Preparation method of radix rehmanniae polysaccharide liposome

A polysaccharide and liposome technology of Rehmannia glutinosa is applied in the directions of liposome delivery, non-central analgesics, antipyretics, etc. The effect of encapsulation efficiency, saving raw materials and improving bioavailability

Active Publication Date: 2014-12-10
NANJING AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when rehmannia polysaccharides are directly used in clinical practice, there are disadvantages such as fast metabolism of polysaccharides in the body, short action time, non-concentrated action range, and large clinical dosage.

Method used

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  • Preparation method of radix rehmanniae polysaccharide liposome
  • Preparation method of radix rehmanniae polysaccharide liposome
  • Preparation method of radix rehmanniae polysaccharide liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation of RGPL by ethanol injection method

[0059] Weigh 0.4g of soybean lecithin, 0.05g of cholesterol and 0.1g of Tween 80 and dissolve them in 10mL of absolute ethanol, and dissolve them fully by ultrasonic; -1 The PBS (pH 7.0) solution of rehmannia polysaccharide was slowly introduced into the former, kept at 50 °C and continued to shake for 30 min; placed in a 250 mL round bottom flask, evaporated under reduced pressure at 60 °C to remove ethanol, and then placed in an ultrasonic cell pulverizer for ultrasonic treatment (intensity 50 %, open at 2.5s, stop at 2.5s, and act for 1h), so that RGP can be fully and evenly fused into liposomes, and at the same time make the particle size of RGPL more uniform, so as to obtain RGPL suspension; then squeeze them separately Microporous membranes with a pore size of 0.45 μm and 0.22 μm were repeated three times each to obtain the RGPL solution. Store at 4°C.

[0060] According to calculation, the encapsulatio...

Embodiment 2

[0061] Embodiment 2 film dispersion method prepares RGPL

[0062] Weigh 0.4g of soybean lecithin, 0.05g of cholesterol and 0.1g of Tween 80 and dissolve it in 10mL of chloroform and methanol (1:1) solution, sonicate to fully dissolve it; place it in a 250mL round bottom flask, and evaporate it under reduced pressure at 60°C Organic solvent, when a uniform film is formed on the wall of the flask, introduce 20mL of -1 The PBS (pH7.0) solution of rehmannia polysaccharide was evaporated under reduced pressure at 60°C to elute the film on the bottle wall; hydrated at 25°C for 1 hour; s stop, act for 1h), so that RGP is fully and uniformly fused into liposomes, and also makes the particle size of RGPL more uniform, so as to obtain RGPL suspension; microporous membrane, each repeated three times to obtain the RGPL solution. Store at 4°C.

[0063] According to calculation, the encapsulation efficiency of RGPL prepared by this method is 32.560%.

Embodiment 3

[0064] Embodiment 3 Ammonium sulfate gradient method prepares RGPL

[0065] Weigh 0.4g of soybean lecithin, 0.05g of cholesterol and 0.1g of Tween 80 and dissolve them in 10mL of absolute ethanol, and ultrasonically dissolve them fully; under the vibration of a water bath shaker at 50°C, introduce the former into 10mL of 10% ammonium sulfate solution, Then put it in a 250mL round bottom flask, evaporate the organic solvent under reduced pressure at 60°C; dialyze in PBS (pH7.0) for 24h; -1 The PBS (pH 7.0) solution of rehmannia polysaccharide was slowly introduced into the former, kept at 50°C and continued to shake for 30 minutes; then placed in an ultrasonic cell pulverizer for ultrasonic treatment (intensity 50%, 2.5s on, 2.5s off, 1h), so that RGP Fully and evenly fused into liposomes, and at the same time make the particle size of RGPL more uniform, so as to obtain RGPL suspension; then squeeze it through microporous membranes with pore diameters of 0.45 μm and 0.22 μm, an...

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Abstract

The invention discloses a preparation method of radix rehmanniae polysaccharide liposome, which comprises the following steps: taking soybean lecithin, cholesterol and Tween 80, dissolving in a solvent, and carrying out ultrasonic dissolution; carrying out vacuum evaporation at 30-70 DEG C to remove the organic solvent, and adding aether for dissolution; introducing a radix rehmanniae polysaccharide PBS (phosphate buffer solution) into a reaction vessel to form a two-phase system, and carrying out ultrasonic treatment in an ice water bath to form a stable W / O emulsion; carrying out vacuum evaporation at 30-70 DEG C to form a colloid, adding the PBS, and continuing rotary evaporation to remove the organic solvent; carrying out ultrasonic treatment in an ultrasonic cell disruptor until the radix rehmanniae polysaccharide is fused in liposome, thereby obtaining a radix rehmanniae polysaccharide liposome suspension; and extruding the suspension respectively through microporous filter membranes to obtain the radix rehmanniae polysaccharide liposome. The radix rehmanniae polysaccharide is prepared into the liposome for the first time, and the preparation method of the radix rehmanniae polysaccharide liposome is a reversed-phase evaporation process; by optimizing the response surface, the method can maximally save the raw material and obtain higher drug entrapment efficiency; and by combining the ultrasonic action, the prepared liposome has higher uniformity and higher stability.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a preparation method of Rehmannia glutinosa polysaccharide liposome (RGPL). Background technique [0002] Rehmannia glutinosa has a long history of medicinal use in my country. Rehmannia glutinosa is often used as medicine in two forms: raw rehmannia glutinosa and rehmannia glutinosa. Rehmannia glutinosa has the effects of clearing heat and cooling blood, nourishing yin and promoting body fluid, and rehmannia glutinosa has the effects of nourishing yin and blood, nourishing essence and filling marrow. Rehmannia glutinosa polysaccharide (RGP) is one of the main active ingredients of Rehmannia glutinosa, which has the functions of anti-inflammatory and enhancing the body's immunity. However, when rehmannia polysaccharides are directly used in clinical practice, there are disadvantages such as rapid metabolism of polysaccharides in the body, short action ti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/715A61P29/00A61P37/04
Inventor 王德云黄叶娥胡元亮刘家国余韵陶阳武毅
Owner NANJING AGRICULTURAL UNIVERSITY
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