Artesunate and dihydroarteannuin medicine preparation for proofing formation of blood vessel and use thereof

An anti-angiogenesis and dihydroartemisinin technology, applied in the field of pharmaceutical preparations of artemisinin and its derivatives, artesunate and dihydroartemisinin, can solve the problem of low oral activity and recurrence rate High, low water solubility and other issues, to achieve the effect of prolonging the drug action time

Inactive Publication Date: 2003-10-15
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Immediately attracted worldwide attention, due to the shortcomings of low oral activity,

Method used

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  • Artesunate and dihydroarteannuin medicine preparation for proofing formation of blood vessel and use thereof
  • Artesunate and dihydroarteannuin medicine preparation for proofing formation of blood vessel and use thereof
  • Artesunate and dihydroarteannuin medicine preparation for proofing formation of blood vessel and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0029] Example 1: A method for preparing artesunate microsphere injection

[0030] The artesunate is ground with slow-release polymer (Polycaprolactone, PCL), and the molten mixture prepared is made into microsphere injection with biocompatible and biodegradable polymers. The polymer used is hydrolyzed into degradation products (water and carbon dioxide) that are harmless to the human body after release. After intramuscular injection of the microsphere injection, the drug is slowly released and absorbed at the administration site, so that the action time is prolonged, and it can be used for the treatment of tumors and other angiogenesis-related diseases.

Example Embodiment

[0031] Example 2: The overall inhibition of angiogenesis experiment of artesunate microsphere injection

[0032] (1) Inhibit angiogenesis of chicken embryo allantoic membrane

[0033] Experimental materials: artesunate (raw material provided by Guangxi Guilin Second Pharmaceutical Factory) using the microsphere injection of the present invention; hydrocortisone (product of Zhejiang Xianju Pharmaceutical Factory); breeding eggs (purchased from Hangzhou Sijiqing Famous Chicken Farm).

[0034] Method: Open the window of chicken embryos of 7-8 days, add artesunate, positive control substance (hydrocortisone) and solvent control substance (blank microsphere injection) respectively, after incubating for 24 hours, use methanol and acetone 1 :1 The mixed solution fixes the chick embryo allantoic membrane to prepare a specimen, and counts the number of blood vessels under a dissecting microscope.

[0035] result:

[0036] Angiogenesis inhibition rate Artesunate at the doses of 15, 30, 6...

Example Embodiment

[0056] Example 3: In vitro experiment of inhibiting angiogenesis by artesunate and dihydroartemisinin

[0057]Experimental materials: artesunate, dihydroartemisinin (raw materials provided by Guangxi Guilin Second Pharmaceutical Factory)

[0058] method:

[0059] (1) Human umbilical vein endothelial cells (HUVEC) culture

[0060] Take a fresh and healthy fetal umbilical cord, infuse it with 5% collagenase, water bath at 37°C for 15-20 minutes, rinse the umbilical vein with PBS, centrifuge, discard the supernatant, suspend the cells in the culture medium, and place it in a culture flask for culture, the next day The medium was changed once, and the culture medium was DMEM containing 15% calf serum and 10ng / ml VEGF. After the rabbit anti-human factor VIII antibody was used for immunohistochemical identification, the second to third passage cells were used for research.

[0061] (2) HUVEC proliferation inhibition

[0062] Convert HUVEC to 5×10 4 Inoculate in a 24-well culture plate a...

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Abstract

The present invention relates to medicine preparation of arteannuin and dihydroartemisine for resisting vascularization and its use. The preparation has arteannuin or dihydroartemisine as main component and is prepared into microball injection. It is used in treating tumor vascularization and other vascularization relevant diseases and may be also used in chemotherapy of tumor. Its slow release and absorption in the administrated part results in the acting period of the medicine. The present invention is based on vascularization theory, describes the function and mechanism of single Chinese medicinal component, is one important direction for developing Chinese medicine theory and provides basis for developing the new use of artemisine medicine.

Description

Technical field [0001] The invention belongs to pharmaceutical preparations, and relates to pharmaceutical preparations of artemisinin and its derivatives and uses thereof. In particular, it relates to pharmaceutical preparations of artesunate and dihydroartemisinin and their use in anti-angiogenic effects. Background technique [0002] Angiogenesis is the budding or division of existing blood vessels (capillaries and venules) to create new blood vessels. Angiogenesis occurs under physiological and pathological conditions, such as embryogenesis, female reproductive cycle, inflammatory response, wound healing, and tumorigenesis. Especially under pathological conditions, according to statistics, about 20 to 40 human diseases are related to the up-regulation or down-regulation of angiogenesis. In 1971, Folkman established the theory of the connection between angiogenesis and tumor growth, and proposed that angiogenesis can not only provide abundant nutrients for tumor cells t...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/55A61P35/00
Inventor 周慧君陈欢欢王玮琴
Owner ZHEJIANG UNIV
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