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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 the pharmacokinetics of Silymarin Superabsorbent Self-Microemulsion (S-SMEDDS) in rats. Methods Twelve male Sprague-Dawley rats were randomly divided into control group and experimental group, with 6 rats in each group. Rats in control group were given silybin micro-emulsion (SMEDDS) 533 mg / kg, Siberian-S-SMEDDS 533 mg / kg. Blood samples were taken from Accusampler conscious animal blood collection device at different time points. The plasma concentration of silybin was determined by HPLC after ig silybin-S-SMEDDS. Statistical pharmacokinetic analysis was performed using non-compartmental model parameter. Results The tmax of the control group and the experimental group were (1.00 ± 0.40) and (1.50 ± 0.84) h, respectively. The Cmax values were 5.68 ± 0.52 and 16.10 ± 4.06 μg / mL, respectively. The AUC0 → t were (27.30 ± 3.29 ), (82.64 ± 12.36) μg.h.mL 1. Conclusion Silymarin can be made into S-SMEDDS to further improve oral bioavailability.