药物动力学的西地那非在健康男性受试者:单剂量口服后绝对生物利用度、食物效应和剂量比例。

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尼科尔斯DJ, Muirhead GJ,利用农协

药物动力学的西地那非在健康男性受试者:单剂量口服后绝对生物利用度、食物效应和剂量比例。

Br中国新药杂志。2002;53增刊1:5S-12S。

PubMed ID

11879254 (在PubMed

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文摘

目的:确定绝对生物利用度、剂量比例和食品的药物动力学的影响单口服剂量枸橼酸西地那非。方法:三个非盲、随机交叉在健康男性受试者进行研究。绝对生物利用度是决定通过比较药代动力学数据经过政府的一次性口服给药和静脉注射50毫克剂量的西地那非(n = 12科目)。食物影响检查通过比较西地那非和其主要循环代谢物的药代动力学数据,英国- 103320,经过政府的单一口服100毫克剂量在禁食和美联储(n = 34科目)。剂量比例从获得药代动力学数据评估后管理四个单一口服剂量的西地那非(25、50、100和200毫克)32。西地那非的安全性和耐受性也在所有这些研究中评估。结果:计算绝对西地那非口服生物利用度为41%(90%置信区间CI: 36 - 47)。食物吸收的速度放缓,推迟意味着最高温度约1 h和Cmax减少29%(90%置信区间CI: 19 - 38)。评估的系统性风险,意味着血浆浓度——时间曲线下面积(AUC),降低了11%(90%置信区间CI: 6 - 16)。这些食物并不被认为是影响的临床意义。 There was statistical evidence of nonproportionality in Cmax and AUC over the dose range 25--200 mg. However the degree of nonproportionality was small, with predicted increases in Cmax and AUC of 2.2- and 2.1-fold, respectively, for a doubling in dose, and was thought to be clinically nonsignificant. Sildenafil was well tolerated in the three studies; the majority of adverse events were mild and transient. CONCLUSIONS: Sildenafil had a mean absolute bioavailability of 41%. Food caused small reductions in the rate and extent of systemic exposure; these reductions are unlikely to be of clinical significance. Across the dose range of 25--200 mg, systemic exposure increased in a slightly greater than dose-proportional manner.

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