Abstract: Asiatic acid and its derivatives are the most common triterpenoids in traditional popular medicinal herb Centella asiatica, and have been reported to possess various pharmacological activities such as anti-inflammatory, anticancer and antidepressant. However, their oral bioavailability is low. This article reviews recent advances in pharmacokinetics from the absorption, distribution, metabolism and excretion (ADME), to figure out the possible causes for their low oral bioavailability, and further to investigate the strategy for bioavailability improvement.