A comparison of the pharmacokinetics of three different preparations of total flavones of Hippophae rhamnoides in beagle dogs after oral administration

Abstract

Pharmacokinetic properties of isorhamnetin, quercetin, and kaempferol in three different total flavones of Hippophae rhamnoides (TFH) preparations were compared after oral administration to beagle dogs by a UPLC-MS method. The pharmacokinetic results showed that C max of isorhamnetin and quercetin in TFH solid dispersion (TFH-SD) and TFH self-emulsifying (TFH-SE) preparations was significantly enhanced than that in TFH preparations (p < 0.05). The AUCs of isorhamnetin and quercetin in TFH-SD were 5.9- and 3.1-fold higher than that of TFH, while the AUCs of isorhamnetin and quercetin in TFH-SE were 3.4- and 2.4-fold higher than that of TFH. These findings suggested that the oral bioavailability of isorhamnetin and quercetin in beagle dogs can be significantly increased in TFH-SD and TFH-SE preparations compared to TFH preparations, which was helpful to explore the new forms for oral administration TFH and explain their in vivo processes.

Fabrication and Optimization of Self‐Microemulsions to Improve the Oral Bioavailability of Total Flavones of Hippophaë rhamnoides L

“…Compared with Duan (Duan and others ) and Xie's (Xie and others ) work on solid dispersion formulations (composed of Poloxamer 188 and ethanol), our study contained less surfactants but performed a comparable bioavailability improvement, all of which could increase the bioavailability of quercetin around 3.0‐fold of those in suspension. Although similar components (MCT, CrEL, and Trans HP at ratios of 13.26: 60.38: 26.36) were used to form self‐microemulsions as a comparison to Duan and Zhao's development (SE composed of MCT CrEL, and 1,2‐propanediol at ratios of 5:57:38; Zhao and others ; Duan and others ), quite different enhancement levels were existed. When taken the TFH suspension as the same control group, our approach could improve the bioavailability of quercetin about 2‐fold of this reported SE formulation.…”

“…When take the same compound, quercetin as the representative of TFH, literatures have reported several approaches to improve the bioavailability of TFH. The relevant bioavailability of quercetin was enhanced 3.1 times and 2.4 times when encapsulated in solid dispersions (SD) and self‐emulsions (SE), respectively after oral administration in beagle dogs (Duan and others ), and in the case of oral administration in rats, this bioavailability of quercetin was boosted to 3.16 (in SD form) and 1.55 (in SE form) times, separately (Zhao and others ). Compared with Duan (Duan and others ) and Xie's (Xie and others ) work on solid dispersion formulations (composed of Poloxamer 188 and ethanol), our study contained less surfactants but performed a comparable bioavailability improvement, all of which could increase the bioavailability of quercetin around 3.0‐fold of those in suspension.…”

“…The relevant bioavailability of quercetin was enhanced 3.1 times and 2.4 times when encapsulated in solid dispersions (SD) and self‐emulsions (SE), respectively after oral administration in beagle dogs (Duan and others ), and in the case of oral administration in rats, this bioavailability of quercetin was boosted to 3.16 (in SD form) and 1.55 (in SE form) times, separately (Zhao and others ). Compared with Duan (Duan and others ) and Xie's (Xie and others ) work on solid dispersion formulations (composed of Poloxamer 188 and ethanol), our study contained less surfactants but performed a comparable bioavailability improvement, all of which could increase the bioavailability of quercetin around 3.0‐fold of those in suspension. Although similar components (MCT, CrEL, and Trans HP at ratios of 13.26: 60.38: 26.36) were used to form self‐microemulsions as a comparison to Duan and Zhao's development (SE composed of MCT CrEL, and 1,2‐propanediol at ratios of 5:57:38; Zhao and others ; Duan and others ), quite different enhancement levels were existed.…”

“…It has been demonstrated that the promising absorption enhancement of TFH had reached to a certain extent by adding absorption enhancers, such as phytic acid and sea buckthorn oils (Suomela and others ; Xie and others ) or by formation of tablets, capsules, and solid dispersions, β‐cyclodextrin complex as well as self‐emulsifying system (Yue and others ; Xie and others ; Duan and others ). Of all these reported and other solubilization approaches, nanocarriers to encapsulate drugs, and nutraceuticals have been drawn much attention, such as microemulsions, nanoemulsions, micelles, and solid lipid nanoparticles (Bilia and others ).…”

Flavonoids from sea buckthorn: A review on phytochemistry, pharmacokinetics and role in metabolic diseases

“…Besides, quercetin reached the Tmax at 5.58 hr, 4.50 hr, 4.25 hr, and kaempferol reached the Tmax at 7.08 hr, 6.00 hr, 7.00 hr at low, middle and high doses, respectively (Li et al, 2012). In beagle dogs, Tmax of isorhamnetin and quercetin were 2.6 hr and 1.0 hr (Duan et al, 2016). These studies indicated that both passive diffusion and active transport involved in absorption forms of FSBT, and passive diffusion process was dominated.…”