The comparative steady-state bioavailability of the active ingredients of madecassol

Abstract

The comparative steady-state bioavailability of asiatic acid was studied in 12 healthy male and female volunteers following oral administration 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 dermatological product Madecassol. Asiaticoside is converted in vivo to asiatic acid by hydrolytic cleavage of the sugar moiety. Steady-state AUC0-12h values for asiatic acid on either regimen were similar (614 +/- 250 ng.h/ml following asiatic acid compared to 606 +/- 316 ng.h/ml following asiaticoside) indicating comparable bioavailability for asiatic acid with the two ingredients at approximately equimolar doses. Since asiatic acid is considered to be the most therapeutically active ingredient of Madecassol, the current data suggest that the therapeutic effects of asiaticoside may be mediated through conversion to asiatic acid.

Centella asiatica attenuates Aβ-induced neurodegenerative spine loss and dendritic simplification

“…Each compound was evaluated at a concentration similar to its percent composition in the dose of CAW tested with the exception of AA and MA. These triterpenes were negligible or undetectable in the extract (Table 1) but were tested at the same concentration as their glycosidic counterparts because of the potential for metabolism of AS and MS into AA and MA in vivo [21]. …”

“…The triterpene asiatic acid also has neuroprotective properties [19, 20]. The concentrations used were similar to their percent abundance in 50ug/mL CAW (Table 1), with the exception of AA and MA which were tested at higher concentrations equivalent to the molar concentrations of their glycoside counterpart (AS and MS respectively) since in vivo the glycosides would be metabolized into the aglycone form [21]…”

Centella asiatica triterpenes for diabetic neuropathy: a randomized, double-blind, placebo-controlled, pilot clinical study

“…18,33,39,40 have focused on AA alone. While there was considerable variation in the AA and MA concentrations of the patient samples that were analyzed, the mean values are consistent with previous reports on the pharmacokinetics of asiatic acid in human plasma.…”

“…On oral administration, AS is hydrolyzed in the gut and appears in the blood stream as AA. 18 Therefore plasma levels of AA and MA were monitored in subjects receiving CAST.…”

Asiaticoside Inhibits TNF-α-Induced Endothelial Hyperpermeability of Human Aortic Endothelial Cells

“…A previous study has reported that only approximately 3 μM of asiaticoside was detected within 5 min in rat plasma after a single intravenous injection of 40 mg/kg of asiaticoside; while no asiaticoside was detected in plasma following a single intragastric administration of 200 mg/kg of asiaticoside (Liu et al , ). Nevertheless, asiaticoside could be administered as a prodrug that causes an increase in the plasma concentration of asiatic acid (Rush et al , ).…”