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Emulsion containing astilbin and preparation method thereof

A technology of gynecin emulsion and astilbin, applied to medical preparations containing active ingredients, anti-inflammatory agents, pharmaceutical formulas, etc., can solve the problems of high incidence of allergic reactions, large amount of organic solvents, and limited clinical application, etc., to achieve No allergies, improved bioavailability, less side effects

Inactive Publication Date: 2015-06-17
张涛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Astilbin has pharmacological effects such as anti-myocardial ischemia, immune regulation, anti-inflammation, and analgesia, but its clinical application is limited due to its insolubility in water
[0003] Because astilbin compounds are hydrophobic, the preparation of injections requires a large amount of organic solvents or solubilizers with toxic side effects, such as the use of surfactants such as polyoxyethylene castor oil (Cremophor-EL). Drugs are sensitizing, and the incidence of allergic reactions after a large amount of use is high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0020] Preparation Example 1: Preparation of Astilbin Emulsion

[0021] Add 0.5g astilbin, 1.2g egg yolk phospholipid, 0.04g oleic acid to 10g refined soybean oil, heat (60-90 degrees), mix until clear, and get astilbin 50mg / g oil solution. Disperse 1.2g of poloxamer and 2.25g of glycerin into water for injection to obtain an aqueous phase, and under stirring conditions, add dropwise the oily solution of phospholipids containing astilbin to obtain an oily phase into the aqueous phase dispersion system to make a coarse emulsion , add water to 100ml. The obtained coarse emulsion is further emulsified by a milk homogenizer under the condition of a pressure of 100Mpa. After the emulsification, it can be sterilized at 115°C for 30 minutes, and then packaged to obtain a 5mg / ml emulsion.

preparation example 2

[0022] Preparation Example 2: Preparation of Astilbin Emulsion

[0023] Add 0.5g of astilbin, 2g of soy lecithin, and 0.5g of oleic acid into 10g of refined soybean oil, heat, and mix until clear to obtain an oil solution containing astilbin 50mg / g. Add 2.25 g of glycerin and 1.2 g of poloxamer to water for injection to prepare an aqueous phase. Under the condition of stirring, drop the oil solution of phospholipid containing astilbin into the aqueous phase dispersion system to make a coarse emulsion, add water to 100ml. The obtained coarse emulsion is further emulsified by a milk homogenizer under the condition of a pressure of 100Mpa. After the emulsification, it can be sterilized at 115°C for 30 minutes, and then packed to obtain a 5mg / ml emulsion.

preparation example 3

[0024] Preparation Example 3: Preparation of Astilbin Emulsion

[0025] Add 0.5g of astilbin, 3.0g of egg yolk phospholipid, and 0.1g of oleic acid into 10g of refined soybean oil, mix until clear, and obtain an oil solution containing 20mg / g of astilbin. Add 2.25g of glycerin into the water for injection, and slowly add the oil solution of egg yolk phospholipid and oleic acid containing ginsenoside dropwise under stirring condition to the dispersion system to make a coarse emulsion, and add water to 100ml. The obtained coarse emulsion is further emulsified by means of a milk homogenizer under a pressure of 100 MPa. After emulsification, it can be sterilized at 115° C. for 30 minutes, and then packaged to obtain a 5 mg / ml emulsion.

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PUM

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Abstract

The invention provides an emulsion containing astilbin and a preparation method thereof. The emulsion comprises the components of an isotonic agent and a surfactant such as astilbin, water, oil as well as a stabilizing agent. The emulsion does not contain an organic solvent and a solubiliser with toxic and side effects, and has the advantages of no allergy and little side-effect.

Description

field of invention [0001] The invention relates to an emulsion and a preparation method thereof, in particular to an emulsion containing astilbin and a preparation method thereof. Background technique [0002] Astilbin has pharmacological effects such as anti-myocardial ischemia, immune regulation, anti-inflammation, and analgesia, but its clinical application is limited due to its insolubility in water. [0003] Because astilbin compounds are hydrophobic, the preparation of injections requires a large amount of organic solvents or solubilizers with toxic side effects, such as the use of surfactants such as polyoxyethylene castor oil (Cremophor-EL). Drugs are sensitizing, and the incidence of allergic reactions after a large amount of use is high. In view of this, the present invention provides an astilbin emulsion and a preparation method thereof. Contents of the invention [0004] The present invention provides an emulsion containing astilbin. [0005] The invention p...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61P9/10A61P37/02A61P29/00
Inventor 张涛
Owner 张涛
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