The in vitro dissolution profiles of nine sustained-release formulations of (±)-salbutamol were determined. The formulations contained chiral pharmaceutical excipients, such as hydroxypropylmethylcellulose (HPMC) and heptakis (2,6-di-O-methyl)-β-cyclodextrin (DMCD). The influence of the degree of ionization was studied in six formulations that were buffered at different pH values. The quantitative determination of salbutamol enantiomers released by the matrices was carried out using a stereospecific capillary electrophoresis method. The release of salbutamol enantiomers from all formulations was found to be non-enantioselective. Likewise, the addition of buffering agents to the formulation did not provide an enantioselective release of salbutamol enantiomers from the matrices under the conditions established.