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CHEN Yun, ZENG Mei, XU Jingxin, HU Juan, ZHANG Jingqing. In situ intestinal absorption and pharmacokinetic study of metformin-resveratrol compound water-in-oil nanoemulsion[J]. Journal of China Pharmaceutical University, 2021, 52(3): 325-331. DOI: 10.11665/j.issn.1000-5048.20210309
Citation: CHEN Yun, ZENG Mei, XU Jingxin, HU Juan, ZHANG Jingqing. In situ intestinal absorption and pharmacokinetic study of metformin-resveratrol compound water-in-oil nanoemulsion[J]. Journal of China Pharmaceutical University, 2021, 52(3): 325-331. DOI: 10.11665/j.issn.1000-5048.20210309
shu

In situ intestinal absorption and pharmacokinetic study of metformin-resveratrol compound water-in-oil nanoemulsion

  • 1.

    Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016

  • 2.

    Chongqing Huapont Pharm Co., Ltd, Chongqing 401121, China

Funds: This study was supported by Chongqing Science and Technology Innovation Project for Social Undertakings and Livelihood Security (No.cstc2017shmsA130028)
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  • Received Date: January 27, 2021
  • Revised Date: May 10, 2021
    Graphical Abstract
    • 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.
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    • References (22)
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