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Hepatic targeted temperature sensitive microsphere and preparation method therefor

A technology of liver-targeting and microspheres, which is applied in the field of liver-targeting thermosensitive microspheres and its preparation, can solve the problems of toxic and side effects of treatment effects, difficulty in entering solid tumors, short half-life, etc., and achieves easy industrial implementation, good operability, The effect of mild experimental conditions

Inactive Publication Date: 2014-04-09
TIANJIN POLYTECHNIC UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug therapy for liver diseases is mainly to make drug molecules reach the lesion site, kill the pathogenic virus, and repair the damaged tissue. However, the traditional chemotherapy method, chemotherapy drugs are not selective, and will kill the surrounding non-patients while killing cancer cells. Cells, and the half-life is short, it is easy to be inactivated by contact with plasma proteins, and it is difficult to enter solid tumors due to biological barriers, resulting in reduced drug efficacy, and the treatment effect is too toxic and side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0022] (1) Amination modification of glycyrrhetinic acid

[0023] Dissolve 2.895g glycyrrhetinic acid (GA) in 30mL tetrahydrofuran (THF), cool to -10°C, add 1.77g DCC, stir for 30min, add 0.71g SuOH, continue stirring at -10°C for 3h, and then Stir at room temperature at 20°C for 18 h, filter off dicyclohexyl urea (white solid), pour the resulting solution into anhydrous diethyl ether three times its volume, and let stand overnight to obtain a white precipitate, which is filtered and washed with anhydrous diethyl ether. Vacuum drying to obtain white powdery glycyrrhetinic acid succinimide active ester (GSE). Dissolve 1.015g of GSE in 15mL of DMF, and slowly drop it into 3.5mL of ethylenediamine (EDA) with a constant pressure dropping funnel. After the mixture was reacted at 60°C for 24h, it was distilled under reduced pressure until no fraction flowed out, and the concentrated solution was Dropped into distilled water, white precipitates are produced, filtered, washed several...

example 2

[0029] (1) Amination modification of glycyrrhetinic acid

[0030] Dissolve 5.79g of glycyrrhetinic acid (GA) in 30mL of tetrahydrofuran (THF), cool to -10°C, add 3g of DCC, stir for 30min, add 1.16g of SuOH, continue stirring for 4h at -10°C, and then Stir at room temperature at ℃ for 20 h, filter off dicyclohexyl urea (white solid), pour the resulting solution into anhydrous ether three times its volume, and let stand overnight to obtain a white precipitate, filter, wash with anhydrous ether, and vacuum Dry to obtain white powdery glycyrrhetinic acid succinimide active ester (GSE). Dissolve 2.03g of GSE in 20mL of DMF, and slowly add it dropwise into 7mL of ethylenediamine (EDA) with a constant pressure dropping funnel. After the mixture was reacted at 80°C for 20h, it was distilled under reduced pressure until no distillate flowed out. Added to distilled water, a white precipitate was produced, filtered, washed several times with distilled water to remove DMF and EDA, freez...

example 4

[0043] (1) Amination modification of glycyrrhetinic acid

[0044] Dissolve 5.79g of glycyrrhetinic acid (GA) in 30mL of tetrahydrofuran (THF), cool to -10°C, add 1.77g of DCC, stir for 30min, add 1.42g of SuOH, continue stirring at -10°C for 2h, and then Stir at room temperature at 20°C for 20 h, filter off dicyclohexyl urea (white solid), pour the resulting solution into anhydrous diethyl ether three times its volume, and let it stand overnight to obtain a white precipitate, which is filtered and washed with anhydrous diethyl ether. Vacuum-dried to obtain white powdery glycyrrhetinic acid succinimide active ester (GSE). Dissolve 2.03g of GSE in 15mL of DMF, and slowly add it dropwise into 7mL of ethylenediamine (EDA) with a constant pressure dropping funnel. Added to distilled water, a white precipitate was produced, filtered, washed several times with distilled water to remove DMF and EDA, freeze-dried, and obtained white powdered glycyrrhetinic acid amine derivatives (GA-N...

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Abstract

The invention discloses a hepatic targeted temperature sensitive microsphere and a preparation method therefor, and belongs to the functional polymer material field, and especially relates to a drug sustained release and targeted drug delivery material and a preparation method therefor. The temperature response range of the material is 25 DEG C-37 DEG C, and the particle size of the microsphere is about 500nm. The microsphere can be prepared through the following method: glycyrrhetinic acid (GA) is modified by ethylene diamine and acrylic acid (AAc) and vinyl monomers are generated; ammonium persulfate (APS) is employed as an initiator, N,N-methylene bisacrylamide (MBA) is employed as a cross-linking agent, hepatic targeted temperature sensitive microspheres are prepared through a semicontinuous soap-free emulsion polymerization method. The preparation method has simple technological processes, and mild experiment conditions, needs no special devices, has a low investment cost, and has good operability. The reagents are all common reagents. The reaction residues are easy to remove. The preparation method is convenient for industrial implementation.

Description

technical field [0001] The invention relates to a functional polymer material technology, in particular to a liver-targeting temperature-sensitive microsphere and a preparation method thereof. Background technique [0002] The liver is the largest solid organ in the human body and plays a pivotal role in maintaining life and maintaining the stability of the internal environment. However, diseases such as liver cancer and acute liver failure seriously threaten human health. my country is a high-incidence area for liver diseases in the world. The number of deaths due to liver diseases exceeds 100,000 every year, and the incidence rate accounts for more than 50% of the world. Therefore, the treatment of liver disease has become the top priority in the field of medical and health care. Drug therapy for liver diseases is mainly to make drug molecules reach the lesion site, kill the pathogenic virus, and repair the damaged tissue. However, the traditional chemotherapy method, che...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F220/54C08F222/38C08F220/58C08J3/12A61K47/32A61K9/19A61P35/00
Inventor 贺晓凌卢文甲刘泽丽黎湘旭赵月梅陈莉
Owner TIANJIN POLYTECHNIC UNIV
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