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Ginsenoside Rh2 ester lipidosome and preparation method and application

A technology of ginsenosides and esters, which is applied in the field of medicine, can solve the problems of low bioavailability of ginsenoside Rh2, and achieve the effects of high safety, simple preparation process, and high bioavailability

Inactive Publication Date: 2017-03-22
NANCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] It can be seen from the above public documents that most of them are currently studying the production method of ginsenoside Rh2 and its application in cells, but the bioavailability of ginsenoside Rh2 itself is low

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Weigh 6mg of ginsenoside Rh2 ester, 50mg of lecithin, and 10mg of cholesterol, add 10ml of absolute ethanol in a water bath at 50°C until dissolved, inject 15ml of 0.02M phosphate buffer hydration medium while stirring, hydrate at 45°C for 20min, and rotate Remove ethanol by evaporation, ultrasonic 30min, power 100%, obtain ginsenoside Rh2 ester liposome, fill with N 2 Seal and store in the refrigerator.

Embodiment 2

[0025] Weigh 9 mg of ginsenoside Rh2 ester, 75 mg of lecithin, and 15 mg of cholesterol, add 15 ml of absolute ethanol in a 45°C water bath until dissolved, inject 20 ml of 0.02M phosphate buffer hydration medium while stirring, hydrate at 50°C for 25 minutes, and rotate Remove ethanol by evaporation, ultrasonic 25min, power 90%, obtain ginsenoside Rh2 ester liposome, fill with N 2 Seal and store in the refrigerator.

Embodiment 3

[0027] Weigh 21mg of ginsenoside Rh2 ester, 175mg of lecithin, and 35mg of cholesterol, add 10ml of absolute ethanol in a water bath at 50°C until dissolved, inject 15ml of 0.02M phosphate buffer hydration medium while stirring, hydrate at 45°C for 20min, rotate Remove ethanol by evaporation, ultrasonic 30min, power 100%, obtain ginsenoside Rh2 ester liposome, fill with N 2 Seal and store in the refrigerator.

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PUM

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Abstract

The invention discloses ginsenoside Rh2 ester lipidosome and a preparation method and application. The ginsenoside Rh2 ester lipidosome comprises, by mass percentage, 0.2-0.7% of ginsenoside Rh2 ester, 5-10% of lecithin and 1-2% of cholesterol. The preparation method comprises the steps of weight the ginsenoside Rh2 ester, the lecithin and the cholesterol according to the proportions; adding absolute ethyl alcohol, and taking a water bath at the temperature of 50-55 DEG C till the materials are dissolved; injecting 0.01-0.02 M of a phosphate buffer solution while stirring is conducted; conducting hydration for 20-25 minutes at the temperature of 45-50 DEG C; conducting rotary evaporation to remove ethyl alcohol; conducting ultrasonic treatment for 25-35 minutes, so that the ginsenoside Rh2 ester lipidosome is obtained; and introducing N<2>, conducting sealing, and placing the ginsenoside Rh2 ester lipidosome into a refrigerator for refrigerated preservation. The invention further relates to application of the ginsenoside Rh2 ester lipidosome to preparation of injection or preparations in acceptable dosage forms. The ginsenoside Rh2 ester lipidosome and the preparation method and application are simple in preparation process and high in safety and further have the beneficial effects of being high in targeting performance, slow release property and bioavailability.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a ginsenoside Rh2 ester (Rh2-O) liposome and a preparation method thereof. Background technique [0002] Ginsenosides are isolated from the roots of ginseng and are the main active ingredients of ginseng. Studies have shown that ginsenosides have various pharmacological activities and can regulate the occurrence and development of various diseases, such as cancer, hypertension and atherosclerosis. However, natural ginsenosides are poorly absorbed and degrade rapidly in digestion. After oral administration, most ginsenosides will be metabolized in the human small intestine, and a small part of ginsenosides will be absorbed into the human liver for metabolism and excreted with bile. Ginsenosides can be transformed into fatty acid derivatives that can stay in the body for a long time, and then absorbed into the blood circulation and used by the human body to produce pharmacologic...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/704A61K9/19A61K9/08
CPCA61K31/704A61K9/0019A61K9/127A61K9/19
Inventor 胡蒋宁朱雪梅邓泽元
Owner NANCHANG UNIV
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