The present invention aims to provide a pharmaceutical composition for transcolonic absorption capable of delivering a physiologically active substance (in particular, a water-soluble physiologically active substance of high molecular weight) having an intracellular site of action into specific tissue cells with high specificity, noninvasively by a means of administration other than injection. The pharmaceutical composition for transcolonic absorption of the present invention is characterized by comprising at least the following (a) and (b)(a) a physiologically active substance having an intracellular site of action and bound with an introduction substance into lipoprotein, and(b) a compound having an action of enhancing large intestinal mucosal epithelial permeability of the physiologically active substance.
