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THE PHARMACOKINETIC STUDIES OF THE [1-~(14)C]-HAXANOYL ALDEHYDE SODIUM BISULFITE IN THE MOUSE

Li Guanghong Gui Zhining (Laboratory of Nuclear Medicine)  
Haxanoyl aldehyde sodium bisulfite (HASB) was synthesized by the department of chemistry, Sun Yat-Sen University of Medical Sciences. It is an analogue of Houttuynium (Decanoyl Acetalde-hyde). The results of pharmacoklnetic research of C14 -HASB showed that the logarithm of drug concentration in blood versus time curve after intravenous administration was fitted to a two - compartment open model with first order elimination. In the distribution studies the results revealed that radioactivity distributed widely in the body. The concentrations in the liver and kidney were markedly higher than those in the blood and other tissues at 2 and 24 hour time points studied. Except for kidney and liver, radioactivity in tissues observed decreased to quite low levels 4 hours after administration ; the levels of radioactivity in the tumor were comparatively low. Thin layer chromatographic (TLC) analyses of serum urine and homogenates of liver and kidney indicated that most of radioactivity in serum was in the form unchanged C14 - HASB and that the drug could be metabolized rapidly after pass-Ing into some tissue cells in vivo. In excretion studies, the major routes of elimination were found to be via the expiration with 26. 76 % of the C14 as carbon dioxide recovered in 3 hours and via urine with 14. 60% of the C14mainly in the form of metabolites recovered in 24 hours.
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