Vallès J, Pruñonosa J, Menargues A, Nomen M, Obach R
Research Department, S.A. LASA Laboratorios, Barcelona, Spain.
J Pharm Pharmacol. 1989 Jun;41(6):384-7. doi: 10.1111/j.2042-7158.1989.tb06482.x.
The alpha 2-antagonist idazoxan (2- (2- (1,4-benzodioxanyl))-2-imidazoline) has been given intravenously and orally to five beagle dogs at 1, 3 and 10 mg kg-1 doses. Idazoxan plasma levels were determined by a HPLC method. After intravenous administration, a linear kinetic behaviour was obtained. Half-life and mean residence time values ranged 105.2-117.1 and 138.1-154.0 min, respectively. Total plasma clearance values and volume of distribution at steady state values ranged from 25.6-32.1 (mL kg-1) min-1 and 3.60-4.36 L kg-1, respectively. After oral administration, time to peak values averaged around 1 h. Dose normalized peak concentration values ranged 161-182 ng mL-1. Bioavailability values ranged 60-88%. Low idazoxan bioavailability has been described in other animal species and attributed to a first-pass effect.
已以1、3和10mg kg⁻¹的剂量给5只比格犬静脉注射和口服α₂拮抗剂咪唑克生（2-(2-(1,4-苯并二氧杂环戊烯基))-2-咪唑啉）。通过高效液相色谱法测定咪唑克生的血浆水平。静脉给药后，获得了线性动力学行为。半衰期和平均驻留时间值分别为105.2 - 117.1分钟和138.1 - 154.0分钟。总血浆清除率值和稳态分布容积值分别为25.6 - 32.1（mL kg⁻¹）min⁻¹和3.60 - 4.36 L kg⁻¹。口服给药后，达峰时间平均约为1小时。剂量标准化的峰浓度值为161 - 182 ng mL⁻¹。生物利用度值为60 - 88%。在其他动物物种中也描述了咪唑克生的低生物利用度，这归因于首过效应。
