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Dexibuprofen liposome as well as preparation method and application thereof

A technology of liposomes and plastids, which is applied in the field of biomedicine, can solve the problem of easy crystallization and precipitation of Dexibuprofen emulsion or gel, reduce the stability of Dexibuprofen topical preparations, and the solubility of Dexibuprofen Low-level problems, to achieve the effect of increasing skin penetration, promoting penetration through the stratum corneum, and increasing skin retention

Inactive Publication Date: 2018-06-22
张恩景
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But, there are following defects and deficiencies in the application of dextrobuprofen topical preparation: the one, dextrobuprofen is low solubility, poor water dispersibility; 3. Dexibuprofen emulsion or gel is easy to crystallize out during placement, which reduces the stability of Dexibuprofen external preparation

Method used

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  • Dexibuprofen liposome as well as preparation method and application thereof
  • Dexibuprofen liposome as well as preparation method and application thereof
  • Dexibuprofen liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Prepare the oil phase: melt 3.0% dipalmitoylphosphatidylglycerol, 1% dipalmitoylphosphatidylethanolamine, 0.5% cholesterol, and 1.0% diethylene glycol monoethyl ether in a 65°C water bath. Then add 1.0% Dexibuprofen, mix well, and set aside;

[0033] (2) Prepare the water phase: add 0.5% vitamin E polyethylene glycol succinate, 5.0% polyethylene glycol 400, 5.0% glycerin, and 0.2% citric acid into 83.8% water, stir and dissolve in a 65°C water bath;

[0034] (3) Preparation of micron-scale dispersion: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at 4000rpm high-speed shear for 10min to make a micron-scale dispersion;

[0035](4) Preparation of liposomes: heat the nano-dispersion prepared in step (3) at 45° C., and then circulate through high-pressure homogenization at 500 bar for 5 times to obtain ibuprofen liposomes. The particle diameter of the ibuprofen liposome is 140nm, and the encapsulation...

Embodiment 2

[0037] (1) Prepare the oil phase: melt 3.0% dipalmitoylphosphatidylglycerol, 2% dipalmitoylphosphatidylethanolamine, 3.0% cholesterol, and 6.0% diethylene glycol monoethyl ether in a water bath at 85°C. Then add 5.0% Dexibuprofen, mix well, and set aside;

[0038] (2) Prepare the water phase: add 2.0% vitamin E polyethylene glycol succinate, 8.0% polyethylene glycol 400, 10.0% glycerin, and 0.18% citric acid into 60.82% water, stir and dissolve in a water bath at 85°C;

[0039] (3) Preparation of micron-scale dispersion: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at 6000rpm high-speed shear for 5min to make a micron-scale dispersion;

[0040] (4) Preparation of liposomes: the nano-dispersion prepared in step (3) was incubated at 70° C., and then circulated 3 times through high-pressure homogenization at 800 bar to obtain Dexibuprofen liposomes. The particle diameter of the ibuprofen liposome is 171nm, and...

Embodiment 3

[0042] (1) Prepare the oil phase: melt 4.0% dipalmitoylphosphatidylglycerol, 4% dipalmitoylphosphatidylethanolamine, 10.0% diethylene glycol monoethyl ether, and 5.0% cholesterol in a 70°C water bath; Then add 10.0% Dexibuprofen, mix well, and set aside;

[0043] (2) Prepare the water phase: add 3.0% vitamin E polyethylene glycol succinate, 7.0% polyethylene glycol 400, 14.0% glycerin, and 0.15% citric acid to 42.85% water, stir and dissolve in a 70°C water bath;

[0044] (3) Preparation of micron-scale dispersion: add the oil phase prepared in step (1) dropwise to the water phase prepared in step (2) and stir continuously, and then emulsify at 1000rpm high-speed shear for 1min to prepare a micron-scale dispersion;

[0045] (4) Preparation of liposomes: heat the nano-dispersion prepared in step (3) at 50° C., and then circulate 8 times through high-pressure homogenization at 1500 bar to obtain Dexibuprofen liposomes. The particle diameter of the ibuprofen liposome is 178nm, a...

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Abstract

The invention relates to a dexibuprofen liposome as well as a reparation method and application thereof. The dexibuprofen liposome is prepared from the following components in percentage by mass: 1.0to 10.0 percent of dexibuprofen, 3.0 to 8.0 percent of phospholipid, 0.5 to 5.0 percent of cholesterol, 1.0 to 10.0 percent of diethylene glycol monoethyl ether, 0.5 to 5.0 percent of vitamin E polyethylene glycol succinate, 10.0 to 30.0 percent of polylol, 0.1 to 0.2 percent of citric acid and the balance of purified water. An oil phase prepared from the dexibuprofen, the phospholipid, the cholesterol and the diethylene glycol monoethyl ether is dropwise added into a water phase prepared from the vitamin E polyethylene glycol succinate, the polylol, the citric acid and the purified water, andthen an obtained mixture is treated through a high-speed shearing emulsification, high-pressure homogenization or high-pressure micro jet device, and the dexibuprofen liposome prepared by the preparation method is high in drug loading capacity, can be used for promoting the dexibuprofen to penetrate through a skin and retain for a long time in a high-concentration manner, and meanwhile, has favorable stability and safety.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a dexibuprofen liposome and a preparation method and application thereof. Background technique [0002] Dexibuprofen is the S-(+)-isomer of ibuprofen, and its chemical name is (S)-2-(+)-(4-isobutylphenyl)propionic acid isomer (C 13 h 18 o 2 ). Ibuprofen is a propionic acid non-steroidal anti-inflammatory drug, which has analgesic, anti-inflammatory and antipyretic effects. Tissue congestion, swelling, reduce the sensitivity of peripheral nerve pain, it plays an antipyretic effect through the hypothalamic thermoregulatory center. Although ibuprofen is a commonly used non-steroidal anti-inflammatory drug at present, its wide application is affected due to reasons such as large oral dose, poor taste and gastrointestinal irritation. In recent years, there have been many clinical adverse reactions of ibuprofen, such as allergic reactions, anaphylactic shock, lower extremity...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/06A61K31/192A61K47/24A61K47/28A61K47/10A61K47/22A61K47/12A61P29/00
CPCA61K9/0014A61K9/06A61K9/1277A61K31/192A61K47/10A61K47/12A61K47/22A61K47/24A61K47/28
Inventor 张恩景潘静
Owner 张恩景
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