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Details

Autor(en) / Beteiligte
Titel
Pharmacokinetics and biotransformation of 3-cyan-2-morpholino-5-(pyrid-4-yl)pyridine (AWD 122-14) in the rat
Ist Teil von
  • Pharmazie, 1994-01, Vol.49 (1), p.41
Ort / Verlag
Germany
Erscheinungsjahr
1994
Quelle
Electronic Journals Library
Beschreibungen/Notizen
  • A sensitive isocratic HPLC method for the analysis of AWD 122-14 (1) in plasma and urine was developed. The extraction was processed on-line on a short column. The pharmacokinetics of 1 was studied in rats. The plasma concentration-time course was described by an 1-compartment-model. The pharmacokinetic parameters were estimated. The absorption and elimination of 1 are relatively fast. A single oral dose (D = 1 x 10(-5) mol/kg) was rapidly absorbed (absorption rate constant: kI = 6.85 h-1). The elimination rate constant is kE = 1.59 h-1. The absolute bioavailability of a single oral dose equals 11%. In rats 1 is mainly metabolized. Less than 5% of the dose is excreted in the urine as unchanged drug. The chemical structures of 10 of the 12 isolated metabolites were determined using high-resolution mass spectrometry.

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