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Curcumin liposome and its method for preparing freeze-dried powder injection

A technology of freeze-dried powder injection and liposome, which is applied in the field of preparation of curcumin liposome and its freeze-dried powder injection, can solve the problems of instability, poor water solubility of curcumin, difficulty in making injections, etc., and achieve improved stability Sex, increase stability and clinical safety, and reduce the effect of unsafe factors

Inactive Publication Date: 2007-04-11
JIANGSU SIMCERE PHARMACEUTICAL R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The curcumin liposome and freeze-dried powder injection prepared by the film dispersion-high pressure homogenization method are suitable for large-scale industrial production and clinical application, and solve the technical problems that curcumin is poorly soluble in water, unstable, and difficult to make injections

Method used

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  • Curcumin liposome and its method for preparing freeze-dried powder injection
  • Curcumin liposome and its method for preparing freeze-dried powder injection
  • Curcumin liposome and its method for preparing freeze-dried powder injection

Examples

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Effect test

Embodiment 1

[0042]Dissolve 60 mg of curcumin, 0.6 g of hydrogenated soybean lecithin (purity > 95%), and 60 mg of DSPG in a mixed solvent of chloroform / methanol (1:1) to completely dissolve into a clear solution, and dry it under reduced pressure on a constant temperature water bath at 40°C to form a film , placed in a vacuum desiccator for further drying overnight. Add sodium succinate solution (pH6.5) with sucrose to dissolve the membrane at 55°C until multilamellar liposomes (MLV) are formed, and high-pressure homogenization (Niro homogenizer model, NS1001L) to reduce the particle size (1500bar, 5 times) that is to say. After aseptic filtration (the pore size of the membrane filter is 0.22 μm), it is divided into vials and freeze-dried to obtain curcumin liposome freeze-dried powder. After being stored at 40° C. for 3 months, the content of curcumin was 93.2%. Adding water for injection to reconstitute the liposome had an encapsulation efficiency of 89.7% and an average particle diame...

Embodiment 2

[0044] Dissolve 60mg of curcumin, 1.2g of egg yolk lecithin (purity > 95%), and 120mg of DOPG in a mixed solvent of chloroform / methanol (1:1), place in a constant temperature water bath at 35°C to dry under reduced pressure to form a film, and place in a vacuum desiccator Further dry overnight. Add PBS solution (pH6.0) with trehalose to dissolve the membrane at 55°C until multilamellar liposomes (MLV) are formed, and high-pressure homogenization (Niro homogenizer model, NS1001L) reduces the particle size (1500bar , 5 times) to get. After aseptic filtration (the pore size of the membrane filter is 0.22 μm), it is divided into vials and freeze-dried to obtain curcumin liposome freeze-dried powder. After being stored at 40°C for 3 months, the content of curcumin was 94.3%, and the encapsulation efficiency of the liposome reconstituted by adding water for injection was 92.5%, and the average particle diameter was 140.2nm.

Embodiment 3

[0046] Dissolve 60 mg of curcumin, 1.8 g of egg yolk lecithin (purity > 95%), and 180 mg of DSPG in a mixed solvent of chloroform / methanol (1:1) to completely dissolve into a clear solution, and place it in a constant temperature water bath at 38°C to dry under reduced pressure to form a film , placed in a vacuum desiccator for further drying overnight. Add sodium citrate solution (pH5.5) with mannitol to dissolve the membrane at 55°C until multilamellar liposomes (MLV) are formed, and high-pressure homogenization (Niro homogenizer model, NS1001L) to reduce the particle size (1500bar, 5 times) that is to say. After aseptic filtration (the pore size of the membrane filter is 0.22 μm), it is divided into vials and freeze-dried to obtain curcumin liposome freeze-dried powder. After being stored at 40° C. for 3 months, the content of curcumin was 95.6%, and the encapsulation rate of the liposome obtained by adding water for injection to reconstitute was 94.7%, and the average par...

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Abstract

The invention discloses a preparative method for curcumin liposome suitable clinical and mass production and its frozen powder injection, the mass percent for curcumin and natural lipin is 10-60, and for compound one is 1-6, forming frozen powder injection in accordance with percent of 1 lipin and 0.5-2 freeze-dried excipient added.

Description

technical field [0001] The invention belongs to the preparation method of liposome of Chinese herbal medicine extract and its freeze-dried powder injection, specifically curcumin liposome, its liposome freeze-dried powder injection and a corresponding preparation method. Background technique [0002] Curcumin in a broad sense is usually called curcumin, which is derived from commonly used Chinese medicines of the genus Curcuma (Curcuma long L.), Curcuma wenyujin Y.H.Chen et C.Ling, Guangxi Zezhu (Curcuma kwangsiensis S.G.Lee et C.F.Liang) or The active ingredients isolated and extracted from the dried root of Curcuma phaeocaulis Val. include curcumin, demethoxycurcumin and bisdemethoxycurcumin. Curcumin has pharmacological effects such as anti-inflammation, anti-oxidation, lowering blood fat, and anti-tumor. Unless otherwise specified below, curcumin refers to curcumin in a broad sense. [0003] Curcumin is insoluble in water, has low oral bioavailability, and most of it is...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K9/127A61K9/19A61K47/24A61P35/00
Inventor 许向阳林巧平张安元杨士豹王冬春
Owner JIANGSU SIMCERE PHARMACEUTICAL R & D CO LTD
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