绝对的口服生物利用度伐白色在健康成年男性志愿者。

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马丁PD,沃里克MJ,戴恩,布林德利C,短T

绝对的口服生物利用度伐白色在健康成年男性志愿者。

其他。2003年10月,25 (10):2553 - 63。

PubMed ID

14667956 (在PubMed

]

文摘

背景:伐是3-hydroxy-3-methylglutaryl辅酶A-reductase抑制剂治疗血脂异常的发展。临床试验的结果表明它是有效且耐受性良好。目的:本研究的目标是确定的绝对生物利用度口服剂量的伐和描述伐静脉药物动力学的健康志愿者。方法:这是一个随机、非盲、双向交叉研究组成的2天审判分离>或= 7天冲刷时期。健康成年男性志愿者都被赋予了一项单一的口服剂量的伐40毫克的审判的一天和静脉输液伐8毫克/ 4小时。药代动力学和耐受性评估进行了96小时后剂量。3-compartment药代动力学模型拟合获得的血浆浓度时间配置文件为每个志愿者在静脉给药。结果:十个白人男性志愿者进入,完成了试验。他们的平均年龄为35.7岁(范围、21-51年),他们的平均身高是177厘米(范围169 - 182 cm),以及他们的体重是77.6公斤(范围68 - 85公斤)。伐的绝对口服生物利用度约为20.1%,和肝提取比率约为0.63。 The mean volume of distribution at steady state was 134 L. Renal clearance accounted for approximately 28% of total plasma clearance (48.9 L/h). Single oral and intravenous doses of rosuvastatin were well tolerated in this small number of healthy male volunteers. CONCLUSIONS: The absolute oral bioavailability of rosuvastatin in these 10 healthy volunteers was approximately 20%, and absorption was estimated to be 50%. The volume of distribution at steady state was consistent with extensive distribution of rosuvastatin to the tissues. The modest absolute oral bioavailability and high hepatic extraction of rosuvastatin are consistent with first-pass uptake into the liver after oral dosing. Rosuvastatin was cleared by both renal and nonrenal routes; tubular secretion was the predominant renal process.

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药物

伐