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

Autor:	Chhonker YS; Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India., Chandasana H; Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India., Kumar A; Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, India., Kumar D; Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India., Laxman TS; Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India., Mishra SK; Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India., Balaramnavar VM; Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India., Srivastava S; Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India., Saxena AK; Medicinal & Process Chemistry Division, CSIR- Central Drug Research Institute, Lucknow, India., Bhatta RS; Pharmacokinetics & Metabolism Div., CSIR- Central Drug Research Institute, Lucknow, India.
Jazyk:	angličtina
Zdroj:	Drug research [Drug Res (Stuttg)] 2015 Jul; Vol. 65 (7), pp. 380-7. Date of Electronic Publication: 2014 Sep 22.
DOI:	10.1055/s-0034-1387774
Abstrakt:	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. (© Georg Thieme Verlag KG Stuttgart · New York.)
Databáze:	MEDLINE
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