A pharmaceutical composition for oral delivery is provided with a poorly water-soluble drug； solvent with lipophilic tails and hydrophilic ends； an acid initiator； and a foaming agent generating carbon dioxide bubbles when the acid initiator is dissolved into the intestinal fluid to form an acidic environment. The poorly water-soluble drug is dissolved in the solvent to form a self-assembled monolayer carrier system with the bile salts surrounding the carbon dioxide bubbles in water when the pharmaceutical composition is dissolved in an intestinal tract, and lipid oil drops containing the poorly water-soluble drug form when the carbon dioxide bubbles burst at the air-liquid interface in the intestinal tract.本發明提供一種口服釋放之醫藥組合物，其包括：一疏水性藥物；一親脂性或雙親性溶劑；一酸性引發劑；以及一發泡劑係當酸性引發劑溶解於腸液中形成一酸性環境時用以產生二氧化碳氣泡。其中，疏水性藥物溶解於親脂性或雙親性溶劑而形成一自組單層載體系統，當醫藥組合物分散於腸道中時一膽鹽係環繞於水中二氧化碳氣泡周圍；以及當二氧化碳氣泡於腸道中之氣－液界面破裂時會形成含有疏水性藥物之脂質油滴。
