Asade R H, Prizont L, Muiño J P, Tessler J
Dto. Médico, Lab. Datsa S.A., Buenos Aires, Argentina.
Cancer Chemother Pharmacol. 1991;27(5):401-5. doi: 10.1007/BF00688866.
A bioavailability study of randomized cross-over design was carried out in eight volunteers who were given a 48-h flutamide treatment consisting of 250-mg tablets three times daily or 400-mg sustained-release tablets twice daily, followed 3 weeks later by the alternative dosage form. Just before the last dose and 15 times during the subsequent 24 h, blood samples were obtained for the determination of plasma hydroxyflutamide (the active metabolite of flutamide) levels by high-performance liquid chromatography. No statistically significant differences between the two dosage forms were found for the lag time, rate of initial increase in concentration, peak plasma concentration, mean hydroxyflutamide concentration within one dosing interval or 24-h AUC value. One subject presented mild and transient nausea during both treatment periods. After the first treatment period (250-mg tablets), an increase in serum bilirubin was observed in another volunteer, who was withdrawn from the study. It may be concluded that both dosage forms were bioequivalent.
对8名志愿者进行了随机交叉设计的生物利用度研究，这些志愿者接受了为期48小时的氟他胺治疗，治疗方案为每日3次服用250毫克片剂或每日2次服用400毫克缓释片剂，3周后服用另一种剂型。在最后一剂之前以及随后24小时内的15个时间点采集血样，通过高效液相色谱法测定血浆羟基氟他胺（氟他胺的活性代谢产物）水平。两种剂型在滞后时间、浓度初始增加速率、血浆峰浓度、一个给药间隔内的平均羟基氟他胺浓度或24小时AUC值方面均未发现统计学上的显著差异。一名受试者在两个治疗期均出现轻度短暂恶心。在第一个治疗期（250毫克片剂）后，另一名志愿者血清胆红素升高，该志愿者退出了研究。可以得出结论，两种剂型生物等效。
