OBJECTIVE: To investigate the metabolic regularity of ampelopisn in rat liver microsomes and the effect of pharmaceutical excipients on its metabolism.
METHODS: The UPLC-MS/MS method was established to screen metabolic conditions in vitro and evaluate metabolic patterns by detecting the residual concentration of ampelopsin in the metabolic reaction system.
RESULTS: Ampelopisn metabolism was affected by incubation time, liver microsome concentration and initial ampelopisn concentration. Rat hepatocyte pigment P450 subenzyme CYP3A, CYP1A1/2 and CYP2E1 played a major role in serpentine metabolism. The inhibitory effect of pharmaceutical excipients on ampelopsin metabolism was dose-dependent manner. The metabolic kinetics studies revealed that Cremophor RH40, Tween 80, PVP K30, HPBCD and F68 exhibited significant inhibition metabolism in a mixed competition.
CONCLUSION: These pharmaceutical excipients are expected to improve the oral bioavailability of ampelopsin by inhibiting metabolism.
|Translated title of the contribution
|Number of pages
|Chinese Journal of Modern Applied Pharmacy
|Published - Feb 2021
Scopus Subject Areas
- Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
- Drug Discovery
- metabolic inhibition
- metabolic kinetics
- pharmaceutical excipients