CC BY-NC-ND 4.0 · PMIO 2018; 5(02): e39-e47
DOI: 10.1055/a-0600-9750
Original Papers
Eigentümer und Copyright ©Georg Thieme Verlag KG 2018

Comparison of the Pharmacokinetic Profiles of a Standardized Extract of Centella asiatica and A Mixture of Madecassoside and Asiaticoside in Rats

Phisit Khemawoot
1  Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand
2  Preclinical Pharmacokinetics and Interspecies Scaling for Drug Development Research Unit, Chulalongkorn University, Bangkok, Thailand
,
Patcharaporn Hengjumrut
1  Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand
,
Tosapol Anukunwithaya
1  Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand
,
Leng Chee Chang
3  Daniel K. Inouye College of Pharmacy, University of Hawai‘i, Hilo, HI, USA
,
Supakit Wongwiwatthananukit
3  Daniel K. Inouye College of Pharmacy, University of Hawai‘i, Hilo, HI, USA
,
Mayuree H. Tantisira
4  Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, Thailand
› Author Affiliations
Further Information

Publication History

received 16 November 2017
revised 14 March 2018

accepted 19 March 2018

Publication Date:
25 April 2018 (online)

Abstract

Centella asiatica is a tropical plant commonly used as an herbal remedy in traditional medicines in many countries. In an attempt to establish an herbal extract with well-defined characteristics, a standardized extract of C. Asiatica, ECa 233, was developed. This extract contains at least 80% triterpenoid glycosides with the major constituents madecassoside and asiaticoside at a ratio of 1.5±0.5:1. In the present study, comparative pharmacokinetics of ECa 233 with its mixture of madecassoside and asiaticoside were conducted in rats. Following intravenous or oral administration of the test compounds, blood, tissues, urine, and feces were collected for the determination of madecassoside, asiaticoside, and their metabolite levels using liquid chromatography tandem mass spectrometry. Plasma levels of madecassoside and asiaticoside in the ECa 233-treated group were found to be higher than their respective counterparts in the mixture. Madecassoside and asiaticoside in both test formulae appeared to be widely distributed in several organs, and more than 50% of the administered doses were recovered as madecassic acid and asiatic acid in the feces within 24 to 48 h. The results clearly demonstrated the pharmacokinetic advantage of a standardized extract of C. Asiatica, ECa 233, compared with a mixture of madecassoside and asiaticoside at an equivalent amount. Other minor constituents that naturally exist in ECa 233 appeared to positively modulate the pharmacokinetics of its major constituents, resulting in relatively better pharmacokinetic profiles than those from a mixture of pure compounds.

Supporting Information