Injection medicine composition with synergistic action of vitamin C and benzsulfamide compounds
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A technology of benzenesulfonamide and composition, which is applied in the field of pharmaceutical composition for the treatment of malignant tumors, and can solve problems such as poor targeting and large systemic side effects
Inactive Publication Date: 2017-06-13
王子厚
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[0005] The purpose of the present invention is to provide a new type of pharmaceutical composition with definite curative effect and small side effects, aimed at the current clinical cancer treatment, especially the shortcomings of large systemic side effects and poor targeting in existing drugs for the treatment of malignant tumors. Administered in the form of internal, interventional or intravenous injection
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[0128] F-1 to F-15 are all known compounds, wherein F-1 to F-11 are obtained from commercial sources (purchased from Beijing Yinuokai Technology Co., Ltd.), and F-12 to F-15 are prepared according to the following general method: Add 4-hydroxybenzenesulfonamide (F-6, 1.73g, 10mmol) and dimethylformamide (20mL) into a 100mL round bottom flask, stir at room temperature until clear, add 60% NaH (0.8g, 20mmol), and Stir for 5 minutes, then add haloalkane (30 mmol), continue stirring at room temperature, and track and detect by TLC. After the reaction is complete, pour the reaction mixture into water, extract with ethyl acetate (100mL×3), combine the ethyl acetate phases, wash with water (100mL×1), wash with saturated brine (100mL×1), and dry over anhydrous sodium sulfate for 6 hours , filtered, the filtrate was concentrated to dryness under reduced pressure, silica gel column chromatography, petroleum ether / ethyl acetate (10:1, 5:1) was eluted sequentially, the target product was ...
experiment example 1、Vc
[0135] Experimental example 1, the inhibitory effect of Vc combined with various benzenesulfonamide compounds on tumor cells
[0136] experimental method
[0137] drug configuration
[0138] Weigh 88 mg of vitamin C (hereinafter referred to as Vc) and dissolve it in 0.5 mL of autoclaved water to make a 1 mol / L stock solution, filter it with a 0.22 μm disposable needle filter in an ultra-clean workbench, and store it in a -80 °C refrigerator , When used, it is directly added to the culture medium to make a corresponding concentration of liquid medicine.
[0139] MTT assay for cell viability
[0140] After the cell lines in the logarithmic growth phase were digested with 0.25% trypsin, the RPMI1640 culture medium containing 10% fetal bovine serum was used to make a single cell suspension, and 3×10 3 Inoculate in a 96-well plate at a density of cells / mL, add 100 μL of cell suspension to each well, and place at 37°C, 5% CO 2 Cultivate in a sterile incubator in an incubator for 2...
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Abstract
The invention relates to a medicine composition for treating malignant tumors by injection administration. The medicine composition is characterized in that vitamin C is used as an anti-tumor component, and is compounded with one or multiple benzsulfamide compounds so as to prepare a pharmaceutically acceptable injection preparation for administration, or is compounded with one or multiple of benzsulfamide compounds for joint injection administration, especially for the tumor internal injection and interventional administration or vein, artery, muscle and subcutaneous administration. The vitamin C composition preparation has the advantages that the vitamin C composition preparation is directly injected into multiple malignant tumors of liver cancers, pancreatic cancers, brain tumors, esophagus cancers and the like, the medicine concentration in the tumor is increased, the medicine concentration in other tissues is decreased, the therapy effect is improved, and the toxic or side effect of a whole body is reduced; an effective method for overcoming the barriers of blood brain barriers, blood tumor barriers and the like is provided; an ideal therapy selection is provided for a patient of which the tumor cannot be cut off by surgery.
Description
technical field [0001] The invention relates to a pharmaceutical composition for treating malignant tumors, especially a vitamin C anticancer composition for intratumoral injection, interventional administration or intravenous administration, which is composed of vitamin C and one or more benzenesulfonamides The compounds are used in combination, prepared into a pharmaceutically acceptable injection form for administration. The composition of the present invention has excellent physical and chemical stability and definite anti-tumor effect. In vitro cell experiments and tumor-bearing mouse experiments show that the composition is effective for various malignant tumors such as liver cancer and pancreatic cancer. Background technique [0002] Vitamin C, also known as ascorbic acid, chemical formula is C 6 h 8 o 6 , is an antioxidant that participates in various enzymatic reactions in the body and is an important substance for life activities. Nearly 50 years ago, research ...
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