Recirculatory Moment Analysis of Drugs in Man : Estimation of Extraction Ratio and Mean Cycle Time for Single Systemic and Pulmonary Circulation

概要

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The extraction ratio (E_c) and the mean cycle times (t^^-_c) for single systemic and pulmonary circulation were evaluated for 115 drugs in man. Heparin and fluorohydrocortisone, which have the smallest t^^-_c values (about 1min) show the small E_c values (close to zero). This result suggests that these drugs circulate through the body restricted within the blood vessels. The theoretical considerations indicate that the clearances defined by A_i (∞)/AUC differ from E_iQ_i, where A_i(∞) is the amount eliminated by organ i, AUC is the area under the plasma concentration curve, E_i is the extraction ratio and Q_i is plasma flow rate through organ i. The hepatic extraction ratios (E_h) of alprenolol, metoprolol and propranolol calculated from intravenous data alone are large (above 80%). It is also shown that the steady-state volume of distribution (V_<ss>) is rather independent of hepatic and renal extraction ratios, while the mean residence time (MRT) is considerably affected by change of these ratios.
社団法人日本薬学会の論文
1985-02-25