BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum

In vitro assays are economical and easy to perform but to establish relevance of their results to real clinical outcome in animals or human, pharmacokinetics is prerequisite. Despite various in vitro pharmacological activities of extracts of Piper sarmentosum, there is no report of pharmacokinetic...

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Main Authors:	Hussain, Khalid, Ismail, Zhari, Sadikun, Amirin, Ibrahim, Pazillah
Format:	Article
Published:	Hindawi Publishing Corporation 2011
Subjects:	RS1-441 Pharmacy and materia medica
Online Access:	https://doi.org/10.1093/ecam/nep143 https://doi.org/10.1093/ecam/nep143 http://eprints.usm.my/38398/1/Bioactive_Markers_Based_Pharmacokinetic_Evaluation.pdf

id	usm-38398
recordtype	eprints
spelling	usm-383982018-01-17T00:27:35Z BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum Hussain, Khalid Ismail, Zhari Sadikun, Amirin Ibrahim, Pazillah RS1-441 Pharmacy and materia medica In vitro assays are economical and easy to perform but to establish relevance of their results to real clinical outcome in animals or human, pharmacokinetics is prerequisite. Despite various in vitro pharmacological activities of extracts of Piper sarmentosum, there is no report of pharmacokinetics. Therefore, the present study aimed to evaluate ethanol extract of fruit of the plant in dose of 500 mg kg−1 orally for pharmacokinetics. Sprague-Dawley rats were randomly divided into groups 1, 2, and 3 (each n = 6) to study absorption, distribution and excretion, respectively. High performance liquid chromatography (HPLC) with ultraviolet detection was applied to quantify pellitorine, sarmentine and sarmentosine in plasma, tissues, feces and urine to calculate pharmacokinetic parameters. Pellitorine exhibited maximum plasma concentration (Cmax) 34.77 ngmL−1± 1.040, time to achieve Cmax (Tmax) 8h, mean resident time (MRT) 26.00 ± 0.149 h and half life (t1/2) 18.64 ± 1.65 h. Sarmentine showed Cmax 191.50 ± 12.69 ng mL−1, Tmax 6 h, MRT 11.12 ± 0.44 h and t1/2 10.30 ± 1.98 h. Sarmentosine exhibited zero oral bioavailability because it was neither detected in plasma nor in tissues, and in urine. Pellitorine was found to be distributed in intestinal wall, liver, lungs, kidney, and heart, whereas sarmentine was found only in intestinal wall and heart. The cumulative excretion of pellitorine, sarmentine and sarmentosine in feces in 72 h was 0.0773, 0.976, and 0.438 μg, respectively. This study shows that pellitorine and sarmentine have good oral bioavailability while sarmentosine is not absorbed from the gastrointestinal tract. Hindawi Publishing Corporation 2011 Article PeerReviewed application/pdf http://eprints.usm.my/38398/1/Bioactive_Markers_Based_Pharmacokinetic_Evaluation.pdf https://doi.org/10.1093/ecam/nep143 Hussain, Khalid and Ismail, Zhari and Sadikun, Amirin and Ibrahim, Pazillah (2011) BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum. Evidence-Based Complementary and Alternative Medicine, 2011 (980760). pp. 1-7. ISSN 1741-427X http://eprints.usm.my/38398/
institution	Universiti Sains Malaysia Universiti Sains Malaysia
repository_type	Digital Repository
institution_category	Local University
building	USM Repository
collection	Online Access
topic	RS1-441 Pharmacy and materia medica
spellingShingle	RS1-441 Pharmacy and materia medica Hussain, Khalid Ismail, Zhari Sadikun, Amirin Ibrahim, Pazillah BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
description	In vitro assays are economical and easy to perform but to establish relevance of their results to real clinical outcome in animals or human, pharmacokinetics is prerequisite. Despite various in vitro pharmacological activities of extracts of Piper sarmentosum, there is no report of pharmacokinetics. Therefore, the present study aimed to evaluate ethanol extract of fruit of the plant in dose of 500 mg kg−1 orally for pharmacokinetics. Sprague-Dawley rats were randomly divided into groups 1, 2, and 3 (each n = 6) to study absorption, distribution and excretion, respectively. High performance liquid chromatography (HPLC) with ultraviolet detection was applied to quantify pellitorine, sarmentine and sarmentosine in plasma, tissues, feces and urine to calculate pharmacokinetic parameters. Pellitorine exhibited maximum plasma concentration (Cmax) 34.77 ngmL−1± 1.040, time to achieve Cmax (Tmax) 8h, mean resident time (MRT) 26.00 ± 0.149 h and half life (t1/2) 18.64 ± 1.65 h. Sarmentine showed Cmax 191.50 ± 12.69 ng mL−1, Tmax 6 h, MRT 11.12 ± 0.44 h and t1/2 10.30 ± 1.98 h. Sarmentosine exhibited zero oral bioavailability because it was neither detected in plasma nor in tissues, and in urine. Pellitorine was found to be distributed in intestinal wall, liver, lungs, kidney, and heart, whereas sarmentine was found only in intestinal wall and heart. The cumulative excretion of pellitorine, sarmentine and sarmentosine in feces in 72 h was 0.0773, 0.976, and 0.438 μg, respectively. This study shows that pellitorine and sarmentine have good oral bioavailability while sarmentosine is not absorbed from the gastrointestinal tract.
format	Article
author	Hussain, Khalid Ismail, Zhari Sadikun, Amirin Ibrahim, Pazillah
author_facet	Hussain, Khalid Ismail, Zhari Sadikun, Amirin Ibrahim, Pazillah
author_sort	Hussain, Khalid
title	BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
title_short	BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
title_full	BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
title_fullStr	BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
title_full_unstemmed	BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum
title_sort	bioactivemarkers based pharmacokinetic evaluation of extracts of a traditionalmedicinal plant, piper sarmentosum
publisher	Hindawi Publishing Corporation
publishDate	2011
url	https://doi.org/10.1093/ecam/nep143 https://doi.org/10.1093/ecam/nep143 http://eprints.usm.my/38398/1/Bioactive_Markers_Based_Pharmacokinetic_Evaluation.pdf
first_indexed	2018-09-08T09:28:14Z
last_indexed	2018-09-08T09:28:14Z
_version_	1611031007552602112

BioactiveMarkers Based Pharmacokinetic Evaluation of Extracts of a TraditionalMedicinal Plant, Piper sarmentosum

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