Anti solid tumor medicine composition

A technology of tumor drugs and compositions, which is applied in the direction of drug combinations, anti-tumor drugs, active ingredients of heterocyclic compounds, etc., and can solve the problems of limited and difficult local formation of effective drug concentrations in tumors

Inactive Publication Date: 2005-06-22
孔庆忠
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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

[0243] Put 90 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 O6-benzylguanine (O6-BG), re-shake, and then vacuum-dry to remove organic matter. solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anti-solid tumor pharmaceutical composition containing 10% O6-BG. 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

[0245] The method step of being processed into the anti-solid tumor pharmaceutical composition is the same as in Example 1, but the anti-cancer active ingredients contained are:

[0246] (a) 0.1-40% benzylguanine, O6-benzylguanine, O6-butylguanine, O6-methylguanine, O6-alkylguanine, 2-amino-6-oxopurine, O6-benzyl 2'-deoxyguanine, guanine (2-amino-6-hydroxypurine), 8-amino-O6-benzylguanine, 8-methyl-O6-benzylguanine, 8-hydroxy -O6-Benzylguanine; or

[0247] (b) 0.1-40% of, 8-bromo-O6-benzylguanine, 8-oxo-O6-benzylguanine, 8-trifluoromethyl-O6-benzylguanine, O6-benzylguanine Uric acid, O6-benzylxanthine, O6-benzyl-2-fluorohypoxanthine, diacetyl-O6-benzyl-8-oxoguanine, O6-benzyl-8-methylguanine, O6-benzyl Base-8-oxoguanine, O6-benzyl-8-bromoguanine; or

[0248] (c) 0.1-40% of O6-benzyl-8-trifluoromethylguanine, O6-benzyl-N2-methylguanine, O6-benzyl-N2N2-dimethylguanine, O6-benzyl Base-8-trifluoromethyl-9-methylguanine, O6-benzyl-8-bromo-9-methylguanine, O6-benzyl-8-bromo-9-pi...

Embodiment 3

[0253] Put 80 mg of polylactic acid (PLGA) with a molecular weight of 10000 into a container, add 100 ml of methylene chloride to dissolve and mix well, then add 10 mg of O6-benzylguanine (O6-BG) and 10 mg of carmustine (BCNU) , shake again and 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% O6-BG and 10% carmustine. 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.

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PUM

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Abstract

Disclosed is an anti solid tumor medicine composition, which comprises anticancer active constituent and medicinal adjuvant, the anticancer active constituent includes guanopterin, guanopterin derivative, guanopterin analogues or their derivatives which can effectively destroy the DNA restoring function in the tumor cells, thus lower the survivability of tumor cells to Semustine anti-cancer drugs, and the medicinal adjuvant mainly employs biological compactable, degradable and absorbing, which can slowly release the anti-cancer medicament 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. The composition also contain Nitrosoureas anti-cancer drugs, by dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and / or guanopterin and their derivatives 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 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., 51, 3367-3372, 1991)). However, blood vessels, connect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/522A61K45/06A61P35/00
Inventor 孔庆忠
Owner 孔庆忠
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