Pharmacokinetic analysis and tissue distribution of andrographolide in rat by a validated LC-MS/MS method. (March 2014)

• Record Type: Journal Article
• Authors: Bera, Rammohan; Ahmed, S. K. Milan; Sarkar, Lipi; Sen, Tuhinadri; Karmakar, Sanmoy
• Is Part Of: Pharmaceutical biology. Volume 52:Number 3(2014:Mar.)
• Page Start: 321
• Page End: 329
• Publication Date: 2014-03
• Subjects: Pharmacognosy -- Periodicals; Materia medica, Vegetable -- Periodicals; 615.321
• DOI: 10.3109/13880209.2013.836544
• Languages: English
• ISSNs: 1388-0209

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: <italic>Andrographis paniculata</italic> (Burm.f.) Nees (Acanthaceae) is widely used in tribal medicine in India and some other countries for multiple clinical applications. It contains andrographolide (AG) (diterpenoid lactone), a major phytomarker which probably accounts for its medicinal properties.</p> <p> <italic>Objective</italic>: This study investigates the site-specific distribution of AG in different tissues of rats and its pharmacokinetic parameter evaluation by using a validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method.</p> <p> <italic>Materials and methods</italic>: A simple and sensitive LC-MS/MS method has been developed and validated to quantify the presence of AG in plasma and various tissues of rat following oral administration of <italic>A. paniculata</italic> extract and AG in a dose of 133.33 and 100 mg/kg/day, respectively, for four weeks.</p> <p> <italic>Results</italic>: The present study showed that the highest concentration of AG was in kidney (156.12 ng/g) followed by liver, spleen and brain while almost same concentration was found in heart and lung. The apparent <italic>C</italic><sub>max</sub>, <italic>T</italic><sub>max</sub>, elimination half-life and total exposure (AUC<sub>0–</sub><italic><sub>α</sub></italic>) were 115.81 ng/ml, 0.75, 2.45 and 278.44 ngh/ml, respectively.</p> <p> <italic>Conclusion</italic>: This was an attempt to determine the presence of AG (a known biomarker) in tissues such as kidney, heart, lungs, brain and plasma of rats using a validated LC-MS/MS method. Furthermore, the observed reduced concentration in plasma and various tissues from 1 to 8 h might be attributed to relatively rapid elimination or distribution of AG from the central compartment.</p> </abstract>