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1.
J Pharmacol Toxicol Methods ; 127: 107503, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38574874

RESUMO

BACKGROUND: Omadacycline is the first aminomethyl-tetracycline variety to successfully enter clinical applications. To support regular therapeutic drug monitoring (TDM) in clinical practice, an ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method was developed that would allow omadacycline quantification in human serum. METHODS: Proteins were precipitated from serum samples using methanol. Tigecycline was used as the internal standard. Mobile phase A was formic acid in water (0.1% v/v) and mobile phase B was methanol. UPLC-MS/MS was performed for analyte separation using a gradient elution program at a flow rate of 0.3 mL/min and a total run time of 5 min. The chromatography column was a ZORBAX PRHD SB-Aq (3 × 50 mm, 1.8 µm, Agilent, USA). The multiple reaction monitoring transitions at m/z = 557.4/470.3 and 586.5/513.3 were selected for omadacycline and tigecycline in the positive mode, respectively. RESULTS: The validated curve ranges were 0.5-25.0 µg/mL. This method exhibited acceptable selectivity, matrix effects, and recovery. The inter- and intra-run accuracies ranged from 93.5% to 114.8%, and the inter- and intra-run precisions were between 1.29% and 5.55%. CONCLUSIONS: The LC-MS/MS method provided a simple, specific, and rapid quantification of omadacycline in the serum of patients with pulmonary infection.


Assuntos
Antibacterianos , Monitoramento de Medicamentos , Espectrometria de Massas em Tandem , Tetraciclinas , Humanos , Espectrometria de Massas em Tandem/métodos , Tetraciclinas/sangue , Cromatografia Líquida de Alta Pressão/métodos , Monitoramento de Medicamentos/métodos , Antibacterianos/sangue , Reprodutibilidade dos Testes , Tigeciclina/sangue , Espectrometria de Massa com Cromatografia Líquida
2.
Luminescence ; 34(2): 175-182, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30637925

RESUMO

Tigecycline (TIGE) is the newest tetracycline derivative antibiotic with low toxicity, it is used for management of infectious diseases caused by Gram-positive and Gram-negative bacteria. Hence, an efficient, selective and sensitive method was developed for analysis of TIGE in commercial formulations, human plasma and urine. The spectrofluorimetric technique based on the reaction of secondary amine moiety in TIGE with 4-chloro-7-nitrobenzofurazan (NBD-Cl) in slightly alkaline medium producing a highly fluorescent product measured at 540 nm (λex at 470 nm) after heating for 15 min at 75°C. The proposed strategy was upgraded and approved by ICH rules and bio-analytical validated using US-FDA recommendations. A linear relationship between fluorescence intensity and TIGE concentration was observed over the concentration range 40-500 ng mL-1 with limit of quantification (LOQ) 21.09 ng mL-1 and limit of detection (LOD) 6.96 ng mL-1 .The ultra-affectability and high selectivity of the proposed strategy permits analysis of TIGE in dosage form, human plasma and urine samples with good recovery ranged from 97.23% to 98.72% and from 99.36% to 99.80% respectively, without any interfering from matrix components. Also, the developed strategy was used to examine the stability of TIGE in human plasma and applied for pharmacokinetic investigation of TIGE.


Assuntos
Benzoxazóis/química , Composição de Medicamentos , Corantes Fluorescentes/química , Tigeciclina/sangue , Tigeciclina/urina , Voluntários Saudáveis , Humanos , Estrutura Molecular , Espectrometria de Fluorescência , Tigeciclina/farmacocinética
3.
Artigo em Inglês | MEDLINE | ID: mdl-29358291

RESUMO

Tigecycline is a glycylcycline often used in critically ill patients as the antibiotic of last resort. The pharmacokinetics (PK) of tigecycline in intensive care unit (ICU) patients can be affected by severe pathophysiological changes so that standard dosing might not be adequate. The aim of this study was to describe population PK of high-dose tigecycline in patients with sepsis or septic shock and evaluate the relationship between individual PK parameters and patient covariates. The study population consisted of 37 adult ICU patients receiving a 200-mg loading dose of tigecycline followed by multiple doses of 100 mg every 12 h. Blood samples were collected at 0.5, 2, 4, 8, and 12 h after dose administration. A two-compartment model with interindividual (IIV) and interoccasion (IOV) variability in PK parameters was used to describe the concentration-time course of tigecycline. The estimated values of mean population PK parameters were 22.1 liters/h and 69.4 liters/h for elimination and intercompartmental clearance, respectively, and 162 liters and 87.9 liters for volume of the central and peripheral compartment, respectively. The IIV and IOV in clearance were less than 20%. The estimated values of distribution volumes were different from previously published values, which might be due to pathophysiological changes in ICU patients. No systematic relationship between individual PK parameters and patient covariates was found. The developed model does not show evidence that individual tigecycline dosing adjustment based on patient covariates is necessary to obtain the same target concentration in patients with sepsis or septic shock. Dosing adjustments should be based on the pathogens, their susceptibility, and PK targets.


Assuntos
Antibacterianos/farmacocinética , Antibacterianos/uso terapêutico , Sepse/sangue , Sepse/tratamento farmacológico , Choque Séptico/sangue , Choque Séptico/tratamento farmacológico , Tigeciclina/farmacocinética , Adulto , Idoso , Antibacterianos/sangue , Feminino , Humanos , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Estudos Prospectivos , Tigeciclina/sangue , Tigeciclina/uso terapêutico
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