In this study, the formation of caffeine/dapsone (CAF/DAP) cocrystals by scalable production methods, such as liquid-assisted grinding (LAG) and spray drying, was investigated in the context of the potential use of processed cocrystal powder for pulmonary delivery. A CAF/DAP cocrystal (1:1 M ratio) was successfully prepared by slow evaporation from both acetone and ethyl acetate. Acetone, ethyl acetate, and ethanol were all successfully used to prepare cocrystals by LAG and spray drying. The powders obtained were characterized by X-ray diffractometry (XRD), differential scanning calorimetry (DSC), thermogravimetry (TGA), and Fourier transform infrared spectroscopy (FTIR). Laser diffraction analysis indicated a median particle size (D) for spray-dried powders prepared from acetone, ethanol, and ethyl acetate of 5.4 ± 0.7, 5.2 ± 0.1, and 5.1 ± 0.0 μm respectively, which are appropriate sizes for pulmonary delivery by means of a dry powder inhaler. The solubility of the CAF/DAP cocrystal in phosphate buffer pH 7.4, prepared by spray drying using acetone, was 506.5 ± 31.5 μg/mL, while pure crystalline DAP had a measured solubility of 217.1 ± 7.8 μg/mL. In vitro cytotoxicity studies using Calu-3 cells indicated that the cocrystals were not toxic at concentrations of 0.1 and of 1 mM of DAP, while an in vitro permeability study suggested caffeine may contribute to the permeation of DAP by hindering the efflux effect. The results obtained indicate that the CAF/DAP cocrystal, particularly when prepared by the spray drying method, represents a possible suitable approach for inhalation formulations with applications in pulmonary pathologies.

The cattle tick, Rhipicephalus (Boophilus) microplus, has caused serious harm to livestock raising in Brazil, considering the costs of controlling it, loss of revenue due to smaller production of milk and meat, and damage to leather, in addition to transmitting diseases. The use of medicinal plants is considered an alternative to the recurring resistance to chemicals. Due to the need for efficient alternatives with less environmental impact, this study aimed to develop contact formulations with essential oils from the Java citronella (Cymbopogon winterianus) and clove (Syzygium aromaticum) plants and to assess in vitro the effects in different stages of the tick cycle. In the present study, concentrations from 0.5-15.0% of the essential oils incorporated in the formulations were used. The ticks from different geographical areas were treated with those formulations, and their effects on the production levels of eggs, on the larvae hatching, and their efficiency on ticks were assessed. The obtained results were compared with other commercial acaricidal products. After the 20th day of treatment, the formulations with citronella essential oil had 2.09-55.51% efficiency, depending on the concentration of the oil incorporated. The efficiency of the treatment with formulations containing clove essential oil was higher, from 92.47-100%. The results showed the acaricidal effects of the formulations tested when compared to commercial chemical products. In vivo studies should be performed in order to assess the efficiency of those formulations in the fields, aiming to use these products as an alternative for controlling cattle ticks.

RESUMO:A produção magistral do xarope de guaco, obtido a partir do extrato fluido do guaco (Mikania glomerata Spreng., Asteraceae) e comercializada na Farmácia Universitária da UFJF/MG, gerou um projeto de pesquisa com o objetivo principal de estudar a estabilidade do produto acabado, tendo como ponto de referência a determinação do teor de cumarina das amostras armazenadas em diferentes temperaturas. O método aplicado para realizar a análise do teor de cumarina presente no xarope em estudo foi espectrometria no UV com comprimento de onda de 275,4 nm. Utilizouse como veículo para efetuar as diluições da amostra uma mistura de metanol/água destilada, na proporção de 80% v/v. A curva de calibração foi obtida diluindo-se 100 mg de cumarina padrão em 100 mL da solução descrito acima, obtendo-se sete concentrações distintas com variação de 2 µg a 20 µg. Os resultados obtidos demonstraram que a temperatura de armazenamento de 45 °C foi considerada ótima para desenvolver a conversão do isômero trans em cis com subseqüente conversão deste a cumarina. Os valores de cumarina encontrados na forma farmacêutica em estudo foram de 1,19 a 1,37 mg/mL, sendo que o valor mais alto refere-se às amostras armazenadas a 45°C durante seis meses.Unitermos: Xarope, guaco, temperatura, cumarina, Mikania glomerata, Asteraceae ABSTRACT: "Coumarin content of guaco syrup stored at different temperatures". The production of guaco syrup, obtained from guaco (Mikania glomerata Spreng., Asteraceae) fluid extract, and commercialized by the University Pharmacy of the Federal University of Juiz de Fora-MG, Brazil, led to a research project whose main aim was to study the stability of the finished product, with reference to the coumarin content of samples stored at different temperatures. UV spectrophotometry (275.4 nm) was used to assess the coumarin content of the study syrup. An 80% v/v methanol/distilled water mixture was used for sample dilution. The calibration curve was constructed by the dilution of 100 mg standard coumarin in 100 ml of the aforementioned solution, with seven distinct concentrations (ranging from 2 µg a 20 µg) being obtained. The results showed the 45 °C storage temperature to be optimum for the development of trans-cis isomerization, with subsequent conversion of the latter into coumarin. Coumarin content in the studied pharmaceutical presentation ranged from 1.19 to 1.37 mg/mL, the highest value corresponding to the samples stored at 45 °C for six months.Keywords: Syrup, guaco, temperature, cumarine, Mikania glomerata, Asteraceae.vulgarmente por "guaco", "coração-de-jesus", "guacoliso", "cipó-caatinga" e "erva-de-cobra", oficializada na 1ª edição da Farmacopéia Brasileira (Brandão et al., 2006;. É uma das espécies mais estudadas sobre o aspecto Artigo

This work aimed to evaluate advertisement of baby food, rubber nipples, pacifiers and nursing bottles through newspapers as well as on TV, radio, and the internet, in order to check whether the 'Brazilian Norm for Commercialization of Food for Nursling and Children of First Infancy, Rubber Nipples, Pacifiers and Nursing Bottles' (Norma Brasileira de Comercialização de Alimentos para Lactentes e Crianças de Primeira Infância, Bicos, Chupetas e Mamadeiras -NBCAL) has been complied. Samples of all the items above were acquired at discount and department stores to check whether labeling was in compliance with the NBCAL. The development of this research as well as the analyses of commercial promotion were carried out in Juiz de Fora -state of Minas Gerais, from May to July 2006, using convenient, non-representative sampling composed of 680 pieces of advertisement. The results obtained through descriptive statistics showed that 564 of the 680 samples analyzed, or 83.0%, did not meet the NBCAL. Irregularities were detected in 100% of the samples advertised on the media and found in hospitals and drugstores; in 70.1% of the samples purchased at supermarkets, in 37% of those from medical clinics and in 86.6% of those found on the internet. The evidences showed that monitoring must be carried out continuously and educational campaigns on the importance of breast-feeding for the full development of children must be addressed to mothers, the food industry and commercial establishments.Uniterms: Publicity/baby food/evaluation. Advertisement/baby food/evaluation. Childish ware/evaluation of labeling.O presente trabalho teve como objetivo avaliar propagandas e publicidades impressas de alimentos infantis, bicos, chupetas e mamadeiras, além das veiculadas em rádio, TV e internet, para verificar o cumprimento da Norma Brasileira de Comercialização de Alimentos para Lactentes e Crianças de Primeira Infância (NBCAL). Também foi realizada a aquisição de bicos, mamadeiras e chupetas em "lojas de 1,99" e de departamento, para a verificação de rotulagem de acordo com a NBCAL. O desenvolvimento da pesquisa foi realizado no período de maio a julho de 2006, no município de Juiz de Fora, MG, mediante amostragem não representativa, de conveniência. A amostra constituiu-se de 680 peças publicitárias. Os resultados foram analisados pela estatística descritiva. Das 680 peças publicitárias analisadas, 564 (83,0%) não cumpriram a NBCAL. Foram encontradas irregularidades em 100% das amostras captadas em rádio, TV, jornais, revistas, hospitais e farmácias; em 70,1% das amostras captadas em supermercados; em 37% das amostras captadas em clínicas médicas e em 86,6% das captadas na internet. Concluiu-se que há necessidade de intensificar o monitoramento em caráter contínuo e que as ações educativas relativas à importância do aleitamento materno devem ser direcionadas para as mães, indústrias produtoras e empresas que comercializam alimentos infantis.Unitermos: Publicidade/de alimentos infantis/avaliação. Propaganda/de alimentos infantis/avaliação. U...

Leishmaniasis is a neglected tropical disease caused by protozoan parasites belonging to the genus Leishmania. Currently, the drugs available for treatment of this disease present high toxicity, along with development of parasite resistance. In order to overcome these problems, efforts have been made to search for new and more effective leishmanicidal drugs. The aim of this study was to synthesize and investigate the leishmanicidal effect of N,N′-disubstituted thioureas against Leishmania amazonensis, with evaluation of their in silico pharmacokinetics and toxicity profiles. Our results showed that different thioureas could be obtained in high to moderate yields using simple reaction conditions. Nine thiourea derivatives (3e, 3i, 3k, 3l, 3p, 3q, 3v, 3x and 3z) were active against parasite promastigotes (IC 50 21.48-189.10 µM), with low cytotoxicity on mice peritoneal macrophages (CC 50 >200 µM), except for thiourea 3e (CC 50 =49.22 µM). After that, the most promising thioureas (3k, 3l, 3p, 3q and 3v) showed IC 50 ranging from 70 to 150 µM against L. amazonensis amastigotes in infected macrophages. Except for thiourea 3p, the leishmanicidal activity of the derivatives were independent of nitric oxide (NO) production. Thioureas 3q and 3v affected promastigotes cell cycle without disturbing the mitochondrial membrane potential. Furthermore, our derivatives showed satisfactory theoretical absorption, distribution, metabolism, excretion, toxicity (ADMET) properties. These data indicate that thiourea derivatives are good candidates as leading compounds for the development of new leishmanicidal drugs.

Background: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using Gastroplus TM software. Methods and results:The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model. Conclusion: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.

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El calentamiento global y los impactos en los ecosistemas ambientales, sociales y culturales han impulsado un cambio radical en el modo de pensar, producir y circular conocimiento; el foco de la presente discusión incide en el campo del arte contemporáneo y sus implicaciones sociales, políticas, culturales; las prácticas artísticas colaborativas  contemporáneas emergen en un escenario conflictivo y mutante, en que los campos disciplinares son convocados a entrelazamientos para enfrentar la complejidad del contexto global, sus transformaciones aceleradas; desde ahí se observa la emergencia de otros modos de producir y mantener las formas de vida; OPENLAB - residencia artística procesual propone reflejar colectivamente acerca de la dimensión poético-política contemporánea a partir del água como procomún y elemento de cohesión planetária; por medio de convocatoria internacional, abierta a artistas e investigadores, son propuestos espacios de experimentación poética en co-elaboración y en red, a fin de aportar respuestas para operar entre las tensiones “glocales” alrededor de los recursos humanos, naturales, científicos y tecnológicos, proponiendo miradas poético-críticas, en contextos de sostenibilidad situada y glocalizada en el presente, prospectando futuros posibles.