Abstract
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 | 蛇葡萄素在大鼠肝微粒体中的代谢动力学及药用辅料对其抑制作用的研究 |
|---|---|
| Original language | Chinese (Traditional) |
| Pages (from-to) | 305-313 |
| Number of pages | 9 |
| Journal | Chinese Journal of Modern Applied Pharmacy |
| Volume | 38 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - Feb 2021 |
Scopus Subject Areas
- Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
- Drug Discovery
User-Defined Keywords
- ampelopsin
- metabolic inhibition
- metabolic kinetics
- pharmaceutical excipients