title: Pharmacokinetic study of lappaconitine hydrobromide in mice by LC-MS.
abstract: A high sensitive and rapid method was developed for the analysis of lappaconitine in mouse plasma using liquid chromatography coupled to mass spectrometry (LC-MS). Detection was performed by positive ion electrospray ionization (ESI) in multiple reaction monitoring (MRM) mode, monitoring the transitions m/z 585 --> m/z 535 and m/z 356 --> m/z 192, for the quantification of lappaconitine and tetrahydropalmatine (internal standard, IS), respectively. The method was linear over the concentration range of 3.0-2000.0 ng x mL(-1). The lower limit of quantification was 3.0 ng x mL(-1). Intra- and inter-run precisions (RSD) were both less than 9.9% and accuracy (RE) within +/- 4.8%. After single intravenous injections of lappaconitine hydrobromide at 1.0, 2.0 and 4.0 mg x kg(-1), the elimination half-lives (t(1/2)) were 0.47, 0.48 and 0.49 h, and the areas under the curve (AUC(0-t)) were 55.5, 110.5 and 402.9 ng x h x mL(-1), separately. The pharmacokinetic profile of lappaconitine was linear at relatively lower dose levels (1.0-2.0 mg x kg(-1)). When the dose increased farther to 4.0 mg x kg(-1), the Vz and CL decreased, and the increase fold of the AUC was much larger than that of the dose.
authors: School of Pharmaceutical Science and Technology, Dalian University of Technology, Dalian 116024, China.
authors: Qing
authors: Q
authors: Wang
authors: Zi-jing
authors: ZJ
authors: Li
authors: Lu
authors: L
authors: Sun
authors: Li-ying
authors: LY
authors: Gao
authors: Ming-hui
authors: MH
authors: Li
authors: Jia-jia
authors: JJ
authors: Hao
authors: Xin
authors: X
authors: Zhang
authors: Yu-ming
authors: YM
authors: Sun
mesh_terms: D000157:Aconitine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D019540:Area Under Curve; D002853:Chromatography, Liquid / Q000379:methods*; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D015394:Molecular Structure; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*
chemical_list: D018712:Analgesics, Non-Narcotic; D000157:Aconitine; C022150:lappaconitine