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Preparation method for berberine-loaded phospholipid composite nanoparticles

A technology of nanoparticles and berberine, which is applied in the field of pharmaceutical nanotechnology, can solve the problems of low bioavailability, limited wide application, and low solubility of oral berberine tablets, and achieve improved bioavailability, good stability, and uniform particle size Effect

Inactive Publication Date: 2015-09-30
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, berberine has low solubility in water and poor fat solubility, so that it is difficult to be fully absorbed in the gastrointestinal tract. The bioavailability of commercially available oral berberine tablets in humans is very low, which greatly limits its clinical application. widely used

Method used

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  • Preparation method for berberine-loaded phospholipid composite nanoparticles
  • Preparation method for berberine-loaded phospholipid composite nanoparticles
  • Preparation method for berberine-loaded phospholipid composite nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) dissolving soybean lecithin in methylene chloride to prepare a soybean lecithin solution with a concentration of 1 to 10 mg / mL;

[0033] (2) dissolving berberine in hot ethanol to prepare a berberine ethanol solution with a concentration of 1 to 6 mg / mL;

[0034] (3) The above-mentioned berberine ethanol solution is quickly added to the above-mentioned soybean lecithin solution while hot, and rotary evaporation is carried out to obtain a phospholipid monolayer film, wherein the mass ratio of berberine to soybean lecithin is 1:2~6;

[0035] (4) Redissolve the above-mentioned phospholipid monolayer film with 30mL ethanol, then add 15mL ultrapure water and carry out secondary rotary evaporation for 15min to obtain a nanoparticle suspension;

[0036] (5) adding mannose to the nanoparticle suspension to obtain the original medicinal solution, and the concentration of the spray-dried protective agent in the nanoparticle suspension is 2.5%;

[0037] (6) The above-mentione...

Embodiment 2

[0039] (1)~(3) are with embodiment 1;

[0040] (4) Redissolve the above-mentioned phospholipid monolayer film with 20mL ethanol, then add 10mL ultrapure water and carry out secondary rotary evaporation for 15min to obtain a nanoparticle suspension;

[0041] (5) adding mannose to the above-mentioned nanoparticle suspension to obtain the original medicinal solution, and the concentration of the spray-dried protective agent in the nanoparticle suspension is 3.5%;

[0042] (6) The above-mentioned original medicinal liquid is atomized by a single-line micro-jet atomizer under a certain pressure (injection flow rate: 6g / min, resonance frequency: 16kHz, nozzle size: 100 μm), and enters the spray drying tower for drying, and the collection tower The bottom powder was stored at 4°C to obtain the loaded berberine-phospholipid composite nanoparticles with a particle size of 100nm to 200nm. After the prepared nanoparticles were redissolved in water, the obtained solution was measured by d...

Embodiment 3

[0044] (1)~(3) are with embodiment 1;

[0045] (4) Redissolve the above-mentioned phospholipid monolayer film with 25mL of ethanol, then add 10mL of ultrapure water and carry out secondary rotary evaporation for 15min to obtain a nanoparticle suspension;

[0046] (5) adding mannose to the above-mentioned nanoparticle suspension to obtain the original medicinal solution, and the concentration of the spray-dried protective agent in the nanoparticle suspension is 4%;

[0047] (6) The above-mentioned original medicinal liquid is atomized under a certain pressure by a single-line micro-jet atomizer (injection flow rate: 5g / min, resonance frequency: 16kHz, nozzle size: 100 μm), and enters the spray drying tower for drying, and the collection tower The bottom powder was stored at 4°C to obtain the loaded berberine-phospholipid composite nanoparticles with a particle size of 100nm to 200nm. After the prepared nanoparticles were redissolved in water, the obtained solution was measured ...

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Abstract

The invention discloses a preparation method for berberine-loaded phospholipid composite nanoparticles. The preparation method is characterized by comprising the following steps: (1), preparing a soybean phospholipid solution; (2), preparing a berberine ethanol solution; (3), adding the berberine ethanol solution into the soybean phospholipid solution, and carrying out rotary evaporation so as to obtain a phospholipid single-layer film; (4), redissolving the phospholipid single-layer film with an aprotic reaction reagent, and adding ultrapure water for secondary rotary evaporation so as to obtain nanoparticle suspension liquid; (5), adding a spray-drying protective agent into the nanoparticle suspension liquid to obtain an original medical solution; (6), atomizing the original medical solution through a single-line micro jet atomizer under a certain pressure, and drying in a spray-drying tower so as to obtain the berberine-loaded phospholipid composite nanoparticles. The entrapment efficiency of the berberine-loaded phospholipid composite nanoparticles prepared through the preparation method provided by the invention is 85% or above, the berberine-loaded phospholipid composite nanoparticles are uniform in particle size, the particle size is changed slightly after the berberine-loaded phospholipid composite nanoparticles are redissolved in water, in-vitro release of berberine is not influenced, the bioavailability is high and long-term storage stability is high.

Description

technical field [0001] The invention belongs to the field of pharmaceutical nanotechnology, and in particular relates to a preparation method of berberine-loaded phospholipid composite nanoparticles. Background technique [0002] Berberine, also known as berberine, is an isoquinoline alkaloid widely found in Ranunculaceae and other plants. It exists mostly in the form of its own quaternary ammonium salt in nature. As an active ingredient of traditional Chinese medicine, it has been clinically used as a heat-clearing, detoxifying and anti-infective drug for the treatment of gastrointestinal infections. In recent years, with the in-depth research on berberine, other clinical effects of berberine have been widely reported. Existing studies have confirmed that it has good clinical therapeutic effects on neurosis, cardiovascular disease and diabetes. In addition, the combination of berberine and other commercialized drugs has a good synergistic effect in the treatment of arrhyt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/4375A61P31/04A61P1/00A61P3/10A61P9/06A61P9/00A61P3/06A61P25/00
Inventor 陈晓东于飞车黎明
Owner XIAMEN UNIV
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