Baicalin cyclodextrin clathrate compound, preparation and preparing method thereof

A technology of baicalin cyclodextrin and glycoside cyclodextrin, which is applied in the field of medicine, can solve the problems of difficult to achieve therapeutic effect, low bioavailability, insoluble in water, etc., and achieve high drug content, good curative effect, and avoid toxicity Effect

Inactive Publication Date: 2004-12-08
毛友昌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because baicalin is almost insoluble in water, difficult to dissolve in water, oral administration, slow absorption, low bioavailability, it is difficult to achieve the expected therapeutic effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of baicalin β-cyclodextrin inclusion compound: weigh baicalin and β-cyclodextrin according to the above ratio; take baicalin and add appropriate amount of NN-dimethylformamide to dissolve; take another β-cyclodextrin -Cyclodextrin is made into a saturated solution with an appropriate amount of water in a constant temperature water bath at 50-70°C, slowly add the NN-dimethylformamide solution of baicalin dropwise under stirring / ultrasound at a certain speed, and continue to stir / ultrasound for a specified time , stop heating, continue to stir / ultrasound, refrigerate for 24 hours, filter with suction, wash, and dry the precipitate at low temperature to obtain.

Embodiment 2

[0020] Example 2: Preparation of baicalin hydroxypropyl-β-cyclodextrin inclusion compound: Baicalin and hydroxypropyl-β-cyclodextrin were weighed according to the above proportions for later use. Add an appropriate amount of water to hydroxypropyl-β-cyclodextrin, stir to dissolve; take another baicalin and dissolve it with an appropriate amount of NN-dimethylformamide, then drop / add it directly to the above solution, continue to stir / ultrasound, and use a 0.45μ film Filter and then filter with a 0.22μ membrane, and the resulting solution is vacuum-dried / spray-dried / freeze-dried to obtain the obtained solution.

Embodiment 3

[0021] Example 3: Preparation of baicalin hydroxypropyl-β-cyclodextrin inclusion compound: Weigh baicalin and β-cyclodextrin according to the above ratio, add appropriate amount of water / 7 alcohol and water, and keep the temperature at 50-70°C In a water bath, adjust the pH value to 6.0-7.0, stir to dissolve, slowly adjust the pH value to 2-5 under stirring / ultrasound, stop heating, continue stirring / ultrasonic to the specified time, filter with a 0.45μ membrane and then use a 0.22 μ membrane filter, adjust the pH value of the filtrate to about 6.0, and vacuum dry / spray dry / freeze dry to obtain. The resulting powder can be purified once more with ethanol.

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PUM

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Abstract

A scutelloside-cyclodextrin inclusion compound prepared from scutelloside and cyclodextrin or its derivative (beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin), its various preparations including oral-applied ones, suppository, spray, injection, etc. and their preparing process are disclosed. Its advantages are high water solubility, stability and curative effect and low by-effect.

Description

technical field [0001] The present invention relates to the technical field of medicine, specifically, it utilizes cyclodextrin or its derivatives to form an inclusion complex with baicalin or increases the solubility and stability of baicalin in water by adding cyclodextrin or its derivatives, thereby producing into baicalin cyclodextrin inclusion compound and its preparation. Background technique [0002] Baicalin is the main active ingredient in the traditional Chinese medicine Scutellaria baicalensis. It has a wide range of pharmacological effects such as clearing heat and detoxifying, lowering blood pressure, anti-inflammatory and antibacterial, anti-virus, anti-mutation and anti-tumor. It is clinically used for pneumonia, hypertension, hepatitis, infection and other diseases. Its pharmacological research shows that: baicalin can scavenge free radicals and inhibit aldose reductase, which is a promising new way to prevent and treat diabetic ...

Claims

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Application Information

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IPC IPC(8): A61K9/02A61K9/08A61K9/12A61K9/19A61K9/20A61K9/48A61K31/7048A61K47/40A61P9/12
Inventor 毛友昌毛小敏
Owner 毛友昌
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