Obach R, Pruñonosa J, Menargues A, Nomen M, Vallès J
Research Department of S.A. LASA Laboratories, Barcelona, Spain.
Biopharm Drug Dispos. 1988 Sep-Oct;9(5):501-11. doi: 10.1002/bod.2510090508.
In a pharmacokinetic study, 15, 30, 60, and 150 mg kg-1 intravenous and oral doses of methocarbamol were administered to rats. Differences observed in plasma clearance values, i.e. 0.0203, 0.0156, 0.0123, and 0.0085 1 kg-1 min-1 for 15, 30, 60, and 150 mg kg-1, respectively, suggested a dose-dependent pharmacokinetic behaviour of the drug. Elimination according to a biocompartmental open model and Michaelis-Menten kinetics fits the plasma level data. Estimated Km and Vmax values were 38.49 +/- 3.71 mg l-1 and 1.24 +/- 0.06 mg l-1 min-1, respectively. After oral administration of 15, 30, and 60 mg kg-1 the peak plasma levels were reached earlier. The tmax values were 6, 6, and 10 min, respectively. After 150 mg kg-1 oral doses, peak plasma levels were reached later (tmax = 150 min). Estimated bioavailability ranged between 77 and 112 per cent.
在一项药代动力学研究中，给大鼠静脉注射和口服15、30、60和150mg/kg的美索巴莫。观察到的血浆清除率值存在差异，即15、30、60和150mg/kg时分别为0.0203、0.0156、0.0123和0.0085 l/kg/min，这表明该药物具有剂量依赖性药代动力学行为。根据二房室开放模型和米氏动力学进行的消除符合血浆水平数据。估计的Km和Vmax值分别为38.49±3.71mg/l和1.24±0.06mg/l/min。口服15、30和60mg/kg后，血浆峰值水平出现得更早。tmax值分别为6、6和10分钟。口服150mg/kg剂量后，血浆峰值水平出现得较晚（tmax = 150分钟）。估计的生物利用度在77%至112%之间。
