RESUMO
Secnidazole is an antimicrobial agent used primarily in the treatment of amoebiasis. For this bioequivalence study of secnidazole, twenty-eight healthy female volunteers were enrolled in a randomized crossover study. Each volunteer was given a single oral dose of secnidazole test preparation and then the reference preparation, or vice versa, with a wash out interval of two weeks. The plasma concentrations of secnidazole were determined by HPLC, and the samples were extracted with tert-butyl-methyl-ether: dicloromethane (60:40, v/v). Secnidazole and its parent compound metronidazole were separated on a C18 column with water:acetonitrile (85:15, v/v) as the mobile phase, and monitored at 310 nm. The ratio of mean Cmax, AUC0-t and AUC0-∞ values for the test and reference products were within the predetermined range established by ANVISA, demonstrating that the two formulations are bioequivalent in rate and extent of absorption.
Secnidazol é um agente antimicrobiano utilizado principalmente no tratamento da amebíase. Para este estudo de bioequivalência de secnidazol em voluntários saudáveis, foram incluídos vinte e oito voluntárias mulheres no estudo randomizado cruzado. Cada voluntária recebeu uma única dose oral de secnidazol do produto teste e referência para comparação, com um intervalo de wash-out de duas semanas. As concentrações plasmáticas de secnidazol foram determinados por CLAE, as amostras foram extraídas com terc-butil-metil-éter: dicloromethano (60:40, v/v). O secnidazol e seu padrão interno metronidazol foram separados em uma coluna (C18 ) com fase móvel água ultra-pura:acetonitrila (85:15, v/v) e monitorado em 310 nm. As razões entre as médias geométricas de Cmáx, ASC0-t e ASC0-∞, encontraram-se dentro do estabelecido pela ANVISA, demonstrando que as formulações são bioequivalentes quanto à taxa e extensão de absorção.
Assuntos
Humanos , Feminino , Adolescente , Adulto , Pessoa de Meia-Idade , Anti-Infecciosos , Disponibilidade Biológica , Química Farmacêutica/métodos , Experimentação Humana Terapêutica , Amebíase/imunologia , Amebíase/tratamento farmacológico , Amebíase/terapiaRESUMO
beta-carboline alkaloids are found in several medicinal plants and display a variety of actions on the central nervous, muscular and cardiovascular systems. The aim of the present study was to evaluate the effects of systemic administration of beta-carboline alkaloids on object recognition in mice. Adult Swiss mice received an intra-peritoneal injection (i.p.) of alkaloids (1.0, 2.5 or 5.0 mg/kg) 30 min before training in an object recognition task. The fully aromatic beta-carbolines, harmine and harmol, induced an enhancement of short-term memory (STM) at all doses tested when compared to controls. Harmaline, a dihydro beta-carboline and inverse agonist of the MK-801 binding site on the N-methyl-d-aspartate (NMDA) receptor, also induced an enhancement of both short-term memory (STM) and long-term memory (LTM). These results demonstrate that systemic administration of beta-carboline alkaloids can improve object recognition memory in mice.