Anti solid tumor medicine composition

A tumor drug and composition technology, applied in the field of drugs, can solve the problems of local formation of effective drug concentration in difficult tumors, dose limitation of administration, etc., and achieve the effect of strengthening the anti-cancer effect

Inactive Publication Date: 2005-06-22
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 concent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0178] Put 90 mg of polylactic acid (PLA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of methoxyamine (MX), re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer compound containing 10% by weight of MX. 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 about 30-40 days.

Embodiment 2

[0180] The method step of being processed into anti-solid tumor pharmaceutical composition is identical with embodiment 1, but contained active ingredient is:

[0181] Ethylene Vinyl Acetate Copolymer (EVAc) 85 mg

[0182] Dichloromethane 100ml

[0183] DNA Repair Enzyme Inhibitor (MX) 15 mg

[0184] It is made into a drug-containing compound containing 15% by weight of MX according to the above-mentioned method.

Embodiment 3

[0186] The method step of being processed into anti-solid tumor pharmaceutical composition is identical with embodiment 1, but contained active ingredient is:

[0187] PLGA (copolymer of lactic acid and glycolic acid) with a molecular weight of 20,000 75 mg

[0188] Dichloromethane 100ml

[0189] Hydroxylamine (HX) 25 mg

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PUM

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Abstract

Disclosed is an anti solid tumor medicine composition, which comprises medicinal adjuvant and DNA restoring enzyme inhibitor and/or Nitrosoureas anti-cancer drugs, wherein the DAN restoring enzyme inhibitor is selected from methoxamine, hydroxylamine and their analogues, which can effectively destroy the DNA restoring function in the tumor cells, and lower the survivability of tumor cell to Semustine anti-cancer drugs and their analogues, the medicinal adjuvant is biological compactable, degradable and absorbing macromolecular polymer, which can slowly release the DNA restoring enzyme inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. By dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and/or DNA restoring enzyme inhibitor can be lowered, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

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] 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 inactivation or inhibition of 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, conn...

Claims

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Application Information

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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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