In situ intestinal absorption and pharmacokinetic study of metformin-resveratrol compound water-in-oil nanoemulsion
10.11665/j.issn.1000-5048.20210309
- VernacularTitle:二甲双胍-白藜芦醇复合物油包水型纳米乳在体肠吸收及其药代动力学研究
- Author:
Yun CHEN
1
;
Mei ZENG
;
Jingxin XU
;
Juan HU
;
Jingqing ZHANG
Author Information
1. 重庆医科大学药学院重庆高校药物工程研究中心
- Publication Type:Journal Article
- Keywords:
metformin;
resveratrol;
compound;
nanoemulsion;
intestinal absorption;
pharmacokinetics;
bioavailability
- From:
Journal of China Pharmaceutical University
2021;52(3):325-331
- CountryChina
- Language:Chinese
-
Abstract:
To investigate the in situ intestinal absorption characteristics and pharmacokinetic behavior of metformin-resveratrol compound water-in-oil nanoemulsion (MRCE) in rats, the in situ intestinal perfusion model was constructed in rats to study the intestinal absorption characteristics of MRCE in different intestinal segments. Male Sprague-Dawley rats were randomly divided into two groups. After intragastric administration of metformin and MRCE, blood was taken at a preset time point. The content of metformin in intestinal perfusion samples and blood samples at various time points was determined by HPLC. Plasma concentration-time profiles of free metformin and MRCE were calculated, and the main pharmacokinetic data were processed and analyzed by DAS 2.1.1 software. The absorption rate constant (Ka), the effective permeability (Peff) and the percentage of absorption (PA) of MRCE in each intestinal segment were significantly higher than those of metformin (P < 0.05). The area under the drug-time curve (AUC0-72 h), the half-life (t1/2) and mean residence time (MRT0-72 h) of MRCE were 1.68, 11.25 and 6.97 times of metformin, respectively (P < 0.01).The relative bioavailability of MRCE was 167.6%. The 90% confidence interval of AUC0-72 h was 156.9%-187.4%, which was not within the standard interval of bioequivalence. The intestinal absorption of MRCE was significantly better than that of free metformin; MRCE improved the oral bioavailability of metformin and was not bioequivalent to metformin.
