Percutaneous absorption type cerebral protective agent

Abstract

A percutaneous absorption type cerebral protective agent containing as an active ingredient, 0.1 to 30 percent by mass of 3-methyl-1-phenyl-2-pyrazolin-5-one represented by the following formula: or a medically acceptable salt thereof in a base; a use of the compound as an active ingredient for the manufacture of a percutaneous absorption type pharmaceutical composition for protecting brain; and a method of protecting brain comprising administering to a patient the pharmaceutical composition as an active ingredient.

Description

technical field [0001] The present invention relates to a drug having a brain protective function against all brain dysfunctions including cerebral infarction and subarachnoid hemorrhage, especially a drug containing 3-methyl-1-phenyl-2-pyrazolin-5-one as Transdermal absorption type brain protectant of active ingredients. Background technique [0002] 3-Methyl-1-phenyl-2-pyrazolin-5-one is a brain protective agent with free radical scavenging effect. It is used in the form of injection (intravenous infusion: intravenous injection by drip). In recent years, many people are troubled by brain dysfunction due to aging, diversification of food, and increased stress in daily life. Therefore, rapid and correct measures for brain dysfunction have become one of the important medical issues. [0003] During ischemia such as cerebral infarction and after re-opening of blood flow after ischemia, free radicals such as excess hydroxyl radicals (OH) generated in the human body continuous...

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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