OBJECTIVE: To prepare the Carboprost methyl-hydroxypropyl-β-cyclodextrin (HP-β-CD) clathrate sublingual tablets, and conduct quality evaluation. METHODS: Wet granulation method was used to prepare Carboprost methyl-HP-β-CD clathrate sublingual tablets. Using the appearance, calving time, wetting time and main drug content as investigation indexes, mass ratio of mannitol-lactose, povidone volume fraction and amount of low-substituted hydroxypropylcellulose (L-HPC) as factors, orthogonal test was used to screen the formulation. The calving time, wetting time, main drug content, content uniformity, dissolution degree of sublingual tablets with optimal formulation were evaluated. RESULTS: The optimal formulation was as follow as 78.82 mg of carboprost methyl-HP-β-CD clathrate (containing carboprost methyl 1 mg), 100 mg of mannitol-lactose (mass ratio of 9 ∶ 1) mixed powder, appropriate amount of 2% povidone solution, 30 mg of L-HPC, and 1 mg of magnesium stearate. The calving time of prepared 3 batches of sublingual tablets was (25.30±3.21)-(26.53±2.69) s; wetting time was (64.65±8.07)-(65.54±7.21) s; main drug content was (96.13±0.43)%-(97.06±0.82)%; content uniformity was 5.95-7.68; the cumulative dissolution degree within 10 min was more than 50%, and it can completely dissolute within 30 min. CONCLUSIONS: Carboprost methyl- HP-β-CD clathrate sublingual tablets, which are up to requirements, are prepared successfully.