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Nasal spray or aerosol containing Fasudil

A technology of fasudil and fasudil hydrochloride, which is applied in the field of nasal spray or aerosol, can solve the problems of drug quality, danger brought by patients, and self-administration by patients, so as not to cause allergic reactions , Improve absorption rate, strong and long-lasting effect

Active Publication Date: 2011-08-03
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 use. However, the safety and applicability of the injection are poor because the injection directly enters the human body quickly, and there is no human body. The protection of the normal physiological barrier, so if the dose is improper or the injection is too fast, or there is a problem with the quality of the drug, it may bring danger to the patient, and even cause irreversible consequences
In addition, the pain during injection, the inability to administer drugs by the patient, induration at the injection site, and vascular inflammation caused by intravenous injection are all problems in clinical application.

Method used

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  • Nasal spray or aerosol containing Fasudil
  • Nasal spray or aerosol containing Fasudil
  • Nasal spray or aerosol containing Fasudil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083]

[0084]

[0085] Pass the original and auxiliary materials through a 100-mesh sieve, successively weigh the prescribed amount of sodium dihydrogen phosphate, disodium hydrogen phosphate, bromogeramine, EDTA-2Na, vitamin E, add 80% of the prescribed amount of water and stir to dissolve into a clear solution, add After fasudil hydrochloride dissolves while stirring, adjust the pH to 6.5-7.0, add water to make up to 1000ml, filter the medicinal solution with a 0.22μ microporous membrane, and pack it into 10ml suitable special nasal spray bottles.

Embodiment 2

[0087]

[0088] Pass the original and auxiliary materials through a 100-mesh sieve, successively weigh the prescribed amount of sodium dihydrogen phosphate, disodium hydrogen phosphate, bromogeramine, EDTA-2Na, and vitamin E, add 80% of the prescribed amount of normal saline and stir to dissolve into a clear solution, After adding Fasudil hydrochloride and stirring to dissolve, adjust the pH to 5.5-6.5, add normal saline to make up to 1000ml, filter the medicinal solution with a 0.22μ microporous membrane, and distribute it in 10ml appropriate special nasal spray bottles.

Embodiment 3

[0090]

[0091]

[0092] Pass the original and auxiliary materials through a 100-mesh sieve, successively weigh the prescribed amount of sodium dihydrogen phosphate, disodium hydrogen phosphate, bromogeramine, EDTA-2Na, and vitamin E, add 90% of the prescribed amount of normal saline and stir to dissolve into a clear solution, After adding Fasudil hydrochloride and stirring to dissolve, adjust the pH to 5.5-6.5, add normal saline to make up to 1000ml, filter the medicinal solution with a 0.22μ microporous membrane, and distribute it in 10ml appropriate special nasal spray bottles.

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Abstract

The invention relates to a nasal spray or aerosol containing Fasudil. The active component in the preparation can be absorbed rapidly through the nasal mucosa so that the response is rapid. The nasal spray or aerosol has the advantages of high bioavailability and good compliance, and is convenient in use and carrying. The preparation provided by the invention contains Fasudil hydrochloride and pharmaceutically acceptable excipients.

Description

technical field [0001] The invention relates to a nasal spray or aerosol containing fasudil. The active ingredient in the preparation can be quickly absorbed through the nasal 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, my...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/551A61P9/10
Inventor 姚小青孙长海刘培勋
Owner TIANJIN CHASE SUN PHARM CO LTD
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