Validation of a liquid chromatographic-tandem mass spectrometric method for the determination of loperamide in human plasma

Streel, Bruno; Ceccato, Attilio; Klinkenberg, Régis; Hubert, Philippe

doi:10.1016/j.jchromb.2004.10.050

Cited by 27 publications

(15 citation statements)

References 19 publications

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“…In contrast to loperamide, the pharmacokinetics of the primary CYP3A4-mediated metabolite, N-desmethylloperamide, were unchanged in the presence of GFJ, which may reflect elimination rate-limited kinetics and/or more rapid distribution into peripheral tissues relative to loperamide (Sklerov et al, 2005). The pharmacokinetics of both loperamide and N-desmethylloperamide in the absence of GFJ were consistent with those reported at an equivalent (16 mg) (Mukwaya et al, 2005) or lower (2-4 mg) (Streel et al, 2005;Niemi et al, 2006) loperamide dose after dose normalization.…”

Section: Discussionsupporting

confidence: 73%

Assessment of a Candidate Marker Constituent Predictive of a Dietary Substance–Drug Interaction: Case Study with Grapefruit Juice and CYP3A4 Drug Substrates

Ainslie¹,

Wolf²,

Li³

et al. 2014

J Pharmacol Exp Ther

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Dietary substances, including herbal products and citrus juices, can perpetrate interactions with conventional medications. Regulatory guidances for dietary substance-drug interaction assessment are lacking. This deficiency is due in part to challenges unique to dietary substances, a lack of requisite human-derived data, and limited jurisdiction. An in vitro-in vivo extrapolation (IVIVE) approach to help address some of these hurdles was evaluated using the exemplar dietary substance grapefruit juice (GFJ), the candidate marker constituent 69,79-dihydroxybergamottin (DHB), and the purported victim drug loperamide. First, the GFJ-loperamide interaction was assessed in 16 healthy volunteers. Loperamide (16 mg) was administered with 240 ml of water or GFJ; plasma was collected from 0 to 72 hours. Relative to water, GFJ increased the geometric mean loperamide area under the plasma concentration-time curve (AUC) significantly (1.7-fold). Second, the mechanism-based inhibition kinetics for DHB were recovered using human intestinal microsomes and the index CYP3A4 reaction, loperamide N-desmethylation (K I [concentration needed to achieve one-half k inact ], 5.0 6 0.9 mM; k inact [maximum inactivation rate constant], 0.38 6 0.02 minute 21). These parameters were incorporated into a mechanistic static model, which predicted a 1.6-fold increase in loperamide AUC. Third, the successful IVIVE prompted further application to 15 previously reported GFJ-drug interaction studies selected according to predefined criteria. Twelve of the interactions were predicted to within the 25% predefined criterion. Results suggest that DHB could be used to predict the CYP3A4-mediated effect of GFJ. This time-and cost-effective IVIVE approach could be applied to other dietary substance-drug interactions to help prioritize new and existing drugs for more advanced (dynamic) modeling and simulation and clinical assessment.

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Section: Discussionsupporting

confidence: 73%

Assessment of a Candidate Marker Constituent Predictive of a Dietary Substance–Drug Interaction: Case Study with Grapefruit Juice and CYP3A4 Drug Substrates

Ainslie¹,

Wolf²,

Li³

et al. 2014

J Pharmacol Exp Ther

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“…The accuracy profile expresses the total error as the combination of systematic and random errors, and determines the concentration range for which a procedure provides results within defined acceptance limits [23,24].…”

Section: Accuracy Profile and Loqsmentioning

confidence: 99%

Application of monolithic supports to online extraction and LC‐MS analysis of benzodiazepines in whole blood samples

Bugey

Staub

2007

J of Separation Science

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A column-switching (CS) LC-MS method allowing high-speed determination of benzodiazepines (BZDs) in whole blood is presented. After protein precipitation with ACN followed by evaporation and reconstitution with the loading mobile phase, the online sample clean-up was carried out using a CS device. Two extractive precolumns were evaluated: a conventional restricted access material (RAM) sorbent and a monolithic silica support. Separation was achieved using a Chromolith Performance RP-18e (100 mmx4.6 mm id) monolithic silica column, and detection was performed by atmospheric pressure chemical ionization (APCI) MS. The method with both supports has been fully validated according to an accuracy profile approach. Finally, the monolithic silica column, demonstrating better validation data and a higher robustness than the RAM sorbent, was used for the analysis of several real forensic cases.

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“…the chromatographic signal) and the concentration (amount) of the analyte in the sample system is a very important parameter that must be considered in the validation of an analytical method [31,[34][35][36][37][38][39][40][41][42]. Typically, the linear regression model is used to explain the response function of LC or CE methods, but this model is not always the most appropriate.…”

Section: Prevalidation Stepmentioning

confidence: 99%

Comparison of liquid chromatography and capillary electrophoresis methods for quantification of sodium residuals

Briône

Herbots²,

Kottgen

et al. 2007

Journal of Pharmaceutical and Biomedical Analysis

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Validation of a liquid chromatographic-tandem mass spectrometric method for the determination of loperamide in human plasma

Cited by 27 publications

References 19 publications

Assessment of a Candidate Marker Constituent Predictive of a Dietary Substance–Drug Interaction: Case Study with Grapefruit Juice and CYP3A4 Drug Substrates

Assessment of a Candidate Marker Constituent Predictive of a Dietary Substance–Drug Interaction: Case Study with Grapefruit Juice and CYP3A4 Drug Substrates

Application of monolithic supports to online extraction and LC‐MS analysis of benzodiazepines in whole blood samples

Comparison of liquid chromatography and capillary electrophoresis methods for quantification of sodium residuals

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