Radio Labelling of Drugs in a Metered Dose Inhaler (MDI) and Lung Deposition in Human Subjects

Journal of Aerosol Medicine-deposition Clearance and Effects in The Lung Pub Date : 1994-01-01 DOI:10.1089/JAM.1994.7.173

A. Hammermaier, A. Bidlingmaier, J. Waitzinger, R. Stechert, Harald Wenske, H. Jaeger

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引用次数: 4

Abstract

ABSTRACT The lung deposition (amount and distribution) of drugs from MDIs cannot be quantified using routine pharmacokinetic methods. A growing number of drugs from inhalers has been investigated in recent years using a radiolabel to overcome this difficulty. Fenoterol (Berotec®) and Flunisolide (Inhacort®) both from Boehringer Ingelheim KG are two drugs primarily used by inhalation in the treatment of asthma. These compounds were labelled with 99mTechnetium (Tc) in the MDI. The 99mTc label as observed with a gamma camera was shown to follow the same distribution pattern as the drug particles. Cascade impaction with eight stages resulted in the following distribution 63, 8, 5, 3, 6, 5, 8, and 2 % from Stage 1 to Stage 8. A clinical study with 12 healthy volunteers compared the deposition pattern derived from MDI alone and MDI with spacer. Regions Of Interest (ROIs) were the oropharyngal cavity, esophagus, stomach, and lung (central and peripheral zones). With MDI alone, 73 % of the drug was found in upper...

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计量吸入器(MDI)中药物的无线电标记和人体受试者的肺沉积

常规药代动力学方法无法量化吸入吸入器中药物的肺沉积(数量和分布)。近年来，越来越多的吸入器药物使用放射性标签进行了研究，以克服这一困难。勃林格殷格翰公司(Boehringer Ingelheim KG)的非诺特罗(Berotec®)和氟尼索内特(Inhacort®)是两种主要用于吸入治疗哮喘的药物。这些化合物在MDI中用99mTechnetium (Tc)标记。用伽马照相机观察到的99mTc标签显示出与药物颗粒遵循相同的分布模式。八个阶段的级联撞击导致从阶段1到阶段8的分布为63,8,5,3,6,5,8和2%。一项针对12名健康志愿者的临床研究比较了单独使用MDI和使用间隔剂的MDI的沉积模式。感兴趣的区域(roi)为口咽腔、食管、胃和肺(中央和外周区)。单独使用MDI, 73%的药物在上…

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Journal of Aerosol Medicine-deposition Clearance and Effects in The Lung

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