Di-demethoxycurcumin precursor liposome and preparation method thereof

A technology of double demethoxy curcumin and double demethoxy curcumin, applied in the fields of biomedicine and targeted preparations, can solve the problems of leakage, fusion, and no disclosure of in vivo data of solid dispersion preparations, etc.

Inactive Publication Date: 2009-11-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Scholars at home and abroad expect to increase the in vivo absorption by improving the solubility of drugs. CN 1883497A discloses a method for preparing freeze-dried powder injection of curcumin 1 using cyclodextrin inclusion technology. The solvent method of chloroform and methanol is used for cyclodextrin inclusion , can lead to toxicity problems of organic solvent residues
CN1709228A discloses a preparation method of curcumin 1 solid dispersion. Curcumin 1 and polyvinylpyrrolidone are dissolved in propanol or i

Method used

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  • Di-demethoxycurcumin precursor liposome and preparation method thereof
  • Di-demethoxycurcumin precursor liposome and preparation method thereof
  • Di-demethoxycurcumin precursor liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0075] The specific contents of the high-efficiency jet mixing method provided by the invention are as follows:

[0076] (1) The influence of the lipid solution and the flow rate of the hydration medium: Weigh the medicine and the lipid film material (phospholipid and phospholipid derivatives, cholesterol and its derivatives) according to the optimal prescription amount and dissolve them in ethanol, and the fixed lipid solution flow rate is 10mL / min, adjust the flow rate of the hydration medium, measure the encapsulation efficiency and particle size of the liposome, the results are shown in Table 7:

[0077] The influence of table 7 lipid liquid and hydration medium flow velocity ratio on liposome (n=6)

[0078]

[0079] The results show that the flow rate of the hydration medium is more than 10 times that of the lipid solution, and the particle size of the formed lipid vesicles is smaller. Due to the increase of the flow rate of the polar aqueous phase, the drug-containin...

Embodiment 2

[0085] Weigh 16.0g of soybean lecithin, 6.0g of cholesterol and 0.75g of bis-demethoxycurcumin and ultrasonically dissolve them in 85mL of ethanol, put them into the lipid liquid tank 2, and dissolve 1.0g of poloxamer 188 in 980mL of pH6. 5. Phosphate buffer solution (hydration medium), which is packed into the hydration solution tank 4. Turn on the high-pressure irrigation 1 nitrogen, flow the drug-containing lipid liquid into the jet mixer 3, set the flow rate to 10mL / min, and form fine stream droplets through the small holes of the 250μm nozzle; at the same time, turn on the high-pressure pump of the hydration liquid irrigation 4, and the flow rate is 280mL / min, the hydration medium and the lipid alcohol solution are sprayed and mixed continuously and efficiently, and the mixed solution is poured into the tank 6, and the lipid vesicles are formed by automatic stirring and mixing. Open the circulation pipeline, continue high-speed circulation and mixing until the two phases...

Embodiment 3

[0088] Weigh 15.0g of hydrogenated soybean lecithin, 5.0g of cholesterol and 0.7g of bis-demethoxycurcumin and ultrasonically dissolve them in 80mL of ethanol, and put them into the lipid liquid tank 2; Put water into the hydration fluid tank 4. Turn on the high-pressure irrigation 1 nitrogen, flow the drug-containing lipid liquid into the jet mixer 3 at a flow rate of 20mL / min, and inject the liquid droplets into the circulation pipeline in a thin stream through the small hole of the 250μm nozzle, and turn on the high-pressure pump of the hydration fluid irrigation 4 at the same time , the flow rate is 280mL / min, the hydration medium and the lipid alcohol solution are sprayed and mixed continuously and efficiently, and the mixed solution is poured into the tank 6, and the lipid vesicles are formed by automatic stirring and mixing. Open the circulation pipeline, continue high-speed circulation and mixing until the two phases are completely dispersed, open the organic solvent r...

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Abstract

The invention provides a precursor liposome containing di-demethoxycurcumin and a preparation method capable of industrial application. The weight ratio of the di-demethoxycurcumin to phospholipids together with phospholipid derivatives is 1:5-65, 3 to 20 portions of cholesterol together with derivatives thereof and 0.5 to 5 portions of surfactant are prepared into a freeze-dried powder injection according to the portion ratio of the phospholipids to freeze-drying protective agents being 1:0.25-4. The invention relates to a novel technique and a device for preparing a precursor liposome by an efficient jetting-mixing method, has the advantages of good process reproducibility, controllable technical parameters and the like, and can provide a unilocular liposome with fat-soluble medicaments which are stably wrapped in a phospholipid bilayer. The liposome has the average particle size of between 80 and 300 nm, is narrow in the distribution range of particle size, has entrapment rate of more than 85 percent, is low in leakage rate, and is significantly improved in the stability of preparation storage process. The in vivo circulation time of the novel preparation is obviously prolonged during intravenous injection administration, and the AUC of the novel preparation is 2.67 times that of the common injection.

Description

technical field [0001] The invention belongs to the field of biomedicine and targeted preparations, relates to a proliposome of bisdemethoxycurcumin and a preparation method thereof, and provides a device and new technology for producing proliposomes by a high-efficiency jet mixing method Specifically, it is a preparation method for bisdemethoxycurcumin proliposome freeze-dried powder injection for intravenous injection. technical background [0002] Curcuminoids (curcuminoids) are the main active ingredients of the traditional Chinese medicine turmeric. The three monomers are curcumin (curcumin 1), demethoxycurcumin (curcumin 2) and bisdemethoxycurcumin. (bisdemethoxycurcumin, curcumin 3). Studies have shown that curcuminoids have various pharmacological activities such as anti-cancer, anti-inflammation, anti-oxidation and anti-virus, and have potential advantages in cancer treatment [Chen Minjuan et al. Research progress and application prospects of curcumin. 2003, 15 (1)...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/12A61K47/28A61K47/34A61P1/16A61P35/00A61J3/00A61K47/10A61K47/24A61K47/44
Inventor 李娟王广基赵炎磊戴城烽
Owner CHINA PHARM UNIV
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