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Preparation method of low-ester pectin stabilized composite phospholipid liposome

A technology of low-ester pectin and complex phospholipids, which is applied in liposome delivery, medical preparations of non-active ingredients, drug combinations, etc., can solve the problems of inactivation of active ingredients, reduction of nutritional value, etc., and achieve extended release period , Overcome the effect of low drug loading and reduce leakage

Inactive Publication Date: 2019-03-22
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese Patent No. CN201710396375.8 "A Kind of EGCG Micropill Capsules and Its Preparation Method" discloses a method for making EGCG microcapsules. The traditional microcapsule technology uses spray drying, which will cause the inactivation of active ingredients and greatly reduce the its nutritional value

Method used

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  • Preparation method of low-ester pectin stabilized composite phospholipid liposome
  • Preparation method of low-ester pectin stabilized composite phospholipid liposome
  • Preparation method of low-ester pectin stabilized composite phospholipid liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Accurately weigh 80 mg of soybean lecithin, 80 mg of hydrogenated soybean lecithin, 40 mg of cholesterol, and 10 mg of vitamin C, mix them, dissolve them in 12 mL of absolute ethanol, and ultrasonicate them in a water bath at 300 W for 3 minutes until completely dissolved to obtain a mixture.

[0040] (2) The mixture obtained in step (1) was rotary evaporated under reduced pressure (vacuum degree 0.08 MPa) at 45° C. in a water bath for 40 minutes to remove ethanol until a uniform liposome film was formed on the wall of the rotary evaporation bottle.

[0041] (3) Add 20 mL of 0.05 mol / L phosphate buffer (pH=7.4) and a complex of 5 mg EGCG, 10 mg vitamin E, 5 mg albumin and 5 mg resveratrol to the rotary steamer, and place the mixture in a water bath at 45 ° C. Rotate and hydrate for 45 minutes under the conditions to obtain a liposome suspension.

[0042] (4) Configure 20mL of 0.2g / 100mL low-ester pectin aqueous solution, drop the liposome suspension into the pectin ...

Embodiment 2

[0049] (1) Accurately weigh 90 mg of soybean lecithin, 90 mg of hydrogenated soybean lecithin, 45 mg of cholesterol, and 10 mg of vitamin C, mix them, dissolve them in 10 mL of absolute ethanol, and ultrasonicate them in a water bath at 300 W for 3 minutes until completely dissolved to obtain a mixture.

[0050] (2) The mixture obtained in step (1) was rotary evaporated under reduced pressure (vacuum degree 0.08 MPa) at 45° C. in a water bath for 40 minutes to remove ethanol until a uniform liposome film was formed on the wall of the rotary evaporation bottle.

[0051] (3) Add 20 mL of 0.05 mol / L phosphate buffer (pH=7.4) and a complex of 5 mg EGCG, 10 mg vitamin E, 5 mg albumin and 5 mg resveratrol to the rotary steamer, and place the mixture in a water bath at 45 ° C. Rotate and hydrate for 45 minutes under the conditions to obtain a liposome suspension.

[0052] (4) Configure 20mL of 0.3g / 100mL low-ester pectin aqueous solution, drop the liposome suspension into the pectin ...

Embodiment 3

[0059] (1) Accurately weigh 100 mg soybean lecithin, 100 mg hydrogenated soybean lecithin, 50 mg cholesterol, and 10 mg vitamin C, mix them, dissolve them in 10 mL of absolute ethanol, and ultrasonicate them in a water bath at 300 W for 3 minutes until completely dissolved to obtain a mixture.

[0060] (2) The mixture obtained in step (1) was rotary evaporated under reduced pressure (vacuum degree 0.08 MPa) at 45° C. in a water bath for 40 minutes to remove ethanol until a uniform liposome film was formed on the wall of the rotary evaporation bottle.

[0061] (3) Add 20 mL of 0.05 mol / L phosphate buffer (pH=7.4) and a complex of 5 mg EGCG, 10 mg vitamin E, 5 mg albumin and 5 mg resveratrol to the rotary steamer, and place in a water bath at 45 ° C. Rotate and hydrate for 45 minutes under the conditions to obtain a liposome suspension.

[0062] (4) Configure 20mL of 0.2g / 100mL low-ester pectin aqueous solution, drop the liposome suspension into the pectin solution, mix and stir...

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Abstract

The invention discloses a preparation method of a low-ester pectin stabilized composite phospholipid liposome. The preparation method comprises the following steps: (1) weighing soybean lecithin, hydrogenated soybean lecithin, cholesterol and vitamin C, mixing, dissolving in absolute ethanol, and performing ultrasonic treatment in a water bath till the materials are dissolved completely to obtaina mixture; (2) performing rotary evaporation on the mixture in a water bath of 40 to 50 DEG C under reduced pressure to remove ethanol till a layer of uniform liposome film is formed on the wall of arotary evaporation bottle; (3) adding a phosphate buffer solution and a compound prepared from the EGCG (Epigallocatechin Gallate), vitamin E, albumin and resveratrol in a mass ratio of 1 to 2 to 1 to1 into the rotary evaporation bottle, and performing rotary hydration in a water bath of 40 to 50 DEG C for 30 to 60 min to obtain a liposome coarse suspension; (4) preparing a 0.1 to 0.6 g / 100 mL low-ester pectin aqueous solution, adding the liposome coarse suspension into the pectin solution dropwise, mixing and stirring in a volume ratio of 1 to 1, and finally performing ultrasonic treatment in an ice bath to obtain the low-ester pectin stabilized composite phospholipid liposome. By adopting the preparation method, the slow release performance and oxidization resistance of the liposome canbe improved effectively.

Description

(1) Technical field: [0001] The invention relates to a preparation method of a low-ester pectin-stabilized complex phospholipid liposome. (two) background technology: [0002] Liposome is a kind of conventional drug delivery system in pharmacy, which can be used as the dosage form of poorly soluble drugs to improve their bioavailability. However, ordinary unilamellar liposomes have problems such as low encapsulation efficiency, instability, and easy leakage of drugs during long-term storage, which lead to certain limitations in the development of liposome preparations. As a new type of liposome, complex phospholipid liposomes have the advantages of better stability and no leakage of drugs during long-term storage compared with traditional liposomes, and the intersecting and queuing of complex phospholipids improves the liposome Rigidity has good application prospects. [0003] Traditional liposome-coated resveratrol is usually present in the bimolecules of phospholipids, w...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/36A61K47/24A61K47/42A61K31/05A61P39/06
CPCA61K9/1271A61K9/1277A61K31/05A61K47/24A61K47/36A61K47/42A61P39/06
Inventor 邵平王培冯洁茹孙培龙
Owner ZHEJIANG UNIV OF TECH
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