Wr. Rush et al., THE COMPARATIVE STEADY-STATE BIOAVAILABILITY OF THE ACTIVE INGREDIENTS OF MADECASSOL, European journal of drug metabolism and pharmacokinetics, 18(4), 1993, pp. 323-326
The comparative steady-state bioavailability of asiatic acid was studi
ed in 12 healthy male and female volunteers following oral administrat
ion of approximately equimolar doses of either asiatic acid (12 mg) or
the glycoside derivative of asiatic acid, asiaticoside (24 mg). Both
asiatic acid and asiaticoside are constituents of the marketed dermato
logical product Madecassol. Asiaticoside is converted in vivo to asiat
ic acid by hydrolytic cleavage of the sugar moiety. Steady-state AUC0-
12h values for asiatic acid on either regime were similar (614 +/- 250
ng.h/ml following asiatic acid compared to 606 +/- 316 ng.h/ml follow
ing asiaticoside) indicating comparable bioavailability for asiatic ac
id with the two ingredients at approximately equimolar doses. Since as
iatic acid is considered to bc the most therapeutically active ingredi
ent of Madecassol, the current data suggest that the therapeutic effec
ts of asiaticoside may be mediated through conversion to asiatic acid.