Currently, all commercial available nebulized salbutamol in China is in its racemic form. It is known that only R -salbutamol (eutomer) has therapeutic effects, while S -salbutamol (distomer) may exacerbate asthma after chronic use. Therefore, it is an unmet clinical need to develop R -salbutamol as a nebulized product that is more convenient for young and old patients. In our study, a stable aerosol solution of R -salbutamol sulfate was established, and its antiasthmatic effects were confirmed. The decomposition rate and racemization effect of the R -salbutamol sulfate solution were evaluated over a pH range from 1 to 10 (except pH=7, 8) at 60°C. The aerodynamic particle size of the R -salbutamol sulfate solution and commercial RS -salbutamol sulfate solution were both tested in vitro by Next-Generation Impactor (NGI) in 5°C. Laser diffractometer was used to characterize the droplet-size distribution (DSD) of both solutions. We next conducted an in vivo animal study to document the antiasthmatic effect of R -salbutamol aerosol sulfate solution and determine the relationship to RS -salbutamol. The results showed that the R -salbutamol sulfate solution was more stable at pH 6. In vitro comparison studies indicated that there was no distribution difference between R -salbutamol sulfate solution and the commercial RS -salbutamol solution. The animal results showed that R -salbutamol was more potent than RS -salbutamol against the same dose of histamine challenge. Unlike commercial RS -salbutamol, which was acidified to a pH of 3.5 to extend bench life but may cause bronchoconstriction in asthmatic patients, the neutralized R -salbutamol solution was more suitable for clinic use.