各種新サルフア剤の血中濃度及び腎排泄態度に関する研究
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Sulfisoxasol (SI), as well as sulfisomezole (MS 53), sulfamethoxypyridazine (SMP) and sulfadimethoxine (SDM), the so-called long acting sulfa drugs, was given to persons, both normal and with kidney disturbances; and their plasma concentrations, amounts excreted in the urine, and renal clearance values. were determined. The results are summarized as follows: When normal persons were injected intravenously with SI, its plasma concentrations became more or less stable in 20 minutes. Thereafter, the larger the amount given, the quicker was the fall in plasma concentrations. When the drugs under test were given orally to normal persons, the rise in plasma concentrations of MS 53 and SMP was considerably quick, reaching the highest levels in 3 to 4 hours. On the other hand, the plasma concentration of SDM rose very slowly, reaching the highest levels in about 10 hours. Especially small was the acetylated rate of SDM, which was only 7.7% in 24 hours. Of all the drugs under test, SMP and SDM excreted in 24 hour urine of normal persons were particularly small in percentage. Only 27.0 and 19.5 %, respectively, of the amounts given were excreted. When plasma concentrations of the unconjugated portion of SI were more than 10 mg/dl in normal persons, its renal clearance values tended to increase gradually, while they remained within a certain range when plasma concentrations were less than 10 mg/dl The clearance value in the latter cases was 19.21 cc/min on the average. The renal clearance values of unconjugated portions of MS 53, SMP and SDM in normal persons were 12.56 cc/min, 1.47 cc/min and 1.81 cc/min, respectively, on the average, irrespective of urine volume. The renal clearance values of the acetylated portions of MS 53, SMP and SDM were greater than those of their unconjugated portions. In patients with kidney diseases or diabetes mellitus, the renal clearance value of the unconjugated portion of SI was correlated to a high degree with GFR (γ=0.8250), sharply reflecting glomerular function.
- 千葉大学の論文
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- 各種新サルフア剤の血中濃度及び腎排泄態度に関する研究