocamptothecin, hydroxycamptothecin, 7-ethyl-10-hydroxy-camptothecin Camptothecin, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonylcamptothecin, 10-hydroxy-camptothecin, homocamptothecin, camptothecin , N-[2-(dimethylamino)ethyl)acridine-4-carboxamide, podophyllotoxin, etoposide, teniposide, podophylloside, podophylloside, podophyllotoxin, Trihydroxyisoflavones, amrubicin, daunorubicin, daunorubicin, 4-desmethoxydunorubicin, detorubicin, epirubicin, 7-O-methylnoga -4'-Epirubicin, Esorubicin, Carrubicin, Idarubicin, Rhodobicin, Liurubicin, Medorubicin, Naimorubicin, Doxorubicin, N-trifluorotoxin-14-pentanoate, 2-[4-(7-chloro-2-quinoxalinyloxyphenoxy]-propionic a...

Embodiment 3

[0097] 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 topotecan and 10 mg of doxorubicin, and re-shake 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% topotecan and 10% doxorubicin. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-20 days, and the drug release time in mouse subcutaneous is 30-40 days.

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PUM

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Abstract

A composite medicine for treating tumor by locally putting it in the tumor is composed of the active anticancer components (topoenzyme inhibitor and its symergist chosen from taxol-type anticancer medicnie, antineoplastic antibiotic and antimetabolitic 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 containing a topozyme inhibitor, 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, topoase inhibitors are more effective 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., 5...

Claims

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Application Information

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IPC IPC(8): A61K45/08
Inventor 孔庆忠孙娟孙静孙宪德
Owner DASEN BIOLOGICAL PHARMA CO LTD
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