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Baicalin emulsion and preparation method thereof

A technology of baicalin emulsion and baicalin, which is applied in anti-inflammatory agents, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of content reduction, low oral bioavailability, and instability of baicalin solution, so as to improve stability, Effects suitable for industrial production

Inactive Publication Date: 2014-06-04
QINGDAO BAICAOHUI INST OF CHINESE HERBAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Baicalin is insoluble in water, and its oral bioavailability is very low. lead to lower content

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0015] Preparation Example 1: Preparation of Baicalin Oral Emulsion

[0016] Dissolve 50 mg of baicalin, 2.0 g of soybean lecithin, and 0.5 g of cholesterol in ethanol, add them to 10 g of refined soybean oil, mix until clear, and remove the alcohol by rotary evaporation or nitrogen evaporation to obtain 5 mg / g of baicalin, soybean Phospholipids 200mg / g and 50mg / g cholesterol in oil.

[0017] Disperse 1.0 g of poloxamer into an appropriate amount of water for injection, slowly add baicalin-containing phospholipid and cholesterol oil solution dropwise into the water dispersion system under high-speed stirring conditions to make a coarse emulsion, and dilute with water to 100ml. After the emulsification is completed, sterilize at 100°C for 30 minutes, and dispense to obtain an emulsion containing baicalin 0.5 mg / ml.

preparation example 2

[0018] Preparation Example 2: Preparation of Baicalin Injectable Emulsion

[0019] Dissolve 500 mg of baicalin and 500 mg of oleic acid in ethanol and add them to 10 g of refined soybean oil, mix until clear, and remove the alcohol by rotary evaporation or nitrogen evaporation to obtain 50 mg / g of baicalin and 50 mg / g of oleic acid. soybean oil solution.

[0020] Add 3.0 g of poloxamer and 2.25 g of glycerin to an appropriate amount of water for injection, and slowly add the oil solution containing baicalin and oleic acid dropwise into the above water dispersion system under high-speed stirring conditions to prepare a coarse emulsion. Dilute to 100ml with water for injection. The obtained coarse emulsion was further emulsified by means of a milk homogenizer under the condition of a pressure of 60 MPa. After emulsification, it was sterilized at 100° C. for 30 minutes, and then packaged to obtain 5 mg / ml baicalin emulsion for injection.

preparation example 3

[0021] Preparation Example 3: Preparation of Baicalin Oral Emulsion

[0022] Dissolve 5000 mg of baicalin and 3.0 g of egg yolk phospholipids in ethanol and add them to 40 g of corn oil, mix until clear, and remove the alcohol by rotary evaporation to obtain a corn oil solution containing 125 mg / g of baicalin and 75 mg / g of egg yolk phospholipids.

[0023] Under the condition of high-speed stirring, slowly add the oil solution of phospholipids containing baicalin dropwise and add an appropriate amount of 1% hydroxypropyl β-cyclodextrin in the aqueous solution to make a coarse emulsion, add pure water to 100ml, and divide into baicalin to obtain baicalin Emulsion 50mg / ml.

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PUM

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Abstract

The invention provides a baicalin oral emulsion and an injection emulsion. The emulsion contains baicalin, oil, an emulsifier and water, and the injection emulsion also contains an isoosmotic adjustment agent and the like.

Description

[0001] Summary [0002] The invention provides baicalin oral emulsion and injection emulsion, the emulsion contains baicalin, oil, emulsifier and water, and the injection emulsion also contains isotonic agent. technical field [0003] The present invention relates to baicalin emulsion and its preparation method and application. Background technique [0004] Baicalin (Baicalin) is a flavonoid compound extracted from Scutellaria baicalensis root, which has significant biological activity, antibacterial, diuretic, anti-inflammatory, anti-allergic and antispasmodic effects, and has a strong anti-cancer response equal physiological performance. It has occupied an important position in clinical medicine. Baicalin can also absorb ultraviolet rays, scavenge oxygen free radicals, and inhibit the formation of melanin, so it can be used in both medicine and cosmetics, and is a good raw material for functional cosmetics. [0005] Baicalin is insoluble in water, its oral bioavailabil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/7048A61K47/44A61P7/10A61P21/02A61P29/00A61P31/04A61P35/00A61P37/08
Inventor 张伟福
Owner QINGDAO BAICAOHUI INST OF CHINESE HERBAL MEDICINE
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