水飞蓟宾过饱和自微乳给药系统在大鼠体内的药动学研究

Pharmacokinetics of supersaturable self microemulsion drug delivery system of silybin in rats

目的研究水飞蓟宾过饱和自微乳给药系统(S-SMEDDS)在大鼠体内的药动学特征。方法 12只雄性SD大鼠随机分为对照组和实验组,每组6只,对照组大鼠ig给予水飞蓟宾自微乳(SMEDDS)533 mg/kg,实验组大鼠ig给予水飞蓟宾-S-SMEDDS 533 mg/kg。采用Accusampler清醒动物自动采血装置于不同时间点采血,HPLC法测定大鼠ig水飞蓟宾-S-SMEDDS后水飞蓟宾的血药浓度,非房室模型的统计矩分析方法计算药动学参数。结果对照组和实验组的tmax分别为(1.00±0.40)、(1.50±0.84)h,Cmax分别为(5.68±0.52)、(16.10±4.06)μg/mL,AUC0→t分别为(27.30±3.29)、(82.64±12.36)μg.h.mL 1。结论将水飞蓟宾制成S-SMEDDS可进一步提高其口服生物利用度。

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： tmaxiS （1.00 ± 0.40） and （1.50 ± 0.84） h, Cmax is （5.68 ± 0.52） and （16.10 ± 4.06） ug/mL, AUC 0-t is （27.30 ± 3.29） and （82.64 ± 12.36） ug.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