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Pharmacokinetics (ADME)

June 09, 2020

Pharmacokinetics (ADME)  by

Chlorogenic acid, scutellarin, and scutellarein, the main active constituents in E. breviscapus, had higher drug exposure in plasma of middle cerebral artery occlusion rats than in sham-operated rats. Chen 2018


Developed a rapid, sensitive and specific ultra-high performance liquid chromatography-tandem mass spectrometry method to determine the pharmacokinetics of 12 active bioactive constituents from Erigeron breviscapus in rat plasma following oral administration. Tian 2017


Study of the binding mechanism of breviscapine, a cerebrovascular drug from E. breviscapus, to human serum albumin by various assays indicated that conformation of the protein was slightly altered after interacting with breviscapine. The drug-protein complex was stabilized by electrostatic forces. Liu 2016


Scutellarin, from E. breviscapus, inhibited cytochrome P450 isoenzyme 1A2 (CYP1A2) directly, but weakly, in rats. These in vivo study results are in accordance with in vitro results. Jian 2012


Pharmacokinetic profiling of scutellarin, an active component from E. breviscapus, suggested that a large amount of scutellarin ingested by rats was metabolized into scutellarein in the GI tract and then excreted with the feces, with significant gender differences in pharmacokinetic parameters. Xing 2011


Used UPLC/TOF MS to profile the metabolites of scutellarin, a flavone glucuronide and the main active component of the traditional Chinese botanic drug Erigeron breviscapus, in rats following oral administration. Liu 2009


Polyamidoamine (PAMAM) dendrimers can greatly increase the solubility of breviscapine (total flavonoids from E. breviscapus) in water and can improve the oral bioavailability of breviscapine significantly, as tested in rats. [Article in Chinese] Lu 2009


Isolated 2 major urinary metabolites from rat urine following oral administration of scutellarin, the main effective constituent of breviscapine, a cerebrovascular and cardiovascular drug consisting of total flavonoids of Erigeron breviscapus. Qiu 2007


The metabolites of brevisvapine, total flavonoid components from the dried whole plant of E. breviscapus, were excreted in rat urine as glucuronidated, sulfated or methylated forms, as well as the aglycone of scutellarin-scutellarein after oral administration. Xia 2007


In a crossover study, breviscapine liposomes (from E. breviscapus) injected in Beagle dogs had a much higher concentration in plasma compared with reference preparation, and contained sustained-release characteristics, which ameliorated scutellarin's pharmacokinetic properties. [Article in Chinese] Lo 2006


Investigated the pharmacokinetics of scutellarin and its aglycone conjugated metabolites after intraperitoneal injection and oral administration of breviscapine, a flavonoid glycoside mixture extracted from E. breviscapus, in rats. The relative bioavailability of oral administration was very low. Huang 2005


Breviscapine, from E. breviscapus, had a short half-life after intravenous administration to dogs and rabbits, which show breviscapine is eliminated rapidly and has short action time. [Article in Chinese] Liu 2005


Establishhed a RP-HPLC method for determination of plasma scutellarin concentration and studied the pharmacokinetic behavior of scutellarin in rat after ig administration of breviscapine and its beta-cyclodextrin complex.[Article in Chinese] Zhang 2005