Abstract: AIM: To prepare salbutamol sulfate osmotic pump controlled tablet and study the pharmacokinetics and relative bioavailability of two kinds of salbutamol sulfate oral osmotic pump controlled tablets in healthy volunteers. METHODS: Tablet core, made mainly of sodium chloride, was coated with cellulose acetate and then drilled by laser to make osmotic pump controlled tablets. HPLC method was employed to detect the plasma drug concentration in 12 healthy volunteers. Two one sided tests and analysis of variance were performed to evaluate the bioequivalence of the two formulations. RESULTS: The pharmacokinetic parameters of self prepared controll tablets and imported tablets were listed below: T_max were (6. 30±1.0) h and (6.8±1.3) h,C_max were (8.60±1.93) ng·mL^-1 and (8.20±1.40) ng·mL^-1, AUC were (63.67±10.37) ng·h·mL^-1 and (60.21±11.65) ng·h·mL^-1 respectively. For multi dose administration, the fluctuation degree (FD) were 1.09±0.23 and 1.14±0.25 respectively. CONCLUSION: The two formulations were found to be bioequivalent.