Fasudil-containing oral spray or aerosol

A technology of fasudil and fasudil hydrochloride, which is applied in the field of oral spray or aerosol, can solve the problems of drug quality, self-administration by patients, and danger brought by patients, so as not to cause allergic reactions , prolong the residence time and improve the absorption rate

Active Publication Date: 2011-08-10
TIANJIN CHASE SUN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The injection of fasudil hydrochloride currently on the market has the advantages of fast onset of action, high bioavailability, and significant therapeutic effect, but the safety and applicability of the injection are poor because the injection directly enters the human body quickly, and no human body is normal. The protection of the physiological barrier, so if the dose is im

Method used

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  • Fasudil-containing oral spray or aerosol
  • Fasudil-containing oral spray or aerosol
  • Fasudil-containing oral spray or aerosol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089]

[0090] Preparation:

[0091] Pass the original and auxiliary materials through a 100-mesh sieve, add 80% of the prescribed amount of water for injection and stir to dissolve into a clear solution, add fasudil hydrochloride and stir to dissolve, adjust the pH to 6.5-7.0, add water to make up to 1000ml, and The solution is filtered with a 0.22μ microporous membrane, and distributed into suitable special oral spray bottles.

Embodiment 2

[0093]

[0094]

[0095] Pass the raw materials and auxiliary materials through 100-mesh sieve respectively, weigh the prescribed amount of sodium dihydrogen phosphate, disodium hydrogen phosphate, bromogeramine, EDTA-2Na, vitamin E, and sodium carboxymethyl cellulose in sequence, and add 80% of the prescribed amount of normal saline Stir to dissolve into a clear solution, add fasudil hydrochloride to dissolve after stirring, adjust the pH to 6.5-7.0, add normal saline to make it 1000ml, filter the liquid medicine with a 0.22μ microporous membrane, and pack it in a suitable special-purpose Oral spray bottle.

Embodiment 3

[0097]

[0098] Pass the raw materials and auxiliary materials through 100-mesh sieve respectively, weigh the prescribed amount of sodium dihydrogen phosphate, disodium hydrogen phosphate, bromogeramine, EDTA-2Na, vitamin E, and sodium carboxymethyl cellulose in sequence, and add 80% of the prescribed amount of normal saline Stir to dissolve into a clear solution, add fasudil hydrochloride to dissolve after stirring, adjust the pH to 6.5-7.0, add normal saline to make it 1000ml, filter the liquid medicine with a 0.22μ microporous membrane, and pack it in a suitable special-purpose Oral spray bottle.

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PUM

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Abstract

The invention relates to fasudil-containing oral spray or aerosol in which active constituents can be quickly absorbed through the mouth mucosa to work quickly; and the spray or the aerosol has the advantages that the spray or the aerosol is high in bioavailability, excellent in compliance, portable, convenient to use and the like. The spray or the aerosol comprises the following constituents: fasudil hydrochloride, and pharmaceutically acceptable accessories selected from buffering agent, osmotic pressure regulator, flavoring agent, preservative, absorbefacient, antioxidant, bioadhesive agent, pH modifier, dissolvent and the like.

Description

technical field [0001] The invention relates to an oral spray or aerosol containing fasudil. The active ingredient in the preparation can be quickly absorbed through the oral mucosa and take effect quickly, has high bioavailability, good compliance, and is convenient to carry and use Etc. Background technique [0002] Fasudil [hexahydro-1-(5-sulfonylisoquinoline)-1(H)-1,4-diazepine, Fasudil] is jointly developed by Japan Asahi Kasei Co., Ltd. and Nagoya University Pharmacology Laboratory A novel isoquinoline sulfonamide derivative. As a new type of high-efficiency vasodilator, Fasudil can effectively relieve cerebral vasospasm and improve the prognosis of patients with subarachnoid hemorrhage (SAH). cerebral vasospasm. Launched in China in 2002, it is used for the improvement of symptoms of ischemic cerebrovascular diseases caused by cerebral vasospasm after subarachnoid hemorrhage. [0003] Fasudil acts by inhibiting a variety of protein kinases, such as Rho kinase, myo...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/551A61K47/44A61P9/10
Inventor 姚小青孙长海刘培勋
Owner TIANJIN CHASE SUN PHARM CO LTD
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