Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers

Abstract The formula of a standardized extract of Centella asiatica (ECa 233) was modified to improve its dissolution, with implications for pharmacokinetics and metabolomic profile. This study aimed to understand the resultant changes in disposition kinetics of ECa 233 and alterations to human meta...

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Autores principales:	Phanit Songvut, Pajaree Chariyavilaskul, Phisit Khemawoot, Rossarin Tansawat
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/46f92f94d82946d1baf9471d1a54b3ca
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spelling	oai:doaj.org-article:46f92f94d82946d1baf9471d1a54b3ca2021-12-02T11:45:03ZPharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers10.1038/s41598-021-86267-22045-2322https://doaj.org/article/46f92f94d82946d1baf9471d1a54b3ca2021-03-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-86267-2https://doaj.org/toc/2045-2322Abstract The formula of a standardized extract of Centella asiatica (ECa 233) was modified to improve its dissolution, with implications for pharmacokinetics and metabolomic profile. This study aimed to understand the resultant changes in disposition kinetics of ECa 233 and alterations to human metabolome after oral administration. This study was a two-sequence of dosages (250 and 500 mg), with an open-label phase I clinical trial. The modified formula was administered in single and multiple doses to twelve healthy Thai volunteers. The major parent compounds, madecassoside and asiaticoside, were rarely absorbed, instead undergoing biotransformation into active metabolites, madecassic acid and asiatic acid with possibility to be eliminated via fecal route. Increasing the dose of ECa 233 resulted in significantly greater plasma levels of those active metabolites, with accumulation of asiatic acid after multiple oral administration for seven days. Examining the impacts of accumulation behavior on metabolomics, the study traced changes in levels pre- and post-dose of five relevant human metabolites. Administration of ECa 233 was found to be significantly associated with an increase of choline, an endogenous metabolite with documented benefits for learning and memory. Therefore, ECa 233 may be useful in mitigating cognitive impairment, through its role in modulating human metabolites.Phanit SongvutPajaree ChariyavilaskulPhisit KhemawootRossarin TansawatNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-13 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Phanit Songvut Pajaree Chariyavilaskul Phisit Khemawoot Rossarin Tansawat Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
description	Abstract The formula of a standardized extract of Centella asiatica (ECa 233) was modified to improve its dissolution, with implications for pharmacokinetics and metabolomic profile. This study aimed to understand the resultant changes in disposition kinetics of ECa 233 and alterations to human metabolome after oral administration. This study was a two-sequence of dosages (250 and 500 mg), with an open-label phase I clinical trial. The modified formula was administered in single and multiple doses to twelve healthy Thai volunteers. The major parent compounds, madecassoside and asiaticoside, were rarely absorbed, instead undergoing biotransformation into active metabolites, madecassic acid and asiatic acid with possibility to be eliminated via fecal route. Increasing the dose of ECa 233 resulted in significantly greater plasma levels of those active metabolites, with accumulation of asiatic acid after multiple oral administration for seven days. Examining the impacts of accumulation behavior on metabolomics, the study traced changes in levels pre- and post-dose of five relevant human metabolites. Administration of ECa 233 was found to be significantly associated with an increase of choline, an endogenous metabolite with documented benefits for learning and memory. Therefore, ECa 233 may be useful in mitigating cognitive impairment, through its role in modulating human metabolites.
format	article
author	Phanit Songvut Pajaree Chariyavilaskul Phisit Khemawoot Rossarin Tansawat
author_facet	Phanit Songvut Pajaree Chariyavilaskul Phisit Khemawoot Rossarin Tansawat
author_sort	Phanit Songvut
title	Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
title_short	Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
title_full	Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
title_fullStr	Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
title_full_unstemmed	Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers
title_sort	pharmacokinetics and metabolomics investigation of an orally modified formula of standardized centella asiatica extract in healthy volunteers
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/46f92f94d82946d1baf9471d1a54b3ca
work_keys_str_mv	AT phanitsongvut pharmacokineticsandmetabolomicsinvestigationofanorallymodifiedformulaofstandardizedcentellaasiaticaextractinhealthyvolunteers AT pajareechariyavilaskul pharmacokineticsandmetabolomicsinvestigationofanorallymodifiedformulaofstandardizedcentellaasiaticaextractinhealthyvolunteers AT phisitkhemawoot pharmacokineticsandmetabolomicsinvestigationofanorallymodifiedformulaofstandardizedcentellaasiaticaextractinhealthyvolunteers AT rossarintansawat pharmacokineticsandmetabolomicsinvestigationofanorallymodifiedformulaofstandardizedcentellaasiaticaextractinhealthyvolunteers
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Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers

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