Everard M L, Devadason S G, Sunderland V B, Le Souef P N
Department of Respiratory Medicine, Princess Margaret Hospital for Children, Perth, Western Australia.
Thorax. 1995 May;50(5):517-9. doi: 10.1136/thx.50.5.517.
The advent of novel treatments such as aerosolized amiloride are potentially useful additions to the therapeutic options available for the treatment of cystic fibrosis. Unfortunately, amiloride and other aerosolized drugs such as antibiotics are generally administered via jet nebulisers which are time consuming to use, and thus limit the acceptance and efficacy of these forms of treatment. In vitro experiments were performed in order to determine whether amiloride could be administered in dry powder form using a Turbohaler.
Amiloride was micronised and loaded into 200 micrograms Turbohalers. The dose delivered per actuation and particle size distribution of the generated aerosol were assessed using a flow of 60 l/min through the Turbohaler. The dose of amiloride delivered was measured by collecting the aerosol on a filter and the quantity of drug was assayed by an ultraviolet spectrophotometric method. The particle size distribution was assessed using a Malvern MasterSizer laser particle sizer and compared with that generated by a commercially available 200 micrograms budesonide Turbohaler.
The mean (SD) dose delivered per actuation was 246.3 (40.4) micrograms. The volume median diameter of the amiloride aerosol was 3.80 (0.68) micron compared with 3.07 (1.47) microns for budesonide.
These results suggest that therapeutic doses of micronised amiloride could be delivered effectively and conveniently as a dry powder aerosol using a Turbohaler.
诸如雾化阿米洛利等新型治疗方法的出现，可能为囊性纤维化的治疗提供了更多潜在的治疗选择。不幸的是，阿米洛利和其他雾化药物（如抗生素）通常通过喷射式雾化器给药，使用起来耗时较长，因此限制了这些治疗方式的接受度和疗效。为了确定阿米洛利是否可以使用都保以干粉形式给药，进行了体外实验。
将阿米洛利微粉化并装入200微克的都保中。通过都保以60升/分钟的流速评估每次按压所递送的剂量以及所产生气雾剂的粒径分布。通过将气雾剂收集在滤器上测量所递送的阿米洛利剂量，并通过紫外分光光度法测定药物量。使用马尔文MasterSizer激光粒度分析仪评估粒径分布，并与市售的200微克布地奈德都保所产生的粒径分布进行比较。
每次按压所递送的平均（标准差）剂量为246.3（40.4）微克。阿米洛利气雾剂的体积中值直径为3.80（0.68）微米，而布地奈德为3.07（1.47）微米。
这些结果表明，使用都保可以将微粉化阿米洛利的治疗剂量有效地且方便地作为干粉气雾剂递送。
