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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, low water solubility, high recurrence rate, etc., the expansion of application is limited

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

Embodiment 1

[0029] Embodiment 1: A kind of method of preparation artesunate microsphere injection

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

Embodiment 2

[0031] Example 2: Artesunate Microsphere Injection Overall Inhibition of Angiogenesis Experiment

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

[0033] Experimental material: artesunate (crude drug is provided by Guangxi Guilin No. 2 Pharmaceutical Factory) adopts the microsphere injection of the present invention; Hydrocortisone (Zhejiang Xianju Pharmaceutical Factory product); Breeding eggs (purchased from Hangzhou Sijiqing Famous Chicken farm).

[0034] Method: Open the window of 7-8 day old chicken embryos, add artesunate, positive control substance (hydrocortisone) and solvent control substance (blank microsphere injection) respectively, after incubation for 24 hours, use methanol, acetone 1 : 1 mixed solution to fix the allantoic membrane of chicken embryos, make a specimen, and count the number of blood vessels under a dissecting microscope.

[0035] result:

[0036] angiogenesis inhibition rate When the doses of artesunate were 15, 30, 6...

Embodiment 3

[0056] Example 3: Artesunate and dihydroartemisinin inhibit angiogenesis in vitro

[0057]Experimental materials: artesunate, dihydroartemisinin (the raw materials are provided by Guangxi Guilin No. 2 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, bathe in 37°C water for 15-20 minutes, wash the umbilical vein with PBS solution, centrifuge, discard the supernatant, suspend the cells with the culture medium, put them in a culture bottle and cultivate them, the next day The medium was changed once, and the culture medium was DMEM containing 15% calf serum and 10ng / ml VEGF. The 2nd to 3rd passage cells were collected for research after immunohistochemical identification with rabbit anti-human factor VIII antibody.

[0061] (2) HUVEC proliferation inhibition

[0062] HUVEC in 5×10 4 seed / ml density in 24-well culture plate, put in...

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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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