RESUMO
A new, simple, and reproducible method for determination of carboxylic acid metabolite of clopidogrel in human plasma has been developed. After liquid-liquid extraction in acidic medium with chloroform, samples were quantified on a Nova-pak C(8), 5 microm column using a mixture of 30 mM K(2)HPO(4)-THF-acetonitrile (pH = 3, 79:2:19, v/v/v) as mobile phase with UV detection at 220 nm. The flow rate was set at 0.9 mL/min. Ticlopidine was used as internal standard and the total run time of analysis was about 12 min. The method was linear over the range of 0.2-10 microg/mL of clopidogrel metabolite in plasma (r(2) > 0.999). The within-day and between-day precision values were in the range 1.0-4.8%. The limit of quantification of the method was 0.2 microg/mL. The method was successfully used to study the pharmacokinetics of clopidogrel in healthy volunteers.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Inibidores da Agregação Plaquetária/sangue , Ticlopidina/análogos & derivados , Adulto , Ácidos Carboxílicos/sangue , Clopidogrel , Humanos , Masculino , Inibidores da Agregação Plaquetária/farmacocinética , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Ticlopidina/sangue , Ticlopidina/metabolismo , Ticlopidina/farmacocinéticaRESUMO
A series of 2-phenoxybenzoic acid and N-phenylanthranilic acid hydrazides were synthesized and evaluated for their analgesic activities. Several compounds were significantly more potent than mefenamic acid and diclofenac sodium in abdominal constriction and formalin tests.
Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/farmacologia , Hidrazinas/síntese química , Hidrazinas/farmacologia , ortoaminobenzoatos/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Hidrazinas/química , Hidrazinas/uso terapêutico , Masculino , Camundongos , Estrutura Molecular , Dor/tratamento farmacológico , Medição da Dor , Relação Estrutura-Atividade , ortoaminobenzoatos/farmacologiaRESUMO
A series of new 2-substituted-5-[2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles has been synthesized and screened for their anticonvulsant activities. Compound 3 shows considerable anticonvulsant activity both in PTZ and MES models. It seems that this effect is mediated by benzodiazepine receptors and other unknown mechanism, respectively.
