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Curcumin-zinc compound as well as solid dispersion preparation and uses thereof

A solid dispersion and zinc compound technology, which is applied in the direction of zinc organic compounds, aldehyde/ketone chelate preparation, medical preparations of non-active ingredients, etc., can solve the problems of single drug application and unsatisfactory curative effect, and achieve The preparation method is simple, the single applicable disease of the drug is overcome, and the curative effect is remarkable

Active Publication Date: 2008-06-25
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a curcumin-zinc compound and its solid dispersion preparation with remarkable curative effect and wide application in view of the common problem of single drug application and unsatisfactory curative effect in the existing treatment of senile diseases

Method used

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  • Curcumin-zinc compound as well as solid dispersion preparation and uses thereof
  • Curcumin-zinc compound as well as solid dispersion preparation and uses thereof
  • Curcumin-zinc compound as well as solid dispersion preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 curcumin-zinc compound

[0021] Curcumin, 99.6% pure, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Zinc acetate dihydrate (abbreviation: zinc acetate), analytically pure, provided by Guangzhou Chemical Reagent Wholesale Department.

[0022] 4.8 grams of curcumin were dissolved in 300ml of absolute ethanol, 2.9 grams of zinc acetate were dissolved in 150ml of absolute ethanol, the zinc acetate ethanol solution was added dropwise in the curcumin ethanol solution, stirred while dropping, and heated under reflux for 3 hours, When the precipitation is complete, collect the precipitate by suction filtration, shake and suspend the precipitate with 300ml of 5°C absolute ethanol again, centrifuge at 5000rpm for 5min, collect the precipitate, then shake and suspend with 300ml of absolute ethanol, and centrifuge at 5000rpm for 5min to obtain 4.9 grams of curcumin...

Embodiment 2

[0023] The preparation of embodiment 2 curcumin solid dispersion, curcumin-zinc compound solid dispersion

[0024] Curcumin, a curcumin-zinc compound with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Polyvinylpyrrolidone PVP-k30 (referred to as PVP), imported and repackaged, provided by Guangzhou Chemical Reagent Wholesale Department.

[0025] 10.0 grams of curcumin were dissolved in 400ml of dehydrated ethanol solution containing 80.0 grams of PVP, protected by nitrogen gas, homogenized by a high-pressure homogenizer, and spray-dried to obtain 86.7 grams of curcumin-zinc solid dispersion.

[0026] 10.0 grams of curcumin-zinc compounds were dissolved in 400ml of dehydrated ethanol solution containing 80.0 grams of PVP, protected by nitrogen, homogenized by a high-pressure homogenizer, and spray-dried to obtain 86.2 grams of curcumin-zinc solid dispersion.

Embodiment 3

[0027] Embodiment 3 to mouse acute toxicity test

[0028] Experimental sample: curcumin-zinc solid dispersion (mass ratio curcumin-zinc:PVP:SDS=1:6), provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Life Sciences, Sun Yat-sen University. Experimental animals: NIH mice, 18-22g, 60, half male and half male, provided by Guangdong Medical Experimental Animal Center.

[0029] Method and Results:

[0030] Choose healthy NIH line mice, body weight 20 ± 2g, 20, half male and half male, after the mice are fasted and watered for 12h, each group of mice is fed with curcumin-zinc solid dispersion (200mg / 0.5 ml) solution 0.8ml, observed continuously for 7 days, the mice were active and agile, did not cause death or abnormal reaction, limited to the test sample volume can not be increased, so the maximum tolerance test was carried out.

[0031] Select 20 healthy NIH mice in addition, with a body weight of 20 ± 2g, half male and half female. After t...

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Abstract

The invention discloses a curcumin-zinc compound, a preparation method and application of solid dispersions of curcumin-zinc compounds. The weight ratio of the curcumin-zinc compounds to the polyvinylpyrrolidone K30 ranges from 1 to 1 to 1 to 28. The curcumin and the acetic acid are dissolved in the organic solvents and the organic solutions containing the zinc acetate are added drop by drop in the organic solutions containing the curcumin under the protection of the nitrogen; the obtained mixtures are stirred, refluxed, cooled down and filtered; the precipitates are collected and then washed; the precipitates are dried in a vacuum environment so as to obtain the curcumin-zinc compounds. The curcumin-zinc compounds and the PVP-k30 are mixed with each other and dissolved in the ethanol under the protection from the pumped nitrogen; the obtained mixtures are homogeneously filtered and then the filtrates are subject to the spray drying so as to obtain the solid dispersions of the curcumin-zinc compounds. The solid dispersions of the curcumin-zinc compounds overcome various weakpoints of the curcumin, are outstandingly effectively in treatment of various senile diseases, solve the problems widely existing in the treatment of senile diseases that the drug indication is single and the efficacy is not ideal, have simple preparation method and wide application prospect.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to the structure of a curcumin-zinc compound, the preparation method of the curcumin-zinc compound and its solid dispersion, and its medical and health care applications. Background technique [0002] Total curcumin [including curcumin, demethoxycurcumin, bisdemethoxycurcumin], the main active ingredient is curcumin, which has a good free radical scavenging , anti-oxidation, anti-mutation, anti-aging, anti-radiation, anti-virus, anti-cancer, anti-cancer, lowering blood fat and cholesterol, anti-atherosclerosis, treatment of depression and other health care and pharmacological effects. [0003] Although curcumin has a wide range of pharmacological effects, it is extremely difficult to dissolve in water, has extremely low bioavailability, and is unstable under alkaline conditions or light conditions, which greatly limits its application in drug development. Oral administrat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F3/06A61K9/00A61K31/555A61P37/00A61P1/00A61P9/00A61P25/00A61P31/00A61P35/00
CPCC07C45/77C07C49/92C07F3/003A61K47/481A61K9/0095A61K9/1635A61K47/55A61P1/00A61P1/04A61P25/00A61P25/28A61P29/00A61P31/00A61P35/00A61P3/06A61P37/00A61P9/00
Inventor 梅雪婷许东晖许实波
Owner SUN YAT SEN UNIV
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