[Pharmacokinetics of ponsinomycine with repeated ingestion in healthy volunteers].
Ponsinomycin or miocamycin (MOM) is a new macrolide which is totally metabolized in vivo. The disposition of its 3 major metabolites (Mb12, Mb6 and Mb9a), was investigated following multiple dosing with ponsinomycin at a dose of 800 mg every 12 h, for 8 days, in healthy volunteers. Drug measurements were conducted by high performance liquid chromatography. In agreement with the low values of their apparent elimination half-lives, respectively less than 1.5 h and 3.0 h, metabolites Mb12 and Mb9a did not accumulate with time. Their pharmacokinetics was apparently stable with time. Conversely Mb6 did accumulate, by approximatively a factor 2, although its apparent elimination half-life was only close to 2 h. This value must therefore be considered with caution. A dose dependency effect was previously observed, Mb6 pharmacokinetics could be non linear with time as well. The relative importance of this metabolite is therefore greater at steady-state, following multiple administration than after single dosing with ponsinomycin.
Couet
W
W
CEMAF, Poitiers.
Reigner
B G
BG
Ingrand
I
I
Girault
J
J
Istin
B
B
Bizouard
J
J
Fourtillan
J B
JB
D000284:Administration, Oral; D000328:Adult; D002850:Chromatography, Gel; D005260:Female; D006801:Humans; D008297:Male; D015644:Miocamycin / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*
D015644:Miocamycin
Pharmacocinétique de la ponsinomycine administrée en prises répétées chez le volontaire sain.