{"title":"Thickness of the aqueous boundary layer in stirred microtitre plate permeability assays (PAMPA and Caco-2), based on the Levich equation.","authors":"Alex Avdeef","doi":"10.5599/admet.1568","DOIUrl":null,"url":null,"abstract":"The stirring frequency exponent of -1/2 in the theoretical Levich expression appears to apply to PAMPA and Caco-2 assays, where efficient individual-well magnetic stirring ( > 20 RPM) is used. If a single molecule is used as a stirring calibrant, then scaling suggested by Eq. (5) with microtitre plate data may be used. The error in calculating hABL based on unscaled hABLref can be as high as 30%. This is of practical importance in PAMPA, and perhaps cellular assays as well.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"249-252"},"PeriodicalIF":3.4000,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793457/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ADMET and DMPK","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.5599/admet.1568","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The stirring frequency exponent of -1/2 in the theoretical Levich expression appears to apply to PAMPA and Caco-2 assays, where efficient individual-well magnetic stirring ( > 20 RPM) is used. If a single molecule is used as a stirring calibrant, then scaling suggested by Eq. (5) with microtitre plate data may be used. The error in calculating hABL based on unscaled hABLref can be as high as 30%. This is of practical importance in PAMPA, and perhaps cellular assays as well.
期刊介绍:
ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study