期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 176, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ejps.2022.106255
关键词
absorption; in situ single-pass intestinal perfusion; mPEG-PR; permeability; water flux
资金
- Basic Research Projects of Liaoning Provincial Education Department [2020LJC12]
- Disruptive Technologies Innovation Fund of Shenyang Pharmaceutical University [DFJJ2018208]
This study investigated the applicability of mPEG-PR as a novel non-absorbable indicator in the in situ single-pass intestinal perfusion (SPIP) experiment. The results showed that mPEG-PR was a stable and accurate method for correcting water flux and predicting the fraction dose absorbed in human.
Phenol red and PEG-4000, the usual non-absorbable indicators, have non-negligible absorption problems in measuring water flux. mPEG-PR, combined phenol red with mPEG-4000, was first synthesized and could decrease absorption. However, its application has not been confirmed. The purpose of this study was to explore the applicability of mPEG-PR as a novel non-absorption indicator in the in situ single-pass intestinal perfusion (SPIP) experiment. Six model drugs (atenolol ranitidine, ibuprofen, ketoprofen, antipyrine, hydrochlorothiazide) were used to compare the accuracy of four measuring methods including phenol red, mPEG-PR, gravimetric, and non-corrected methods of correcting intestinal fluid transport. Moreover, we evaluated the correlations between the effective permeability coefficients (P-eff) in rat and fraction dose absorbed (F-abs) in human, P-eff in human, and apparent permeability coefficients (P-app) by the Ussing Chamber system using human tissue. Among these methods, mPEG-PR was the most reliable approach, which avoided the absorption of phenol red method and mucous shedding or water evaporation of gravimetric method. An excellent correlation was obtained between the P-eff of rat and F-abs of human. Our results of this study indicated that mPEG-PR was a stable and accurate non-absorbable indicator to correct water flux in the in situ SPIP model, which could be developed to predict the human F-abs.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据