高脂食物对氨茶碱控释片药代动力学的影响

本文采用荧光偏振免疫分析法,对6名健康受试者空腹或食用高脂早餐后立即服单剂量氨茶碱控释片的血药浓度进行测定,并计算其药代动力学参数。结果表明,高脂食物显著降低氮茶碱控释片的吸收速率,T_(max)从空腹状态下的3.53±0.44h上升至6.54±2.08h(p<0.01),AUC_0→∞增加20％,但无显著差异(p>0.05)。两组的C_(max)、Ke、t_(1/2)和CL没有明显改变。提示高脂肪食物能延缓氨茶碱控释片的吸收,不影响其体内代谢过程和吸收量。由于起效时间减慢,可能会影响临床治疗效果。

The Influence of High Fat Diet on the Pharmacokinetics of Controlled Release Aminophylline Tablets

The effect of high fat diet on the pharmacokinetics of theophylline from controlled release aminophylline tablets has been observed in six healthy volunteers. The drug was administrated in single oral doses (400mg)after an overnight fast or immediately after the consumption of a high fat breakfast in an autocontrol study. Serum theophylline levels were measured by fluorescence polarization immunoassay. The absorption of theophylline was markedly delayed by high fat diet with significant difference in I_(max) (3.53±0.44h vs 6.54±2.08h, p<0.01). Food ingestion did not significantly affect C_(max), AUC and CL,so it had no obvious effect on the extent of drug absorption or its metabolism. It is considered that high fat diet may influence the theapeutie efficacy of controlled release aminophylline tablets due to a delay in the time of maximum theophylline plasma concentration.