OBJECTIVE To evaluate the in vitro and in vivo correlation of the release characteristics of tetrandrine targeted sustained release dosage forms.METHODS The percentage of the drug released in vitro was measured.The pharmacological activity measured at the targeted site was selected as the efficacy in vivo.The correlative fitting and statistic analysis were carried out.RESULTS The results in vitro and in vivo correlated well significantly(P＜0.001).CONCLUSION It is feasible and reasonable to put pharmacological values into practice for correlation analysis.The drug release properties in vitro can be used to indicate the sustained release characteristics in vivo.