title: Plasma pharmacokinetics and tissue distribution study of roemerine in rats by liquid chromatography with tandem mass spectrometry (LC-MS/MS).
abstract: In the present study, a new LC-MS/MS method for the determination of roemerine in rat plasma and tissue samples was developed and successfully used to study the pharmacokinetics and tissue distribution of roemerine after oral and intravenous (i.v.) administration in rats. The plasma and tissue samples were processed by liquid-liquid extraction with n-hexane. Isocorydine was used as the internal standard (IS) for sample processing and analysis. The MS/MS detection was carried out by monitoring the transitions of m/z 280→249 and m/z 342→279 for roemerine and the IS, respectively. The calibration curve displayed excellent linearity over the concentration range of 10-2000ng/mL (n=8, r(2)≥0.995), and the lower limit of quantification (LLOQ) was determined to be 10ng/mL. This method was rapid, accurate, highly sensitive, and fully validated. The pharmacokinetic study showed that roemerine was rapidly absorbed and eliminated with a tmax of 0.22±0.08h, t1/2 of 1.59±0.46h, CL of 4.44±0.42L/h/kg, and Vd of 10.16±2.95μg/L following oral administration. Additionally, roemerine showed an excellent oral bioavailability of 84% and a wide tissue distribution with brain penetration. Highest concentrations of roemerine were found in the liver and lung, followed by kidney, spleen, heart, and brain, in that order.
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China; Department of Pharmacy, Wenshan city People' Hospital, Wenshan 663000, PR China.
authors.forename: Yue-Qiong
authors.initials: YQ
authors.lastname: Liu
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China.
authors.forename: Gong-Hao
authors.initials: GH
authors.lastname: He
authors.affiliation: Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Hong-Liang
authors.initials: HL
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China.
authors.forename: Jiang-Chang
authors.initials: JC
authors.lastname: He
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China.
authors.forename: En-Fu
authors.initials: EF
authors.lastname: Feng
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China.
authors.forename: Lan
authors.initials: L
authors.lastname: Bai
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China.
authors.forename: Cheng-Ying
authors.initials: CY
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming 650032, PR China. Electronic address: xuguili08@126.com.
authors.forename: Gui-Li
authors.initials: GL
authors.lastname: Xu
mesh_terms: D000470:Alkaloids / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004355:Drug Stability; D005260:Female; D016014:Linear Models; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D053719:Tandem Mass Spectrometry / Q000379:methods*; D014018:Tissue Distribution
chemical_list: D000470:Alkaloids; C030169:roemerine
keywords: LC–MS/MS; Pharmacokinetics; Roemerine; Tissue distribution