Huchon G J, Montgomery A B, Lipavsky A, Hoeffel J M, Murray J F
J Nucl Med. 1987 May;28(5):894-902.
To determine the influence of varying molecular weight (mol wt) on respiratory clearance of aerosolized solutes, we studied eight radiopharmaceuticals, each administered to four dogs: sodium 99mTc pertechnetate (TcO4), 99mTc glucoheptonate ([99mTc]GH), 51Cr-ethylenedinitrotetraacetate ([51Cr]EDTA), 99mTc diethylenetriaminepentaacetate ([99mTc] DTPA), 111In diethylenetriaminepentaacetate ([111In]DTPA), 67Ga desferoxaminemesylate ([67Ga]DFOM), 99mTc dextran ([99mTc]DX) and 111In transferrin ([111In]TF). After aerosolization (0.8 m MMD, 2.4 GSD), clearance was determined for 30 min and then corrected by intravenous injection for nonairspace radioactivity. In-TF clearance (0.11 +/- 0.10%/min) was lower than TcO4 (6.32 +/- 0.62%/min), [99mTc]GH (1.50 +/- 0.37%/min), [51Cr]EDTA (2.38 +/- 1.02%/min), [99mTc]DTPA (3.51 +/- 0.40%/min), [111In]DTPA (2.35 +/- 0.42%/min), [67Ga] DFOM (1.99 +/- 0.49%/min) and [99mTc]DX (1.81 +/- 0.75%/min) clearances (p less than 0.001). TcO4 clearance was higher than others (p less than 0.001). Technetium binding to DX was unsatisfactory; aerosolization caused unbinding from DTPA. We conclude that respiratory clearance of large mol wt solutes within 30 min is negligible and, that clearance of molecules between 347-5,099 daltons differs greatly, suggesting that binding and/or intrapulmonary retention affect transfer.
为了确定不同分子量对雾化溶质经呼吸道清除的影响，我们研究了8种放射性药物，每种药物对4只犬进行给药：高锝[99mTc]酸钠（TcO4）、葡庚糖酸[99mTc]（[99mTc]GH）、乙二胺四乙酸[51Cr]（[51Cr]EDTA）、二乙三胺五乙酸[99mTc]（[99mTc]DTPA）、二乙三胺五乙酸[111In]（[111In]DTPA）、甲磺酸去铁胺[67Ga]（[67Ga]DFOM）、葡聚糖[99mTc]（[99mTc]DX）和转铁蛋白[111In]（[111In]TF）。雾化后（平均质量直径0.8μm，几何标准差2.4），测定30分钟的清除率，然后通过静脉注射校正非肺泡放射性。铟标记的转铁蛋白（[111In]TF）清除率（0.11±0.10%/分钟）低于高锝酸钠（TcO4，6.32±0.62%/分钟）、葡庚糖酸[99mTc]（[99mTc]GH，1.50±0.37%/分钟）、乙二胺四乙酸[51Cr]（[51Cr]EDTA，2.38±1.02%/分钟）、二乙三胺五乙酸[99mTc]（[99mTc]DTPA，3.51±0.40%/分钟）、二乙三胺五乙酸[111In]（[111In]DTPA，2.35±0.42%/分钟）、甲磺酸去铁胺[67Ga]（[67Ga]DFOM，1.99±0.49%/分钟）和葡聚糖[99mTc]（[99mTc]DX，1.81±0.75%/分钟）的清除率（p<0.001）。高锝酸钠（TcO4）清除率高于其他药物（p<0.001）。锝与葡聚糖（DX）的结合不理想；雾化导致其与二乙三胺五乙酸（DTPA）解离。我们得出结论，30分钟内大分子溶质的经呼吸道清除可以忽略不计，并且分子量在347 - 5099道尔顿之间的分子清除率差异很大，这表明结合和/或肺内潴留影响转运。
