|The invention relates to an oral drug composition including a prodrug and a carrier. The prodrug is formed by covalent bonding of an active drug to a spacer. The carrier includes β-1,3-D-glucan and is provided for carrying the prodrug with an efficient amount. Therefore, the oral drug composition can target microfold cells of the intestinal tract, allowing the oral drug composition of the present invention to effectively transport across the intestinal epithelium in a membrane phagocytic mode to break through the mucosal barrier to the desired location. Thus, the oral drug composition can be used to prepare anticancer drugs.