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Drug composition containing hydroxyfasudil compound

A technology of fasudil hydrochloride and its composition, applied in the field of medicine, can solve problems such as intracranial hemorrhage (1.63%), gastrointestinal bleeding, pulmonary hemorrhage, epistaxis, subcutaneous hemorrhage, etc.

Active Publication Date: 2013-04-17
罗诚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, existing studies have shown that Fasudil hydrochloride has certain side effects, which are specifically manifested in the occurrence of intracranial hemorrhage (1.63%), gastrointestinal bleeding, pulmonary hemorrhage, epistaxis, subcutaneous hemorrhage (0.29%) and other bleeding conditions. In addition, symptoms such as hypotension and anemia

Method used

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  • Drug composition containing hydroxyfasudil compound
  • Drug composition containing hydroxyfasudil compound
  • Drug composition containing hydroxyfasudil compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 Fasudil hydrochloride pharmaceutical composition (injection)

[0024] Formula 1: Fasudil hydrochloride 30g, sodium dihydrogen phosphate 15g, dextran 405g, methionine 3g, water for injection 2000ml.

[0025] Formula 2: Fasudil hydrochloride 10g, sodium dihydrogen phosphate 10g, dextran 403g, methionine 2g, water for injection 500ml.

[0026] Formula 3: Fasudil hydrochloride 50g, sodium dihydrogen phosphate 20g, dextran 4010g, methionine 5g, water for injection 50000ml.

[0027] Formula 4: Fasudil hydrochloride 20g, sodium dihydrogen phosphate 13g, dextran 403g, methionine 1g, water for injection 1000ml.

[0028] Formula 5: Fasudil hydrochloride 40g, sodium dihydrogen phosphate 17g, dextran 407g, methionine 4g, water for injection 10000ml.

[0029] The preparation method is as follows:

[0030] Stir and dissolve sodium dihydrogen phosphate, methionine, fasudil hydrochloride and dextran in sequence with water for injection, add 0.3% activated carbon by weig...

Embodiment 2

[0032] 1. Vascular stimulation experiment

[0033] Take 30 New Zealand white rabbits with a body weight of 2.0-2.5 kg, and divide them into 6 groups randomly, 5 rabbits in each group, including blank control group and experimental groups 1-5 (configuration 1-5 in embodiment 1). Slowly inject into rabbit ear vein, the injection volume is 10ml / kg body weight / time (dilute with sodium chloride injection according to the configuration of Examples 1-5 to 0.5mg / ml of Fasudil hydrochloride). Among them, the blank control group used sodium chloride injection, and the experimental groups 1-5 respectively used configurations 1-5 of Example 1, respectively added water for injection to dissolve and then injected.

[0034] Once a day, administered continuously for 7 days, the rabbit ears were cut short 24 hours after the last administration, placed in 10% formaldehyde solution to fix the specimen, and then sent to pathology for histological examination (in 5 different parts of the rabbit ea...

Embodiment 3

[0043] Embodiment 3 stability test

[0044] The sample obtained from configurations 1 to 5 of embodiment 1 and the sample of control 1 (sodium dihydrogen phosphate and methionine were not added in configuration 1 of embodiment 1) were subjected to appearance, clarity, and related parameters according to the requirements of "Chinese Pharmacopoeia" (2010 edition). Detection of substances and content and other indicators and long-term stability test.

[0045]Content determination method: determine according to high performance liquid chromatography (Chinese Pharmacopoeia 2010 edition two appendix V D). Chromatographic conditions and system suitability test: use octadecylsilane bonded silica gel as filler; use 0.08moL / L potassium dihydrogen phosphate solution-acetonitrile-10% tetrabutylammonium hydroxide-triethylamine (88:12:0.5 : 2.5) (adjust pH value 7.0 with phosphoric acid) is mobile phase; Detection wavelength is 220nm. The number of theoretical plates should not be less th...

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PUM

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Abstract

The invention provides a drug composition containing a hydroxyfasudil compound, which comprises hydroxyfasudil, sodium dihydrogen phosphate, dextran 40, methionine and water for injection. A preparation method of the drug composition comprises the following steps of stirring and dissolving sodium dihydrogen phosphate, methionine, hydroxyfasudil and dextran with the water for the injection, adding active carbon for decoloration, filtering removing carbon, and then conducting filter sterilization and autoclaved sterilization. The drug composition containing hydroxyfasudil is simple in prescription and reduces the possibility of hypotension, the stability is improved by reasonable configuration, and application and popularization of a hydroxyfasudil injection is facilitated.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition containing fasudil hydrochloride compound capable of alleviating vasospasm and a preparation method thereof. Background technique [0002] Subarachnoid hemorrhage (SAH) is an acute hemorrhagic cerebrovascular disease in which blood vessels rupture at the base of the brain or on the surface of the brain and spinal cord due to various etiologies. The blood directly flows into the subarachnoid space, also known as primary arachnoid. Inferior hemorrhage. Common causes are cerebral arterial malformations, aneurysms, blood diseases, etc. Subarachnoid hemorrhage accounts for approximately 10% of acute strokes and 20% of hemorrhagic strokes. Delayed cerebrovascular recovery is the most serious complication after SAH, often leading to death or disability of the patient. [0003] Calcium channel antagonists are commonly used to reduce vasospasm. Commonly u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/551A61K47/36A61K47/18A61K47/02A61P25/00A61P25/28
Inventor 罗诚
Owner 罗诚
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