Smith R M, Spragg R G
Department of Medicine, University of California, San Diego.
Am J Med. 1988 Jun 24;84(6A):48-51. doi: 10.1016/0002-9343(88)90158-1.
The feasibility of aerosol administration of alpha-1-proteinase inhibitor (human) (A1PI) was assessed. Of three different methods of aerosolizing A1PI that were evaluated, an ultrasonic nebulizer was found to be best suited to the present purpose, producing particles of a size that allowed them to reach the distal air spaces of the lung and that retained specific A1PI anti-elastase activity. Administration of 20 mg/kg of A1PI and 150 microCi of 131iodine-A1PI to three dogs was accomplished without complications. Gamma camera scans documented a relatively homogenous distribution throughout the lungs. Bronchial lavage fluid that was recovered from the lungs of the dogs six hours after administration contained large amounts of human A1PI and showed a proportional elevation of anti-elastase activity. There was no evidence of acute toxicity.
评估了雾化吸入α-1-蛋白酶抑制剂（人）（A1PI）的可行性。在评估的三种不同雾化A1PI的方法中，发现超声雾化器最适合当前目的，产生的颗粒大小能够使其到达肺的远端气腔，并保留特定的A1PI抗弹性蛋白酶活性。给三只狗施用20mg/kg的A1PI和150μCi的131碘-A1PI，未出现并发症。γ相机扫描记录了在整个肺部相对均匀的分布。给药六小时后从狗肺中回收的支气管灌洗液含有大量人A1PI，并显示抗弹性蛋白酶活性成比例升高。没有急性毒性的证据。
