Ginkgo biloba has a very high medicinal value. The flavonol glycosides and terpene lactones contained in G. biloba extract (GBE) have such pharmacological effects as antioxidant, anti-platelet aggregation and memory improvement, enhancement of immune function. However, the ginkgolic acid (GA) contained in GBE is proved to be highly allergenic and cytotoxic, even minimal residual could also cause severe adverse effects. To minimize the potential safety hazards of ginkgo leaf preparations, this study focuses on GA's chemical structure, adverse effects, toxicity and genesis mechanism, desorption and attenuation in the hope of providing a new thought for studies on safety of Ginkgo biloba preparations.