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

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 asi...

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Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 1993-10, Vol.18 (4), p.323-326
Main Authors: RUSH, W. R, MURRAY, G. R, GRAHAM, D. J. M
Format: Article
Language:English
Subjects:
Adult
Anti-Infective Agents - blood
Anti-Infective Agents - pharmacokinetics
Biological and medical sciences
Biological Availability
Double-Blind Method
Female
General pharmacology
Humans
Male
Medical sciences
Pentacyclic Triterpenes
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Triterpenes - blood
Triterpenes - pharmacokinetics
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Summary: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.
ISSN:0378-7966
2107-0180
DOI:10.1007/BF03190180