Burdock aglycone microemulsion

A technology of arctigenin and milk preparation, applied in the field of medicine, can solve the problems of low oral bioavailability, poor water solubility of arctigenin, poor water solubility and the like

Active Publication Date: 2011-10-12
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The bioavailability of intragastric administration in rabbits is only 9.5%. The main reason for the analysis is that arctigenin is a fat-soluble compound with poor water solubility, which leads to very low oral bioavailability.
Invention patent application publication specification CN 101036644A discloses a pharmaceutical composition containing arctigenin, the invention includes arctigenin in cyclodextrin derivatives to solve the problem of poor water solubility and bioavailability of arctigenin low problem
[0008] However, there are many difficulties in the preparation of microemulsions.

Method used

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  • Burdock aglycone microemulsion
  • Burdock aglycone microemulsion
  • Burdock aglycone microemulsion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1 Preparation and quality evaluation of arctigenin microemulsion

[0064] 1. The prescription of arctigenin microemulsion concentrate

[0065] Component

Weight / g

Arctigenin

5

Glyceryl caprylate

15

Nonylphenol Polyoxyethylene Ether

50

[0066] 1,2-Propanediol

12.5

Absolute ethanol

12.5

[0067] 2. The preparation process of arctigenin microemulsion

[0068] Weigh the prescription amount of glyceryl caprylate, nonylphenol polyoxyethylene ether, 1,2-propylene glycol, and absolute ethanol, mix and stir well, then add arctigenin, ultrasonic treatment to accelerate the dissolution, to obtain a clear concentrate , Which is the arctigenin microemulsion concentrate. The microemulsion concentrate obtained above is diluted with water in a weight ratio of 1:10-20 to a clear solution to obtain microemulsion.

[0069] 3. Investigation on the physical and chemical properties of arctigenin microemulsion and its quality evaluation method

[0070] 3.1 Appearance t...

Embodiment 2

[0097] Example 2 Microemulsion concentrate

[0098] Component

[0099] Preparation process: Weigh the prescription amount of caprylic acid glyceride, polyoxyethylene castor oil EL-40, 1,2-propanediol, mix and stir evenly, then add arctium aglycone to dissolve, ultrasonic treatment to accelerate the dissolution, to obtain a clear concentrate, that is It is arctigenin microemulsion concentrate. The microemulsion concentrate obtained above is diluted with water in a weight ratio of 1:10-20 to a clear solution to obtain microemulsion. The laser particle size analyzer measured its particle size and the average particle size was 15nm.

Embodiment 3

[0100] Example 3 Microemulsion concentrate

[0101] Component

[0102] The preparation process is the same as in Example 2. The particle size was measured by a laser particle size analyzer, and the average particle size was 35nm.

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Abstract

The invention belongs to the field of medicines and relates to microemulsion. Particularly, the invention relates to microemulsion containing burdock aglycone and a microemulsion carrier, wherein the microemulsion carrier contains an oil phase and an emulsifier; and the average particle size of the microemulsion is 10 to 90 nanometers. The burdock aglycone microemulsion can improve the oral administration bioavailability and tumor suppressing effect of the burdock aglycone obviously.

Description

Technical field [0001] The invention belongs to the field of medicine and relates to a microemulsion preparation. Specifically, the present invention relates to a microemulsion preparation of arctigenin. Background technique [0002] Burdock is the dry and mature fruit of burdock of the compositae family. It is a commonly used traditional Chinese medicine. It has the functions of evacuation of wind-heat, spreading lungs, clearing rash, detoxification, and throat. Itchy cheek erysipelas, carbuncle and sore toxin. This Chinese medicine contains lignan compounds, mainly arctiin and arctigenin. Although the content of arctigenin (also called arctigenin) in burdock seeds is very low, its precursor arctiin has a higher content in the fruits of Chinese medicine burdock and burdock, so a large amount of burdock can be obtained through arctiin Aglycone. According to reports in the literature, arctiin is decomposed into arctigenin in the body to produce numerous pharmacological effects...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/365A61K47/14A61K47/32A61K47/34A61K47/44A61P9/00A61P25/28A61P31/04A61P31/12A61P35/00
CPCA61K9/1075A61K31/365A61K31/7048A61P9/00A61P11/00A61P25/28A61P31/00A61P31/04A61P31/12A61P35/00
Inventor 赵志全郝贵周姚景春
Owner LUNAN PHARMA GROUP CORPORATION
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