健康成人におけるpivmecillinamの経口投与時の5%glucose負荷による水分利尿の影響

抄録

The influence of water diuresis on the absorption and excretion of mecillinam after the oral administration of pivmecillinam at the dose of 146. 2 mg (equimolar to 100 mg mecillinam) was studied in six healthy male adults on three different experimental states by the cross over method ; the state 1, hydropenic one by overnight fasting, the state 2, hydropenic one shifted to hydrated one by the intravenous infusion of 1, 000 ml of 5% glucose solution in 60 minutes, 3 hours after the administration of the drug, and the state 3, hydrated one by the same method as the state 2 followed immediately after dosing.
The concentrations of mecillinam in the serum or urine and the amounts excreted in the urine after the administration of pivmecillinam were compared between the three states, and the following results were obtained.
1) The differences between each serum concentration of the three states were statistically not significant.
2) The averages of the urinary concentration within 3 hours after dosing were 319. 5, 173. 5 and 38. 5 jug/ml in the state 1, 2 and 3 respectively, and the differences between the state 3 and 1 (P<0. 01), and 2 (P<0. 05), were statistically significant. But in the state 3, the average of the urinary level during the period of 3-6 hours after dosing was 103. 5 μg/ml and it was significantly higher than that during the period of 3-6 hours after dosing.
3) The differences of the cumulative amount of mecillinam excreted in the urine within 3 hours after dosing were statistically not significant between the three states, but the amount in the state 3 during the period of 3-6 hours after dosing was statistically higher than those in the other two states (P< 0. 01). The averages of the urinary recovery rate within 6 hours after dosing were 28. 1, 27. 5 and 43. 1 % in the state 1, 2 and 3 respectively, and the differences between the state 3 and 1, and the state 3 and 2, were statistically significant (P<0. 01).