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Anti-solid tumors pharmaceutical combination containing topological enzyme inhibitor

A technology of tumor drugs and compositions, which is applied in the direction of anti-tumor drugs, drug combinations, medical preparations containing active ingredients, etc., and can solve the problem of difficult local formation of effective drug concentrations in tumors

Inactive Publication Date: 2008-08-20
SHANDONG LANJIN PHARMA +1
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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.1998Oct; 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

[0099]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

[0101] As described in Example 1, the difference is that the contained anticancer active ingredients are:

[0102] (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 ...

Embodiment 3

[0106] 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

The invention relates to a solid tumor resistant combined medicine with topoisomerase inhibitor, which comprises anti-cancer effective ingredients and medical auxiliary materials, wherein, the anti-cancer effective ingredients comprise topoisomerase inhibitor and topoisomerase inhibitor synergistic agent; the topoisomerase inhibitor synergistic agent mainly comprises paclitaxel anti-cancer medicines and / or antitumor antibiotics and / or anti-metabolite; the medical auxiliary materials mainly comprises biological soluble, degradable and absorbable macromolecule polymer, which enables to release the anti-cancer medicine slowly on the tumor in the degradation and absorption process, and thereby reduce the body toxic reaction obviously and maintain the effective medical concentration on the tumor at the same time. The solid tumor resistant combined medicine has the advantages of reducing the body toxic reaction, selectively improving the medical concentration on the tumor and enhancing the treatment effect of chemotherapeutics, radiation therapy and other non-surgery treatments.

Description

[0001] This application is a divisional application of No. 200510042236.2 patent with the same name (1) Technical field [0002] 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 [0003] 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. [0004] It has recently been found that inactivating or inhibiting intracellular DNA repair proteins can enhance the sensitivity of some tumor cells to ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K47/30A61P35/00
Inventor 孔庆忠孙娟孙静孙宪德
Owner SHANDONG LANJIN PHARMA
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