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Angiectasis medicine fasudil hydrochloride composition

A technology for fasudil hydrochloride and vasodilation, which is applied in the field of medicine and can solve the problems of low binding strength, easy hydration of the surface between particles, and large surface free energy per unit.

Inactive Publication Date: 2015-11-04
QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compounds with different crystal structures are in different energy states due to the difference in molecular arrangement order. Generally, amorphous drugs have greater potential energy, and the bonding strength between particles is smaller than that of crystal forms. The total unit surface free The energy is large, and the surface between the particles is easy to hydrate, resulting in a difference in solubility from that of crystalline drugs

Method used

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  • Angiectasis medicine fasudil hydrochloride composition
  • Angiectasis medicine fasudil hydrochloride composition
  • Angiectasis medicine fasudil hydrochloride composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of Fasudil Hydrochloride Crystals

[0024] (1) Grind the crude product of Fasudil hydrochloride, pass it through a 90-mesh sieve, add it to 45% aqueous solution of N-methylacetamide, and raise the temperature to 30°C while stirring; mix the crude product of Fasudil hydrochloride with 45% of The weight ratio of the N-methylacetamide aqueous solution is 1:10; the stirring speed is 180 rpm; adding activated carbon, stirring for 50 minutes and sterile filtering;

[0025] (2) Add diethyl ether while stirring, and lower the temperature to -2°C; the stirring speed is 240 rpm; the weight of diethyl ether is 7 times the weight of the mixed solution of fasudil hydrochloride and 45% N-methylacetamide aqueous solution , the adding rate is 95 ml / min; the cooling rate is 10°C / hour;

[0026] (3) After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and vacuum-dried for 6 hours to obtain the fasudil hyd...

Embodiment 2

[0028] Example 2: The preparation method of fasudil hydrochloride composition, the steps are as follows:

[0029] The composition comprises: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.001 part by weight of anhydrous sodium carbonate.

[0030] The preparation method is:

[0031] (1) Weigh fasudil hydrochloride crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0032] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0033] Example 3: The preparation method of fasudil hydrochloride composition, the steps are as follows:

[0034] The composition comprises: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.0015 part by weight of anhydrous sodium carbonate.

[0035] The preparation method is:

[0036] (1) Weigh fasudil hydrochloride crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0037] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention discloses an angiectasis medicine fasudil hydrochloride composition, and belongs to the technical field of medicine. Components of the composition include fasudil hydrochloride and anhydrous sodium carbonate. Fasudil hydrochloride is crystals. An X-ray powder diffraction pattern obtained by conducting measurement through Cu-K alpha rays is shown in figure 1. The new crystal form of the fasudil hydrochloride is different from a crystal form in the prior art, and through experimental verification, it is surprisingly found that the composition of the new crystal form is high in purity, mobility and stability, low in impurity content, not prone to moisture absorption and safe and reliable in clinical application and a powder injection manufactured through the composition of the new crystal form is high in stability, high in stability after being compatible with solvent, extremely low in insoluble particle content and quite suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a composition of fasudil hydrochloride, a vasodilator drug. Background technique [0002] Fasudil hydrochloride (fasudil hydrochloride, 1) is a new type of isoquinoline sulfonamide derivatives jointly developed by Asahi Kasei Co., Ltd. and Nagoya University. As a RHO kinase inhibitor and novel intracellular Ca 2 + Antagonist, the drug can dilate blood vessels by increasing the activity of myosin light chain phosphatase, reduce the tension of endothelial cells, improve the microcirculation of brain tissue, protect ischemic brain tissue, and at the same time antagonize inflammatory factors and protect nerves against apoptosis , promote nerve regeneration. In June 1995, it was listed by Asahi Kasei Corporation of Japan, and it was listed in China in 2004. It is mainly used to improve the symptoms of ischemic cerebrovascular diseases caused by cerebral vasospasm after subarachnoid h...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61P9/08A61P9/10C07D401/12
Inventor 刘学键
Owner QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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