Berberine-oryzanol compound, and preparation method and application thereof

A compound and synthesis method technology, applied in the field of drug synthesis, can solve the problems of inconvenient administration, large dosage, unsatisfactory absorption, etc., and achieve the effects of improved fat solubility, easy industrialization, and simple synthesis method

Inactive Publication Date: 2011-11-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But practice result shows, when taking above-mentioned medicine, there is following defect: as, take inconvenient, and complicated, need to take 33 pills a day, the shortcoming of big dose, unsatisfactory absorption
[0004] Several studies at home and abroad have reported methods for improving the absorption of berberine, but they have not been able to solve the existing related defects

Method used

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  • Berberine-oryzanol compound, and preparation method and application thereof
  • Berberine-oryzanol compound, and preparation method and application thereof
  • Berberine-oryzanol compound, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 prepares berberine (1)

[0024] According to the synthetic route of formula (II),

[0025]

[0026] In the formula, n=1, X=CH, Y=C=O.

[0027] Dissolve oryzanol (3) in pyridine, slowly add berberine-8-acetyl chloride (2) at room temperature, stir at room temperature for 4 hours after the addition is completed, and pour the reaction mixture into stirring ice water to precipitate Crystallized, filtered, washed with water and dried to obtain crude product. Take the crude product and recrystallize it with ethanol to obtain the fine product of berberine (1).

Embodiment 2

[0028] Embodiment 2 prepares berberine (1)

[0029] According to the synthetic route of formula (II),

[0030]

[0031] In the formula, n=1, X=CH, Y=CH 2

[0032] Dissolve 8-chloroethyl berberine (2) in DMF, add oryzanol sodium salt, stir at 40°C for 10 hours, after the reaction is complete, pour the mixture into ice water under stirring, precipitate crystals, filter, wash with water, and dry , get crude products. Take the crude product and recrystallize it with ethanol to obtain the fine product of berberine (1).

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical synthesis, and particularly relates to a berberine-oryzanol compound having a structure shown in formula (I), and a preparation method and application thereof. In the invention, oryzanol (3) and berberine derivates (2) used as initial reactants are subjected to linking reaction under proper conditions, thus obtaining a berberine-oryzanol compound (1). After going into a human body, the compound is stable in the stomach; and after going into the intestinal tract, the compound can be resolved into berberine derivates and oryzanol in the alkaline environment to produce a medication effect. The compound has high fat solubility and good absorption performance. The compound can be further prepared into medicaments for treating cardiovascular diseases, especially medicaments for treating metabolic syndromes. The synthesis method has the advantages of simplicity and low price, and can be easily industrialized, thereby having very good prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and specifically relates to the compound berbutrine and its preparation method and application. Background technique [0002] At present, my country has entered an aging society, and there are more and more geriatric diseases accompanying it, among which metabolic syndrome, such as hypertension, hyperlipidemia, hyperglycemia and hyperuric acid, is particularly prominent, and these diseases are becoming younger and younger. The emerging situation has attracted the attention of relevant departments and researchers. [0003] In the current clinical treatment of metabolic syndrome, berberine drugs are often used, and the treatment results show that they have a good effect. But because described berberine medicine is a quaternary ammonium salt, for a long time, there is the shortcoming of poor absorption always. Studies have shown that the combination of oryzanol and berberine can increase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00C07J75/00A61K31/58A61P9/00A61P3/00
Inventor 张沪跃
Owner FUDAN UNIV
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