Enhanced pharmacokinetic behavior and hepatoprotective function of ginger extract-loaded supersaturable self-emulsifying drug delivery systems
Enhanced pharmacokinetic behavior and hepatoprotective function of ginger extract-loaded supersaturable self-emulsifying drug delivery systems
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生姜提取物负载的过饱和自乳化给药系统增强的药代动力学行为和保肝功能
DOI：
10.1016/j.jff.2017.08.035
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发表时间：
2018
影响因子：
5.6
通讯作者：
Onoue Satomi
中科院分区：
文献类型：
--
作者：
Ogino Mizuki;Yakushiji Keisuke;Suzuki Hiroki;Shiokawa Kenichi;Kikuchi Hiroshi;Seto Yoshiki;Sato Hideyuki;Onoue Satomi
本研究的目的是利用超饱和自乳化给药系统(S-SEDDS)来提高生姜提取物的营养特性。制备了由中链甘油三酯、溶血磷脂和甘油组成的Ge的SEDDS(SEDDS/Ge)。将羟丙基甲基纤维素作为沉淀阻聚剂加入到S SEDDS/Ge中，制备了Ge的SEDDS/Ge(S-SEDDS/Ge)。对Ge制剂的理化、药代动力学和保肝性能进行了表征。这两种配方都改善了Ge的溶解行为，这是因为形成了中值直径约为110 nm的细小胶束。大鼠口服Ge样品后，S-SEDDS/Ge组的6-姜酚和8-姜酚的相对生物利用度分别是Ge组的3倍左右。Ge/S-SEDDS(100 mg-Ge/kg)灌胃给药对四氯化碳肝毒性大鼠有明显的保肝作用。从这些观察，S-SEDDS方法可能是有效的，以提高Ge的营养特性。
The aim of present study was to enhance the nutraceutical properties of ginger extract (GE) by employing supersaturable self-emulsifying drug delivery systems (S-SEDDS). SEDDS of GE (SEDDS/GE), consisting of medium-chain triglyceride, lysolecithin and glycerin, was produced. To prepare S-SEDDS of GE (S-SEDDS/GE), hydroxypropyl methylcellulose was added to the SEDDS/GE as a precipitation inhibitor. Physicochemical, pharmacokinetic, and hepatoprotective properties of GE formulations were characterized. Both formulations improved the dissolution behavior of GE due to the formation of fine micelles with a median diameter of ca. 110 nm. After oral administration of GE samples in rats, the relative bioavailabilities of 6-gingerol and 8-gingerol in the S-SEDDS/GE-treated group were ca. 3-fold higher than those of GE-treated group, respectively. Repeated oral administration of GE/S-SEDDS (100 mg-GE/kg) provided a hepatoprotective effect in a rat model of carbon tetrachloride-induced hepatotoxicity. From these observations, the S-SEDDS approach might be efficacious for enhancing the nutraceutical properties of GE.