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Fasudil-containing preparation and method of improving stability thereof

A technology of fasudil and photostability, applied in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc., can solve problems such as difficulty in confirming the state of the internal liquid medicine, and achieve excellent visibility, Effect of cost control and stability improvement

Inactive Publication Date: 2011-01-19
ASAHI KASEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] According to the conventional technology, there are the following problems: if a colored container is used, it is difficult to confirm the state of the internal chemical solution, and it is still not fully satisfactory from the viewpoint of detection of insoluble foreign matter or visual inspection.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0058] [reference manufacture example]

[0059] Add homopiperazine (3.413g) to tetrahydrofuran (57ml), stir and dissolve, then cool to -5°C, and add 5-isoquinolinesulfonyl chloride hydrochloride while keeping the internal temperature at or below 10°C Salt (3.00g), stirred at 5°C for 4 hours. Next, the reaction mixture was returned to room temperature, the insoluble matter was filtered off, and the filtrate was concentrated under reduced pressure, then ethyl acetate (57 ml), water (17 ml), and 3 standard hydrochloric acid (6.4 ml) were added for separation to obtain an aqueous layer. After washing the obtained aqueous layer with ethyl acetate (7 ml), water (6 ml), ethyl acetate (57 ml), and 6 standard aqueous sodium hydroxide solution (3 ml) were added to the aqueous layer, and the layers were separated to obtain an organic layer. After concentrating the organic layer under reduced pressure, fasudil (1.36 g) was obtained by drying under reduced pressure. The yield in this cas...

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PUM

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Abstract

Fasudil-containing preparations that despite the use of a container excelling in the visibility of contents without particularly blocking of light, exhibit high stability against light; and a method of improving the stability of the preparations against light, or storing the same. By regulating the pH value of aqueous solution of fasudil charged in a colorless transparent container to <= 5.5, there can be provided fasudil-containing preparations excelling in stability against light; and can be provided a method of improving the stability of the aqueous solution of fasudil against light, and storing the same.

Description

technical field [0001] The present invention relates to a preparation containing fasudil hydrochloride with good light stability, a method for improving the light stability of the preparation and a preservation method for fasudil hydrochloride aqueous solution in a transparent container. Background technique [0002] 1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride (hereinafter referred to as "fasudil hydrochloride") has excellent vasodilator effect, and its trade name is Eril Inj. (registered trademark; Asahi Seika Pharmaceutical Co., Ltd. Co., Ltd.), which is also clinically used as an injection for the purpose of improving cerebral vasospasm after subarachnoid hemorrhage surgery and the accompanying cerebral ischemic symptoms (Patent Document 1). [0003] In addition, the crystals of fasudil hydrochloride are now known, and there are crystals without crystal water (hereinafter referred to as "fasudil hydrochloride anhydrate") and crystals with crystal water (hereina...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/551A61K9/08A61P9/10A61P25/00C07D403/12A61K9/00A61K47/02C07D401/12
CPCA61K47/02C07D401/12A61K31/551A61K9/0019A61P25/00A61P9/10A61K9/08
Inventor 前岛卓治大岛美纪
Owner ASAHI KASEI PHARMA