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Purification preparation method of isoalantolactone and application of isoalantolactone in preparation of anti-tumor drugs

A kind of technology of isoaurinolide and anticancer drug, which is applied in the purification and preparation of isoaurinolide and its application in the preparation of antineoplastic drugs, can solve the problems of many side effects and impurity of the extract, and achieve the product Increased yield, good crystal form, and large output

Inactive Publication Date: 2011-08-24
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, inulin and its derivatives contained in inulin volatile oil are easily soluble in alcohol, so its extract is impure and has many side effects (see Institute of Materia Medica, Chinese Academy of Medical Sciences, etc. Chinese Materia Medica (Volume 1) [ M〕Beijing: People's Health Publishing House, 1979, 86)

Method used

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  • Purification preparation method of isoalantolactone and application of isoalantolactone in preparation of anti-tumor drugs
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  • Purification preparation method of isoalantolactone and application of isoalantolactone in preparation of anti-tumor drugs

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Effect test

Embodiment 1

[0044] Purification and Preparation of Isoalactone

[0045] a) using Hebei Asteraceae Inula inulata as raw material, extracting by cold soaking with 99% ethanol, filtering, and concentrating the filtrate under reduced pressure to obtain an extract;

[0046] b) Suspend the extract in saturated brine to make the concentration about 1g / ml, and extract it with petroleum ether for 3 times at 75°C, and the volume of the extraction solvent is 2 / 3 and 1 / 2 of the volume of the aqueous solution respectively , 1 / 3, combined petroleum ether extracts, and with anhydrous Na 2 S0 4 After dehydration, concentrate under reduced pressure until nearly free of water, and obtain petroleum ether extracts;

[0047] c) Separation by silica gel column chromatography, gradient elution with petroleum ether-ethyl acetate solvent system, the eluent ratio is 10:1, 8:2, 6:4, 5:5, and finally ethyl acetate , Methanol flushes the column until the elution is complete, the eluent is received by volume, each ...

Embodiment 2

[0048] Embodiment 2 pharmaceutical granules of the present invention

[0049] Grind the dried material of the xenoglycan lactone prepared in Example 1 into powder, add ethanol as a binder, add starch as a filler, and press into granules.

Embodiment 3

[0050] Embodiment 3: medicine oral liquid of the present invention:

[0051] Dissolve the xenocystolide prepared in Example 1 in 1000ml of water to make a 2.5% aqueous solution, add an appropriate amount of suspending agent, mix evenly, put it into a 20ml medicine bottle, seal and sterilize.

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Abstract

The invention discloses a purification preparation method of isoalantolactone and an application of isoalantolactone in preparation of anti-tumor drugs. The method disclosed by the invention comprises the following steps of: taking elecampane as a raw material, quenching and extracting with ethanol of 90-99%, and concentrating the filtered solution under the reduced pressure to obtain an extract; suspending the extract in saturated brine, extracting for three times with petroleum ether at 60-90 DEG C, mixing the petroleum ether extracting solutions, dehydrating with anhydrous Na2SO4, and then, concentrating under the reduced pressure for nearly drying to respectively obtain petroleum ether extracts; separating by adopting a silica gel column chromatography, carrying out gradient elution with a petroleum ether-ethyl acetate solvent system, sequentially ramming with ethyl acetate and methanol until the elution is complete, receiving eluent by volume (500mL for each fraction), concentrating each fraction under the reduced pressure, and mixing the same fractions; and obtaining the compound isoalantolactone at 8-19 fractions. The isoalantolactone prepared by the method disclosed by the invention has the advantages of high purity, good crystal form and large yield.

Description

[0001] This patent application is a divisional application with an application date of July 10, 2008, an application number of 200810055376.7, and an invention title of "A Purification and Preparation Method of Heterocarcinolide and Its Application in the Preparation of Antitumor Drugs". technical field [0002] The present invention relates to a method for the purification and preparation of a compound and its medical use, in particular to a method for the purification and preparation of isogastrolide and its application in the preparation of antineoplastic drugs. technical background [0003] Inulahelenium is the dried root of Inulahelenium L of Compositae. The root of inulin contains 1-3% volatile oil, and the main components in the oil are inulin, heteroinulin, dihydroinulin and the like. In traditional medicine, the functions of Tumuxiang are mainly to invigorate the spleen and stomach, promote qi and relieve depression, relieve pain and induce miscarriage. Clinically,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P35/00
Inventor 丛斌史清文董玫
Owner HEBEI MEDICAL UNIVERSITY