Pharmacokinetics, Tissue Distribution and Plasma Protein Binding Studies of Rohitukine: A Potent Anti-hyperlipidemic Agent

Rohitukine (RH) is a chromone alkaloid considered as one of the major active component of Dysoxylum binectariferum, exhibiting diverse pharmacological activities such as anti-hyperlipidemic, 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 animals, 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 50mg/kg oral dose. It rapidly reached systemic circulation and distributed to various tissues, and highest concentration was observed in liver. The pharmacokinetic parameters such as clearance (CL/F) was 3.95 +/- 0.9L/h/kg, volume of distribution (V-d/F) was 17.34 +/- 11.34L/kg and elimination half-life was 2.62 +/- 1.34h. RH shows moderate protein binding similar to 60% and found stable in gastro-intestinal fluid, a property that favors oral administration.