[Analog computer analysis of radioactivity kinetics in man following oral administration of tilidine HCl-14C].

1975 
: Models for studying the absorption and elimination kinetics of 14-C labelled DL-Ethyl-trans-2-dimethylamino-1-phenyl-cyclohex-3-ene-trans-1-carboxylate-hydrochloride (Tilidine - HCl, Valoron) are developed, based on the concentration vs. time of radioactivity in the plasma following a single oral administration in man. For this purpose, the average concentration values in the plasma of 3 healthy adults, as given by Vollmer and Poisson [12] were employed. 1. Two three-compartment-models were developed which simulate with sufficient accuracy the 14-C-Valoron concentration curve in the plasma. 2. Computer analysis enables one to determine the distribution of 14-C-Valoron among the intra- and extravasal compartments and the half life for absorption t1/2 equals 0.57 h, for transport from plasma into the extravasal compartment t1/2 equals 3.31 h, for resorption t1/2 equals 4.11 h, for elimination with feces t1/2 equals 29.5 h and for elimination in urine t1/2 equals 8.75 h. 3. The use of two different models allows one to draw conclusions concerning the participation of parenchymatous organs in storage and elimination. 4. The probable radioactivity curve is calculated for repeated oral application of 14-C-Valoron in 8 hours intervals.
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