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Considering the importance of the evaluation of quality and performance attributes of herbal medicines, this work evaluated a gynecological gel containing aroeira (Schinus terebinthifolius Raddi), which was previously registered in 2001, and is still marketed in Brazil. Using the updated guides and legislation as a basis, the product was evaluated by checking the pH, spreadability, rheological behavior, in vitro release test, ex vivo permeation and retention study using porcine vaginal mucosa in Franz diffusion cells, and histological evaluation of the porcine vaginal mucosa before and after application of the product. After the permeation study, it was verified that gallic acid (chemical marker quantified) does not cross the mucosa, therefore, it is safe for local use. In addition, the pH of the formulation is within the range considered normal for use in healthy women. Finally, the histological evaluation of the mucosa showed changes compatible with the application of tannins (major compounds of the plant), and without changes indicative of loss of tissue integrity.

A rutina (RUT) é um flavonóide encontrado em uma ampla variedade de vegetais. Possui múltiplas propriedades terapêuticas, sendo especialmente indicada como venotônico para o tratamento da insuficiência venosa crônica (IVC). Para obtenção de medicamentos compostos pela RUT ou associados com outros fármacos é necessário avaliar inicialmente a estabilidade do insumo farmacêutico ativo (IFA), a fim de garantir a eficácia e qualidade dos produtos, bem como a segurança dos consumidores. Apesar de ser um pressuposto para o registro de medicamentos, há na literatura escassez de dados referentes a estabilidade do IFA de RUT e seus produtos derivados, portanto este trabalho teve como objetivo realizar uma análise crítica das publicações que abordam essa temática. Diante da prospecção foi possível dividir as informações em três grupos: avaliação da estabilidade decorrida do processo extrativo em derivados vegetais, de sistemas de liberação desenvolvidos com a finalidade de contornar limitações físico-químicas intrínsecas da molécula e em meios reativos e condições ambientais projetados para degradar a molécula. Os resultados demonstraram que os estudos de estabilidade são desafiadores do ponto de vista técnico e analítico, uma vez que para condução dos testes de degradação forçada e desenvolvimento de métodos indicativos de estabilidade (MIEs), apesar da existência de guias, resoluções e compêndios internacionais com as diretrizes para norteamento dos ensaios, cada molécula tem uma natureza química única. Portanto é fundamental a construção de um perfil de estabilidade, a fim de propor o controle dos processos e o desenvolvimento de formulações que contenham adjuvantes que permitam a formação de produtos mais estáveis.

Terconazole (TCZ) was the first triazole antifungal drug launched in the market and has been used in the treatment of vulvovaginal candidiasis. It is also indicated to treat dermatophytosis and fungal ocular infections. However, some of the degradation products from triazole drugs have been reported to be toxic, justifying the need of further investigations about the stability of TCZ. identification of its degradation products and evaluation of their toxicity considering the new possibilities of therapeutic indications. Therefore, in this work a systematic investigation regarding photostability of TCZ was conducted. The active pharmaceutical ingredient (API) and its methanolic solution (100 µg mL

As diferenças anatômicas e fisiológicas entre os gêneros masculino e feminino podem modificar o processo farmacocinético de um fármaco e assim, interferir em sua biodisponibilidade, tornando um determinado medicamento não bioequivalente quando comparado em apenas um gênero. Dito isto, o objetivo deste trabalho foi avaliar a influência do gênero na bioequivalência de três medicamentos testes na forma de comprimido revestido: Metildopa 500 mg, Diazepam 10 mg e Butilbrometo de Escopolamina 10mg. Para tanto, os parâmetros farmacocinéticos que determinam a bioequivalência, ASC0-t, ASC0-∞ e Cmáx, foram recalculados considerando os gêneros em separado. Os estudos do Diazepam e Escopolamina foram bioequivalentes para ambos os sexos, mas bioinequivalentes quando considerado apenas o sexo feminino. O estudo de bioequivalência da Metildopa não foi bioequivalente para ambos os sexos e nem para os sexos em separado. Assim, faz se necessário ampliar as discussões sobre a forma de analisar e definir a bioequivalência de medicamentos a fim de garantir a eficiência e segurança dos tratamentos para ambos os sexos.

In order to evaluate dermal absorption during typical working conditions in family farming, the amount of dimethoate on clothing and in the stratum corneum (SC) was measured in three rural workers. This was achieved by using cotton patches on the worker’s clothes and SC quantification by the tape stripping approach. To mimic the above study, an in vitro approach was performed using Franz cells by applying dimethoate (0.4 and 1.8 μg) direct to pig skin or, on a section of cotton before contact with pig skin. The in vivo case results demonstrated the high levels and variability of agrochemicals to which these farmers are subjected, with the total potential dermal absorption between 0.87–2.85 mg/person/h and the estimated SC penetration factor (PF) between 0–54.0 and 0–28.9 % for the back of the neck and the arms respectively. This probably demonstrates the impact of correct protective clothing. For the in vitro study, the amount of pesticide retained in the SC was 52.63 ± 10.73and 135.15 ± 31.8 ng/cm2 after applying 0.4 and 1.8 μg of pesticide directly on SC, and demonstrated close agreement with the in vivo approach. Further studies performed with this and other pesticides with different characteristics will contribute to the understanding of their transport through the skin.

Chagas disease (CD) is recognized as one of the major neglected global tropical diseases. Benznidazole (BNZ) is the drug of choice for the treatment of adults, young infants, and newborns with CD., Chagas disease (CD) is recognized as one of the major neglected global tropical diseases. Benznidazole (BNZ) is the drug of choice for the treatment of adults, young infants, and newborns with CD. However, the pharmacokinetics (PK) of BNZ have been poorly evaluated in all age groups, with consequent gaps in knowledge about PK-pharmacodynamic relationships in CD. The purpose of this study was to develop and validate a bioanalytical method to quantify BNZ levels in small-volume whole-blood samples collected as dried blood spots (DBS). The analysis was performed using high-performance liquid chromatography-positive electrospray tandem mass spectrometry. PK evaluation in healthy male volunteers was conducted to verify the correlation between DBS and plasma BNZ concentrations. The calibration curve was linear from 50 to 20,000 ng · ml−1. Intra- and interday precision and bias values were less than 14.87% (n = 9) and 9.81% (n = 27), respectively. The recovery rates ranged from 94 to 100% with no matrix effect. There was no hematocrit level effect in a range of 20 to 70%. The PK results obtained from DBS and plasma were comparable (r2 = 0.8295) and equivalent to previously published information on BNZ. BNZ in DBS was stable at room temperature for more than one year. This article describes the first microsampling method for measuring BNZ levels in DBS that has the potential to facilitate broad implementation of PK in clinical trials involving adult and pediatric patients in remote areas and helps to address existing knowledge gaps in the treatment of CD.