Abstract: To study the preparation process of Ficus hirta Vahl effervescent tablets, the active ingredients were extracted with the aid of ultrasound using water as solvent, and the extract species were determined by high performance liquid chromatography-mass spectrometry (HPLC-MS/MS), and the formulation of Ficus hirta Vahl effervescent tablets was optimized by single-factor experiments and orthogonal optimization experiment. The results showed that 433 substances were detected in the aqueous extract of Ficus hirta Vahl, and the three most species were carboxylic acids and derivatives (103 species), fatty acyls (45 species) and benzene and substituted derivatives (36 species). The main active ingredients were 23 sugars (6.71% content), 9 flavonoids (0.22% content), 16 phenols (1.65% content), 5 coumarins (0.51‰ content) and 9 phenylpropanoic acids. The best preparation conditions of the effervescent tablets were 25% dried aqueous extract of Ficus hirta Vahl, 50% disintegrant (1:1.5 mass ratio of citric acid to sodium bicarbonate), 20% mannitol, 5% PEG-6000, and the solution of Ficus hirta Vahl effervescent tablets was brownish-yellow, clear and transparent with a sweet and sour taste. The DPPH free radical scavenging ability IC₅₀ was 1.65 mg/mL. The preparation of effervescent tablets from the aqueous extract of Ficus hirta Vahl was rich in active ingredients and possesses antioxidant activity.