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Medicinal fasudil hydrochloride composition for treating ischemic cerebrovascular diseases

A technology for fasudil hydrochloride and cerebrovascular diseases, which is applied in the field of medicine and can solve problems such as differences in solubility of crystalline drugs, low binding strength, and large free energy per unit surface

Inactive Publication Date: 2015-12-09
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 ischemic cerebrovascular diseases
  • Medicinal fasudil hydrochloride composition for treating ischemic cerebrovascular diseases
  • Medicinal fasudil hydrochloride composition for treating ischemic cerebrovascular diseases

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Example 1: Preparation of Fasudil Hydrochloride Crystals

[0021] Dissolve fasudil hydrochloride in a mixed solvent of methanol and acetonitrile whose volume is 10 times the weight of fasudil hydrochloride at 35°C. The volume ratio of methanol and acetonitrile is 3:1. After the dissolution is completed, add a volume of hydrochloric acid Diethyl ether solvent 6 times the weight of Fasudil, the temperature is lowered to room temperature within 1-2 hours, kept at room temperature for 3 hours, then further cooled to 0-5 °C, and then placed at 0-5 °C for 2 After -3 hours, crystals were precipitated to obtain fasudil hydrochloride crystals.

[0022] The prepared Fasudil hydrochloride crystals use Cu-Kα rays to measure the X-ray powder diffraction pattern obtained as figure 1 Shown, its purity as determined by high performance liquid chromatography is 99.9%.

Embodiment 2

[0023] Example 2: Preparation of fasudil hydrochloride composition

[0024] The composition is: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.001 part by weight of arginine.

[0025] The preparation method is:

[0026] (1) Weigh fasudil hydrochloride crystals and arginine in proportion and mix them thoroughly;

[0027] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0028] Example 3: Preparation of fasudil hydrochloride composition

[0029] The composition is: 1 part by weight of fasudil hydrochloride crystal prepared by the present invention, and 0.002 part by weight of arginine.

[0030] The preparation method is:

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

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

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Abstract

The invention discloses a medicinal fasudil hydrochloride composition for treating ischemic cerebrovascular diseases, which belongs to the technical field of medicines. The composition is prepared from fasudil hydrochloride and arginine, wherein the fasudil hydrochloride is a crystal, and an X-ray powder diffraction pattern, which is obtained by measurement of Cu-Kalpha rays, of the crystal, is as shown in figure 1. The new crystalline form of the fasudil hydrochloride provided by the invention is different from a crystalline structure in the prior art; by experimental verification, the medicinal fasudil hydrochloride composition is pleasantly found to have the advantages of high purity, good flowability, good stability, low content of impurities, low possibility of moisture absorption, and safety and reliability in clinical application; a power injection prepared from the new crystalline compound is good in stability, is good in stability after being matched with a solvent, is extremely low in content of insoluble particles, and is very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a drug fasudil hydrochloride composition for treating ischemic cerebrovascular diseases. 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 vas...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/551A61K47/18C07D401/12A61P9/10A61P25/00
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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