Simons K J, Simons F E
J Pharm Sci. 1979 Oct;68(10):1327-9. doi: 10.1002/jps.2600681038.
The pharmacokinetics and urinary excretion of a single dyphylline dose were studied in five normal volunteers. The mean dyphylline half-life was 1.8 +/- 0.2 hr; the mean total body clearance rate and mean renal clearance rate were 333 +/- 62 and 276 +/- 52 ml/min, respectively; and the mean volume of distribution was 0.8 +/- 0.2 liter/kg. In the urine, 83 +/- 5% of the dose was excreted as unchanged drug, and theophylline was not detected. Dyphylline doses of 19--27 mg/kg, resulting in peak serum dyphylline concentrations of 19.3--23.5 micrograms/ml, were tolerated well by four subjects. One subject had a severe headache following a 28-mg/kg dose, associated with a peak serum dyphylline concentration of 36.4 micrograms/ml. This study confirms speculation that dyphylline is not metabolized to theophylline in vivo.
在五名正常志愿者中研究了单剂量二羟丙茶碱的药代动力学和尿排泄情况。二羟丙茶碱的平均半衰期为1.8±0.2小时；平均全身清除率和平均肾清除率分别为333±62和276±52毫升/分钟；平均分布容积为0.8±0.2升/千克。在尿液中，83±5%的剂量以原形药物排泄，未检测到茶碱。19至27毫克/千克的二羟丙茶碱剂量使血清二羟丙茶碱峰值浓度达到19.3至23.5微克/毫升，四名受试者耐受性良好。一名受试者在接受28毫克/千克剂量后出现严重头痛，血清二羟丙茶碱峰值浓度为36.4微克/毫升。本研究证实了二羟丙茶碱在体内不会代谢为茶碱的推测。
