title: Pharmacokinetics, Tissue Distribution and Plasma Protein Binding Studies of Rohitukine: A Potent Anti-hyperlipidemic Agent.
abstract: 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 50 mg/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±0.9 L/h/kg, volume of distribution (Vd/F) was 17.34±11.34 L/kg and elimination half-life was 2.62±1.34 h. RH shows moderate protein binding ~ 60% and found stable in gastro-intestinal fluid, a property that favors oral administration.
authors.affiliation: Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: Y S
authors.initials: YS
authors.lastname: Chhonker
authors.affiliation: Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: H
authors.initials: H
authors.lastname: Chandasana
authors.affiliation: Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, India.
authors.forename: A
authors.initials: A
authors.lastname: Kumar
authors.affiliation: Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: D
authors.initials: D
authors.lastname: Kumar
authors.affiliation: Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: T S
authors.initials: TS
authors.lastname: Laxman
authors.affiliation: Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: S K
authors.initials: SK
authors.lastname: Mishra
authors.affiliation: Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: V M
authors.initials: VM
authors.lastname: Balaramnavar
authors.affiliation: Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: S
authors.initials: S
authors.lastname: Srivastava
authors.affiliation: Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
authors.affiliation: Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
authors.forename: R S
authors.initials: RS
authors.lastname: Bhatta
mesh_terms: D000818:Animals; D002867:Chromones / Q000097:blood* / Q000737:chemistry / Q000302:isolation & purification / Q000493:pharmacokinetics*; D006224:Cricetinae; D004355:Drug Stability; D000960:Hypolipidemic Agents / Q000097:blood / Q000737:chemistry / Q000302:isolation & purification / Q000493:pharmacokinetics; D008297:Male; D029582:Meliaceae / Q000737:chemistry*; D010880:Piperidines / Q000097:blood* / Q000737:chemistry / Q000302:isolation & purification / Q000493:pharmacokinetics*; D024301:Plant Bark / Q000737:chemistry; D010949:Plasma / Q000737:chemistry*; D011485:Protein Binding / Q000187:drug effects*; D051381:Rats; D012995:Solubility; D014018:Tissue Distribution
chemical_list: C573233:5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4H-1-benzopyran-4-one; D002867:Chromones; D000960:Hypolipidemic Agents; D010880:Piperidines