Screening of high permeability classification tool drugs through PAMPA studies
GUAN Hao-yue
LIU Xue-jing
HUANG Han-han
LIU Qian
ZHANG Zun-jian
NIU Jian-zhao
Abstract：Objectives:To develop a parallel artificial membrane model to determine the intestinal permeability of drugs and select suitable high-permeability classification tool drugs.Methods:Taking the parallel artificial membrane model as the main model,the μDissTM optical fiber drug dissolution permeability test system and the Caco-2 cell transport experiment were used to determine the effective permeability rate(Pe)and apparent permeability rate(Papp)of eight high permeability model drugs.High-permeability classification tool drugs suitable for in vitro and in vivo permeability evaluation of drugs were screened and used for the permeability study of the high-permeability drug quetiapine fumarate and low-permeability drug captopril for verification of the applicability of the tool.Results:All the model drugs were highly permeable(Pe/Papp＞10-6 cm·s-1),and passive transport was the main absorption mode(efflux rate＜2).The effective Pe(s)of five drugs measured by the established method were basically consistent with those in human jejunum reported in the literature(r=0.919 6).Conclusion:Five drugs,i.e.,phenytoin,propranolol hydrochloride,metoprolol tartrate,carbamazepine,and minoxidil,were established as tool drugs for hypertonic classification.The findings of this study provide new tools and methods for the evaluation of drug permeability,which are conducive to high-throughput screening and permeability assessment of drugs.
Keywords：high permeability classification tool drugsparallel artificial membranesCaco-2 cellseffective permeability rateapparent permeability rate
Publication Date：2024-11-30
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：8( 2338-2345 )