Aaes-Jørgensen T, Liedholm H, Melander A
Department of Biochemistry, H. Lundbeck A/S, Copenhagen, Denmark.
Drug Nutr Interact. 1987;5(3):157-60.
The single-dose kinetics of the neuroleptic thioxanthene zuclopenthixol was assessed in 12 healthy volunteers who ingested 10 mg of the drug orally, both on an empty stomach and together with a standardized breakfast of 1840 kj (440 kcal). The serum concentrations of zuclopenthixol were measured by HPLC. Concomitant food intake did not influence the peak concentration nor the time to reach the peak concentration or the elimination half-life of zuclopenthixol, but the AUC values were significantly increased. Hence it seems likely that concomitant food intake enhances the bioavailability of zuclopenthixol, without influencing its absorption rate. The most likely mechanism is that food reduces the presystemic clearance of the drug. As the increase in AUC was only 26%, it is doubtful whether zuclopenthixol has to be administered in a standardized relation to meals.
在12名健康志愿者中评估了抗精神病药硫杂蒽类珠氯噻醇的单剂量动力学，这些志愿者分别在空腹状态下以及与一份能量为1840千焦（440千卡）的标准早餐一起口服10毫克该药物。通过高效液相色谱法测定珠氯噻醇的血清浓度。同时摄入食物既不影响珠氯噻醇的峰值浓度，也不影响达到峰值浓度的时间或消除半衰期，但曲线下面积值显著增加。因此，同时摄入食物似乎有可能提高珠氯噻醇的生物利用度，而不影响其吸收速率。最可能的机制是食物降低了该药物的首过清除率。由于曲线下面积的增加仅为26%，珠氯噻醇是否必须与进餐保持标准化的给药关系值得怀疑。
