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Compound of stable Fasudil hydrochloride hydrate

A technology of fasudil hydrochloride and hydrate, applied in organic chemistry, drug combination, medical preparations containing active ingredients, etc.

Active Publication Date: 2011-10-26
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the mechanism of its cerebral cardiovascular activity and its in-depth mechanism still need to be further studied, fasudil hydrochloride has a promising prospect, and its clinical application may continue to expand

Method used

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  • Compound of stable Fasudil hydrochloride hydrate
  • Compound of stable Fasudil hydrochloride hydrate
  • Compound of stable Fasudil hydrochloride hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] In a 5000ml reaction bottle equipped with stirring, thermometer and condenser, add 300g of fasudil hydrochloride and 3000ml of n-butanol-acetonitrile-water (6:2:2) mixture, start stirring, and heat up to 65 ℃-70℃, after all the solution is clear, add 1.8 grams of potassium nitrate, and filter while it is hot. The filtrate was naturally cooled to room temperature, and then incubated for 12 hours to precipitate crystals, filtered, and dried indoors to obtain 273.1 grams of high-purity white crystals of the three hemihydrates of fasudil hydrochloride. Determined by Karl Fischer method, it contains 16.15% (weight percent) of water.

[0075] Elemental Analysis Results:

[0076] Measured value (calculated value), C:42.94(43.02),H:6.39(6.45),N:10.68(10.75),

[0077] S: 8.11 (8.20), Cl: 9.01 (9.07).

[0078] H NMR spectrum (D 2 O):

[0079] 9.782(s,1H),8.967-8.950(d,1H),8.716-8.666(m,3H), 8.121-8.081(t,1H),3.780-3.754(t,2H),3.599-3.568(t,2H ), 3.430-3.389(q,4H), 2.169-2.1...

Embodiment 2

[0085] Granules containing three hemihydrates of fasudil hydrochloride

[0086] Prescription: 45 grams of fasudil hydrochloride three hemihydrates, 690 grams of lactose, 88 grams of crospovidone, 90 grams of PEG-4000, 150 grams of hydroxypropyl methylcellulose, appropriate amount of distilled water, made into 1000 bags .

[0087] Process: PEG-4000 and the three hemihydrates of Fasudil hydrochloride are crushed together, passed through an 80-mesh sieve, mixed with other materials, made into soft materials with distilled water, granulated, dried at low temperature, and then packed into granules.

Embodiment 3

[0089] Capsules containing three hemihydrate cloths of Fasudil Hydrochloride

[0090] Prescription: 50 grams of fasudil hydrochloride three hemihydrates, 1.5 ml of propylene glycol, and 160 grams of starch, made into 1000 capsules.

[0091] Process: Moisten Fasudil hydrochloride three hemihydrates and starch with 15% propylene glycol aqueous solution, mix well, sieve and granulate, dry at 60°C, granulate, and fill capsules.

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Abstract

The invention which belongs to the technical field of medicines concretely relates to a Fasudil hydrochloride hydrate and a preparation method thereof. Fasudil hydrochloride prepared in the invention which has three and a half crystal waters has the advantages of high purity, good stability, unapparent weight gain of moisture absorption in a high humidity condition and good formability. The invention also relates to an application of the hydrate in preparing drugs for improving and preventing ischemic cerebrovascular diseases caused by a plurality of reasons, such as cerebral infarction, vertebrobasilar artery insufficiency, delayed cerebrovascular disease caused by subarachnoid hemorrhage, cerebral vasospasm caused by brain surgery and interventional therapies, and transient ischemic attack.

Description

[0001] technical field [0002] The invention belongs to the technical field of medicine, in particular to fasudil hydrochloride hydrate compound and its preparation method, and the invention also relates to the use of this hydrate to improve and prevent ischemic cerebrovascular diseases caused by various reasons, such as cerebral infarction , vertebrobasilar artery insufficiency, delayed cerebrovascular disease caused by subarachnoid hemorrhage, cerebral vasospasm caused by brain surgery and interventional therapy, transient ischemic attack and other cerebral ischemia-related diseases . Background technique [0003] Fasudil hydrochloride is currently the only clinically available Rho kinase inhibitor, that is, a new type of intracellular Ca antagonist. The main pharmacological effects are: [0004] It has an anti-vasospasm effect, which is significantly stronger than the vasodilator effects of verapamil and nimodipine. In vitro experiments have found that fasudil can effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/551A61P9/10A61P9/00
Inventor 严洁黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH
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