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Neovascularization promoters

An angiogenesis and accelerator technology, applied in the field of enhancers of angiogenesis and accelerators of angiogenesis, can solve problems such as poor chemical stability

Inactive Publication Date: 2000-12-27
LTT BIO PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] known prostaglandin E 1 (PGE 1 ) exist in trace amounts in organisms and have a variety of physiological functions, but their chemical stability is poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 (CD inclusions)

[0043] Dissolve 17 mg of 9-butyryloxy-11α, 15S-dihydroxyprostate-8,13E-diene-1-carboxylate (hereinafter referred to as "AS") in 0.2 ml of ethanol, and add to the A solution prepared by dissolving 257 mg of β-cyclodextrin in 6 ml of water was added to the solution, heated and dissolved at 45°C, cooled to room temperature, and precipitated. After standing overnight at 0° C., it was filtered, washed with 50% ethanol aqueous solution, and dried under reduced pressure to obtain cyclodextrin (CD) inclusions.

Embodiment 2

[0044] Embodiment 2 (liposome)

[0045] After dissolving 60 mg of lecithin and 11 mg of oleamide in 5 ml of chloroform, a solution obtained by dissolving 30 μg of AS in 100 μl of ethanol was added, the solution was added to an eggplant flask, and the solvent was distilled off with a rotary evaporator. 1 ml of 0.1M isotonic phosphate buffer (pH5) was added thereto, and after shaking, ultrasonic treatment and centrifugation, the supernatant was filtered with a 0.2 μm membrane filter to obtain a liposome preparation.

Embodiment 3

[0046] Embodiment 3 (ethanol solution)

[0047] 500 µg of AS was dissolved in 1 ml of ethanol to obtain an ethanol solution preparation. When used, dilute with physiological saline or glucose solution, etc.

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Abstract

An angiogenesis promoter containing a compound of the following formula (I) <CHEM> wherein R<1> is acyl, R<2> is alkyl, R<3> and R<4> are the same or different and each is hydrogen atom or hydroxy protecting group and R<5> is alkyl, as an active ingredient. This compound itself not only has an angiogenesis promoting effect but also potentiates the angiogenic effect by a drug (e.g., b-FGF) having such effect. Therefore, it can express the angiogenesis promoting effect more effectively in the ischemic tissues and the site under different disease state, where b-FGF has locally increased.

Description

technical field [0001] The present invention relates to prostaglandin E 1 The invention of the new use of the precursor, specifically the accelerator of angiogenesis, and the enhancer of angiogenesis caused by growth factors. Background technique [0002] known prostaglandin E 1 (PGE 1 ) exist in trace amounts in living organisms and have various physiological functions, but their chemical stability is poor. Therefore, for preparation improvement and PGE 1 Modification research is ongoing, especially PGE 1 Precursors (prodrugs) have received attention. The object of the present invention is to provide a kind of PGE 1 Novel uses of precursors. Summary of the invention [0003] The inventors found that specific PGE 1 The precursor has an angiogenesis-promoting action and can also enhance the angiogenesis action of growth factors such as basic fibroblast growth factor (hereinafter referred to as "b-FGF"), thereby com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/557A61K31/5575A61K38/18A61K45/06
CPCA61K31/727A61K31/5575A61K38/1825A61K45/06A61K31/557A61K31/70A61K31/715A61P9/00A61K31/505A61K2300/00
Inventor 江木康阳久保佳史木户秀明西川昌邦林一孝井上理
Owner LTT BIO PHARMA
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