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Medicinal fasudil hydrochloride composition for treating cerebral ischemia

A technology of fasudil hydrochloride and a composition, applied in the field of medicine, can solve the problems of easy hydration of the surface between particles, large free energy per unit surface, low bonding strength and the like

Inactive Publication Date: 2015-12-16
QINGDAO HUAZHICAO PHARMA 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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  • Medicinal fasudil hydrochloride composition for treating cerebral ischemia
  • Medicinal fasudil hydrochloride composition for treating cerebral ischemia
  • Medicinal fasudil hydrochloride composition for treating cerebral ischemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Fasudil Hydrochloride Crystals

[0025] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 1:4;

[0026] 2) Take fasudil hydrochloride raw material, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of fasudil hydrochloride is 10ml:1g, stir to dissolve all Add 0.1% g / ml activated carbon to the resulting solution for decolorization and filtration to obtain a clear solution;

[0027] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 3.5:2;

[0028] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.8KW, where the amount of mixed solution B added is 5 times the volume of mixed solution A, and turn off the ultrasonic field after adding , cooled to 0° C., allowed to stand for 3 hours, crystals were precipitated, and dried to obtain t...

Embodiment 2

[0030] Example 2: Preparation of fasudil hydrochloride composition

[0031] The composition is: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.003 part by weight of sodium dihydrogen phosphate.

[0032] The preparation method is:

[0033] (1) Weigh fasudil hydrochloride crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0034] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0035] Example 3: Preparation of fasudil hydrochloride composition

[0036] The composition is: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.004 part by weight of sodium dihydrogen phosphate.

[0037] The preparation method is:

[0038] (1) Weigh fasudil hydrochloride crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0039] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention discloses a medicinal fasudil hydrochloride composition for treating cerebral ischemia, and belongs to the technical field of medicines. The composition is prepared from fasudil hydrochloride and sodium dihydrogen phosphate, wherein the fasudil hydrochloride is crystal, and the X-ray powder diffraction pattern obtained by using Cu-K alpha ray measurement is as shown in a diagraph 1. Different from the crystal form structure in the prior art, experimental verification surprisingly discovers that the novel crystal form of fasudil hydrochloride has the advantages of high purity, good fluidity, good stability, low impurity content, difficult moisture absorption and safe and reliable clinical application. A powder injection prepared by utilizing the novel crystal form compound has good stability after being mixed with a solvent, is low in content of insoluble particles, and is particularly suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a drug composition of fasudil hydrochloride for treating cerebral ischemia. Background technique [0002] Fasudil hydrochloride (fasudilhydrochloride, 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551A61P9/10A61P25/00C07D401/12
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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