当前位置: X-MOL 学术J. Microencapsul. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
[6]-Shogaol/β-CDs inclusion complex: preparation, characterisation, in vivo pharmacokinetics, and in situ intestinal perfusion study.
Journal of Microencapsulation ( IF 3.9 ) Pub Date : 2019-08-14 , DOI: 10.1080/02652048.2019.1649480
Ran Li 1 , Rui Bao 1 , Qiu-Xuan Yang 1 , Qi-Long Wang 1 , Michael Adu-Frimpong 1 , Qiu-Yu Wei 1 , Toreniyazov Elmurat 2, 3 , Hao Ji 2, 4 , Jiang-Nan Yu 1 , Xi-Ming Xu 1
Affiliation  

Aims: The aim was to improve the absorption and bioavailability of [6]-shogaol with β-cyclodextrin (β-CD) prior to in vitro and in vivo evaluation.

Methods: [6]-Shogaol/β-CDs inclusion complexes (6-S-β-CDs) were developed using saturated aqueous solution method and characterised with appropriate techniques. The absorption and bioavailability potential of [6]-shogaol was evaluated via in vivo pharmacokinetics and in situ intestinal perfusion.

Results: The results of characterisation showed that 6-S-β-CDs (drug loading, 7.15%) were successfully formulated. In vitro release study indicated significantly improved [6]-shogaol release. Pharmacokinetic parameters such as Cmax, AUC0–36 h, and oral relative bioavailability (about 685.36%) were substantially enhanced. The in situ intestinal perfusion study revealed that [6]-shogaol was markedly absorbed via passive diffusion in the intestinal segments, and duodenum followed by ileum and jejunum.

Conclusions: Cyclodextrin inclusion technology could enhance the intestinal absorption and oral bioavailability of hydrophobic drugs like [6]-shogaol.



中文翻译:

[6] -Shogaol /β-CDs包合物:制备,表征,体内药代动力学和原位肠灌注研究。

目的:在体外体内评估之前,目的是提高β-环糊精(β-CD)对[6]-松果酚的吸收和生物利用度。

方法:采用饱和水溶液法制备[6] -Shogaol /β-CDs包合物(6-S-β-CDs),并采用适当的技术对其进行表征。[6] -shogaol的吸收和生物利用度潜力通过体内药代动力学和原位肠道灌注进行评估。

结果:表征结果表明成功制备了6-S-β-CDs(载药量为7.15%)。体外释放研究表明[6]-松香酚的释放明显改善。诸如C max,AUC 0–36 h和口服相对生物利用度(约685.36%)之类的药代动力学参数已大大提高。该原位肠灌注研究表明,[6] -姜烯酚显着通过被动扩散吸收在肠节段,和十二指肠随后回肠和空肠。

结论:环糊精包合技术可以增强[6] -shogaol等疏水性药物的肠道吸收和口服生物利用度。

更新日期:2019-08-14
down
wechat
bug