Comparative pharmacokinetics between madecassoside and asiaticoside presented in a standardised extract of Centella asiatica, ECa 233 and their respective pure compound given separately in rats

Abstract

1. ECa 233, the standardised extract of Centella asiatica, contains not less than 80% triterpenoid glycosides, in a madecassoside:asiaticoside ratio of 1.5 (±0.5):1.

2. The pharmacokinetic comparison of madecassoside and asiaticoside was performed in rats following intravenous and oral administration of ECa 233, or an equivalent dose of the individual compounds. Blood, tissues, urine and faeces were collected after dosing to determine drug and metabolite levels using liquid chromatography–tandem mass spectrometry.

3. Our study demonstrated that plasma levels of madecassoside, and to a lesser extent asiaticoside, were higher after administration of ECa 233 than the corresponding values for the pure compounds. There was a bidirectional interconversion between asiaticoside and madecassoside consistent with the increased exposure of madecassoside and asiaticoside in ECa 233.

4. Both madecassoside and asiaticoside appeared to be widely distributed in several organs and metabolized extensively; following intravenous administration of either compound, approximately 80–90% of the dose was recovered as madecassic acid and asiatic acid in the faeces.

Keywords:

• Asiaticoside
• Centella asiatica
• ECa 233
• madecassoside
• pharmacokinetics

Acknowledgements

The authors are deeply grateful to Dr. Thomayant Prueksaritanont from Chulalongkorn University Drug and Health Products Innovation Promotion Centre for invaluable advice and review of the manuscript. Technical language amendment was conducted under supervision of Dr. Delia Bethell. This research was supported by the Ratchadaphiseksomphot Endowment Fund of Chulalongkorn University (RES560530205-HR).

Declaration of interest

All authors declare no conflict of interest.

We express our gratitude to the Faculty of Pharmaceutical Sciences, Chulalongkorn University for providing research funds to Dr. Phisit Khemawoot [Grant number, Phar 2558-RG01].