OBJECTIVE: To prepare the Compound anisodamine and neostigmine sustained-release tablet and study the in vitro drug release behavior. METHODS: Using raceanisodamine and neostigmine methyl sulfate as main medicines, hydroxypropyl methyl cellulose as sustained release skeleton material, magnesium stearate as the lubricant, polyvinyl pyrrolidone as the adhesive, pregelatinized starch as the thinner, microcrystalline cellulose as the disintegrant and filler, Compound anisodamine and neostigmine sustained-release tablet was prepared by wet granulation method and direct compression method. The in vitro cumulative release rate within 12 h of the 2 main medicines was detected by HPLC method. RESULTS: Compound anisodamine and neostigmine sustained-release tablet was successfully prepared, and the in vitro release was basically completed within 12 h, with accumulative release rate of 91.3% for anisodamine and 96.5% for neostigmine. CONCLUSIONS: Compound anisodamine and neostigmine sustained-release tablet that can cumulatively release for 12 h is successfully prepared.