ABSTRACT
Objective: To study in vivo pharmacokinetic characteristic of supersaturable self microemulsion drug delivery system (S-SMEDDS) of silybin in rats. Methods: According to the random design, 12 male rats were divided into one control group and one experimental group by six each. SMEDDS of silybin was given to the control group and S-SMEDDS of silybin to the experimental group by both ig administration at dosage of 533 mg/kg, respectively. Blood sampling was conducted by means of an automated blood sampling device (Accusampler) at different time points. After ig administration of S-SMEDDS of silybin to rats, the silybin concentrations in plasma were determined by HPLC and the pharmacokinetic parameters were calculated by non-compartment model of statistical moment analysis. Results: The main pharmacokinetic parameters of the control and experimental groups were as follows: tmax is (1.00 ± 0.40) and (1.50 ± 0.84) h, Cmax is (5.68 ± 0.52) and (16.10 ± 4.06) μg/mL, AUC0→1 is (27.30 ± 3.29) and (82.64 ± 12.36) μg·h·mL-1, respectively. Conclusion: This assessment demonstrates that the oral absorption bioavailability could be substantially improved via the approach: by S-SMEDDS of silybin.