Ginger extract-loaded solid dispersion system with enhanced oral absorption and anti-hypothermic action
Ginger extract-loaded solid dispersion system with enhanced oral absorption and anti-hypothermic action
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具有增强口服吸收和抗低温作用的生姜提取物固体分散体系统
DOI：
10.1021/acs.jafc.6b04740
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发表时间：
2017
影响因子：
6.1
通讯作者：
Satomi Onoue
中科院分区：
文献类型：
--
作者：
2)Hideyuki Sato;Mizuki Ogino;Keisuke Yakushiji;Hiroki Suzuki;Ken-ichi Shiokawa;Hiroshi Kikuchi;Yoshiki Seto;Satomi Onoue
采用固体分散体法研究生姜提取物（GE）的抗低温作用。对制备的GE SD（GE/SD）进行了理化和药代动力学特性表征。在大鼠低温模型中评价GE样品的抗低温作用。GE/SD表现出GE中主要活性成分6-姜辣素（6 G）和8-姜辣素（8 G）的溶出行为改善，溶出水平分别比GE高12倍和31倍。即使在加速条件下储存后，在GE/SD中也观察到6 G和8 G的有限降解，尽管6 G和8 G在GE中轻微降解。口服GE（300 mg/kg）和GE/SD（100 mg GE/kg）后，6 G和8 G在GE/SD中的相对生物利用度分别是GE的5.0倍和5.8倍。口服GE/SD（30 mg GE/kg）可抑制乙醇引起的体温降低，因为6 G和8 G的口服吸收得到改善。从这些观察结果来看，SD方法可能有效地提高了GE的营养潜力。
The aim of this study is to enhance the antihypothermic action of ginger extract (GE) employing a solid dispersion (SD) approach. The prepared SD of GE (GE/SD) was characterized in terms of physicochemical and pharmacokinetic properties. The antihypothermic action of GE samples was evaluated in a rat model of hypothermia. GE/SD exhibited improved dissolution behavior of the major active ingredients in GE, 6-gingerol (6G) and 8-gingerol (8G), with levels of dissolution 12- and 31-fold higher than that of GE, respectively. Even after storage under accelerated conditions, limited degradations of 6G and 8G were observed in GE/SD, although 6G and 8G were slightly degraded in GE. After oral administration of GE (300 mg/kg) and GE/SD (100 mg of GE/kg), the relative bioavailabilities of 6G and 8G in GE/SD were 5.0- and 5.8-fold higher than those in GE, respectively. Orally administered GE/SD (30 mg of GE/kg) inhibited ethanol-evoked hypothermia because of improved oral absorption of 6G and 8G. From these observations, the SD approach might be efficacious for enhancing the nutraceutical potentials of GE.