Anti-glioma drugs based on Venenum Bufonis extract and preparation method thereof

A brain glioma, extract technology, applied in the field of anti-tumor drugs, can solve problems such as unsatisfactory curative effect and poor prognosis

Inactive Publication Date: 2016-04-13
赵婷
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, chemical drugs and general anti-tumor traditional Chinese medicines are difficult to kill glioma cells and penetrate the blood-brain barrie...

Method used

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  • Anti-glioma drugs based on Venenum Bufonis extract and preparation method thereof
  • Anti-glioma drugs based on Venenum Bufonis extract and preparation method thereof
  • Anti-glioma drugs based on Venenum Bufonis extract and preparation method thereof

Examples

Experimental program
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Effect test

experiment example 1

[0050] The preparation of bufolin, cinobufagin and bufabugenin combined content greater than 95% of the toad venom extract comprises the following steps:

[0051] (1) Pulverize the toad venom medicinal material into coarse powder, pass through a 60 mesh sieve, and dissolve in ethanol with a volume concentration of 80%. Wherein, the quality of ethanol is 10 times that of the coarse powder, and is dissolved by heating in a water bath, and the heating temperature of the water bath is 80 ℃, the heating time is 1h; then suction filtration, the ethanol in the filtrate is evaporated and dried to obtain the crude extract.

[0052] (2) Add the crude extract to distilled water, wherein the quality of distilled water is 10 times of the quality of the crude extract, and ultrasonically suspend to obtain a suspension; then add ethyl acetate for extraction, wherein the quality of ethyl acetate is 10 times that of the quality of the suspension times, the extract was obtained; the ethyl acetat...

experiment example 2

[0059] The common solution (bufadienolidessolution, BU-S) of the above-mentioned toad venom extract is used for anti-glioma drugs, and its 5mL standard dosage composition is: 2.5mg bufadienolide extract, 2.5mL the first solvent propylene glycol, and the rest is the second Solvent injection water. Wherein, the comprehensive content of bufolin, cinobufagin and lipobufagenin in the toad venom extract is greater than 95%. This experimental example 2 uses the toad venom extract prepared in experimental example 1.

[0060] The preparation method of the common solution of the above-mentioned toad venom extract comprises the following steps: weigh 2.5 mg of the toad venom extract, put it in a 5 mL measuring bottle, add 2.5 mL of propylene glycol, dissolve it by ultrasonic, add water for injection to dilute to a constant volume of 5 mL, shake well, and use 0.22 Filter through a μm filter membrane.

experiment example 3

[0062] A kind of anti-glioma drug based on toad venom extract of the present invention is bufaxin submicroemulsion preparation (BU-SCP), and its 100mL standard dose components are: 50mg toad venom extract, 10g medium chain triglyceride Ester (MCT), 3g lecithin, 0.2g poloxamer 188 (F-68), 2.5g glycerin, 0.05g sodium oleate, and the rest is water for injection. Wherein, the comprehensive content of bufolin, cinobufagin and lipobufagenin in the toad venom extract is greater than 95%. This experimental example 3 uses the toad venom extract prepared in experimental example 1.

[0063] The preparation method of the above-mentioned bufaxin submicroemulsion preparation (BU-SCP) is characterized in that the preparation of its 100mL standard dose comprises the following steps:

[0064] (1) Add 3g of lecithin and 50mg of toad venom extract to 10g of medium-chain triglyceride (MCT) respectively, heat and stir to dissolve, and obtain a clear drug-containing oil phase; wherein, the heating...

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Abstract

The invention relates to antitumor drugs and discloses anti-glioma drugs based on Venenum Bufonis extract and a preparation method thereof, the drugs being a bufotalin submicron emulsion and a bufotalin nanoparticle preparation, wherein the bufotalin submicron emulsion comprises Venenum Bufonis extract, medium chain triglyceride, a lecithin, poloxamer 188, glycerol, sodium oleate and injection water; the bufotalin nanoparticle preparation comprises Venenum Bufonis extract, glycerol monostearate, medium-chain fatty acid glyceride, oleic acid, a lecithin, poloxamer 188, sodium deoxycholate and injection water. Both the two preparations can combine with endothelial cells in cerebral blood capillaries, enabling the drugs to be transmitted into the brain through membranes or by means of adsorption, medication, endocytosis and transferring, cerebral targeting of the drugs is improved, and further increase of bufotalin in the brain is facilitated, and glioma resistance is achieved by inducing apoptosis and excessive autophagy of cells.

Description

technical field [0001] The invention relates to antitumor drugs, in particular to an anti-glioma drug based on toad venom extract and a preparation method thereof. Background technique [0002] Glioma is the most common primary brain tumor due to the canceration of glial cells in the brain and spinal cord, accounting for about 35% to 61% of intracranial tumors. It is highly invasive and has a poor prognosis. Malignant tumors with high incidence and disability. At the beginning of the onset of brain glioma, there are usually no typical symptoms, and the invasive growth characteristics of glioma located in important functional areas and deep parts make it difficult to completely resect, and it is not very sensitive to radiotherapy and chemotherapy, and it is very easy to relapse. However, chemical drugs and general anti-tumor traditional Chinese medicines are difficult to kill glioma cells and penetrate the blood-brain barrier at the same time, and the curative effect is not ...

Claims

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Application Information

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IPC IPC(8): A61K35/65A61K9/107A61K9/14A61P35/00
Inventor 赵婷
Owner 赵婷
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