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Production method of hydrophilic betulinic acid preparation

A betulinic acid, hydrophilic technology, applied in the directions of anti-inflammatory agents, antiviral agents, pharmaceutical formulations, etc., can solve the problems of low solubility of β-cyclodextrin and low drug inclusion efficiency, and achieve the promotion of inclusion , Improve solubility, increase the effect of solubility

Inactive Publication Date: 2014-09-03
NORTHEAST FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But β-cyclodextrin itself is not very soluble in water, so the efficiency of inclusion of drugs is relatively low

Method used

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  • Production method of hydrophilic betulinic acid preparation
  • Production method of hydrophilic betulinic acid preparation
  • Production method of hydrophilic betulinic acid preparation

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Experimental program
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Effect test

specific Embodiment approach 1

[0017] Specific embodiment one: the preparation method of hydrophilic type betulinic acid preparation of the present embodiment, carry out according to the following steps:

[0018] 1. Weigh 40-60g of β-cyclodextrin and add it to 400-500mL of distilled water to obtain a cyclodextrin solution. Dissolve 6-7g of NaOH in 20-25mL of distilled water to obtain a NaOH solution. Add the prepared NaOH solution dropwise into the cyclodextrin solution to obtain a homogeneous transparent solution, take 7-10g p-toluenesulfonyl chloride and dissolve it in 30-40mL acetonitrile to obtain a mixed solution, add the mixed solution dropwise to the homogeneous transparent solution, and stir at room temperature React for 2 to 4 hours, filter with suction to obtain a precipitate, store the filtrate at 0 to 5°C for 12 hours, and then filter with suction to obtain a precipitate, dry the precipitate obtained twice in vacuum for 12 to 16 hours to obtain a white solid, wash the white solid with absolute et...

specific Embodiment approach 2

[0022] Specific embodiment 2: The difference between this embodiment and specific embodiment 1 is that in step 2, 2g of 6-p-toluenesulfonyl-β-cyclodextrin, 25 mg of KI and 0.57 mL of diethylenetriamine were dissolved in 5 mL of dry N- in methylpyrrolidone. Others are the same as in the first embodiment.

specific Embodiment approach 3

[0023] Embodiment 3: This embodiment differs from Embodiment 1 or Embodiment 2 in that: the specification of the resin column in step 2 is: 25×450 mm, 724 weakly acidic cation exchange resin, and the resin filling height is 250 mm. Others are the same as in the first or second embodiment.

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Abstract

The invention provides a production method of a hydrophilic betulinic acid preparation and relates to a preparation method of a betulinic acid preparation. The production method of the hydrophilic betulinic acid preparation aims at solving the problem that the use of the betulinic acid in the aspect of medical preparations is limited because the betulinic acid is insoluble in water. The method comprises the following steps: 1, preparing 6-p-toluenesulphonyl-beta-cyclodextrin, 2, preparing 6-diethylenetriamine chain-beta-cyclodextrin, 3, preparing a diethylenetriamine bridged-beta-cyclodextrin dimer, and 4, weighing 6-diethylenetriamine chain-beta-cyclodextrin or the diethylenetriamine bridged-beta-cyclodextrin dimer and putting the weighed sample in a sample tube, adding distilled water to the sample tube for dissolving the sample, next, adding the betulinic acid, carrying out ultrasonic oscillation, continuing oscillating on an oscillator, centrifuging, filtering the supernatant liquor by use of a water-phase cellulose filter membrane, and then drying the filtrate, thereby obtaining a white powder, namely the hydrophilic betulinic acid preparation. The production method is used for producing the betulinic acid preparation.

Description

technical field [0001] The invention relates to a preparation method of betulinic acid preparation. Background technique [0002] Betulinic acid, also known as betulinic acid, is a pentacyclic triterpenoid compound, widely present in birch bark and other plants, and can also be synthesized from betulin, with a molecular weight of 456.71g / mol, colorless Needle crystal, molecular formula: C 30 h 48 o 3 , Molecular structure formula: [0003] As a natural bioactive substance, betulinic acid has antimalarial and anti-inflammatory effects. The study found that betulinic acid has a good anti-cancer effect on human melanoma, and also has a good therapeutic effect on lymphoma, prostate cancer and other diseases. Betulinic acid has attracted extensive attention from researchers because of its anti-tumor growth effects and its new mechanism of action in the fight against acquired immunodeficiency syndrome (AIDS). Betulinic acid not only has many medicinal mechanisms, but also ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/56A61P33/06A61P29/00A61P35/00A61P31/18
Inventor 王霆董仕辉阎秀峰王洋
Owner NORTHEAST FORESTRY UNIVERSITY
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