Abstract: OBJECTIVE To provide guidance and basis for establishing reasonable dissolution method by establishing and predicting of the doxazosin mesylate sustained-release tablets pharmacokinetic(PK) model. METHODS The PK model was established by GastroPlus^TM, and the dissolution curves in vivo was obtained by deconvolution operation, which comparating the results of dissolution in vitro. RESULTS The PK model in vivo of doxazosin mesylate sustained release tablets was established. The AUC and C_max of the dissolution curves in vitro was significantly higher than that of the measured value by comparing the dissolution curves in vivo and in vitro. CONCLUSION The current in vitro dissolution test method can not accurately reflect the in vivo process, in vivo-in vitro correlation is poor, and the method needs to be further improved.