Studies on the Metabolic Fate and the Pharmacokinetics of 5-n-Buty1-1-cyclohexy1-2, 4, 6-trioxoperhydropyrimidine (BCP) in Man. IV. Pharmacokinetics of BCP in Man following Oral Administration

• Published in: Chemical & pharmaceutical bulletin Vol. 19; no. 5; pp. 869 - 880
• Main Authors: YASHIKI, TAKATSUKA, MATSUZAWA, TAI, YAMADA, MASAHIRO, KONDO, TAKAO, UDA, YOSHIAKI, HOKAZONO, ZENZO, MIMA, HIROYUKI
• Format: Journal Article
• Language: English
• Published: The Pharmaceutical Society of Japan 1971
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.19.869

In order to elucidate the behavior of BCP in man, plasma concentration of BCP and urinary excretion of total BCP and its metabolites were determined periodically after its oral administration. By analysis of the data with an analogue computer, the characteristic behavior of BCP was found that the maximum tissue amount of BCP increased almost linearly with dose both in the single and successive administration, whereas the maximum plasma concentration did not increase linearly with dose and approached an asymptotic value. This behavior of BCP was considered due to its high degree of binding property to plasma albumin which was saturated at the plasma concentration of 13 mg/100 ml, kinetical conditions and to the dosage range in which the maximum plasma water concentration of BCP increased almost linearly with the dose given. It was also suggested that by increasing the dose to a reasonable extent, increased clinical effect might be expected, though the maximum plasma concentration approached a limiting value.