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Phospholipid complex of natural Baikal skullcap root active ingredients as well as preparation method and preparation thereof

A technology for phospholipid complexes and active ingredients, which is applied in the field of phospholipid complexes and their preparations, and can solve problems such as poor water solubility and fat solubility.

Active Publication Date: 2013-03-27
BEIJING WEHAND BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] The purpose of the present invention is to provide a phospholipid complex of the natural active ingredients of Scutellaria baicalensis, so as to solve the problem that the above-mentioned natural active ingredients of Scutellaria baicalensis are poor in water solubility and fat solubility. The shortcomings of chemical degradation, improve the hydrophilicity and lipophilicity of the active ingredients of Scutellaria baicalensis, in order to improve the bioavailability of oral preparations, or meet the design requirements of injection preparations and mucosal administration preparations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: drug-loaded phospholipid complex (I)

[0048] Take 0.6g of the active ingredient of baicalein, 3.66g of soybean lecithin, add 40ml of tetrahydrofuran, compound at 40°C for 1 hour, remove the tetrahydrofuran by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C) to obtain the drug-loaded phospholipid complex. Airtightly packaged and stored in the refrigerator.

Embodiment 2

[0049] Embodiment 2: drug-loaded phospholipid complex (II)

[0050] Take 0.6g of the active ingredient of baicalein and 3.62g of soybean lecithin, add 40ml of acetone preheated to 40°C, compound at 40°C for 1 hour, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C), to obtain The drug-loaded phospholipid complex is sealed and stored in a refrigerator.

Embodiment 3

[0051] Embodiment 3: drug-loaded phospholipid complex (III)

[0052] Take 0.4g of the active ingredient of baicalein and 2.43g of soybean lecithin, add 60ml of ethanol acetone preheated to 40°C, compound at 40°C for 2 hours, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C), that is The drug-loaded phospholipid complex is obtained, sealed and packaged, and stored in a refrigerator.

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PUM

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Abstract

The invention discloses a phospholipid complex of natural Baikal skullcap root active ingredients and a preparation method thereof. The natural Baikal skullcap root active ingredients mean an active fraction (the baicalein content is more than 50 percent) or an active ingredient (the baicalein content is more than 90 percent) of baicalein extracted and separated from Baikal skullcap roots serving as a Chinese medicament and an active fraction (the wogomin content is more than 50 percent) or an active ingredient (the wogomin content is more than 90 percent) of wogomin. The water solubility and lipid solubility of the natural Baikal skullcap root active ingredients are poor, the dissolubility of the active ingredients is increased along with rise of the pH value of a solution, and the active ingredients are easily chemically degraded under an alkali condition. Due to the insufficiency of the physical and chemical properties of the natural Baikal skullcap root active ingredients, the active ingredients cannot be prepared into injection, and the bioavailability is low after the active ingredients are orally taken. Through a phospholipid complex technology, the water dispersibility and lipophilic property of the Baikal skullcap root active ingredients are obviously improved, and then the Baikal skullcap root active ingredients can be prepared into high-bioavailability oral preparation, freeze-dried injection or lipid emulsion to meet the requirement for injection or mucosa administration.

Description

[0001] This application is a divisional application of a Chinese patent application with an application date of June 12, 2006, an application number of 200610087480.5, and an invention title of "phospholipid complex of natural active ingredients of Scutellaria baicalensis and its preparation method and preparation". technical field [0002] The invention relates to a phospholipid complex of natural active ingredients of Scutellaria baicalensis and its preparation. Using phospholipids as materials to prepare drug-loaded phospholipid complexes can not only significantly improve the hydrophilicity of the natural active ingredients of Scutellaria baicalensis, but also improve their lipophilicity. On this basis, the design and preparation of various preparations can improve oral bioavailability , or meet the requirements of injection administration and mucosal administration. Background technique [0003] The root of Scutellaria baicalensis Georgi, a plant in the Labiatae family,...

Claims

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Application Information

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IPC IPC(8): A61K36/539A61K47/24A61K47/28A61K47/36A61P1/04A61P1/16A61P11/00A61P11/04A61P13/12A61P31/04
Inventor 刘玉玲曲敬来温纯青温育青曾晓莲刘家琛高雪
Owner BEIJING WEHAND BIO PHARMA CO LTD
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