《Table 1 Main pharmacokinetic parameters of hesperetin in rats after oral administration of hesperet

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《高水溶性、抗氧化活性和口服吸收率的橙皮素纳米制剂的制备（英文）》

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Cmax:peak plasma concentration；Tmax:the time to Cmax；AUC0–t:area under the concentration–time curve；MRT:mean residence time；t1/2z:half-life of drug；Clz:clearance；Vz:volume of distribution.Oral administration of hesperetin suspension:100 mg/kg，per oral (

Plasma concentration–time profiles of the hesperetin suspension，hesperetin-TPGS micelles，and hesperetin-PC complexes after oral administration are shown in Fig.7 and the main pharmacokinetic parameters are listed in Table 1.The micelles and complexes significantly increased the Cmax of hesperetin from 2.64μg/mL to 20.67 and 33.09μg/mL，respectively.Importantly，these two formulations increased the AUC to 16.2-fold（53.01 h·μg/mL vs.3.28 h·μg/mL）and 18.0-fold（59.13 h·μg/mL vs.3.28 h·μg/mL），indicating that TPGS micelles and PC complexes remarkably improved the oral bioavailability of hesperetin.Although there were no significant statistical differences in the pharmacokinetic parameters between the micelles and the complexes，the mechanisms of the enhanced solubility andoral absorption may be distinct.Absorbed hesperetin is reported to be pumped out by P-glycoprotein（P-gp），which is extensively expressed in the intestinal epithelium and pumps xenobiotics back into the intestinal lumen（Brand et al.，2008）.TPGS functions as an inhibitor of P-gp（Dintaman and Silverman，1999）.In addition，increased solubility of hesperetin could accelerate the absorption and reduce the exposure time to bacteria，resulting in decreased hesperetin degradation by intestinal bacteria.Therefore，TPGS can not only increase the water solubility and the oral absorption of hesperetin through micelle formation，but it can also reduce the degradation and prevent the excretion of absorbed hesperetin by P-gp inhibition.As a component of the cell membrane，PC is easily absorbed into gastrointestinal tract，facilitating the membrane transport of the dispersed and encapsulated hesperetin.In addition，lipid-based nanoparticles，especially those containing phospholipids，are absorbed by the lymphatic system，through which the hepatic first-pass effect can be avoided（Attili-Qadri et al.，2013；Zhao et al.，2018）.