Nano emulsion of containing ginsenoside, preparation method and usage

A technology of ginsenosides and nanoemulsions, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, emulsion delivery, etc., can solve the problems of high incidence and large quantities of allergic reactions, and achieve improved antitumor effect, small side effects, The effect of improving bioavailability

Inactive Publication Date: 2005-06-15
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Protopanaxadiol is a single-component compound of ginsenoside, but because it is hydrophobic, a large amount of organic solvents or solubilizers using a large amount of toxic and side effects are required for the preparation of injections, such as using polyoxyethylene castor oil (Cremophor-EL ) and other surfactants, which are sensitizing, and the incidence of allergic reactions after a large amount of use is high, see [Wei Xiaohui, et al. Chinese Journal of Pharmaceuticals 2001, 32(4): 188-192]

Method used

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  • Nano emulsion of containing ginsenoside, preparation method and usage
  • Nano emulsion of containing ginsenoside, preparation method and usage

Examples

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preparation example 1

[0014] Preparation Example 1: Preparation of Ginsenoside Emulsion

[0015] Add 0.5g of 20(S) protopanaxadiol, 1.2g of egg yolk phospholipid, and 0.04g of oleic acid into 10g of refined soybean oil, heat (60-90°C), mix until clear, and obtain an oil solution containing 50mg / g of ginsenosides . 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 an oil solution of phospholipids containing ginsenosides 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

[0016] Preparation Example 2: Preparation of Ginsenoside Emulsion

[0017] Add 0.5g protopanaxadiol, 2g soy lecithin and 0.5g oleic acid into 10g refined soybean oil, heat and mix until clear to obtain an oil solution containing 50mg / g ginsenoside. 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, add dropwise the oil solution of phospholipid containing ginsenoside into the aqueous phase dispersion system to make a coarse emulsion, and 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

[0018] Preparation Example 3: Preparation of Ginsenoside Emulsion

[0019] Add 0.5g of 20(R) protopanaxadiol, 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 ginsenosides. 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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Abstract

The invention provides a nanoemulsion of ginsenoside, its preparation method and application. The ginsenoside emulsion provided by the invention contains ginsenoside, water, oil, an isotonic agent and a surfactant, and may also contain a stabilizer. The emulsion provided by the invention does not contain organic solvents and solubilizers with toxic and side effects, so it is non-allergic and has small side effects; and the content of active ingredients in the oil phase of the nanoemulsion provided by the invention is relatively high, which meets the high clinical efficacy requirements. At the same time, the emulsion can also change the distribution of saponins in the human body, improve the bioavailability of the drug, and can make the ginsenosides concentrate in the tumor site in the body, so as to improve the antitumor effect of the compound.

Description

field of invention [0001] The invention relates to a nanoemulsion and its preparation method and application, in particular to a nanoemulsion containing protopanaxadiol, its preparation method and application. Background technique [0002] Protopanaxadiol is a single-component compound of ginsenoside, but because it is hydrophobic, a large amount of organic solvents or solubilizers using a large amount of toxic and side effects are required for the preparation of injections, such as using polyoxyethylene castor oil (Cremophor-EL ) and other surfactants, which are sensitizing, and the incidence of allergic reactions after a large amount of use is high, see [Wei Xiaohui, et al. Chinese Journal of Pharmaceuticals 2001, 32(4): 188-192]. In view of this, the present inventor provides a protopanaxadiol nanoemulsion that does not contain an organic solvent and has little toxic and side effects. Contents of the invention [0003] The present invention provides a nanoemulsion cont...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/704A61P35/00
Inventor 林东海张雪梅王振华刘培丽刘珂
Owner SHANDONG LUYE PHARMA CO LTD
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