Pharmacokinetics of Salazosulfapyridine (Sulfasalazine, SASP). (I). Plasma kinetics and plasma metabolites in the rat after a single intravenous or oral administration.
スポンサーリンク
概要
- 論文の詳細を見る
Salazosulfapyridine (Sulfasalazine, SASP, 2-hydroxy-5-[[4-[(2-pyridinylamino) sulfonyl] phenyl] azo] benzoic acid) labelled with <SUP>14</SUP>C in the carboxyl group and with <SUP>3</SUP>H in chemically as well as metabolically stable positions in the benzenesulfonyl ring was administered either intravenously or orally to male and female rats in order to study the plasma pharmacokinetics of SASP and the plasma profiles of the metabolites. After intravenous administration SASP was eliminated rapidly from plasma with a half-life (t<SUB>1/2</SUB>) of 8min. The volume of distribution (Vd<SUB>ss</SUB>) of SASP was 0.2<I>l</I>/kg and total clearance (CLtot) was 18m<I>l</I>/min × kg. After oral administration, SASP was present in plasma mainly during the first 4 hours. The time for maximal concentration (T<SUB>max</SUB>) varied for SASP between 1 ?? 3 hours, for <SUP>14</SUP>C, corresponding to 5ASA metabolites, between 3 ?? 10 hours and for <SUP>3</SUP>H, corresponding to sulfapyridine metabolites, between4 ?? 12 hours. The inter-individual variation was considerable. The bioavai lability of SASP was 9% and independent of the dose. The maximal concentration(C<SUB>max</SUB>) and area under the curve (AUC) increased proportionally with the dose. The absorption of SASP was not influenced by fasting overnight.<BR>There was a clear sex difference in the metabolism of SASP. The plasma concentration of sulfapyridine metabolites in female rats was twice that in male rats. No hydroxylated metabolites were found in female rat plasma, whereas in the male rats, the hydroxylated sulfapyridine metabolites were the major metabolites.
- 日本薬物動態学会の論文
日本薬物動態学会 | 論文
- COMPETITIVE DISPLACEMENT OF SERUM PROTEIN BINDING TO REGULATE PHARMACOKINETICS OF A CEREBRAL BLOOD FLOW RADIOPHARMACEUTICAL
- Studies on the Metabolic Fate of Felodipine. (IV). Identification of New Metabolites of Felodipine in Rat.
- Metabolic Fate of Pergolide Mesylate. (2): Absorption, Distribution, Excretion of 14C-Pergolide Mesylate in Rats after Repeated Administration.
- Studies on the Metabolic Fate of 3H-TJN-101. (III): Absorption, Distribution and Excretion after Multiple Oral Administration to Rats.
- Studies on the Pharmacokinetics of Perindopril Erbumine in Rats. (1): Plasma Level Profile, Distribution, Metabolism and Excretion after Single Oral Administration.