Pharmacokinetic Studies of Propiverine hydrochloride (4) Feto-placental Transfer and Excretion into Milk in Rats

Abstract

The distribution of radioactivity of ¹⁴C-Propiverine hydrochloride (¹⁴C-P-4) in the fetuses and the excretion to the milk was studied following oral administration at a dose of 100mg/kg to pregnant or lactating rats.
1. After oral administration to pregnant rats, a low radioactivity was detected in the fetal tissues. The peak radioactivity in the fetus was 2 times lower when compared to the maternal plasma level and was decreased rapidly.
2. On day 18 of gestation, the ratio of the concentration in the fetal liver to that in its total body was relatively lower, and the distribution to the fetus was not pronounced.
3. Following oral administration of ¹⁴C-P-4 to lactating rats, the radioact ivity transfered into the milk was about 1.2-1.7 times higher than that in maternal plasma. Elimination half-life of the radioactivity from the milk was 13.29 hour. The elimination parameters from the milk were similar to those observed in the plasma.