Curcumin nano crystallization preparation and preparation method thereof

A nano-crystal, curcumin technology, applied in the directions of antitoxins, anti-inflammatory agents, pharmaceutical formulations, etc., can solve the problems of less absorption, poor compliance, and unsatisfactory solubility, and achieve the effect of improving stability and promoting dissolution and absorption.

Inactive Publication Date: 2009-02-11
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, curcumin is almost insoluble in water, and its solubility in various oils is not ideal, so it has little absorption through the gastrointestinal tract, low oral bioavailability, and injection administration is inconvenient to use, and patients cannot self-administer the drug, and the compliance is poor

Method used

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  • Curcumin nano crystallization preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Accurately weigh 1 g of Tween 80 and lecithin (molar ratio 3:1), add it to 200 ml of distilled water, and dissolve to form a dispersion medium (solution A). Add 1 g of curcumin and disperse evenly by ultrasonic to obtain suspension B. Continue to shear with a high-speed shearer (DIAX 900, Germany) at 1000 rpm for 1 min to obtain colostrum C. Then the colostrum is circulated in the high-pressure milk homogenizer for 2 times at 150 bar, 5 times at 500 bar, and 20 times at 1500 bar or 1300 bar to obtain the curcumin nanocrystal suspension.

[0034] Take an appropriate amount of the suspension, drop it on the copper grid, carry out negative staining with 2% phosphotungstic acid solution, and observe it under the transmission electron microscope (TEM) after natural drying. Between 30-500nm, it can be judged that the preparation is nano-crystal according to the size and shape of the particle.

[0035] Add 2g of mannitol to the above-prepared suspension and put it into a via...

Embodiment 2

[0037] Accurately weigh 0.5g poloxamer (F68), 0.6g phosphatidylcholine, 0.25g sodium cholate, 5g mannitol in 100ml distilled water, add 1.5g of curcumin powder, 10000rpm high-speed shearing 1min, obtained Colostrum, and then the colostrum is circulated 10 times under 1500bar in a high-pressure milk homogenizer to obtain curcumin nano crystal suspension.

[0038] Measure 2ml of the above suspension into a 10ml vial, pre-freeze in a refrigerator at -80°C for 24h, then put it in a freeze dryer at -40°C, 0.10mbar for 48h.

Embodiment 3

[0040] Accurately weigh 0.3g Tween 80, 0.3g poloxamer (F68), 0.05g sodium cholate in 100ml distilled water, add 1g of curcumin powder, 10000rpm high-speed shearing for 1min to obtain colostrum, and then colostrum The milk was circulated 10 times under 1500 bar in a high-pressure milk homogenizer to obtain a curcumin nanocrystal suspension.

[0041] Measure 2ml of the prepared suspension, add 0.1g of sucrose, put it into a vial, put it in the refrigerator for pre-freezing at -80°C for 24h, and then put it in a freeze dryer at -40°C, 0.10mbar for 48h to obtain curcumin nanocrystals Freeze-dried formulations.

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Abstract

The invention relates to a curcumin nano crystal formulation and a preparation thereof. The formulation consists of curcumin and a surface active agent, can be prepared to be lyophilized powders and used for oral dosing. The nano crystal can increase the solubility of the curcumin, promote the absorption thereof in gastrointestinal tract and improve bioavailability. The absorption efficiency of the curcumin nano crystal in the gastrointestinal tract is higher than that of the curcumin micelle formulation obviously, therefore the oral absorption of the curcumin and the bioavailability are improved.

Description

technical field [0001] The invention relates to a curcumin nano crystal preparation and a preparation method thereof. Background technique [0002] Curcumin (curcumin) is a natural active ingredient extracted from the rhizomes of turmeric, curcuma, turmeric, etc. 21 h 20 o 6 . Pharmacological experiments have shown that in addition to anti-inflammatory, anti-cancer, and anti-oxidative effects, curcumin also has various pharmacological effects such as protecting the kidney, inhibiting pulmonary fibrosis, inhibiting liver fibrosis, helping muscle damage repair, treating cataracts, and anti-parasitic diseases , and the toxic and side effects are small, safe to use, and have good prospects for clinical application. However, curcumin is almost insoluble in water, and its solubility in various oils is not ideal, so it has little absorption through the gastrointestinal tract and low oral bioavailability, and injection administration is inconvenient to use, and patients cannot s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/12A61K47/34A61K47/24A61P29/00A61P35/00A61P39/06A61K47/10A61K47/26A61K47/28A61K47/32
Inventor 翟光喜娄红祥高艳李厚丽刘安昌曹丰亮
Owner SHANDONG UNIV
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