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Medicinal composition for tumor body

A technology of tumor drugs and compositions, applied in the field of drugs, can solve problems such as difficulty in forming effective drug concentrations, and achieve the effects of increasing sensitivity, reducing or inhibiting DNA repair function

Inactive Publication Date: 2005-10-12
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

[0070] Put 80 mg of polylactic acid (PLGA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of oxaliplatin and 10 mg of O6-benzylguanine, re-shake and remove by vacuum drying Organic solvents. The dried solid composition is formed immediately, subpackaged and sterilized by radiation to obtain an anti-solid tumor pharmaceutical composition containing 10% oxaliplatin and 10% O6-benzylguanine. 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

[0072] As described in Example 1, the difference is that the anticancer active ingredients are:

[0073] 1-50% cisplatin, carboplatin, heptaplatin, denaplatin, enloplatin, epithioplatinum, cispiroplatin, dextroomaplatin, isoproplatin, lobaplatin, miplatin, nedaplatin, omaplatin , Siplatin, Spiroplatin, Oxaliplatin or Zheniplatin with 1-50% benzylguanine, O6-benzylguanine, O6-butylguanine, O6-methylguanine, O6-alkane Baseguanine, 2-amino-6-oxopurine, O6-benzyl 2'-deoxyguanosine, guanine (2-amino-6-hydroxypurine), 8-amino-O6-benzylguanine, 8- Methyl-O6-Benzylguanine, 8-Hydroxy-O6-Benzylguanine, 8-Bromo-O6-Benzylguanine, 8-Oxo-O6-Benzylguanine, 8-Trifluoromethyl -O6-benzylguanine, O6-benzyluric acid, O6-benzylxanthine, O6-benzyl-2-fluorohypoxanthine, diacetyl-O6-benzyl-8-oxoguanine, O6-benzyl Base-8-methylguanine, O6-benzyl-8-oxoguanine, O6-benzyl-8-bromoguanine, 6-benzyl-8-trifluoromethylguanine, O6-benzyl Base-N2-methylguanine, O6-benzyl-N2N2-dimethylguanine, O6-benzyl-8-tri...

Embodiment 3

[0075] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Cisplatin and 10 mg O6-butylguanine, re-shake well and vacuum-dry 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% cisplatin and 10% O6-butylguanine. 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 applied locally for treating the solid tumor is prepared from the Pt compound, guanine or its analog, and the biocompatible and biodegradable high-molecular polymer as medicinal additive.

Description

(1) Technical field [0001] The invention relates to a pharmaceutical composition for resisting solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, the effect of platinum compounds is more obvious, and has been widely used in various malignant tumors. Since platinum compounds exert their anti-tumor effect by binding to DNA to inhibit 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 becomes focus of current research. [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", 1991, 51, pp. 3367-3372 (Dolan et al., Cancer Res., 51, 3367-337...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61K45/06A61P35/00
Inventor 孔庆忠孙娟刘恩祥张婕
Owner DASEN BIOLOGICAL PHARMA CO LTD
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