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Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil.

Shen JY, Yang XL, Yang ZL, Kou JP, Li F - Drug Des Devel Ther (2015)

Bottom Line: 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.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.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.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, People's Republic of China.

ABSTRACT

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.

No MeSH data available.


Related in: MedlinePlus

Stability and nonspecific binding of ECH.Notes: (A) ECH remaining percent after 2 h in K–R buffer solution and homogenates of rat intestinal segments. (B) Binding of ECH to tubes and different sections of intestine after 2-h incubation. Results were shown as mean ± SD (n=3 in each group).Abbreviations: ECH, echinacoside; h, hours; K–R, Krebs–Ringer; SD, standard deviation.
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f2-dddt-9-4685: Stability and nonspecific binding of ECH.Notes: (A) ECH remaining percent after 2 h in K–R buffer solution and homogenates of rat intestinal segments. (B) Binding of ECH to tubes and different sections of intestine after 2-h incubation. Results were shown as mean ± SD (n=3 in each group).Abbreviations: ECH, echinacoside; h, hours; K–R, Krebs–Ringer; SD, standard deviation.

Mentions: ECH was found to be stable both in K–R buffer solution and intestinal perfusate in 2-hour incubation. The results showed that no ECH was absorbed by intestinal wall and tubes in everted gut sac and single-pass intestinal perfusion experiment (Figure 2). The incubation results suggested that any loss of drug from the perfusion should be attributed to intestinal absorption.


Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil.

Shen JY, Yang XL, Yang ZL, Kou JP, Li F - Drug Des Devel Ther (2015)

Stability and nonspecific binding of ECH.Notes: (A) ECH remaining percent after 2 h in K–R buffer solution and homogenates of rat intestinal segments. (B) Binding of ECH to tubes and different sections of intestine after 2-h incubation. Results were shown as mean ± SD (n=3 in each group).Abbreviations: ECH, echinacoside; h, hours; K–R, Krebs–Ringer; SD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4544722&req=5

f2-dddt-9-4685: Stability and nonspecific binding of ECH.Notes: (A) ECH remaining percent after 2 h in K–R buffer solution and homogenates of rat intestinal segments. (B) Binding of ECH to tubes and different sections of intestine after 2-h incubation. Results were shown as mean ± SD (n=3 in each group).Abbreviations: ECH, echinacoside; h, hours; K–R, Krebs–Ringer; SD, standard deviation.
Mentions: ECH was found to be stable both in K–R buffer solution and intestinal perfusate in 2-hour incubation. The results showed that no ECH was absorbed by intestinal wall and tubes in everted gut sac and single-pass intestinal perfusion experiment (Figure 2). The incubation results suggested that any loss of drug from the perfusion should be attributed to intestinal absorption.

Bottom Line: 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.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.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.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, People's Republic of China.

ABSTRACT

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.

No MeSH data available.


Related in: MedlinePlus