Percutaneous absorption type cerebral protective agent

Abstract

The present invention provides a transdermal absorption type brain protectant, which is characterized in that the matrix contains 0.1 to 30 mass % of the following formula: 3-methyl-1-phenyl-2- Pyrazolin-5-one or a pharmaceutically acceptable salt thereof also provides a use of the compound as an active ingredient of a transdermal pharmaceutical composition for protecting the brain, and a method for administering the pharmaceutical composition to a patient Drugs as active ingredients of the brain protection method.

Description

Technical field [0001] The present invention relates to a medicament having a brain protective function against all brain dysfunctions including cerebral infarction or subarachnoid hemorrhage, in particular to a drug containing 3-methyl-1-phenyl-2-pyrazoline-5-one as A transdermal absorption type brain protective agent with active ingredients. Background technique [0002] 3-Methyl-1-phenyl-2-pyrazoline-5-one is a brain protective agent with a free radical elimination effect, as a neurological syndrome, disturbance of activities of daily living, and dysfunction of the human body accompanied by acute cerebral infarction The improvement medicine of the medicine is used in the form of injection (intravenous drip: intravenous injection by drip). In recent years, brain dysfunction caused by aging, diversification of foods, and increased stress in daily life have also plagued many people. Therefore, rapid and correct countermeasures for brain dysfunction have become one of the importan...

AI Technical Summary

Problems solved by technology

[0007] Furthermore, since 3-methyl-1-phenyl-2-pyrazolin-5-one is rapidly metabolized in the liver through glucuronic acid conjugation or sulfuric acid conjugation, when it is administered orally, due to the Very low effectiveness due to first-pass effect

In addition, 3-methyl-1-phenyl-2-pyrazolin-5-one is disclosed as an inhibitor of lipid peroxidation (for example, refer to Japanese Patent Laid-Open No. 62-108814), an antiulcer agent (for example, See Japanese Patent Laid-Open No. 3-215425), blood sugar elevation inhibitors (for example, see Japanese Patent Laid-Open No. 3-215426), pharmaceutical preparations for ophthalmic diseases (for example, see Japanese Patent Laid-Open No. 7-25765), treatment and prevention of acute renal insufficiency (For example, refer to Japanese Patent Application Laid-Open No. 9-52831), etc., but the administration methods of these drugs are all oral administration, intravenous administration or rectal administration, therefore, there are the above-mentioned shortcomings in clinical practice.

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