Anti solid tumor medicine composition

A tumor drug and composition technology, applied in the field of medicine, can solve the problem of local formation of effective drug concentration in difficult tumors, and achieve the effect of strengthening the anti-cancer effect

Inactive Publication Date: 2006-10-18
南京天一药业有限公司
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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.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

[0092] Put 90 mg of polylactic acid (PLA) with a molecular weight of 10000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of methoxyamine (MX), shake again and vacuum dry to remove organic solvents. The dried solid composition is immediately shaped, and then irradiated to sterilize it after packaging to obtain an anti-cancer complex containing 10% by weight of MX. The drug release time of the anti-solid tumor drug composition in vitro in physiological saline is 15-20 days, and the drug release time under the skin of mice is about 30-40 days.

Embodiment 2

[0094] The method steps for processing into an anti-solid tumor pharmaceutical composition are the same as in Example 1, but the active ingredients contained are:

[0095] Ethylene Vinyl Acetate Copolymer (EVAc) 85 mg

[0096] Dichloromethane 100 ml

[0097] DNA repair enzyme inhibitor (MX) 15 mg

[0098] According to the above method, it was made into a compound containing 15% MX by weight.

Embodiment 3

[0100] The method steps for processing into an anti-solid tumor pharmaceutical composition are the same as in Example 1, but the active ingredients contained are:

[0101] PLGA (copolymer of lactic acid and glycolic acid) with a molecular weight of 20,000 75 mg

[0102] Dichloromethane 100 ml

[0103] Hydroxylamine (HX) 25 mg

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PUM

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Abstract

An anti-solid tumor pharmaceutical composition belongs to the technical field of medicines. Including pharmaceutical excipients and DNA repair enzyme inhibitors and / or nitrosourea anticancer drugs. The DNA repair enzyme inhibitors are selected from methoxyamine, hydroxylamine and their analogs, which can effectively destroy the DNA repair function in tumor cells, thereby reducing the tolerance of tumor cells to nitrosourea anticancer drugs and their analogs The pharmaceutical excipients are biocompatible, degradable and absorbable polymers, which can slowly release DNA repair enzyme inhibitors to local tumors during the process of degradation and absorption, thus significantly reducing their systemic toxicity. At the same time, it can also maintain the effective drug concentration locally in the tumor. Local tumor placement of the anti-solid tumor composition can not only reduce the systemic toxicity of nitrosourea anticancer drugs and / or DNA repair enzyme inhibitors, but also selectively increase the drug concentration in the local tumor, and enhance the effect of chemotherapy drugs and radiation. Therapeutic effect of non-surgical therapy such as treatment.

Description

(1) Technical field [0001] The invention relates to an anti-solid tumor pharmaceutical composition, which belongs to the technical field of medicine. (2) Background technology [0002] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutics used, nitrosourea anticancer drugs have obvious effects and have been widely used in a variety of malignant tumors. However, further studies have found that the DNA repair function in many tumor cells is significantly increased after treatment. The latter often leads to increased tolerance of tumor cells to nitrosourea anticancer drugs, and the result is treatment failure. [0003] Recently, it has been discovered that inactivating or inhibiting DNA repair proteins in cells can enhance the sensitivity of some tumor cells to chemotherapy (see Dulan et al. "06-Benzylguanine analogues on the cytotoxic sensitivity of human tumor cells to alkylating agents The role of "Cancer Researc...

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 南京天一药业有限公司
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