ABSTRACT Spironolactone (SPR) is a steroidal drug administered as a potassium-sparing diuretic for high blood pressure treatment. The drug shows incomplete gastrointestinal absorption due to its poor aqueous solubility. The physicochemical properties of SPR in crystal forms I and II suggest that differences in their aqueous solubility may lead to a lack of bioequivalence between solid-state formulations. In this study, SPR polymorphs in five batches of active pharmaceutical ingredients (APIs) from three manufacturers were characterized using powder X-ray diffraction, infrared spectroscopy, thermal analysis, and solubility measurements. SPR tablets (50 mg) were manufactured in our laboratory using API in pure form II, and API in form II contaminated with form I, which was found in a commercial batch. Physicochemical quality evaluations of the manufactured tablets, along with five SPR tablets marketed in Brazil, were performed, and results indicated differences in their dissolution profiles. In the manufactured tablets, differences were associated with the increased solubility of API in form II contaminated with form I compared to API in pure form II. In the marketed SPR tablets, the formulation composition demonstrated an important role in the dissolution rate of the drug, leading to lack of pharmaceutical equivalence among the drug products.

Estudamos a ação da amitriptilina (AMI) na síndrome de hiperatividade com déficit de atenção (SHDA). Procedeu-se a análise de 25 crianças que consultaram por SHDA, divididas em dois grupos: o grupo que fez uso da AMI (n=18) na dose de 1,6 mg/kg/dia e o grupo que fez uso de placebo (n=7). Os dois grupos foram submetidos a duas avaliações no intervalo de 30 dias, que constaram do exame neurológico evolutivo (ENE) e os subtestes números, completar fíguras e código da escala de WISC. Os resultados mostraram que a AMI produziu melhora na função persistência motora.

We studied the action of amitriptyline (AMI) in the attention deficit hyperactivity disorder (ADHD). Twenty-five children who came to consultantion for ADHD were analized, in two groups: the group which used AMI (n=18) at 1.6 mg/kg/day and the group which used placebo (n=7). Both groups were submitted to two assessments in a 30 days interval, which consisted of the evolutive neurological evolution examination (ENE) and the WISC scale subtests on numbers, drawings to be completed and the code. The results showed that the AMI produced an improvement in performance in the motor persistence tests.