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A kind of preparation 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 efficiency of inclusion drugs and low solubility of β-cyclodextrin, and achieve the promotion of inclusion , Improve solubility, increase the effect of solubility

Inactive Publication Date: 2016-12-07
NORTHEAST FORESTRY UNIVERSITY
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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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  • A kind of preparation method of hydrophilic betulinic acid preparation
  • A kind of preparation method of hydrophilic betulinic acid preparation
  • A kind of preparation method of hydrophilic betulinic acid preparation

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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 to 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 the reaction at room temperature 2 to 4 hours, to obtain a precipitate by suction filtration, store the filtrate at 0 to 5°C for 12 hours, and then to obtain a precipitate by suction filtration, dry the precipitate obtained twice in vacuum for 12 to 16 hours to obtain a white solid, wash the white solid with absolute e...

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

A preparation method of a hydrophilic betulinic acid preparation relates to a preparation method of a betulinic acid preparation. The present invention aims to solve the problem that betulinic acid is insoluble in water and limits its application in pharmaceutical preparations. Method: 1. 6‑p-toluenesulfonyl‑β‑cyclodextrin; 2. 6‑diethylenetriamine chain‑β‑cyclodextrin; 3. Diethylenetriamine bridged‑β‑cyclodextrin dimer ; 4. Weigh 6-diethylenetriamine chain-β-cyclodextrin or diethylenetriamine-bridged-β-cyclodextrin dimer in a sample tube, add distilled water to dissolve, then add betulinic acid, and ultrasonically oscillate Finally, continue shaking on the shaker, centrifuge, take the supernatant and filter it with a water-phase cellulose filter, and then dry the filtrate to obtain a white powder, which is the hydrophilic betulinic acid preparation. The invention can effectively improve the solubility of betulinic acid in water, thereby solving the difficult problem of betulinic acid in biological preparations. The invention is used for preparing betulinic acid preparations.

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 Patents(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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