Kinetics of cocaine in humans after intravenous and intranasal administration.
Kinetics of cocaine in humans after intravenous and intranasal administration.
复制标题
静脉内和鼻内给药后可卡因在人体中的动力学。
DOI：
10.1002/bdd.2510040104
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发表时间：
1983
影响因子：
2.1
通讯作者：
Davis,JM
中科院分区：
文献类型：
--
作者：
Javaid,JI;Musa,MN;Fischman,M;Schuster,CR;Davis,JM
在4名受试者中研究静脉内和鼻内给药后的凝血动力学。对于静脉内给药，在1分钟内以1 ml体积注射溶于生理盐水的盐酸可卡因（32 mg）。鼻内可卡因以100 mg粉末给药，由适当剂量的盐酸可卡因（64和96 mg）与乳糖粉末混合组成。指导受试者在1分钟内通过5 cm吸管吸入混合物。静脉注射后，CO2动力学符合一级消除的一室开放模型。鼻内给药后，可卡因动力学符合一级吸收和一级消除的一室模型。4名受试者静脉注射可卡因的平均半衰期为41·4±8·2 min（平均值± S.E.M.）。范围为19 ~ 64 min。静脉和鼻内给药后，平均浓度-时间曲线下面积（AUC）存在统计学显著性差异。AUC具有剂量依赖性，64 mg鼻内可卡因给药后吸收的剂量分数显著低于96 mg剂量（p<0.05）。
Cocaine kinetics were studied in four subjects after intravenous and intranasal administration. For intravenous administration cocaine hydrochloride (32 mg) dissolved in physiological saline was injected in 1 ml volume over a 1 min period. Intranasal cocaine was administered as 100mg powder consisting of an appropriate dose of cocaine hydrochloride (64 and 96 mg) mixed with lactose powder. Subjects were instructed to inhale the mixture through a 5 cm straw within 1 min. Cocaine kinetics, after intravenous injection, conform to a one‐compartment open model with first‐order elimination. After intranasal administration, cocaine kinetics conform to a one‐compartment model with first‐order absorpton and first‐order elimination. The mean half‐life of cocaine for intravenous injection in four subjects was 41·4±8·2 min (mean ± S.E.M.) and the range was 19 to 64min. There were statistically significant differences in the mean area under the concentration‐time curve (AUC) following intravenous and intranasal administration. The AUC was dose‐dependent and the fraction of the dose absorbed after 64mg intranasal cocaine was significantly lower than after 96 mg dose (p< 0·05).