Highly variable mycophenolate mofetil bioavailability following nonmyeloablative hematopoietic cell transplantation
Highly variable mycophenolate mofetil bioavailability following nonmyeloablative hematopoietic cell transplantation
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DOI：
10.1177/0091270006295064
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发表时间：
2007-01-01
影响因子：
2.9
通讯作者：
Weisdorf, Daniel
中科院分区：
文献类型：
--
作者：
Jacobson, Pamala;Green, Kathleen;Weisdorf, Daniel
本研究测定了接受非清髓性造血细胞移植的患者口服霉酚酸（霉酚酸酯的活性代谢产物）的生物利用度。18名成年人接受准备方案含有氟达拉滨，环磷酰胺，全身照射进行了研究。免疫抑制包括环孢素和霉酚酸酯1g，每日两次。静脉和口服给药后的药代动力学变异性较高。静脉给药导致曲线下面积（AUC）中位数为28.3 μ g（.）h/mL（范围，9.96-70.4）和口服AUC（0-12）为16.7 μ g（.）h/mL（范围，9.38-35.3）。静脉和经口给药后的C-max分别为12.18和5.29 μ g/mL。中位口服生物利用度为72.3%（20.5%-172%），变异性为8倍。5例患者（28%）的口服生物利用度
This study determined the oral bioavailability of mycophenolic acid, the active metabolite of mycophenolate mofetil, in patients undergoing nonmyeloablative hematopoietic cell transplantation. Eighteen adults receiving a preparative regimen containing fludarabine, cyclophosphamide, and total body irradiation were studied. Immune suppression consisted of cyclosporine and mycophenolate 1 g twice daily. Pharmacokinetic variability was high after intravenous and oral dosing. Intravenous dosing resulted in a median area under the curve (AUC) of 28.3 mu g(.)h/mL (range, 9.96-70.4) and an oral AUC(0-12) of 16.7 mu g(.)h/mL (range, 9.38-35.3). C-max after intravenous and oral dosing was 12.18 and 5.29 mu g/mL, respectively. The median oral bioavailability was 72.3% (20.5%-172%), with 8-fold variability. Five patients (28%) had an oral bioavailability