Journal of Bioequivalence & Bioavailability

Pharmacokinetic, bioavailability, metabolism and plasma protein binding evaluation of NADPHoxidase inhibitor apocynin

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Veenu Bala1, Hardik Chandasana1, Yashpal S Chhonker1, Yarra D Pradsad2, Telaprolu K Chaitanya2, Vishnu L Sharma1 and Rabi S Bhatta1,2

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

Introduction: Picrorhiza kurroa is a medicinal plant that grows in the Himalayan mountains and traditionally been used to treat
disorders of the liver and respiratory tract in Ayurvedic system of medicine. Apocynin is a catechol based active constituent of
Picrorhiza kurroa and has inhibitory effect on superoxide generating NADPH-Oxidase enzyme exhibiting potent anti-inflammatory
activity.
Materials & Methods: To elucidate detailed pharmacokinetic profile of apocynin like bioavailability, pH dependent stability, in vitro
metabolism and protein binding. To investigate these studies, rapid, sensitive, and simple high-performance liquid chromatography
coupled with tandem mass spectrometry (HPLC–MS/MS) assay was developed and in rat and human plasma.
Results: Apocynin was rapidly absorbed, and peak plasma level achieved within five min; moreover, plasma levels were observed
up to 48 hrs at 50 mg/kg dose in rat. Apocynin plasma protein binding was 83.41- 86.07 % in the rat and 71.39 - 73.34 % in human.
Apocynin found completely stable in all three tested pH conditions (1.2, 6.8 and 7.4).
Conclusion: This report provide a detailed pharmacokinetics of apocynin, and these finding could help for the further development
of apocynin and better elucidation of its pharmacological efficacy. Together, these data provide crucial information for its continued
development toward the potential clinical candidate for inflammatory disease.