Given the inherent dangers associated with racemic pharmaceuticals, exhaustive studies of techniques designed to separate enantiomers have been conducted. This paper reports a brief review of the different physical, chemical, and enzymatic methods used for the enantiomeric separation of rac-ibuprofen. The possible contribution of each technique to the preparation of enantiomerically pure drugs is reviewed in the context of competitive approaches that depend on the scale of application, with special emphasis on the recent progress achieved in this particular area.