The purpose of the present invention is to provide a pharmaceutical composition for transcolonic absorption which is capable of delivering a biologically active substance (in particular, a water-soluble biologically active substance with a high molecular weight) having sites of action in the cell, not by injection, noninvasively and with high specificity into cells in specific tissues. This pharmaceutical composition for transcolonic absorption is characterized by comprising at least (a) and (b) below: (a) a biologically active substance having sites of action in the cell and to which a lipoprotein introduction substance is bonded, and (b) a compound having a large intestine mucous membrane epithelium permeability enhancing effect for the biologically active substance.
