Chrzanowski F A, Niebergall P J, Mayock R L, Taubin J M, Sugita E T
Clin Pharmacol Ther. 1977 Aug;22(2):188-95. doi: 10.1002/cpt1977222188.
The pharmacokinetics of theophylline was studied in 6 normal, nonsmoking, adult male volunteers. A constant-rate intravenous infusion of 3.84 to 4.98 mg/kg of theophylline (as the ethylenediamine salt, aminophylline) was administered over 40 min. Serum theophylline concentrations were measured for 24 hr by means of a gas chromatographic method specific for theophylline. Within 30 min of an average intravenous dose of 4.4 mg/kg of theophylline, serum levels reached 10 microgram/ml. The highest serum level at the end of the infusion was 17 microgram/ml. The serum concentration-time data were fitted to a two-compartment open model and yielded a mean serum half-life (t1/2) of 11.02 hr, a value longer than those previously reported. Our results indicated that after the original loading dose of 4.4 mg/kg was infused for 40min, an immediate infusion rate of 1.40 mg/kg/hr (1.65 mg/kg/hr aminophylline) would be necessary to maintain a serum level of 10 microgram/ml.
在6名正常、不吸烟的成年男性志愿者中研究了茶碱的药代动力学。以3.84至4.98毫克/千克的茶碱（以乙二胺盐，即氨茶碱形式）进行40分钟的恒速静脉输注。通过一种针对茶碱的气相色谱法测量血清茶碱浓度达24小时。在平均静脉注射剂量为4.4毫克/千克茶碱后的30分钟内，血清水平达到10微克/毫升。输注结束时的最高血清水平为17微克/毫升。血清浓度 - 时间数据拟合为二室开放模型，得出平均血清半衰期（t1/2）为11.02小时，该值比先前报道的要长。我们的结果表明，在最初40分钟输注4.4毫克/千克的负荷剂量后，需要立即以1.40毫克/千克/小时（1.65毫克/千克/小时氨茶碱）的输注速率来维持10微克/毫升的血清水平。
