Borgström L, Newman S, Weisz A, Morén F
Department of Human Pharmacology, Astra Draco, Lund, Sweden.
J Pharm Sci. 1992 Aug;81(8):753-5. doi: 10.1002/jps.2600810807.
Deposition from a multidose powder inhaler (Turbuhaler, Astra) delivering 500 micrograms of terbutaline sulfate per metered dose was compared by two techniques in a group of six healthy volunteers. The deposition of the radionuclide 99mTc, which was used to label terbutaline sulfate powder, was quantified by gamma camera (G-method). Simultaneously, the gastrointestinal absorption of swallowed drug was blocked with activated charcoal, and the amount of terbutaline in a urine sample, collected over a period of 48 h and corrected by a pharmacokinetic internal standard of intravenous deuterated terbutaline, was used as a measure of lung deposition (U-method). The mean (standard deviation) depositions in lung were 26.9 (3.8%) of the dose for the G-method and 21.1 (3.2)% of the dose for the U-method. Possible reasons for the differences between the two means are discussed. Both methods are suitable for assessing deposition from medical aerosol inhalers; the U-method requires access to gas chromatography-mass spectrometric equipment, and the G-method requires access to gamma camera facilities.
采用两种技术，在6名健康志愿者中比较了多剂量粉末吸入器（都保，阿斯特拉公司），其每揿剂量为500微克硫酸特布他林的药物沉积情况。用放射性核素99mTc标记硫酸特布他林粉末，通过γ相机（G法）对其沉积进行定量分析。同时，用活性炭阻断吞咽药物的胃肠道吸收，收集48小时尿液样本中的特布他林量，并通过静脉注射氘代特布他林的药代动力学内标进行校正，以此作为肺沉积的量度（U法）。G法肺内平均（标准差）沉积量为剂量的26.9（3.8）%，U法为剂量的21.1（3.2）%。讨论了两种平均值之间差异的可能原因。两种方法均适用于评估医用气雾剂吸入器的沉积情况；U法需要使用气相色谱-质谱设备，G法需要使用γ相机设备。
