Drug composition containing hydroxyfasudil compound

A technology of fasudil hydrochloride and a composition, applied in the field of medicine, can solve the problems of current intracranial hemorrhage (1.63%), gastrointestinal hemorrhage, pulmonary hemorrhage, epistaxis, subcutaneous hemorrhage and the like

Active Publication Date: 2014-06-18
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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] Example 1 Fasudil Hydrochloride Pharmaceutical Composition (Injection)

[0024] Formulation 1: 30 g of fasudil hydrochloride, 15 g of sodium dihydrogen phosphate, 405 g of dextran, 3 g of methionine, and 2000 ml of water for injection.

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

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

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

[0028] Formulation 5: 40 g of fasudil hydrochloride, 17 g of sodium dihydrogen phosphate, 407 g of dextran, 4 g of methionine, and 10000 ml of water for injection.

[0029] The preparation method is as follows:

[0030] Dissolve sodium dihydrogen phosphate, methionine, fasudil hydrochloride and dextran in sequence with water for injecti...

Embodiment 2

[0032] 1. Vascular irritation experiment

[0033] Thirty New Zealand white rabbits weighing 2.0-2.5 kg were randomly divided into 6 groups, 5 in each group, including blank control group and experimental group 1 to 5 (configuration 1 to 5 in Example 1). Slowly inject the rabbit ear veins with an injection volume of 10 ml / kg body weight / time (diluted with sodium chloride injection to 0.5 mg / ml fasudil hydrochloride according to the configuration of Examples 1 to 5). Among them, the blank control group used sodium chloride injection, and the experimental groups 1-5 used the configurations 1 to 5 of Example 1, respectively, which were dissolved in water for injection and injected.

[0034] Once a day for 7 consecutive days, the rabbit ears were cut short 24 hours after the last administration, and the specimens were fixed in 10% formaldehyde solution, and then sent to pathology for histological examination (5 in different parts of the rabbit ear veins) Take the material, that is, mak...

Embodiment 3

[0043] Example 3 Stability Test

[0044] The samples obtained from configurations 1 to 5 of Example 1 and the samples of control 1 (sodium dihydrogen phosphate and methionine were not added in Configuration 1 of Example 1) were tested for appearance, clarity, and correlation according to the requirements of the Chinese Pharmacopoeia (2010 Edition) Testing and long-term stability test of indicators such as substance and content.

[0045] Assay method: According to high performance liquid chromatography (Chinese Pharmacopoeia 2010 edition two appendix V D) determination. 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 the pH to 7.0 with phosphoric acid) as the mobile phase; the detection wavelength is 220 nm. The number of theoretical plates should not be less than 3000 according to Fasud...

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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 reducing vasospasm and a preparation method thereof. Background technique [0002] Subarachnoid hemorrhage (Subarachnoid hemorrhage, SAH) is an acute hemorrhagic cerebrovascular disease in which blood vessels at the base of the brain or on the surface of the brain and spinal cord are ruptured due to various causes. Blood flows directly into the subarachnoid space, also known as primary arachnoid. Bleeding from the lower cavity. Common causes are cerebral artery malformations, aneurysms, blood diseases, etc. Subarachnoid hemorrhage accounts for about 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. [0003] At present, calcium channel antagonists are commonly used to reduce vasospasm. ...

Claims

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Application Information

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