Micellar liquid chromatography for prediction of drug transport

The mixed micellar liquid chromatography is a mode that uses mixed micellar system of Brij35/SDS (85 : 15) as a mobile phase under adequate experimental conditions, can simulate the resting membrane potential and the conformation of the long hydrophilic polyoxyethylene chains remains unchanged. In this article, the applications of biopartitioning micellar chromatography, using mixed micellar system to describe and estimate bioactivities of alkaloids, has been focused. The BMC(Brij35/SDS)-QRAR models of half-life time, volume of distribution, plasma clearance and area under concentration-time curve were obtained using Brij35-SDS retention data. The aim is to take a look at the capability of the mixed micellar liquid chromatography model to describe and/or estimate the bioactivity of alkaloids.

Section: Reagents and Standardsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development of predictive quantitative retention–activity relationship models of alkaloids by mixed micellar liquid chromatography

Chen

et al. 2009

“…In order to obtain predictive and interpretative models, the retention data of ACEIs and the corresponding biological responses were adjusted to a second-order polynomial model [eqn (6)]. It has also been demonstrated in previous QRAR studies that this is the usual retention-activity relationship for pharmacokinetics and biological response of drugs (Molero-Monfort et al, 2000;Escuder-Gilabert et al, 2001.…”

Section: Retention-activity Relationships For the Aceis In Bmcmentioning

confidence: 99%

“…The predictive and interpretative capability of quantitative chromatographic retention-biological activity (QRAR) models is supported by the fact that in adequate experimental conditions the solute partitioning into the chromatographic system can emulate the solute partitioning into the lipid bilayer of a biological membrane, which is the basis for drug and metabolite uptake, passive transport across the membrane and bioaccumulation (Molero-Monfort et al, 2000;EscuderGilabert et al, 2001). Furthermore, there are a number of similarities between the modified stationary phase, mobile phase in BMC and the membrane-water interface.…”

Section: Introductionmentioning

confidence: 99%

Mixed micellar liquid chromatography methods: modelling quantitative retention–activity relationships of angiotensin converting enzyme inhibitors

Cui

Xiong

et al. 2008

The capability of biopartitioning micellar chromatography (BMC), using pure Brij35 solution and mixed micellar system of Brij35-SDS (85:15) as mobile phase, to describe and estimate bioactivities of angiotensin converting enzyme inhibitors at different pH has been studied. Quantitative retention-activity relationships (QRAR) in BMC were investigated for these compounds. The obtained BMC(Brij35-SDS)-QRAR models were compared with the traditional BMC(Brij35)-QRAR, and better statistically models were obtained using Brij35-SDS retention data. The superiority of BMC(Brij35-SDS)-QRAR is due to the fact that the mixed micellar mobile phase can simulate the resting membrane potential and the conformation of the long hydrophilic polyoxyethylene chains remains unchanged.

“…Under adequate experimental conditions, the properties (hydrophobic, electronic and steric) determine the behaviour of chemical compounds in both the biological and chromatographic environments (Molero-Monfort et al, 2000;EscuderGilabert et al, 2001;Detroyer et al, 2003). Therefore, BMC can be used as a powerful chromatography for estimating physicochemical parameters and biological activities.…”

Section: Introductionmentioning

confidence: 99%

Biopartitioning micellar chromatography separation methods: modelling quantitative retention–activity relationships of cephalosporins

Chen

et al. 2008

In this article, recent applications of chromatographic systems, particularly biopartitioning micellar chromatography (BMC) systems based on amphiphilic structures, have been reported. The aim is to take a look at the capability of quantitative retention-activity relationship (QRAR) models with BMC to describe and/or estimate the bioactivity of cephalosporins. Better qualification of BMC systems was obtained according to the octanol-water partition coefficient (log P); the bioactivity parameters (Lag-T, T(1/2beta), F%, T(1/a), P%, AUC and C(max)) were correlated with the retention factors of cephalosporins processed by Alltech-chromstation software, and the classical data were compared with the predictive values based on QRAR models. The results indicate that using only one descriptor (the retention factor, k) to explain the pharmacokinetic and pharmacodynamic properties of cephalosporins is adequate, and this in vitro approach is an advanced tool for pharmacodynamics research.