水飞蓟宾纳米乳的制备及家兔体内药动学

Preparation of Silybin Nanoemulsion and Its Pharmacokinetics in Rabbits

目的:研制具有一定缓释效果的水飞蓟宾纳米乳并考察其家兔体内药物动力学。方法:通过制备水飞蓟宾磷脂复合物,提高了水飞蓟宾在油中的溶解度,利用均匀设计优化了乳剂的处方工艺,采用乳化法研制了稳定的水飞蓟宾纳米乳,考察了水飞蓟宾纳米乳在家兔体内的代谢过程。结果:优化的处方工艺制备的水飞蓟宾纳米乳平均光强粒径为21.2 nm,Zeta电位-26.9 mV,稳定性好;家兔体内药动学经时过程表明本制剂具有一定的缓释效果。结论:与溶液剂相比,水飞蓟宾纳米乳肌肉注射液延长了药物在体内的驻留时间,具有一定的缓释效果。

AIM： To prepare stable silybin nanoemulsion for intramuscular injection and to study the in vivo disposition behaviors. METHODS： Silybin-phospholipid complex was prepared to enhance silybin＇s solubility in the oil ;The formulation of the silybin nanoemulsion was optimized by the uniform design;Following administration of the nanoemulsion to rabbits, the in vivo disposition of silybin was evaluated. RESULTS： The silybin nanoemulsion with optimized formulation was stable with the average paritcle size being 21.2 nm and Zeta potential being - 26.9 mV. And the release profile in rabbits showed a sustained-release manner. CONCLUSION： Silybin nanoemulsion for intramuscular injection could increase silybin MRT in vivo. In comparison to silybin aqueous injection, the intramuscularly injected nanoemulsion could sustain the in vivo release of silybin with improved bioavailability.