Placental transfer of rosiglitazone in the ex vivo human perfusion model
Placental transfer of rosiglitazone in the ex vivo human perfusion model
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DOI：
10.1016/j.ajog.2006.03.054
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发表时间：
2006-12-01
影响因子：
9.8
通讯作者：
Bawdon, Roger E.
中科院分区：
文献类型：
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作者：
Holmes, Heather J.;Casey, Brian M.;Bawdon, Roger E.
目的：利用体外人胎盘模型确定罗格列酮(文迪雅)经胎盘通过。研究设计：对10个足月、无并发症分娩的胎盘进行血流灌注研究。测试了8毫克口服剂量的典型浓度(216至692 ng/毫升)以及浓度增加2至3倍的浓度(734至1261 ng/毫升)。结果：低浓度和高浓度罗格列酮的清除指数分别为0.14+/-0.04和0.20+/-0.08，表明药物通过胎盘的速率较低。在8 mg剂量下，5个胎盘中只有1个胎盘出现胎儿蓄积(16.4 ng/mL，5%)，高浓度罗格列酮在0~74 ng/mL(5%~8%)的5个胎盘中，有2个胎盘发生胎儿蓄积。(C)2006 Mosby，Inc.保留所有权利。
Objective: The objective of the Study was to determine transplacental passage of rosiglitazone (Avandia) using the ex vivo human placental model.Study design: Perfusion Studies were performed on 10 placentas from term, uncomplicated deliveries. Concentrations typical for an 8-mg oral dose (216 to 692 ng/mL) as well as 2- to 3-fold increased concentrations were tested (734 to 1261 ng/mL). Transfer of rosiglitazone was assessed and accumulation was determined using the C-14-antipyrinc reference method.Results: The clearance index for low and high concentrations were 0.14 +/- 0.04 and 0.20 +/- 0.08, suggesting that the drug passes through the placenta at a relatively low rate. Fetal accumulation occurred in only 1 of 5 placentas Lit 16.4 ng/mL (5%) for the 8-mg dose and in 2 of 5 placentas ranging from 0 to 74 ng/mL (5% to 8%) at higher concentrations.Conclusion: There is minimal transfer and fetal accumulation of rosiglitazone according to the ex vivo human perfusion model. (c) 2006 Mosby, Inc. All rights reserved.