Köhler D
Fachkrankenhaus Kloster Grafschaft, Schmallenberg, Federal Republic of Germany.
Lung. 1990;168 Suppl(Suppl 1):677-84. doi: 10.1007/BF02718194.
The development of a new group of drugs (polypeptides) have recently increased the interest of alternative administration to the enteral route because of its proteolytic activity and the catabolism of the "first-pass effect." Aside from the "needle," the administration in the respiratory tract via aerosol is the method with the best efficiency. But several problems prohibited its spreading: (1) the accuracy and the reproducibility of the inhaled dose (range ca. 1:4); (2) the small amount of inhaled drug in relation to the dose in the aerosol delivery system (range ca. 1%-10%); (3) the fear of allergic reactions of the respiratory system; (4) the variability of the drug transport into the systemic circulation. New approaches and data raise hopes in reducing the problems: (1) aerosol delivery systems with defined particle spectrum and storage systems; slow vital capacity inhaling maneuver; (2) delivery systems that nebulizes nearly the total amount of drug; (3) all studies with the inhalation application of insulin, heparin, ergotamin, ribavirin, aminoglycosides, and "cigarette smoke" do not reveal any relevant allergic reaction; (4) many studies were performed in the last 10 years on the influence of substances and especially of diseases on the transport of molecules through the respiratory tract. Only a few of them are relevant (exogen allergic alveolitis, active sarcoidosis, active smoking). Aerosols for (exogen allergic alveolitis, active sarcoidosis, active smoking). Aerosols for systemic drug treatment seems to be a gained alternative to the "syringe."
由于其蛋白水解活性和“首过效应”的分解代谢,一组新型药物(多肽)的研发最近增加了人们对肠外给药途径的兴趣。除了“注射针剂”外,通过气雾剂经呼吸道给药是效率最高的方法。但有几个问题阻碍了它的推广:(1)吸入剂量的准确性和可重复性(范围约为1:4);(2)与气雾剂输送系统中的剂量相比,吸入药物的量较少(范围约为1%-10%);(3)对呼吸系统过敏反应的担忧;(4)药物进入体循环的变异性。新的方法和数据为减少这些问题带来了希望:(1)具有确定粒径谱的气雾剂输送系统和储存系统;慢肺活量吸入动作;(2)能雾化几乎全部药物量的输送系统;(3)所有关于胰岛素、肝素、麦角胺、利巴韦林、氨基糖苷类药物和“香烟烟雾”吸入应用的研究均未发现任何相关的过敏反应;(4)在过去10年里进行了许多关于物质尤其是疾病对分子通过呼吸道转运影响的研究。其中只有少数是相关的(外源性过敏性肺泡炎、活动性结节病、主动吸烟)。用于(外源性过敏性肺泡炎、活动性结节病、主动吸烟)的气雾剂。用于全身药物治疗的气雾剂似乎是“注射器”之外的一种可行选择。