1. [6]-Shogaol/β-CDs inclusion complex: preparation, characterisation, in vivo pharmacokinetics, and in situ intestinal perfusion study.
- Author
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Li, Ran, Bao, Rui, Yang, Qiu-Xuan, Wang, Qi-Long, Adu-Frimpong, Michael, Wei, Qiu-Yu, Elmurat, Toreniyazov, Ji, Hao, Yu, Jiang-Nan, and Xu, Xi-Ming
- Subjects
INCLUSION compounds ,BIOAVAILABILITY ,PERFUSION ,INTESTINAL absorption ,PHARMACOKINETICS ,DRUG bioavailability ,AQUEOUS solutions - Abstract
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 C
max , 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. [ABSTRACT FROM AUTHOR]- Published
- 2019
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