相对生物利用度研究triflusal口服溶液与triflusal胶囊在健康受试者。一个单一的、随机的、双向交叉、开放的第一阶段研究。

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Izquierdo我哈J·罗维拉年代,Pelagio P,托雷斯F, Cebrecos J, Garcia-Rafanell J

相对生物利用度研究triflusal口服溶液与triflusal胶囊在健康受试者。一个单一的、随机的、双向交叉、开放的第一阶段研究。

Arzneimittelforschung。2010; 60 (1): 36-41。doi: 10.1055 / s - 0031 - 1296246。

PubMed ID

20184225 (在PubMed

]

文摘

Triflusal (ca 322-79-2)是一个不可逆转的抗血小板剂乙醯化环氧酶同种型1 (COX-1),因此抑制凝血恶烷生物合成。的主要代谢物triflusal, 2-hydroxy-4-trifluoromethyl苯甲酸(HTB),还拥有antiaggregant活动。最近一个新的口服600毫克(10毫升)解决方案的形式triflusal已经发达。本临床试验的目的是研究新的口服溶液的相对生物利用度triflusal与胶囊的配方,同时管理单剂量。这是一个随机、双向、交叉、非盲,单第一阶段临床试验,在24个健康志愿者接受triflusal一样600毫克口服溶液和两个300毫克胶囊在一个单一的政府被冲刷段至少17天。血液样本收集和HTB测定血浆浓度。药代动力学参数用于生物等效性评价包括AUC (0-t), AUC (0-inf)和Cmax。配方被认为bioequivalent如果AUC的几何平均比率(0-t), AUC (0-inf)和Cmax在预先确定的等效范围内(80%到125%)。耐受性是基于不良事件的记录(AEs)、体格检查、心电图(ECG)和实验室测试。生物等效性的参数,意味着(SD)值如下:AUC (0-t) (microg x h /毫升):3574.08 (628.17)triflusal口服溶液和3901.78 [698.43]triflusal胶囊; AUC(0-infinity) (microg x h/ml): 4089.21 [842.54] for triflusal oral solution and 4471.33 [905.93] for triflusal capsules; Cmax, (microg/ml): 91.24 [12.88] for triflusal oral solution and 88.61 [13.46] for triflusal capsules; Cmax/AUC(0-infinity) (h(-1)): 0.03 (0.00) for triflusal oral solution and 0.02 (0.00) for triflusal capsules. The 90% confidence intervals for the ratio experimental/control by analysis of variance after log transformed AUC(0-infinity), AUC(0-t), and Cmax were within 80% to 125%. Similar results were found for the data without log transformation. All adverse events were of mild or moderate intensity and all subjects recovered. Nine and 12 subjects reported at least one adverse event during treatment with triflusal oral solution and with triflusal capsules, respectively. The most frequently reported adverse events were headache and dizziness. It was concluded that the 600-mg solution of triflusal appeared to be bioequivalent to the reference formulation capsules. Both formulations were well tolerated.

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药物

Triflusal