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Phosphatide composition of active skull cap components and its prepn process and prepn

A technology of phospholipid complexes and active ingredients, applied in the field of phospholipid complexes and their preparations, can solve the problems of poor water solubility and fat solubility

Active Publication Date: 2007-12-19
BEIJING WEHAND BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] 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

[0041] Embodiment 1: drug-loaded phospholipid complex (I)

[0042] 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

[0043] Embodiment 2: drug-loaded phospholipid complex (II)

[0044] 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

[0045] Embodiment 3: drug-loaded phospholipid complex (III)

[0046] 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 present invention discloses phosphatide composition of active skullcap components and its preparation. The active skullcap components are prepared through extracting and separating skullcap root, and contain baicalin or wogonin over 50 %. The active skullcap components have low water solubility and fat solubility, solubility increasing with raised solution pH value, and easy chemical degradation in alkaline condition, so that the active skullcap components can not be prepared into injection and oral preparation directly. By means of phosphatide composition technology, the present invention improves the water dispersivity and lipophilicity of the active skullcap components, so as to prepare oral preparation with high bioavailability, freeze dried powder for injection, fat emulsion and mucous membrane administration preparation.

Description

technical field [0001] 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 [0002] The root of Scutellaria baicalensis Georgi, a plant in the Labiatae family, has the functions of clearing away heat and dampness, purging fire and detoxification, stopping bleeding and preventing miscarriage. The active ingredients of Scutellaria baicalensis are flavonoids, mainly including four components: baicalin, baicalein, wogomin, and wogonoside. Baicalin (baicalein-7-O-glucuronide) p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/539A61K9/19A61K9/107A61K9/12A61K9/16A61K9/20A61K9/48A61K9/72A61K47/24A61K47/28A61K47/36A61P11/04A61P11/00A61P1/16A61P1/04A61P13/12A61P31/04A61P31/12A61K47/54
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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