English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

Baicalin purified from the root of  Radix scutellariae  is widely used in clinical practices. This study aimed to evaluate the effect of baicalin on the pharmacokinetics of nifedipine, a CYP3A probe substrate, in rats  in vivo  and  in vitro . In a randomised, three-period crossover study, significant changes in the pharmacokinetics of nifedipine (2 mg/kg) were observed after treatment with a low (0.225 g/kg) or high (0.45 g/kg) dose of baicalin in rats. In the low- and high-dose groups of baicalin-treated rats,  C   max  of total nifedipine decreased by 40%±14% ( P <0.01) and 65%±14% ( P <0.01), AUC 0–∞  decreased by 41%±8% ( P <0.01) and 63%±7% ( P <0.01), V d  increased by 85%±43% ( P <0.01) and 224%±231% ( P <0.01), and CL increased by 97%±78% ( P <0.01) and 242%±135% ( P <0.01), respectively. Plasma protein binding experiments  in vivo  showed that  C   max  of unbound nifedipine significantly increased by 25%±19% ( P <0.01) and 44%±29% ( P <0.01), respectively, and there was a good correlation between the unbound nifedipine (%) and baicalin concentrations ( P <0.01). Furthermore,  in vitro  results revealed that baicalin was a competitive displacer of nifedipine from plasma proteins.  In vitro  incubation experiments demonstrated that baicalin could also competitively inhibit CYP3A activity in rat liver microsomes in a concentration-dependent manner. In conclusion, the pharmacokinetic changes of nifedipine may be modulated by the inhibitory effects of baicalin on plasma protein binding and CYP3A–mediated metabolism.

plos one

Contribution of Baicalin on the Plasma Protein Binding Displacement and CYP3A Activity Inhibition to the Pharmacokinetic Changes of Nifedipine in Rats In Vivo and In Vitro