OBJECTIVE： To investigate the effect of Wuzhi soft capsule on the pharmacokinetics of sirolimus in rats. METHODS： Wistar rats were randomly divided into 5 groups， with 6 rats in each group. They were given very low-dose， low-dose， medium-dose and high-dose of Wuzhi soft capsule （67， 134， 268 and 536 mg/kg） ig or blank solvent， respectively； and then given sirolimus 0.4 mg/kg. The blood 100 μl was sampled by capillary eyes before giving sirolimus （0 h） and 0.5， 0.75， 1， 1.5， 2， 2.5， 3， 4， 6， 8， 12， 24 and 36 h after giving sirolimus and put into edetic acid anticoagulation tube. Blood concentration of sirolimus was assayed by LC-MS/MS. The pharmacokinetic parameter was calculated by DAS 2.0 software using non-compartment model. RESULTS： The pharmacokinetic parameters of sirolimus in very low-dose， low-dose， medium-dose and high-dose groups and blank solvent group were cmax of （6.79±1.15），（17.40±3.13），（21.24±3.14），（22.06±4.82），（2.80±0.72） ng/ml； t1/2 of （11.01±0.82），（12.20±2.02），（12.28±2.38），（12.36±0.73），（10.59±0.69） h； AUC0-∞ of （85.79±15.26），（162.18±41.75），（273.12±73.69），（268.79±28.46），（36.72±3.01） ng·h/ml， respectively. Compared with blank solvent group， cmax and AUC0-∞ of sirolimus were all increased in very low-dose， low-dose， medium-dose and high-dose groups， but t1/2 changed slightly. CONCLUSIONS： Wuzhi soft capsule can substantially enhance the absorption of sirolimus in rats.