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健康志愿者中锰福地吡三钠的磁共振成像特性及药代动力学

MR imaging properties and pharmacokinetics of MnDPDP in healthy volunteers.

作者信息

Wang C, Gordon P B, Hustvedt S O, Grant D, Sterud A T, Martinsen I, Ahlström H, Hemmingsson A

机构信息

Department of Diagnostic Radiology, University Hospital, Uppsala, Sweden.

出版信息

Acta Radiol. 1997 Jul;38(4 Pt 2):665-76. doi: 10.1080/02841859709172399.

Abstract

PURPOSE

Thirteen male volunteers were studied to evaluate the MR imaging properties and pharmacokinetics of 10 mM mangafodipir trisodium infusion (MnDPDP, Teslascan).

MATERIAL AND METHODS

Doses of 5 and 10 mumol/kg b.w. were administered by bolus injection (< 1 min) to 5 subjects, and by infusion (20 min) to 8 subjects, with a 3-week wash-out between doses. Infusion subjects underwent MR imaging.

RESULTS

At 1 h after infusion, the plasma concentration of Mn was reduced to approximately 15% of the maximum value. Fifteen to 20% of Mn was recovered in the urine, and 50-60% was recovered in the faeces. The rapid initial plasma clearance of Mn is consistent with both rapid tissue uptake and rapid renal elimination. Increases in signal intensity were apparent on T1-weighted images of the liver, pancreas, spleen, renal cortex and the renal medulla, but not in regions of the brain protected by an intact blood-brain barrier. Increases were seen in the choroid plexus and pituitary. Contrast-related adverse events, only flushing of moderate intensity, occurred in bolus injection subjects.

CONCLUSION

At 5 and 10 mumol/kg, mangafodipir produces relatively long-lasting enhancement of several abdominal organs, including the liver, pancreas and kidney.

摘要

目的

对13名男性志愿者进行研究,以评估10 mM三钠锰福地吡(MnDPDP,泰乐影)静脉输注的磁共振成像特性和药代动力学。

材料与方法

5名受试者接受5和10 μmol/kg体重的剂量静脉推注(<1分钟),8名受试者接受静脉输注(20分钟),两次给药之间有3周的洗脱期。接受输注的受试者进行磁共振成像。

结果

输注后1小时,血浆锰浓度降至最大值的约15%。15%至20%的锰从尿液中回收,50%至60%从粪便中回收。锰的快速初始血浆清除率与快速的组织摄取和快速的肾脏清除一致。在肝脏、胰腺、脾脏、肾皮质和肾髓质的T1加权图像上信号强度增加,但在血脑屏障完整的脑区未见增加。脉络丛和垂体有信号增强。静脉推注受试者出现与造影剂相关的不良事件,仅为中度脸红。

结论

在5和10 μmol/kg时,锰福地吡可使包括肝脏、胰腺和肾脏在内的多个腹部器官产生相对持久的强化。

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