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Nano emulsion containing ginsenoside, preparation method and usage

A technology of ginsenoside and nanoemulsion, which is applied in the field of nanoemulsion containing ginsenoside C-K and its preparation, can solve the problems of a large number of organic solvents and the high incidence of allergic reactions, and achieve improved bioavailability, antitumor effect, and side effects small effect

Inactive Publication Date: 2009-06-10
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Because ginsenoside single-component compounds are mostly hydrophobic, so the preparation of injection requires a large amount of organic solvent or use a large amount of solubilizers with toxic and side effects, such as using surfactants such as polyoxyethylene castor oil (Cremophor-EL), the Surfactants 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 containing ginsenoside, preparation method and usage
  • Nano emulsion containing ginsenoside, preparation method and usage
  • Nano emulsion containing ginsenoside, preparation method and usage

Examples

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preparation example 1

[0015] Preparation Example 1: Preparation of Ginsenoside Emulsion

[0016] Add 0.5g of 20(S) ginsenosides C-K, 1.2g of egg yolk phospholipids, and 0.04g of oleic acid into 10g of refined soybean oil, heat (60-90°C), and mix until clear to 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

[0017] Preparation Example 2: Preparation of Ginsenoside Emulsion

[0018] Add 0.5g of ginsenosides C-K, 2g of soybean lecithin, and 0.5g of oleic acid into 10g of refined soybean oil, heat, and mix until clear to obtain an oil solution containing 50mg / g of ginsenosides. 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

[0019] Preparation Example 3: Preparation of Ginsenoside Emulsion

[0020] Add 0.5g of 20(R) ginsenosides C-K, 3.0g of egg yolk phospholipids, 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 present invention provides a nano emulsion of containing ginsenoside, preparation method and usage. The emulsion of containing ginsenoside contains ginsenoside, water, oil, isotonic regulator and surfactant, also can contain stabilizing agent. The emulsion according to the invention does not contain organic menstruum and solubilizer having toxic and side effect, thus the emulsion has not irritability and little side effect; and the active ingredient in the nano emulsion oil is relative high, which satisfies high thickness required by clinical efficacy of the drug, meantime the emulsion also can change distribute of saponin in human body to improve the bioavailability of the drug, the ginsenoside in human body can be concentrated at tumour position to improve the restraining effect of the compound to tumour.

Description

field of invention [0001] The invention relates to a nanoemulsion, its preparation method and application, in particular to a nanoemulsion containing ginsenoside C-K, its preparation method and application. Background technique [0002] Ginsenoside C-K is a compound extracted from ginseng. Ginsenoside C-K has good effects of inhibiting and killing tumor cells in vitro, and reverses the multidrug resistance of tumor cells in vitro. See [Int.Ginseng Symp.(Seoul) 2002 :335-342]. [0003] Because ginsenoside single-component compounds are mostly hydrophobic, so the preparation of injection requires a large amount of organic solvent or use a large amount of solubilizers with toxic and side effects, such as using surfactants such as polyoxyethylene castor oil (Cremophor-EL), the Surfactants 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 thi...

Claims

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Application Information

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