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首页> 外文期刊>Investigative radiology >Gadocoletic acid trisodium salt (b22956/1): a new blood pool magnetic resonance contrast agent with application in coronary angiography.
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Gadocoletic acid trisodium salt (b22956/1): a new blood pool magnetic resonance contrast agent with application in coronary angiography.

机译：ado酸三钠盐（b22956 / 1）：一种新型血池磁共振造影剂，在冠状动脉造影中得到应用。

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RATIONALE AND OBJECTIVES: Inversion recovery, three-dimensional, gradient-recalled echo magnetic resonance coronary angiography (IR-3D-GRE-MRCA), performed after administration of an intravascular T1-relaxing agent with prolonged permanence in the blood, is one of the most promising approaches to noninvasive magnetic resonance imaging (MRI) of the coronaries. The aim of the present study was the evaluation of the physicochemical properties in solution, pharmacokinetics, elimination from the body, protein binding, and signal enhancement characteristics of gadocoletic acid trisodium salt (B22956/1), a candidate gadolinium-based MRI contrast agent for coronary angiography. METHODS: The pharmacokinetics and elimination from the body of gadocoletate ion, the contrastographically active component of gadocoletic acid trisodium salt, was evaluated after intravenous administration in rats and monkeys, using for assays high-performance liquid chromatography, x-ray fluorescence, and inductively coupled plasma atomic emission spectrometry. The binding of the gadocoletate ion to animal and human serum albumin was studied by means of ultrafiltration. The imaging properties of blood outside coronary arteries after contrast agent administration were evaluated in cynomolgus monkeys (Macaca fascicularis) by measuring aortic signal-to-noise and contrast-to-noise ratios in lower body angiograms. The suitability of gadocoletic acid trisodium salt for achieving contrast-enhanced magnetic resonance coronary angiography (ceMRCA) was tested in Yucatan micropigs with an IR-3D-GRE sequence. All in vivo relaxation rate measurement and images were obtained using a 1.5 T Siemens Symphony scanner. RESULTS: The fractional binding of gadocoletate ion at a concentration of 0.5 mM to serum albumin at the physiological concentration was 95%, 92%, 88%, and 86% for human, monkey, pig, and rat, respectively. In rats and monkeys, gadocoletate ion was excreted unmetabolized through the biliary and urinary routes. It was recovered with feces depending on the injected dose in percentages from 18% to 97%, providing evidence for a saturable biliary pathway. Plasma pharmacokinetics showed the complete elimination of gadocoletate ion within 24 hours after administration. In the monkey, the gadocoletate ion showed the pharmacokinetic behavior of a compound with partial vascular confinement and long plasma half-life, which may be ascribed to elevated binding to serum albumin. These properties manifested themselves in lower body angiograms with excellent image contrast between vessels and muscle. The slowly decaying aortic blood signal-to-noise and contrast-to-noise ratios over a 15-minute period is expected to allow 3-dimensional coronary angiography. The potential of gadocoletic acid trisodium salt for ceMRCA was also demonstrated in Yucatan micropigs. Elevated blood signal intensity and almost total myocardial signal suppression was maintained for almost 1 hour after administration, ie, for much longer than expected to be necessary for coronary angiography. During the whole period high resolution images of the right coronary artery could be obtained. CONCLUSIONS: On the basis of the pharmacokinetic profile and imaging characteristics, gadocoletic acid trisodium salt shows promise as a MR contrast agent for coronary angiography.
机译：理由和目的：倒置恢复，三维梯度回波磁共振冠状动脉造影（IR-3D-GRE-MRCA）是在血液中长期服用血管内T1松弛剂后进行的一项手术，冠状动脉的无创磁共振成像（MRI）的最有前途的方法。本研究的目的是评估solution基三乙酸钠盐（B22956 / 1）的溶液的理化性质，药代动力学，从体内清除，蛋白质结合以及信号增强特性，这是一种基于g的MRI造影剂，用于冠状动脉造影。方法：在大鼠和猴子中静脉内给药后，评估了ado酸三钠盐的造影活性成分g糖酸根离子的药代动力学和从体内的消除，使用高效液相色谱，X射线荧光和感应耦合进行测定等离子体原子发射光谱法。通过超滤研究了ado糖离子与动物和人血清白蛋白的结合。在食蟹猴（猕猴）中，通过测量下肢血管造影的主动脉信噪比和对比噪声比，评估了对比剂给药后冠状动脉外血液的成像特性。在带有IR-3D-GRE序列的尤卡坦微型猪中，测试了ado酸三钠盐对实现对比增强磁共振冠状动脉造影（ceMRCA）的适用性。使用1.5 T Siemens Symphony扫描仪获得所有体内弛豫率测量值和图像。结果：在生理浓度下，浓度为0.5 mM的gadocoletate离子与血清白蛋白的结合分数对于人，猴，猪和大鼠分别为95％，92％，88％和86％。在大鼠和猴子中，g胆酸离子通过胆汁和尿液途径被代谢而未代谢。根据注射剂量（从18％到97％的百分比），粪便可以回收它，为胆道的饱和提供了证据。血浆药代动力学显示，给药后24小时内完全消除了葡萄糖酸根离子。在猴子中，gadocoletate离子显示出具有部分血管限制和长血浆半衰期的化合物的药代动力学行为，这可能归因于与血清白蛋白结合的增加。这些特性在下肢血管造影中表现出来，在血管和肌肉之间具有出色的图像对比度。在15分钟内，主动脉血的信噪比和对比噪声比逐渐下降，有望进行3维冠状动脉造影。 Yu碳酸钠三钠盐对ceMRCA的潜力在尤卡坦微型猪中也得到了证实。给药后将近1小时维持血液信号强度升高和几乎完全的心肌信号抑制，即，比冠状动脉造影所需的时间长得多。在整个期间，可以获得右冠状动脉的高分辨率图像。结论：基于药代动力学特征和影像学特征，g乙酸三钠盐有望作为冠状动脉造影的MR造影剂。

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