Pharmacokinetics, tissue distribution and plasma protein binding studies of rohitukine: an potent anti-hyperlipidmic agent

Abstract

Rohitukine (RH) is a chromone alkaloid considered as one of the major active components of Dysoxylum binectariferum, exhibiting diverse pharmacological activities such as anti-hyperlipidmic, anti-cancer, anti-inflammatory, immuno-modulatory, anti-leishmanial, anti ulcer and anti-fertility. There’s still a lack of information of RH, inclusive of pharmacokinetics, tissue distribution and excretion, in vivo studies in experimental animal, such as hamster and rats. In this study, a selective and sensitive bioanalytical method was developed and validated using HPLC-UV system. The assay was applied to estimate pharmacokinetics, tissue distribution and excretion of RH in hamster at 50 mg/kg oral dose. It rapidly reached in systemic circulation and distributed to various tissues, and highest concentration was observed in liver. The pharmacokinetics parameters such as clearance (CL/F) was 3.95 ± 0.9 L/h/kg, volume of distribution (Vd/F ) was 17.34 ± 11.34 L/kg and elimination half-life was 2.62 ± 1.34 hr. RH shows moderate protein binding around ~60% and found stable in gastro-intestinal fluid, a property that favors oral administration.