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已发表论文
用维拉帕米 (Verapamil) 或丁香油增强松果菊苷 (echinacoside) 的吸收和生物利用度
Authors Shen JY, Yang XL, Yang ZL, Kou JP, Li F
Received 29 April 2015
Accepted for publication 3 June 2015
Published 14 August 2015 Volume 2015:9 Pages 4685—4693
DOI http://dx.doi.org/10.2147/DDDT.S87581
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Qinbo Zhou
Peer reviewer comments 3
Editor who approved publication: Professor Shu-Feng Zhou
Purpose: This present study investigated the absorption kinetics of echinacoside (ECH) in situ and in vitro and its oral bioavailability in rats. Additional aim was to find an agent(s) to promote ECH absorption and oral bioavailability among two efflux proteins and three absorption promoters.
Methods: ECH absorption behaviors were investigated by everted gut sac model in vitro and single-pass intestinal perfusion model in situ. Pharmacokinetics study was performed to investigate the influences of verapamil and clove oil on ECH bioavailability in vivo. All samples were measured at different time intervals by high performance liquid chromatography.
Results: The results showed that the effective permeability coefficient (P eff) and apparent permeability coefficient of ECH were 0.83×10-6–3.23×10-6 cm/s and 2.99×10-6–9.86×10-6 cm/s, respectively. The P eff among duodenum, jejunum, and ileum were not statistically different, but they were higher than colon (P <0.01), which demonstrated that intestinal ECH absorption was poor and site dependent. Additionally, verapamil and clove oil significantly increased the jejunal P eff of ECH both in situ and in vitro. Moreover, the bioavailability of ECH in combination with verapamil and clove oil were increased by 1.37-fold (P <0.05) and 2.36-fold (P <0.001), respectively, when compared to ECH group. Overall, verapamil and clove oil facilitated ECH absorption and oral bioavailability.
Conclusion: The absorption and bioavailability of ECH were enhanced by verapamil and clove oil, respectively, both in vitro and in vivo. Consequently, the combination of verapamil and clove oil with ECH will be a promising and effective approach to promote intestinal absorption and oral bioavailability of ECH.
Keywords: intestinal absorption, efflux protein inhibitor, absorption promoter
Methods: ECH absorption behaviors were investigated by everted gut sac model in vitro and single-pass intestinal perfusion model in situ. Pharmacokinetics study was performed to investigate the influences of verapamil and clove oil on ECH bioavailability in vivo. All samples were measured at different time intervals by high performance liquid chromatography.
Results: The results showed that the effective permeability coefficient (P eff) and apparent permeability coefficient of ECH were 0.83×10-6–3.23×10-6 cm/s and 2.99×10-6–9.86×10-6 cm/s, respectively. The P eff among duodenum, jejunum, and ileum were not statistically different, but they were higher than colon (P <0.01), which demonstrated that intestinal ECH absorption was poor and site dependent. Additionally, verapamil and clove oil significantly increased the jejunal P eff of ECH both in situ and in vitro. Moreover, the bioavailability of ECH in combination with verapamil and clove oil were increased by 1.37-fold (P <0.05) and 2.36-fold (P <0.001), respectively, when compared to ECH group. Overall, verapamil and clove oil facilitated ECH absorption and oral bioavailability.
Conclusion: The absorption and bioavailability of ECH were enhanced by verapamil and clove oil, respectively, both in vitro and in vivo. Consequently, the combination of verapamil and clove oil with ECH will be a promising and effective approach to promote intestinal absorption and oral bioavailability of ECH.
Keywords: intestinal absorption, efflux protein inhibitor, absorption promoter
