頁籤選單縮合
題名 | Preclinical Evaluation of Fe-(5-C[feaf]H忦-EHPG)-as a Contrast Agent in MR Imaging of Hepatobiliary System=肝膽磁振造影對比劑Fe-(5-C[feaf]H忦-EHPG)-臨床前之評估 |
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作者姓名(中文) | 許瑞昇; 劉金昌; 王雲銘; 趙垂勳; 陳小鳴; 郭禹廷; | 書刊名 | The Kaohsiung Journal of Medical Sciences |
卷期 | 13:2 1997.02[民86.02] |
頁次 | 頁75-85 |
分類號 | 414.93 |
關鍵詞 | 肝膽磁振造影對比劑; MRI; Contrast media; Hepatobiliary system; |
語文 | 英文(English) |
中文摘要 | Iron(III)-N,N’-ethylenebis[2-(2-hydrox-5-phenyl)glycine][Fe-(5-C2H5-EHPG)¯]是一種專為肝膽系統而設計的順磁性肝膽磁振造影對比劑。Fe-(5-C2H5-EHPG)¯其急性耐受毒性半致死劑量 (LD50) 達3.49mmol/kg。注射標幟同位素111In -(5-C2H5-EHPG)¯ 10分鐘,30分鐘及60分鐘之肝臟生物體分佈分為4.78±0.97, 5.34±0.91, 4.53±0.35 (%ID) 或0.88±0.18, 0.99±0.17, 0.84±0.0 6(% ID/gm);血液為5.78±0.15, 5.75±0.15, 4.00±0.04 (%ID),或0.49±0.03, 0.49±0.05, 0.34±0.0 1 (%ID/gm);及腎臟為1.27±0.91, 1.46±1.00, 1.52±0.46 (%ID),或0.89±0.17, 1.02±0.18, 1.06±0.08 (%ID/gm)。而動物磁振造影術發肝臟顯影於注射Fe-(5-C2H5-EHPG)¯ 後30分鐘達到最大顯影。控制組,膽道結紮16小時,一週及四週,和急性肝炎實驗組之顯影百分比分別為42.09%±3.59%,17.26%±6.6%,19.80±6.46%,32.20±9.01%及16.50%±4.02%可持續顯影達到60分鐘,且在22小時內恢復至顯影前的基準訊號。此外,同時發現總膽管於注射對比劑10-15分後產生顯影,以上結果證實Fe-(5-C2H5-EHPG) ¯ 可被肝細胞攝入,膽道排除,且能提供足夠的頭磁性以使肝臟顯影。不過肝臟機能障礙會影響Fe-(5-C2H5-EHPG)¯ 的顯影效果,此時仍然能由腎臟排泄,即使肝臟機能障礙仍能排出體外,不會滯留體內。整體而言,Fe-(5-C2H5-EHPG)¯仍不失為具有潛力的肝膽磁振造影對比劑。 |
英文摘要 | Iron(III)-N,N’-ethylenebis[2-(2-hydrox-5-phenyl)glycine][Fe-(5-C2H5-EHPG)¯] is a paramagnetic omplex designed for use as a hepatobiliary agent. Test procedures included synthesis, characterization, toxicity evaluation, biodistribution and experiments for animal MR images. The dose of LD50 in acute toxicity test of Fe-(5-C2H5-EHPG)¯ in mice was 3.49mmol/kg. 111 IN-(5-C2H5-EHPG)¯ biodistribution studies relealed that the activities were (4.78±0.97, 5.34±0.91, 4.53±0.35)%ID and (0.88±0.18, 0.99±0.17, 0.84±0.06)% ID/gm in the liver at time intervals of 10, 30 and 60 minutes after injection; (5.76±0.15, 5.75±0.15, 4.00±0.04)%ID and (0.49±0.03, 0.49±0.05, 0.34±0.01)%ID/gm in the blood;(1.27±0.91, 1.46±1.00, 1.52±0.46)%ID and (0.89±0.17, 1.02±0.18, 1.06±0.08)%ID/gm in the kidneys, respectively. The results of image enhancement correlated well to the biodistribution. Analysis of the MR images showed degrees of maximal parenchymal % increase of signal to noise ratio (S/N) was 42.09 ±3.59% for normal liver at 30 minutes postinjection, which exceeded the value of pathologic liver with bile duct obstruction 16 hours 17.26±6.6%, 1 week 19.80±6.46% and 4 weeks 32.3±9.01%, respectively, and acute hepatitis 16.5%±4.02%. Persistent enhancement plateau was documented up to 60 minutes after injection and normalized to precontrast value within 22 hours. The common duct was opacified at 10-15 minutes after injection of contrast agent. These results indicated that the Fe-(5-C2H5-EHPG)¯ could be rapidly extracted from the blood stream by the hepatocytes and excreted into the bile duct. The initial evaluation of Fe-(5-C2H5-EHPG)¯ demonstrated that Fe-(5-C2H5-EHPG)¯ was well suited for enhancement of normal liver parenchyma and was compromised with deterioration of liver function. However, the increase of the liver intensities in the animal model of the total biliary obstruction group normalized to precontrast value within 22 hours, which indicated that renal clearance as an effective alternative pathway for biliary excretion. In conclusion, thes results indicate that Fe-(5-C2H5-EHPG)¯ has the potential of becoming a safe and reliable magnetopharmaceutical for the hepatobiliary system. |
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