Abstract: Encouraged by China’s national policies, innovative and complex formulations, as the major driving forces of pharmaceutical innovation, have been widely applied to fill unmet clinical needs. However, research progress on personalized therapies for pediatric and elderly patients has been slow, leading these patients to face difficulties in medication administration, thereby urgently requiring innovative breakthroughs in drug delivery systems. Mini-tablets, characterized by easy swallowing, accurate dosing, flexible dose adjustment, and diverse release profiles, can meet various therapeutic needs. This dosage form has demonstrated high patient compliance particularly in children and the elderly, showing excellent application prospects. This article outlines the formulation characteristics, clinical advantages, and both domestic and international research advancements on mini-tablets, with a focus on analyzing technical challenges in developing mini-tablets. The review aims to provide references for the research and development in mini-tablet drug delivery systems.