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Slow-release liquid crystal nanoparticle containing vinpocetine prepared by supercritical fluid method

A supercritical fluid method, vinpocetine technology, applied in the field of preparations, can solve problems such as difficulties in cubic liquid crystal preparations

Inactive Publication Date: 2011-11-02
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because of the high viscosity of cubic liquid crystals, it is difficult for us to prepare the mixed system of vinpocetine-glycerol monooleate

Method used

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  • Slow-release liquid crystal nanoparticle containing vinpocetine prepared by supercritical fluid method
  • Slow-release liquid crystal nanoparticle containing vinpocetine prepared by supercritical fluid method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038]

[0039] Preparation:

[0040] (a) Glyceryl monooleate and lecithin are added to a certain amount of absolute ethanol, and the water bath is ultrasonically dissolved;

[0041] (b) Vinpocetine is dissolved in 0.1M hydrochloric acid;

[0042] (c) Mix the above two liquids evenly, and pour them into the solution storage tank of the granulation equipment;

[0043] (d) Set supercritical CO 2 The preheating temperature is 65°C, the dry hot air inlet temperature is 75°C, the glycerol monooleate-vinpocetine solution is preheated to 65°C, the gas-liquid mixing chamber is preheated at 65°C, and the saturation pressure is controlled at 10MPa. with supercritical CO 2 The flow ratio is 1:3, prepared with a 0.2mm nozzle;

[0044] (e) Collect the resulting powder.

[0045] (f) Get 25 mg of nanoparticle powder, add it to 0.1% poloxamer solution to disperse, probe ultrasonic (intensity 350W), can obtain vinpocetine slow-release liquid crystal nanoparticles dispersed in water, ta...

Embodiment 2

[0047]

[0048] Preparation:

[0049] (a) Glyceryl monooleate and lecithin are added to a certain amount of absolute ethanol, and the water bath is ultrasonically dissolved;

[0050] (b) Vinpocetine is dissolved in 0.1M hydrochloric acid;

[0051] (c) Mix the above two liquids evenly, and pour them into the solution storage tank of the granulation equipment;

[0052] (d) Set supercritical CO2 The preheating temperature is 65°C, the dry hot air inlet temperature is 75°C, the glycerol monooleate-vinpocetine solution is preheated to 65°C, the gas-liquid mixing chamber is preheated at 65°C, and the saturation pressure is controlled at 10MPa. with supercritical CO 2 The flow ratio is 1:3, prepared with a 0.2mm nozzle;

[0053] (e) collecting the resulting powder;

[0054] (f) Take 25 mg of nanoparticle powder, add it to 0.1% poloxamer solution for dispersion, probe ultrasonic (intensity 350W), and obtain vinpocetine slow-release liquid crystal nanoparticles dispersed in wate...

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Abstract

The invention relates to a slow-release liquid crystal nanoparticle containing vinpocetine prepared by a supercritical fluid method and a preparation method thereof, wherein the nanoparticle comprises active ingredients of vinpocetine, glyceryl monooleate and surfactant. The slow-release liquid crystal nanoparticle of the invention prepared by vinpocetine has an obvious slow-release function relative to a vinpocetine solution and has a remarkably-increased oral bioavailability.

Description

technical field [0001] The invention relates to a sustained-release liquid crystal nanoparticle containing vinpocetine and a preparation method thereof through a supercritical fluid, belonging to the technical field of preparations. Background technique [0002] Vinpocetine (Vinpocetine) is a kind of natural medicine obtained from periwinkle, which belongs to indole alkaloids. At present, this medicine has been widely used in various cardiovascular and cerebrovascular diseases. It is effective for the hyperviscosity of cerebral hemorrhage sequelae and hypertensive coronary heart disease, and is also of great value in understanding the pathology and physiology of cardiovascular and cerebrovascular diseases. However, the oral half-life of vinpocetine in humans is relatively short, about 2 hours, and it needs to be taken 3 times a day. According to literature reports, Vinpocetine belongs to Class 2 drugs in BCS (Biopharmaceutics Classification System), that is, drugs with low ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4375A61K47/34A61K47/28A61K47/24A61P3/06A61P9/10
Inventor 高缘刘承然张建军
Owner CHINA PHARM UNIV