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Medicinal composition containing triphenyl-boroxin for boron neutron catching treatment

A composition, boron neutron technology, applied in the direction of drug combination, boron compound active ingredients, antineoplastic drugs, etc., can solve problems such as the demand for boron-containing drugs, and achieve high stability effects

Inactive Publication Date: 2003-11-26
周凤英
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] A main purpose of the present invention is to provide a boron-containing drug that can be selectively accumulated in high concentrations in cancer cells to solve the demand for boron-containing drugs for boron neutron capture therapy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach 3

[0018] The specific embodiment of the invention is the synthesis of triphenylboroxine (phenylboronic anhydride) (I)

[0019] Take 3 grams of phenylboronic acid powder in a round-bottomed flask, add 1ml of ethanolamine as a catalyst, add a magnet to stir, and heat the round-bottomed flask at 130° C. for 24 hours in an oil bath. At this point the solution was reddish brown. A part of the reddish-brown solution was taken for thin-layer chromatography (TLC), in which n-hexane and ethyl acetate (5:2, V / V) were used as the developing solution, and the silica gel chromatography sheet was fumigated with iodine vapor. , presents a component dark spot at the Rf value of 0.5.

[0020] To remove excess ethanolamine, the reddish-brown solution was eluted in an aluminum oxide packed column with ethyl acetate as the eluent. Collect the eluate from the previous stage, remove the solvent, and then use n-hexane and ethyl acetate (1:8, V / V) as the eluent to carry out the...

Embodiment

[0023] Example: Preparation of triphenylboroxine (phenylboronic anhydride) iodized poppy oil (triphenylboroxin entrappedlipiodol, TEL):

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PUM

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Abstract

The present invention relates to medicinal composition for boron neutron catching treatment, and is a kind medicinal composition for catching boron neutron to treat liver cancer. The medicinal composition includes triphenyl boroxin as the boron source for boron neutron catching treatment and pharmaceutically acceptable carrier, such as iodized opium poppy seed oil.

Description

technical field [0001] The present invention relates to a medical composition for boron neutron capture therapy (boron neutron capture therapy, hereinafter referred to as BNCT), in particular to a medicinal composition containing triphenylboroxine (phenylboronic anhydride) as a boron source. The pharmaceutical composition of BNCT. Background technique [0002] The inventor of this case discloses a boron-containing iodized poppy oil suitable for boron neutron capture therapy of liver cancer in U.S. Patent No. 6,117,852, which is composed of iodized poppy oil, submicron boron powder, lecithin and C12-C22 fatty acid ( such as linoleic acid). The iodized poppy oil has high accumulative property in liver cancer cells, the lecithin has boron powder carrying capacity, and the C12-C22 fatty acid has the property of helping the lecithin dissolve in the iodized poppy oil. The submicron boron powder must have an appropriate particle size distribution range to ...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61P35/00A61P43/00
Inventor 周凤英
Owner 周凤英
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