Burchfield D J, Abrams R M, Miller R L, DeVane C L
University of Florida College of Medicine, Department of Pediatrics, Gainesville 32610.
Life Sci. 1991;48(22):2129-36. doi: 10.1016/0024-3205(91)90145-2.
A pipe for administration of inhaled cocaine and its pyrolytic products in laboratory animals was developed and tested. In-vitro trials showed 30.0 +/- 5.2% (mean +/- SE) recovery of cocaine in solvent. Five non-pregnant ewes were instrumented with tracheal T-tubes and vascular catheters. After surgical recovery, ewes received three doses of cocaine (free base) in a randomized fashion; 2 mg/kg and 4 mg/kg both by inhalation, and 2 mg/kg intravenously. Arterial blood samples were collected and assayed for cocaine and its major metabolites by high performance liquid chromatography. Blood pressure and heart rate were continuously recorded. Cocaine administered by inhalation was eliminated with a half-life of 1.6 +/- 0.5 min (mean +/- SE) compared to 3.4 +/- 0.9 following intravenous administration (p less than 0.03). Likewise, clearance values were greater following inhalation, 5532 +/- 1756 ml/min/kg, than following intravenous administration, 163 +/- 20.6 ml/min/kg (p less than 0.04). Both routes of administration led to significant elevations in blood pressure, 7.5% increase after smoking vs 20% increase after intravenous administration. No correlation was found between inhalational dose of cocaine and peak plasma cocaine concentration.
开发并测试了一种用于在实验动物中给予吸入性可卡因及其热解产物的管道。体外试验表明，可卡因在溶剂中的回收率为30.0±5.2%（平均值±标准误）。对五只未怀孕的母羊安装了气管T型管和血管导管。手术恢复后，母羊以随机方式接受了三剂可卡因（游离碱）；吸入剂量分别为2mg/kg和4mg/kg，静脉注射剂量为2mg/kg。采集动脉血样本，通过高效液相色谱法测定可卡因及其主要代谢产物。连续记录血压和心率。吸入给予的可卡因消除半衰期为1.6±0.5分钟（平均值±标准误），而静脉注射后的半衰期为3.4±0.9分钟（p<0.03）。同样，吸入后的清除率值更高，为5532±1756ml/min/kg，高于静脉注射后的清除率值163±20.6ml/min/kg（p<0.04）。两种给药途径均导致血压显著升高，吸烟后血压升高7.5%，静脉注射后升高20%。未发现吸入可卡因剂量与血浆可卡因峰值浓度之间存在相关性。
