TY - JOUR
T1 - Pharmacokinetics of VP16-213 given by different administration methods
AU - D'Incalci, M.
AU - Farina, P.
AU - Sessa, C.
AU - Mangioni, C.
AU - Conter, V.
AU - Masera, G.
AU - Rocchetti, M.
AU - Pisoni, M. Brambilla
AU - Piazza, E.
AU - Beer, M.
AU - Cavalli, F.
PY - 1982
Y1 - 1982
N2 - Plasma pharmacokinetics of VP16-213 were investigated after a 30-60 min infusion in 14 adult patients and six children. In adults the elimination half-life (T1/2 β), plasma clearance (Clp) and volume of distribution (Vd) were respectively 7.05±0.67 h, 26.8±2.4 ml/min/m2, and 15.7±1.8 l/m2; in children 3.37±0.5 h, 39.34±6.6 ml/min/m2, and 9.97±3.7 l/m2. After repeated daily doses no accumulation of VP16-213 was found in plasma. The unchanged drug found in the 24 h urine after administration amounted to 20-30% of the dose. In eight choriocarcinoma patients plasma levels of VP16-213 were measured after oral capsules and drinkable ampoules. The bioavailability compared to the i.v. route was variable, mean values being 57% for capsules and 91% for ampoules. In one further patient, with abnormal d-Xylose absorption results, VP16-213 was not detectable in plasma after the oral ampoule dose. Steady state levels investigated in three patients after 72 h continuous VP16-213 infusion (100 mg/m2/24 h) were around 2-5 μg/ml. Levels of VP16-213 were undetectable in CSF after i.v. or oral administration.
AB - Plasma pharmacokinetics of VP16-213 were investigated after a 30-60 min infusion in 14 adult patients and six children. In adults the elimination half-life (T1/2 β), plasma clearance (Clp) and volume of distribution (Vd) were respectively 7.05±0.67 h, 26.8±2.4 ml/min/m2, and 15.7±1.8 l/m2; in children 3.37±0.5 h, 39.34±6.6 ml/min/m2, and 9.97±3.7 l/m2. After repeated daily doses no accumulation of VP16-213 was found in plasma. The unchanged drug found in the 24 h urine after administration amounted to 20-30% of the dose. In eight choriocarcinoma patients plasma levels of VP16-213 were measured after oral capsules and drinkable ampoules. The bioavailability compared to the i.v. route was variable, mean values being 57% for capsules and 91% for ampoules. In one further patient, with abnormal d-Xylose absorption results, VP16-213 was not detectable in plasma after the oral ampoule dose. Steady state levels investigated in three patients after 72 h continuous VP16-213 infusion (100 mg/m2/24 h) were around 2-5 μg/ml. Levels of VP16-213 were undetectable in CSF after i.v. or oral administration.
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U2 - 10.1007/BF00254536
DO - 10.1007/BF00254536
M3 - Article
C2 - 7083454
AN - SCOPUS:0020077408
VL - 7
SP - 141
EP - 145
JO - Cancer Chemotherapy and Pharmacology
JF - Cancer Chemotherapy and Pharmacology
SN - 0344-5704
IS - 2-3
ER -