Simple HPLC‐UV for the quantification of a new leishmanicidal candidate (E)‐1‐4(trifluoromethyl) benzylidene)‐5‐(2‐4‐dichlorozoyl) carbonylhydrazine (LASSBio‐1736) in rat plasma for pharmacokinetics assessment |
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| Authors: | Barbra Katyuschya Sanches Moraes Lisiane Bajerski Alcides Parisotto Carlos Eduardo da Rosa Silva Marina Amaral Alves Eliezer de Jesus Barreiro Rodrigo José Freddo Teresa Dalla Costa Lídia Moreira Lima Sandra Elisa Haas |
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| Affiliation: | 1. Curso de Farmácia, Universidade Federal do Pampa, UNIPAMPA, Uruguaiana, CEP, Brasil;2. Programa de Pós‐Gradua??o em Ciências Farmacêuticas, Universidade Federal do Pampa, UNIPAMPA, Uruguaiana, CEP, Brasil;3. Laboratório de Avalia??o e Síntese de Substancias Bioativas – Universidade Federal do Rio de Janeiro, UFRJ, Brasil;4. Programa de Pós‐Gradua??o em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, UFRGS, CEP, Porto Alegre, Brasil |
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| Abstract: | In this study, a sensitive HPLC‐UV assay was developed and validated for the determination of LASSBio‐1736 in rat plasma with sodium diclofenac as internal standard (IS). Liquid–liquid extraction using acetonitrile was employed to extract LASSBio‐1736 and IS from 100 μL of plasma previously basified with NaOH 0.1 M. Chromatographic separation was carried on Waters Spherisorb®S5 ODS2 C18 column (150 × 4.6 mm, 5 μm) using an isocratic mobile phase composed by water with triethylamine 0.3% (pH 4), methanol and acetonitrile grade (45:15:40, v/v/v) at a flow rate of 1 mL/min. Both LASSBio‐1736 and IS were eluted at 4.2 and 5 min, respectively, with a total run time of 8 min only. The lower limit of quantification was 0.2 μg/mL and linearity between 0.2 and 4 μg/mL was obtained, with an R2 > 0.99. The accuracy of the method was >90.5%. The relative standard deviations intra and interday were <6.19 and <7.83%, respectively. The method showed the sensitivity, linearity, precision, accuracy and selectivity required to quantify LASSBio‐1736 in preclinical pharmacokinetic studies according to the criteria established by the US Food and Drug Administration and European Medicines Agency. Copyright © 2016 John Wiley & Sons, Ltd. |
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| Keywords: | LASSBio‐1736 Leishmaniosis HPLC pharmacokinetics |
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