A Pharmacological Study on Sodium 3- (2, 4, 5-Triethoxybenzoyl) Propionate (AA-149-Na) in Healthy Volunteers

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概要

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• Ten healthy male adult volunteers received each of the six oral dose levels of sodium salt of AA-149, a new spasmolytic-cholenetic, to determine their tolerance, absorption and excretion.The dose levels ranged from 10 to 100mg as AA-149. The subjects were given the drug in two doses with an interval of 23 hours except for two. Subjective and objective symptoms were recorded, and blood analysis, blood chemistry tests, urinalysis, physiological function tests as well as determination of serum drug levels and urinary excretion were performed.<BR>The subjects receiving 20mg or more of AA-149 represented a suppressed bowel sound, which was the most characteristic finding in the present study, indicating the spasmolytic action of the drug. The intensity of the suppression, however, was not shown to be clearly related to the dose levels. As subjective symptoms, two subjects of lower dose levels (10 and 20mg) claimed some transient complaints of a slight degree (dull pain in the stomach, epigastric discomfort and feeling of dry mouth).<BR>No abnormal objective findings and laboratory test values were recognized, but serum bilirubin transiently and doseindependently elevated in all the cases within the physiologically normal range.<BR>Serum AA-149 levels elevated in proportion to the dose levels and reached maximum of about 1.5 hours following administration.<BR>The half life of the serum level was about one hour. About 50 to 60% of the given AA-149 was recovered as glucuronide in the 24-hour urines. Two urinary metabolites were found in about 10% in total.

• 一般社団法人 日本臨床薬理学会の論文

著者

• 関 隆

  杏林大学医学部薬理学教室

• 関 隆

  杏林大学医学部薬理

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