The pharmacokinetics of tiopronin and its principal metabolite (2-mercaptopropionic acid) after oral administration to healthy volunteers

We have studied the pharmacokinetics of tiopronin and its principal metabolite, 2-mercaptopropionic acid (2-MPA) in healthy volunteers after the oral administration of 500 mg (2 Acadione tablets), followed by simultaneous assay of the two compounds in plasma over a period of 48 h using a new method...

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Bibliographic Details
Published in:European journal of clinical pharmacology 1992-07, Vol.43 (1), p.93-95
Main Authors: Hercelin, B, Leroy, P, Nicolas, A, Gavriloff, C, Chassard, D, Thébault, J J, Reveillaud, M T, Salles, M F, Netter, P
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Chromatography, High Pressure Liquid
Humans
Male
Sulfhydryl Compounds - blood
Time Factors
Tiopronin - administration & dosage
Tiopronin - blood
Tiopronin - pharmacokinetics
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Summary:We have studied the pharmacokinetics of tiopronin and its principal metabolite, 2-mercaptopropionic acid (2-MPA) in healthy volunteers after the oral administration of 500 mg (2 Acadione tablets), followed by simultaneous assay of the two compounds in plasma over a period of 48 h using a new method (emission of fluorescence after HPLC and post-column derivatization by pyrene-maleimide). The absorption of tiopronin was slow (tmax between 4 and 6 h) and the plasma concentrations subsequently fell biexponentially. The principal metabolite 2-MPA appeared later in the plasma (tmax between 10 and 12 h after a lag-time of 3 h) then disappeared monoexponentially. About 15% of the tiopronin was metabolized to 2-MPA.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF02280762