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Polysaccharide and bile salt lipidosome for oral administration and preparation method of lipidosome

A liposome and bile salt technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as difficulty in oral absorption, difficulty in achieving ideal pharmacological activity in clinical application, and large molecular weight of polysaccharides , to achieve the effect of reducing damage, increasing in vitro stability, and increasing stability

Inactive Publication Date: 2017-08-04
TAISHAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the polysaccharide molecular weight is too large and has strong hydrophilicity, so it is difficult to absorb orally, and it is difficult to achieve the ideal pharmacological activity in clinical application.

Method used

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  • Polysaccharide and bile salt lipidosome for oral administration and preparation method of lipidosome
  • Polysaccharide and bile salt lipidosome for oral administration and preparation method of lipidosome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Prescription composition: soybean lecithin 800 mg, cholesterol 100 mg, sodium deoxycholate 100 mg, cordyceps polysaccharide 80 mg.

[0025] (2) Preparation: Take 800 mg of soybean lecithin, 100 mg of cholesterol, and 100 mg of sodium deoxycholate, add 100 mL of dichloromethane, and dissolve to form a solution. Take 80 mg of Cordyceps polysaccharide, dissolve it in 30 mL of pH7.4 phosphate buffer, inject it into the dichloromethane solution, and pulse ultrasound for 3 min in ice-water bath to form a stable W / O emulsion. The organic solvent was removed by rotary evaporation at 30°C, and the liquid became a viscous colloid. Add 20 mL of 3% mannitol pH 6.8 phosphate buffer solution, and continue rotary steaming for 30 min. The colloids are dispersed in the solution to obtain a liposome suspension. The liposome suspension was subjected to pulse ultrasonication for 5 min, then homogenized through a high-pressure homogenizer (pressure 200 bar, cycle 3 times), and filtered...

Embodiment 2

[0030] (1) Prescription composition: hydrogenated soybean lecithin 800 mg, cholesterol 100 mg, sodium deoxycholate 100 mg, seaweed polysaccharide 80 mg.

[0031] (2) Preparation: Take 800 mg of hydrogenated soybean lecithin, 100 mg of cholesterol, and 100 mg of sodium deoxycholate, add 100 mL of dichloromethane, and dissolve to form a solution. Dissolve 80 mg of seaweed polysaccharide in 25 mL of pH 7.4 phosphate buffer, inject it into the methylene chloride solution, pulse ultrasonic in an ice-water bath for 3 min to form a stable W / O emulsion. The organic solvent was removed by rotary evaporation at 30°C, and the liquid became a viscous colloid. Add 20 mL of 3% mannitol pH 6.8 phosphate buffer solution, continue rotary steaming for 30 min, and colloids are dispersed in the solution to obtain a liposome suspension. The liposome suspension was subjected to pulse ultrasonication for 5 min, then homogenized through a high-pressure homogenizer (pressure 200 bar, cycle 3 times), ...

Embodiment 3

[0034] (1) Prescription composition: soybean lecithin 800 mg, cholesterol 100 mg, sodium glycocholate 100 mg, pine pollen polysaccharide 100 mg.

[0035] (2) Preparation: Take 800 mg of soybean lecithin, 100 mg of cholesterol, and 80 mg of sodium glycocholate, add 100 mL of chloroform, and dissolve to form a solution. Take 100 mg pine pollen polysaccharide, dissolve it in 30 mL pH7.4 phosphate buffer, inject it into the chloroform solution, and pulse ultrasonic for 5 min in an ice-water bath to form a stable W / O emulsion. The organic solvent was removed by rotary evaporation at 30°C, and the liquid became a viscous colloid. Add 25 mL of 3.2% mannitol pH 6.8 phosphate buffer solution, continue rotary evaporation for 30 min, and the colloids are dispersed in the solution. Pulse ultrasound for 5 min, homogenize with a high-pressure homogenizer (pressure 200 bar, cycle 3 times), and filter through a 0.45 μm microporous membrane to obtain a liposome solution. The filtrate was div...

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Abstract

The invention discloses a polysaccharide and bile salt lipidosome for oral administration and a preparation method of the lipidosome. The preparation method comprises the following steps: preparing a polysaccharide and bile salt lipidosome by adopting a reverse evaporating method, combining high pressure homogenization and filtration of a microfiltration membrane to control the particle size, and performing freeze drying by taking mannitol as a freeze-drying protective additive, thereby obtaining the freeze-dried polysaccharide and bile salt lipidosome powder. A molar ratio of the phospholipid to bile salt is (2:1) to (10:1); a mass ratio of the phospholipid to polysaccharides is (5:1) to (50:1); a molar ratio of the phospholipid to cholesterol is (2:1) to (8:1); and the prepared bile salt lipidosome has the particle size of 200-800 nm and the encapsulation efficiency of 45.0-73.7%. By utilizing the high deformability and biocompatibility, the polysaccharide and bile salt lipidosome can promote oral absorption of the polysaccharides and achieves an effect of improving the body immunity.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine preparations, in particular to a polysaccharide bile salt liposome used for oral administration to improve body immunity and a preparation method thereof. Background technique [0002] Cordyceps, Polygonatum, Astragalus, Ganoderma lucidum and other tonic traditional Chinese medicines have the effects of strengthening the body, strengthening the body and eliminating pathogenic factors, and can improve the body's ability to resist diseases. And some foods such as pine pollen, sea cucumber, etc. also have this effect of strengthening the body. For example, pine pollen is called "longevity powder". It has a long history of eating, and there are many traditional foods such as pine flower cake and pine flower wine. Pine pollen was first recorded in the "Shen Nong's Materia Medica" in the Eastern Han Dynasty, which said that pine pollen "smells sweet and flat and non-toxic, and it c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/715A61K47/28A61P37/04
CPCA61K9/127A61K9/0053A61K31/715A61K47/28
Inventor 李菲毕研平王建筑
Owner TAISHAN MEDICAL UNIV
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