A pharmaceutical composition for oral delivery of hydrophobic small molecule drug and hydrophilic small molecule drug concurrently is provided. The pharmaceutical composition includes an enteric layer and a drug layer, in which the drug layer is encapsulated in the enteric layer. The drug layer includes a therapeutically effective amount of a hydrophobic small molecule drug, a therapeutically effective amount of a hydrophilic small molecule drug, a lipophilic solvent, an acidic compound and an effervescent ingredient.
