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Notoginsen triterpenes liposome and prepartion thereof

The technology of total saponins and total saponins of Panax notoginseng is applied in the field of medicine, which can solve the problems of increased side effects, low curative effect, poor permeability and the like, and achieve the effects of improving poor oral absorption, enhancing curative effect and improving compliance.

Inactive Publication Date: 2004-11-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The injection is administered by infusion, the patient's compliance is poor, and the side effects are also increasing day by day, such as allergic reactions, which affect the application of the drug
The clinical application of oral tablets has a low curative effect. According to relevant reports: Panax notoginseng saponins are extremely water-soluble, and have poor permeability in the gastrointestinal mucosa. Gastrointestinal enzymes and intestinal bacteria metabolize, thus resulting in low bioavailability of PNS oral preparations, in which ginsenoside Rb 1 Oral absolute bioavailability is only 4.35%,; Ginsenoside Rg 1 The oral bioavailability is 18.40%, and it is eliminated quickly in the blood

Method used

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  • Notoginsen triterpenes liposome and prepartion thereof
  • Notoginsen triterpenes liposome and prepartion thereof
  • Notoginsen triterpenes liposome and prepartion thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of Panax notoginseng liposomes by thin film method

[0022] Get 1.25 grams of soybean lecithin (Shanghai Taiwei Pharmaceutical Co., Ltd.), 0.3 grams of cholesterol (Shanghai Chemical Reagent Company, China Pharmaceutical Group) and dissolve it in a 250 ml pear-shaped bottle with 60 milliliters of ether, and evaporate the ether under reduced pressure on a rotary evaporator , the lipid forms a thin film on the wall of the bottle, add 15ml of Panax notoginsenosides phosphate buffer and spin hydration to obtain the Panax notoginseng saponins liposomes. The encapsulation efficiency was 81%.

Embodiment 2

[0023] Example 2 Preparation of Panax notoginseng saponins liposomes by reverse phase evaporation

[0024] Dissolve 2 grams of soybean lecithin and 1 gram of cholesterol in a 250 ml pear-shaped bottle with 100 ml of ether, then add 20 ml of Panax notoginseng phosphate buffer, ultrasonically in a water bath to form a homogeneous single-phase system, and evaporate under reduced pressure to remove the ether until it solidifies. After the gel was formed, continue to evaporate under reduced pressure for 15 minutes to obtain liposomes of Panax notoginseng saponins. The encapsulation efficiency is 60%.

Embodiment 3

[0025] Example 3 Preparation of Notoginseng Total Saponins Liposomes by Freeze-drying

[0026] Dissolve 1.25 grams of soybean lecithin and 0.3 grams of cholesterol in a 250 ml pear-shaped bottle with 60 milliliters of ether, evaporate the ether under reduced pressure on a rotary evaporator, the lipid forms a film on the wall of the bottle, add 15 ml of phosphate buffer saline and spin water To obtain a blank liposome, add an appropriate amount of trehalose, mix well, freeze-dry in a vacuum, and then disperse by shaking with Panax notoginseng phosphate buffer solution to obtain Panax notoginseng liposome. The encapsulation efficiency was 55%.

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PUM

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Abstract

The invention relates to a Notoginsen triterpene liposome and method for preparing same, wherein the Notoginsen triterpene liposome is prepared by adding lipophilic additives into Notoginsen triterpene and phosphatides, which can be prepared into powdered inhalant, aerosol and spray through the conventional methods. By non-injection lung administration, the bioavailability of the medicament can be improved, and the curative effect of the Notoginsen triterpenes for cranial vascular diseases can be enhanced.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a liposome of Panax notoginseng saponins and a preparation method thereof. Background technique: [0002] The survey shows that cardiovascular and cerebrovascular diseases are the second largest factor affecting the life expectancy of the population in my country. With the improvement of people's living standards and the increase of work pressure, the prevalence of cardiovascular and cerebrovascular diseases is becoming younger, and the number of patients is on the rise. At present, most of the available drugs are western medicines, while there are few traditional Chinese medicines, and most of the preparations are traditional dosage forms or common dosage forms. Panax notoginseng (Buck.) F.H.Chen is a species of Panax notoginseng (Buck.) F.H.Chen. It is abundant in Yunnan and Guangxi of my country. The pharmacological effects of Panax notoginseng are to dilate cor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P9/10
Inventor 方晓玲沈央沙先谊
Owner FUDAN UNIV
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