Curcumin compound injection and intravenous injection preparation thereof

A technology of curcumin and compounds, which is applied in the field of curcumin compound injection solutions and intravenous injections, can solve the problems of difficult industrial production, complicated operation steps, poor operability, etc., achieve liver protection effect, simple prescription process, and easy operation easy effect

Inactive Publication Date: 2011-10-26
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1. Curcumin liposomes, Li Liping et al. (Research on the preparation process of curcumin liposomes [J]. Journal of Fourth Military Medical University, 2009, 30 (24): 3166-3168), which injected curcumin lipids with ethanol The average encapsulation efficiency of the plastid is only 46.69%, the encapsulation efficiency is low, and it takes a long time to operate steps such as water bath and rotary evaporation, so it is difficult to realize industrial production;
[0005] 2. Sustained-release microspheres, Lin Mei et al. (Preparation and sustained-release performance of curcumin microspheres [J]. Journal of Fujian Medical University, 2010, 44(3): 178-181), the encapsulation efficiency can only reach 15.6 %-62.4%, poor operability;
[0006] 3. Curcumin nanoparticles, Liu Zhanjun et al. (Preparation and drug release performance of curcumin nanoparticles [J]. Chinese Materia Medica, 2009.32(2): 277-279), the drug loading capacity of curcumin nanoparticles is 0.3 g / L The encapsulation efficiency was up to 91.6%, but with the increase of curcumin drug concentration, the encapsulation efficiency was only 79.4% when the drug loading was 0.6 g / L, and the encapsulation efficiency decreased with the increase of drug concentration, Poor druggability, water bath, magnetic stirring, and dialysis are used in the preparation process, the operation time is too long, and the operation steps are complicated;
[0008] Due to the various deficiencies in the above-mentioned injections, so far no curcumin compound injections have been used in clinical practice.

Method used

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  • Curcumin compound injection and intravenous injection preparation thereof
  • Curcumin compound injection and intravenous injection preparation thereof
  • Curcumin compound injection and intravenous injection preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Embodiment 1 prepares curcumin intravenous injection

[0046] 1. Preparation of curcumin injection solution:

[0047]Take 5 grams of curcumin, add it to 90 ml of polyethylene glycol 400 solvent, stir and dissolve at 75 ° C, then use polyethylene glycol 400 to make the volume to 100 ml, adjust the pH to 4.5 with an appropriate amount of citric acid, add 0.48 g of needle Use activated carbon to absorb at 70°C for 25 minutes, then filter with a 0.45 μm microporous membrane, divide the filtrate into 2 ml per bottle, press the cap, and then sterilize with high-pressure steam at 105°C for 60 minutes to obtain curcumin injection solution.

[0048] 2. Prepare the emulsion:

[0049] (1) Prepare the oil phase: put 100 grams of soybean oil for injection and 100 grams of caprylic triglyceride in a water bath, heat to 80° C., stir to dissolve, and obtain the oil phase;

[0050] (2) Prepare the water phase: take 650 ml of water for injection, add 12 grams of soybean lecithin for i...

Embodiment 2

[0054] Embodiment 2 prepares curcumin intravenous injection

[0055] 1. Preparation of curcumin injection solution:

[0056] Take 5 grams of curcumin, add it to 90 ml of polyethylene glycol 300, stir and dissolve at 80 ° C, then use polyethylene glycol 300 to make up to 100 ml, adjust the pH to 4.5 with acetic acid, add 0.35 g of needle Activated carbon, adsorb at 65°C for 30 minutes, then filter with a 0.45 μm microporous membrane, divide the filtrate into 2 ml bottles, press the cap, and then sterilize with high-pressure steam at 115°C for 45 minutes to obtain curcumin injection solution .

[0057] 2. Preparation of Emulsion

[0058] (1) Preparation of the oil phase: 100 grams of caprylic triglyceride for injection, 50 grams of soybean oil, 10 grams of lanmenene oil, 10 grams of linseed oil, 15 grams of seabuckthorn oil, 5 grams of zedoary oil, and oyster oil 10 grams, mixed, placed in a water bath, heated to 68°C, stirred to dissolve, and an oil phase was obtained;

[0...

Embodiment 3

[0062] Embodiment 3 prepares demethoxycurcumin intravenous injection

[0063] 1. Preparation of demethoxycurcumin injection solution:

[0064] Take 0.1 g of demethoxycurcumin, add it to a mixed solution of 58 ml of polyethylene glycol 400, 2 ml of absolute ethanol and 25 ml of dimethylacetamide, add 0.05 g of tocopherol, Stir to dissolve, then dilute to 100 ml with polyethylene glycol 400, adjust the pH to 5.5 with hydrochloric acid and sodium hydroxide, add 0.26 g of activated carbon for needles, adsorb at 100 ° C for 15 minutes, and then filter with 0.45 μm microporous Membrane filtration, the filtrate was divided into 5 ml bottles, capped, and then sterilized with high-pressure steam at 105°C for 60 minutes to obtain demethoxycurcumin injection solution.

[0065] 2. Preparation of emulsion:

[0066] (1) Preparation of the oil phase: mix 100 grams of soybean oil for injection and 100 grams of caprylic triglyceride, place in a water bath and heat to 85°C, add 10 grams of so...

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Abstract

The invention relates to the technical field of medicine, and particularly relates to a curcumin compound injection and an intravenous injection preparation thereof. The curcumin compound injection mainly comprises a curcumin compound, a solvent for injection and a small amount of pH regulator. The curcumin compound intravenous injection preparation is used only by mixing the curcumin compound injection and an emulsifier in a volume ratio of (1:5)-(1:250). After the curcumin compound injection and the emulsifier are mixed, the drug loading rate of the curcumin compound in the intravenous injection preparation is up to 1.5 mg/ml, and no crystal is separated out within 18 hours. The curcumin compound injection provided by the invention has a simple and safe preparation method and good stability, and is convenient for storage and transportation. The curcumin compound intravenous injection preparation has good stability due to the use of the emulsifier as a carrier solvent, and has no toxic and adverse effects. The invention solves the problem that the curcumin compound can not be prepared into the intravenous injection preparation and applied in clinics for a long period of time.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a curcumin compound injection solution and an intravenous injection thereof. Background technique [0002] Curcumin compounds are chemical components extracted from the rhizomes of some plants in Zingiberaceae and Araceae, including curcumin, demethoxycurcumin, bisdemethoxycurcumin, etc. Curcumin compounds are insoluble in water and ether, but soluble in methanol, ethanol, acetone, ethyl acetate, glacial acetic acid and lye. It is unstable in light and alkaline environment, and should be kept away from light. [0003] The main pharmacological effects of curcumin compounds are anti-oxidation, anti-inflammation, anti-coagulation, lipid-lowering, anti-atherosclerosis, anti-aging, eliminating free radicals and inhibiting tumor growth, etc., and has liver protection effect. However, due to the poor water solubility of curcumin, the bioavailability is low when taken orally, and the st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/107A61K31/12A61P1/16A61P3/06A61P7/02A61P9/10A61P29/00A61P35/00A61P39/06
CPCA61K9/0019A61K9/08A61K31/12A61K47/10A61P1/16A61P3/06A61P7/02A61P9/10A61P29/00A61P35/00A61P39/06
Inventor 陈建明揭继龙张广军刘文丽净小龙连建豪张莹莹
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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