Abstract: This paper deals with the formulation, preparation, dissolution and pharmacokinetics of a sustained release procainamide hydrochloride (PA. HCI) tablet——an oral osmotic pump(B). The orifice of B was prepared by a developed laser machine.A dual wavelength UV spectrophotometric method for the determination of PA was established. PA and its active metabolite N-acetylprocainamide(NAPA) in serum or saliva were separated and detected by a modified HPLC method. The pharmacokinetic parameters were fitted by nonlinear least square method with a computer on the basis of two-compartment model. The results showed that the osmotic pump tablet released drug with a zero-order kinetic, and a significant correlation was found between in vitro dissolution and in vivo absorption. The pharmacokineticpharmacodynamie data suggested a good relationship between the drug concentrations in serum or saliva and therapeutic effects.