Nelson E, Powell J R, Conrad K, Likes K, Byers J, Baker S, Perrier D
J Clin Pharmacol. 1982 Feb-Mar;22(2-3):141-8. doi: 10.1002/j.1552-4604.1982.tb02662.x.
The pharmacokinetics and bioavailability of phenobarbital were examined in six healthy adult subjects after a 2.6 mg/kg intravenous and a 2.9 mg/kg oral dose. Serum concentrations of phenobarbital were followed by means of a high pressure liquid chromatographic assay for 21 days after drug administration. After the intravenous dose, the mean distribution half-life was 0.18 hour and the mean elimination half-life was 5.8 days. Mean total body clearance and mean renal clearance were 3.0 ml/hr/kg and 0.8 ml/hr/kg, respectively. The apparent volume of distribution was 0.60 liter/kg. After administration of phenobarbital tablets, the maximum phenobarbital serum concentration was 5.5 mg/liter at 2.3 hours after the dose. Adjusted absolute availability of phenobarbital from the tablets studied was 94.9 per cent (range 81-111.9 per cent). The elimination half-life averaged 5.1 days for the oral dose. There was no evidence of autoinduction of phenobarbital elimination over the study period.
在6名健康成年受试者中,分别静脉注射2.6mg/kg和口服2.9mg/kg苯巴比妥后,对其药代动力学和生物利用度进行了研究。给药后,采用高压液相色谱法测定苯巴比妥血清浓度,持续21天。静脉给药后,平均分布半衰期为0.18小时,平均消除半衰期为5.8天。平均全身清除率和平均肾清除率分别为3.0ml/(小时·千克)和0.8ml/(小时·千克)。表观分布容积为0.60升/千克。服用苯巴比妥片后,给药后2.3小时苯巴比妥血清最高浓度为5.5mg/升。所研究片剂中苯巴比妥的校正绝对生物利用度为94.9%(范围81-111.9%)。口服剂量的消除半衰期平均为5.1天。在研究期间,没有证据表明苯巴比妥消除存在自身诱导现象。