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Stable adriablastina albumin lipid drug-loading system and preparation method thereof

A drug-carrying system, adriamycin technology, applied in the direction of pharmaceutical formulations, liposome delivery, medical preparations containing active ingredients, etc., can solve the problem of no discovery

Inactive Publication Date: 2009-02-11
张文芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The preparation method of albumin microspheres and liposomes and related researches have been found through literature search, but the studies on improving the curative effect of doxorubicin lipid vesicles and the drug loading and encapsulation efficiency of lipid vesicles mosaic albumin have not been found

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Pirarubicin Albumin Lipid Conjugate

[0036] Take 30 mg of pirarubicin, 2.5 g of egg yolk lecithin, 0.5 g of hydrogenated lecithin, 0.1 g of polyethylene glycol butylene glycol cholesteryl ether, 0.2 g of tryptophan, and 0.5 g of albumin, add 50 ml of chloroform / ethanol and stir to make the pirarubicin Ruubicin, egg yolk lecithin, hydrogenated lecithin, and cholesterol were dissolved, and the chloroform / ethanol was distilled off under reduced pressure with a rotary evaporator, and 3 g of sucrose, 2 g of glucose, and PH4 citrate buffer salt were added to a total volume of 50 ml. 2 CO 3 Adjust the pH of the solution to 7.5, heat it at 40°C for 30 minutes, homogenize it with a squeeze filter method or a high-pressure homogenizer until the particle size is 50-200nm, pass through a 0.22 filter membrane and seal it.

[0037] If a freeze-dried preparation is prepared, 5% (weight percent) mannitol is added to the above liquid and freeze-dried.

[0038] If the produ...

Embodiment 2

[0039] Example 2: Epirubicin albumin lipid conjugates

[0040] Take 50 mg of epirubicin, 1 g of egg yolk lecithin, 0.3 g of polyethylene glycol butylene glycol cholesteryl ether, and 3.0 g of albumin, add them into 50 ml of absolute ethanol and stir to dissolve epirubicin, egg yolk lecithin, and cholesterol, and use Rotary evaporator vacuum distillation to remove ethanol, add 5g of sucrose, 0.02g of cysteine ​​hydrochloride, PH6-7 citrate buffer salt to a total volume of 100ml, homogenize with a high-pressure homogenizer until the particle size is 50-200nm, filter through 0.22 The membrane can be packed and sealed.

[0041] If a freeze-dried preparation is prepared, 2-3% mannitol by weight of the system is added to the above liquid as a freeze-drying protectant, and the preparation is obtained after freeze-drying.

[0042] If the product is to be prepared, the environment, heat source, sterility, etc. need to be completed in accordance with the requirements of mass production...

Embodiment 3

[0043] Example 3: Arubicin albumin lipid conjugate

[0044] Take 150 mg of arubicin, 3 g of egg yolk lecithin, 1 g of cholesterol, and 0.7 g of albumin, add 50 ml of dichloromethane and stir to dissolve the arubicin, egg yolk lecithin, and cholesterol, and remove the dichloromethane by distillation under reduced pressure with a rotary evaporator , add 5 grams of sucrose, PH6-7 citrate buffer salt to a total volume of 100ml, homogenize with a high-pressure homogenizer until the particle size is 30-200nm, pass through a 0.22 filter membrane and seal it.

[0045] If a freeze-dried preparation is prepared, 2-3% sucrose by weight of the system is added to the above liquid and freeze-dried according to a conventional process.

[0046] If the product is to be prepared, the environment, heat source, sterility, etc. need to be completed in accordance with the requirements of mass production.

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Abstract

The invention discloses a stable system for carrying adriamycin albumin lipid and a preparation method thereof. The invention is characterized by combining the adriamycin on albumin lipid vesica through ultrasonic, high pressure isotrope or micro-fluidization technique. The invention has the advantages of both significantly improving the efficacy and stability of adriamycin lipid vesica and raising the entrapment rate of medicine in the lipid vesica.

Description

technical field [0001] A stable doxorubicin-albumin lipid drug-loading system and its preparation method, in which albumin is bound to doxorubicin lipid vesicles by ultrasonic, high-pressure homogenization or microfluidization techniques, which can significantly improve the lipid vesicle The stability of the cell and the encapsulation rate of the drug in the lipid vesicle can be improved, especially the therapeutic effect of doxorubicin can be improved. Background technique [0002] Malignant tumor (cancer) is the second most common cause of death in my country after cardiovascular disease. Chemotherapy is one of the important means of treating malignant tumors. Adriamycin drugs have important application value in the treatment of malignant tumors. Due to the high incidence of malignant tumors, new doxorubicin preparations represented by pirarubicin are newly affirmed in the treatment of tumors and other diseases. In the next few years, the use of doxorubicin drugs will cont...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K47/42A61K9/127A61P35/00
Inventor 张文芳
Owner 张文芳
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