Abstract
Enhancing drug extraction from human plasma is a challenging approach that critically affects pharmacokinetic and any further clinical studies based on the drug Cmin and Cmax values. It also has a serious impact on the sensitivity and the lower limit of quantification (LLOQ) value of the bio-analytical methods. An advanced liquid chromatography tandem mass spectrometry (LC-MS/MS) bio-analytical method of omarigliptin (25–1000 nM) was established in human plasma using one-step liquid-liquid extraction. Alogliptin was used as an internal standard (IS) to attain good recovery and reproducibility while reducing the effects of the matrix. Enhanced plasma extraction of omarigliptin was successfully achieved with tertiary butyl methyl ether—diethyl ether (TBME-DEE) mixture as the extracting solvent, while using acetonitrile as the diluent solvent for the IS to effectively decrease the formed emulsion. Multiple Reaction Monitoring (MRM) of the transition pairs of m/z 399.2 to 153.0 for omarigliptin and m/z 340.2 to 116.0 for alogliptin was employed in positive Electro Spray Ionization (ESI) mode. Human plasma samples were collected after 1.5 h (tmax) of Marizev® (12.5 mg) tablets administration to healthy human volunteers showing average concentration of 292.18 nM. Validation results were all satisfactory including successful stability studies with bias below 12%. The proposed study will be valuable for ethnicity comparison studies that will be commenced on omarigliptin in Egypt by the authors in prospective study, following the FDA recommends, to evaluate possible sub-group dissimilarities that include pharmacokinetic parameters.
Highlights
The proposed study will be valuable for ethnicity comparison studies that will be commenced on OTN in Egypt by the authors in a prospective study
An advanced analytical technique and enhanced extraction of drugs from human plasma become a challenging approach that greatly affects pharmacokinetics, other clinical studies based on the drug Cmin and Cmax values and the bio-analytical methods sensitivity
Working on anti-diabetic drugs’ bio-analysis is of great importance in the current days. It opens the door for ethnicity comparisons related to more pharmacokinetic bioequivalence studies and drugs’ approval in more countries leading to better hemoglobin A1c (HbA1c) control and other outcomes
Summary
It is worthy to mention that many recent COVID-19 studies reported that Diabetes Mellitus was a major contributing factor either for non-survivals and/or hospitalization. Diabetic patients represented 12% of non-survivors in a study and represented 22% of the hospitalized patients in another study [1,2]. Diabetes Mellitus are most likely to suffer from different complications when infected with virus. Molecules 2020, 25, x FOR PEER REVIEW either for non-survivals and/or hospitalization. 22% of the hospitalized patients in another study [1,2]. People with Diabetes Mellitus are most likely to suffer from different complications when infected with virus ranging from from mild risk and thethe severity of ranging mild to to severe
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