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
Abstract
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.
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