Bildung und Ausscheidung der Stoffwechselprodukte von p-Aminosalicyls�ure

Bioavailability of Aminosalicylic Acid and Its Various Salts in Humans III: Absorption from Tablets

“…Lauener et a / . (10) published similar results in addition to showing that conversion of drug to the glycine conjugate a t therapeutic doses is first order and independent of dose; therefore the ratio of unchanged drug to the glycine conjugate in urine is constant for an individual independent of dose. Thus, measurements of nonacetylated drug in plasma are essentially measurements of unchanged drug, and cumulative nonacetylated drug in urine will have a constant ratio of unchanged drug to the glycine conjugate.…”

“…The discrepancy between AUC and amounts absorbed can be explained by rate-limited metabolism of drug. Lauener et al (10) showed that while the biotransformation of aminosalicylic acid to the glycine conjugate is first order, the formation of acetylated compound is capacity-limited in humans. Rate-limited acetylation of similar compounds in humans and animals is also known (12, 13).…”

Effect of charcoal‐drug ratio on antidotal efficacy of oral activated charcoal in man.

“…The nonspecific colorimetric method used does not differentiate between unchanged PAS and the glycine conjugated, p-aminosalicyluric acid (PASU). However, on the basis of low concentrations of PASU found in plasma and the doseindependent formation of PASU, it is possible to analyze PAS in plasma by a nonspecific method which gives the same relative error of about 5% regardless of plasma concentration (Lauener et al, 1957;Wan et al, 1974).…”