Alzheimer's disease (AD) is a common progressive neuro-degenerative disease, and the morbidity and mortality are still on the rise. In spite of recent advances in AD treatment, their clinical efficacy has been limited, non-curative and easy to drug resistance. Alpiniae oxyphyllae Fructus (AOF), derived from the dried and mature fruits of the Zingiberaceae plant Alpinia oxyphylla Miq, is a choice in traditional Chinese medicine to treat AD, which has a good effect and has been used for a long time. Recent studies have demonstrated its potent activities in modulating multiple signaling pathways associated with β-amyloid deposition, tau protein phosphorylation, chronic inflammation, oxidative stress. The neuropharmacological mechanism of AOF in AD have been fully illustrated in numerous studies. In this review, we first briefly described the active components of AOF and related mechanism for treating AD. And we also provide a systematic overview of recent progress on the pharmacokinetic characteristics of the active ingredients of AOF and analyzed their bioavailability differences in the development of AD. Thus, AOF hold a great therapeutic potential in the treatment of AD and is worthy of further research and promotion.