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 (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.
Hercelin
B
B
Unité de Pharmacocinétique-Biopharmacie, Laboratoires Cassenne, Osny, France.
Leroy
P
P
Nicolas
A
A
Gavriloff
C
C
Chassard
D
D
Thébault
J J
JJ
Reveillaud
M T
MT
Salles
M F
MF
Netter
P
P
D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008297:Male; D013438:Sulfhydryl Compounds / Q000097:blood*; D013997:Time Factors; D008625:Tiopronin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D013438:Sulfhydryl Compounds; D008625:Tiopronin; C023884:thiolactic acid