ABSTRACT
SUMMARY Mirabegron is a kind of β3 adrenergic receptor agonist which is an effective drug for the treatment of overactive bladder. In this research, a UPLC-MS/MS method is developed and validated for the study of mirabegron pharmacokinetic in rats. A protein precipitation method is applied for sample preparation with acetonitrile. m/z 397.3→379.6, m/z 326.4→121.0 for mirabegron, tolterodine (IS), respectively in the positive ion mode was performed for quantitation. The method is reliable and reproducible in our study (intra-day precision≤11.06%, inter-day precision≤11.43%) with concentration curves linear from 5 to 2500 ng/mL(R2>0.999). Stability studies demonstrated that mirabegron was stable under a variety of storage conditions. This method was successfully applied for determining mirabegron in rats after oral and intravenous administration.
RESUMO Mirabegron é um tipo de agonista do receptor adrenérgico beta 3 que demonstra eficácia no tratamento de bexiga hiperativa. Nesta pesquisa, o método UPLC-MS/MS é desenvolvido e validado para o estudo da farmacocinética mirabegron em ratos. Um método de precipitação de proteínas é aplicado para a preparação de amostras com acetonitrilo. 397.3 → 379.6 M / Z, M / Z 326.4 → 121.0 para mirabegron, tolterodina (IS), respectivamente, para o íon positivo foi realizado para quantificação. O método é fiável e reprodutível em nosso estudo (precisão intradia ≤ 11,06%; precisão entredia ≤ 11.43%), com curvas de concentração linear de 5 a 2 ng/ml (R2 > 0,999). Estudos de estabilidade demonstraram que mirabegron permanece estável sob uma variedade de condições de armazenamento. Este método foi aplicado com sucesso para a determinação de mirabegron em ratos após administração oral e intravenosa.
Subject(s)
Animals , Male , Rats , Thiazoles/pharmacokinetics , Adrenergic beta-3 Receptor Agonists/pharmacokinetics , Acetanilides/pharmacokinetics , Thiazoles/administration & dosage , Thiazoles/blood , Administration, Oral , Reproducibility of Results , Chromatography, High Pressure Liquid , Rats, Sprague-Dawley , Tandem Mass Spectrometry , Adrenergic beta-3 Receptor Agonists/administration & dosage , Adrenergic beta-3 Receptor Agonists/blood , Administration, Intravenous , Acetanilides/administration & dosage , Acetanilides/bloodABSTRACT
A simple model independent approach using a similarity factor [f2] and a difference factor [f1] to compare dissolution profiles as proposed by Moore and Flanner was used to evaluate the in vitro equivalence of two brands of meloxicam tablets. Our results showed that the two meloxicam formulations are not equivalent in vitro. Thus it is recommended that the same formulations should be evaluated to in vivo studies in order to find whether a co-relation exists between in vitro dissolution and in vivo bioavailability
Subject(s)
Tablets , Biological Availability , Anti-Inflammatory Agents, Non-Steroidal , Cyclooxygenase 2 , Thiazoles/pharmacokineticsABSTRACT
Ziprasidone is a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. The initial evidence suggests an effective dosage range of 80-160 mg/day. Clinical trials suggest that the drug is an effective antipsychotic in schizophrenia and schizo-affective disorder with a beneficial effect on negative symptoms and symptoms of depression. The main adverse effects appear to be somnolence (14%) and nausea (10%). Ziprasidone has relatively fewer side effects and yet has at least equivalent efficacy for florid 'positive' symptoms compared to conventional anti psychotics. The additional serotonergic actions deliver further efficacy against 'negative' and affective symptoms of schizophrenia. Reduced effects on cognitive abilities compared to conventional anti psychotics make Ziprasidone more attractive.
Subject(s)
Antipsychotic Agents/pharmacokinetics , Humans , Mental Disorders/drug therapy , Piperazines/pharmacokinetics , Thiazoles/pharmacokineticsABSTRACT
O diabete mellitus é uma patologia de evolução contínua, com conseqüências desastrosas, devido à micro e à macroangiopatia. Diferentes grupos de medicamentos orais, com ações em regiões variadas, procuram minimizar as lesões e retardá-las ao máximo. Infelizmente ainda não temos um grupo de medicamentos que se aproxime do ideal - o qual pudesse atuar retardando tanto quanto possível as complicações crônicas. Neste sentido apresentamos um grupo de substâncias que participam em um mesmo produto e que, devido às suas ações em diferentes regiões do corpo, provavelmente poderão modificar a história evolutiva desta patologia