The invention relates to a pharmaceutical composition including an enteric layer and a drug layer. The drug layer includes a therapeutically effective amount of hydrophobic small molecule drugs, a therapeutically effective amount of hydrophilic small molecule drugs, a lipophilic solvent, an acidic compound and an effervescent ingredient. When the pharmaceutical composition enters the intestinal tract through oral administration, carbon dioxide bubbles are generated. The disturbance caused by the expansion and rupture of the carbon dioxide bubbles causes the pharmaceutical composition to self-emulsify to form lipid oil drops with the hydrophobic small molecule drugs, and the hydrophilic small molecule drugs are dissolved in the intestinal fluid. Therefore, the pharmaceutical composition does not need to use a toxic carrier, and can deliver the hydrophobic small molecule drug and the hydrophilic small molecule drug concurrently through oral administration, and can increase the solubility of the drug to improve oral bioavailability. |