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Microsphere containing adriamycin, its usage and preparation

A technology of doxorubicin and microspheres, which is applied to medical preparations containing active ingredients, medical preparations without active ingredients, and pharmaceutical formulas, etc. It can solve the problems of poor controlled release and difficult sustained release drug administration.

Inactive Publication Date: 2007-04-04
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The carrier materials of these microspheres are highly hydrophilic, and the controlled release effect on water-soluble drugs such as doxorubicin is poor, and the drug release is greater than 80% within 12 hours, and it is difficult to administer locally for a long time.

Method used

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  • Microsphere containing adriamycin, its usage and preparation
  • Microsphere containing adriamycin, its usage and preparation
  • Microsphere containing adriamycin, its usage and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1. Doxorubicin Microspheres Containing 5 mg

[0032] Dissolve 5 mg of doxorubicin in 0.1 ml of water, add the aqueous solution to a dichloromethane solution (200 mg / ml) of polylactic acid-glycolic acid (molecular weight 10,000, ratio of lactic acid to glycolic acid: 50:50), and homogenize at a high speed To form colostrum, add the colostrum into 4% polyvinyl alcohol (PVA) aqueous solution, stir to obtain double emulsion (W / O / W), then add distilled water, and continue stirring for 4 hours to completely evaporate the organic solvent to obtain microspheres . Freeze drying yields dry microsphere powders. The encapsulation efficiency of the microspheres is 81%, and the in vitro release curve is shown in Fig. 1 .

Embodiment 2

[0033] Embodiment 2. Containing 5mg doxorubicin microspheres

[0034] Dissolve 5 mg of doxorubicin in 0.1 ml of water, add the aqueous solution to a dichloromethane solution (400 mg / ml) of polylactic acid-glycolic acid (molecular weight 10,000, ratio of lactic acid to glycolic acid is 50:50), and homogenize at a high speed To form colostrum, add the colostrum into 6% polyvinyl alcohol (PVA) aqueous solution, stir to obtain double emulsion (W / O / W), then add distilled water, and continue to stir for 4 hours to completely evaporate the organic solvent to obtain microspheres . Freeze drying yields dry microsphere powders. The encapsulation efficiency of the microspheres is 87%, and the in vitro release curve is shown in Fig. 2 .

Embodiment 3

[0035] Embodiment 3. Containing 5mg doxorubicin microspheres

[0036]Dissolve 5 mg of doxorubicin in 0.1 ml of water, add the aqueous solution to a dichloromethane solution (300 mg / ml) of polylactic acid-glycolic acid (molecular weight 10,000, ratio of lactic acid to glycolic acid: 75:25), and homogenize at a high speed To form colostrum, add the colostrum into 6% polyvinyl alcohol (PVA) aqueous solution, stir to obtain double emulsion (W / O / W), then add distilled water, and continue to stir for 4 hours to completely evaporate the organic solvent to obtain microspheres . Freeze drying yields dry microsphere powders. The encapsulation efficiency of the microspheres is 92%, and the in vitro release curve is shown in Fig. 3 .

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Abstract

A doxorubicin microball used for arterial embolism, intratumor injection, tumor-side injection, or lumbar injection is prepared from polylactic acid-hydroxyacetic acid copolymer. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a doxorubicin microsphere, its application and its preparation method. Background technique [0002] Doxorubicin (Adriamycin) is a powerful broad-spectrum anticancer drug recognized today. This product can be directly embedded between DNA nucleobase pairs, interfere with the transcription process, prevent the formation of mRNA, and play an anti-tumor effect. It not only inhibits the synthesis of DNA but also inhibits the synthesis of RNA, so it has effects on all stages of the cell cycle. It is a non-specific drug for the cell cycle. It has the strongest effect on the S phase, and also has effects on the M, G1 and G2 phases. In addition, it can also lead to the generation of free radicals, which can combine with metal ions and cell membranes. It also has an effect on hypoxic cells. Doxorubicin can produce a wide range of biochemical effects on the body, and has strong cytotoxicity. Clinically used for acute leukemia (lympho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K9/16A61K47/48A61P35/00A61K47/59A61K47/69
Inventor 梅兴国靳浩吴诚
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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