代谢、排泄和药物动力学的伐在健康成年男性志愿者。

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马丁PD,沃里克MJ,戴恩,希尔SJ,贾尔斯PB,菲利普斯PJ,楞次E

代谢、排泄和药物动力学的伐在健康成年男性志愿者。

其他。2003年11月,25 (11):2822 - 35。

PubMed ID

14693307 (在PubMed

]

文摘

背景:伐是3-hydroxy-3-methylglutaryl辅酶A-reductase抑制剂,或他汀类药物,治疗血脂异常了。目的:本研究评估了代谢,排泄,药物动力学的一个口服剂量的放射性标记的伐([14 c]伐)在健康志愿者。方法:这是一个非随机、非盲,单日审判。健康的成年男性志愿者都被赋予了一项单一的口服剂量的[14 c]伐20毫克(20毫升[14 c]伐解决方案,名义上包含50 microCi放射性物质)。血液、尿液和粪便样本收集剂量后10天。耐受性进行了评估后10天剂量(试验完成)和试验的随访14天内完成。结果:六36 - 52岁的白人男性志愿者(意思是,43.7年)参加了审判。几何平均血浆浓度峰值(C (max))伐6.06 ng / mL,达到的平均剂量后5个小时。C (max),伐占大约50%的放射性物质循环。大约90%的普伐剂量在粪便回收,剩余的尿液中恢复过来。 The majority of the dose (approximately 70%) was recovered within 72 hours after dosing; excretion was complete by 10 days after dosing. Metabolite profiles in feces indicated that rosuvastatin was excreted largely unchanged (76.8% of the dose). Two metabolites-rosuvastatin-5S-lactone and N-desmethyl rosuvastatin-were present in excreta. [14C]-rosuvastatin was well tolerated; 2 volunteers reported 4 mild adverse events that resolved without treatment. CONCLUSIONS: The majority of the rosuvastatin dose was excreted unchanged. Given the absolute bioavailability (20%) and estimated absorption (approximately 50%) of rosuvastatin, this finding suggests that metabolism is a minor route of clearance for this agent.

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药物

伐