Clark D J, Gordon-Smith J, McPhate G, Clark G, Lipworth B J
Department of Clinical Pharmacology, Ninewells Hospital and Medical School, University of Dundee, UK.
Thorax. 1996 Mar;51(3):325-6. doi: 10.1136/thx.51.3.325.
The aim of this study was to determine whether significant differences exist in lung bioavailability between generic (Salamol, Salbulin) and innovator (Ventolin) formulations of inhaled salbutamol given by metered dose inhalers.
Ten healthy volunteers of mean age 20.5 years with a forced expiratory volume in one second (FEV1) of 112.1% predicted were studied in a randomised double blind single dosing crossover study. Salbutamol, 1200 micrograms, was given with mouth rinsing and lung bioavailability was assessed by measuring plasma salbutamol levels and urine excretion of salbutamol.
No differences were seen between innovator and generic salbutamol metered dose inhalers in plasma salbutamol levels, urinary salbutamol excretion, or extrapulmonary beta 2 activity. The maximum plasma salbutamol concentration (mean Cmax) and time to maximum concentration (median Tmax) were: Ventolin (2.93 ng/ml, 10 minutes), Salbulin (3.01 ng/ml, 10 minutes), Salamol (3.33 ng/ml, 10 minutes). The geometric mean ratio and 95% confidence interval for Cmax were: Salbulin/Ventolin 1.02 (0.69 to 1.41) and Salamol/Ventolin 1.13 (0.94 to 1.35).
No differences are apparent between the two generic and innovator formulations of salbutamol metered dose inhaler in terms of lung bioavailability.
本研究旨在确定通过定量吸入器给予的吸入用沙丁胺醇的仿制药（舒利迭、喘乐宁）和创新药（万托林）制剂在肺部生物利用度方面是否存在显著差异。
在一项随机双盲单剂量交叉研究中，对10名平均年龄20.5岁、一秒用力呼气量（FEV1）为预测值112.1%的健康志愿者进行了研究。给予1200微克沙丁胺醇并进行漱口，通过测量血浆沙丁胺醇水平和沙丁胺醇尿排泄量来评估肺部生物利用度。
在血浆沙丁胺醇水平、尿沙丁胺醇排泄量或肺外β2活性方面，创新药和仿制药沙丁胺醇定量吸入器之间未见差异。血浆沙丁胺醇最大浓度（平均Cmax）和达到最大浓度的时间（中位数Tmax）分别为：万托林（2.93纳克/毫升，10分钟）、喘乐宁（3.01纳克/毫升，10分钟）、舒利迭（3.33纳克/毫升，10分钟）。Cmax的几何平均比值和95%置信区间为：喘乐宁/万托林1.02（0.69至1.41），舒利迭/万托林1.13（0.94至1.35）。
两种仿制药和创新药沙丁胺醇定量吸入器在肺部生物利用度方面无明显差异。
