Sioufi A, Sandrenan N, Godbillon J, Trunet P, Czendlik C, Howald H, Pfister C, Ezzet F
Laboratoires Ciba-Geigy, Bioanalytics and Pharmacokinetics, Medical Department, Rueil-Malmaison, France.
Biopharm Drug Dispos. 1997 Aug;18(6):489-97. doi: 10.1002/(sici)1099-081x(199708)18:6<489::aid-bdd36>3.0.co;2-p.
Letrozole is a new non-steroidal inhibitor of the aromatase enzyme system. It is currently under development for the treatment of postmenopausal women with advanced breast cancer. To investigate the influence of food on the bioavailability of letrozole, 12 healthy male volunteers were treated under fed and fasted conditions with single oral doses of 2.5 mg letrozole in film-coated tablets. Plasma concentration profiles were determined. No significant difference in the extent of absorption (AUC or AUC0-8 h) was observed between the two treatments but the rate of letrozole absorption decreased slightly under fed conditions. However, in view of the half-life of about 2 d this small change in the absorption rate is not considered to be of clinical relevance for treatment with repeated administrations.
来曲唑是一种新型非甾体类芳香化酶系统抑制剂。目前正在研发用于治疗绝经后晚期乳腺癌女性。为研究食物对来曲唑生物利用度的影响，12名健康男性志愿者在进食和空腹条件下接受单剂量口服2.5mg薄膜包衣片来曲唑治疗。测定血浆浓度曲线。两种治疗之间在吸收程度（AUC或AUC0 - 8小时）方面未观察到显著差异，但来曲唑在进食条件下的吸收速率略有下降。然而，鉴于半衰期约为2天，这种吸收速率的微小变化在重复给药治疗中不被认为具有临床相关性。
