Abstract The present study consisted in optimizing the extractive method of polyphenols and total tannins of leaves of Syzygium cumini (L) Skeels assisted by microwaves to potentiate the antimicrobial activity of the dried extract of S. cumini against sensitive and resistant strains. A Box-Behnken design that consisted of 27 experimental runs coupled with a desirability function for multiple response optimization was employed to optimize the total polyphenols content and total tannins content. Antimicrobial sensitivity tests were evaluated by obtaining the minimum inhibitory concentration, minimum fungicidal concentration and minimum bactericidal concentration in 96-well petri dishes. The optimal extraction conditions were found to be 8 min of extraction, under 300 w of microwave power, using a 1:34 g/mL solid/solvent ratio and 38% of ethanol concentration as extraction solvent. The parameter with the greatest influence in the extraction was primarily the time, followed by the potency and proportion solid/solvent. This yielded a total polyphenol content of 87.37 ± 1.85 mg TAE g-1ext and a total tannin content of 79.68 ± 1.64 mg TAE g-1 ext. All tested microorganisms were sensitive to the extract, evidencing the effectiveness of the extraction method optimization.

Abstract Syzygium cumini L. Skeels belongs to Myrtaceae family. This species has been recognized by its antidiabetic, anti-inflammatory, and antimicrobial activities. Despite ever-increasing scientific interest for this species there is no pharmacopeia method for characterization and standardization of S. cumini yet. So, toward this aim, the objective of this work was to develop an efficient analytical methodology able to determine polyphenols and tannins content from leaves hydroethanolic extract of S. cumini using Folin-Ciocalteu method by ultraviolet absorption spectrophotometry (UV-Vis). The analytical methodology was developed for the first time in the literature for leaves of this specie shown to be fast and low-cost with results expressed through tannic acid equivalent (TAE). Moreover, the methodology presented selectivity with maximum absorption at 706 nm wavelength, linearity with R2>0.99; limit of detection 0.275 µg TAE mL-1 and 0.102 µg TAE mL-1; limit of quantification 1.046 µg TAE mL-1 and 0.912 µg TAE mL-1 for total polyphenols and total tannins, respectively. Furthermore, the methodology was accurate with recover value greater than 98%, as well as exact, reproductive, and robust with coefficient of variation values less than 15% for both compounds. All the results are found within the fixed limits according to RDC 166/2017.

Cnidoscolus quercifolius Pohl is a Brazilian medicinal plant from Caatinga biome and possesses several pharmacological properties. Phytochemical investigations have attributed some of these properties to the presence of flavonoids. In this paper, we report the influence of the extraction process on the flavonoid content obtained from leaves of C. quercifolius and its antioxidant activity. A factorial design 22 was performed, using temperature and agitation as independent variables. Qualitative and quantitative analyzes of the extracts were performed by HPLC-DAD. Rutin and apigenin were identified in the extracts and chosen as analytical markers. Pareto chart and Surface response plots suggested that rutin content was increased up to 3.93 times when temperature was employed during the extraction process. However, apigenin content was significantly reduced in the method whose temperature or agitation were used (p<0.05). A higher antioxidant activity was observed in extracts whose rutin extraction was favored, suggesting that this flavonoid contributes at least in part to the antioxidant potential of the species.

This study aimed to prepare a complex of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and 6CN10, a poorly water soluble 2-aminothiophene derivative with antifungal properties, by freeze-drying technique. The complex was characterized by thermal analysis, infrared/Raman spectroscopy, X-ray diffraction and scanning electron microscopy. In addition, we used the data of the phase solubility study, 1H, and 2D NMR spectroscopy and molecular modeling in order to investigate the interactions between 6CN10 and HP-β-CD. The apparent solubility of 6CN10 with HP-β-CD increased more than 29 fold. The phase solubility assay in water at 25 ºC showed an AP-type curve, with an apparent stability constant K1:1 and K1:2 of 96 and 0.1989 M-1, respectively. The results of IR, NMR and docking indicate that 6CN10 is able to form complexes with HP-β-CD (1:1 and 1:2 stoichiometric ratios), generating the formation of inclusion and preferably, non-inclusion complexes. The antifungal activity against Cryptococcus neoformans demonstrated the superior performance of the complex (46.66 µg mL-1) when compared with the free drug (166.66-333.33 µg mL-1). The present study provides useful information for the potential application of complexation with low soluble compounds and about the type of complex formation between 6CN10 and HP-β-CD.

Própolis é uma mistura complexa, formada por material resinoso e balsâmico. Sua composição química é complexa e variada, estando relacionada com a flora de cada região visitada pelas abelhas e com o período de coleta da resina. Inclui flavonóides, ácidos aromáticos, terpenóides e fenilpropanóides, ácidos graxos e vários outros compostos. A própolis tem sido objeto de intensos estudos farmacológicos e químicos nos últimos 30 anos. Em várias partes do mundo é indicada para melhorar a saúde e prevenir doenças. Atualmente, é disponível em várias formas farmacêuticas como cápsulas, extratos, enxaguatório bucal, na forma de pó, entre outras. Ainda são necessários estudos correlacionando a composição química com a atividade biológica, definindo cada tipo de própolis com a sua aplicação terapêutica. É uma tarefa imprescindível para um mercado cada vez maior e exigente em todo o mundo.

Propolis (bee glue) is a complex mixture, formed by resinous and balsamic material. Its chemical composition is variable and complex, being related with the flora of each region visited by the bees and with the period of resins collection. Flavonoids, aromatic acids, terpenoids and phenylpropanoids, fatty acids, and other compounds are found in propolis. In the last 30 years, propolis has become subject of intense pharmacological and chemical studies. In different parts of the world it is indicated to improve health and prevent illnesses. Currently, it is available in some pharmaceutical forms as capsules, extracts, mouthrinses, powder form, among others. Indeed, studies correlating the chemical composition with the biological activity are necessary, defining each type of propolis with its therapeutic application. It is an essential task for a market ever bigger and demanding in the whole word.

Furosemida (40mg) foi administrada a 20 cães de rua (cães SRD), 10 machos e 10 fêmeas, em duas formas farmacêuicas distintas: (1) furosemida comprimido 40mg formulada na Universidade Federal de Pernambuco (UFPE-comprimido) e (2) uma formulação comercial bioequivalente produzida pelo Laboratório de Tecnologia Farmacêutica do Estado de Pernambuco (LAFEPE-furosemida). O estudo objetivou avaliar a cinética de dissolução do UFPE-comprimido para analisar o comportamento da liodisponibilidade dos comprimidos buscando a melhor formulação para uso veterinário. As concentrações plasmáticas de furosemida para determinação de parâmetros farmacocinéticos, foram analisadas por cromatografia líquida de alto desempenho (HPLC). O estudo in vitro realizado através de análises físico-químicas demonstrou que as fórmulas dos comprimidos de furosemida preencheram os requisitos farmacêuticos de acordo com USP 23 e a Farmacopéia Brasileira. Avaliações realizadas em cães da formulação UFPE-comprimidos administrados em dose única, demonstrou uma uniformidade nos níveis sangüíneos indicando estabilidade na manutenção da forma farmacêutica e eficiência na absorção do princípio ativo. Estes valores não são significativamente diferentes em relação ao limite de confiança de 5%. Em relação a concentração de máximo (Tmax) e ao tempo de biodisponibilidade global avaliados por meios de AUC, não houve nenhuma diferença considerável. O comprimido UFPE-furosemide exibiu AUC de 743.492µg/mL.h e o LAFEPE-furosemide teve uma média de 537.284µg/mL.h.

Furosemide (40mg) was administered to 20 street dogs, 10 males and 10 females, in two different pharmaceutical forms: (1) compressed furosemide 40mg formulated at the Federal University of Pernambuco (UFPE-tablet), and (2) a commercial formulation with equal bioequivalence produced by the Laboratory for Pharmaceutical Technology of Pernambuco State (LAFEPE), the LAFEPE-furosemide. The study aimed to evaluate the kinetics of dissolution of the UFPE-tablet in order to analyze the behavior of bioavailability of the best formulation for veterinary use. The plasmatic concentrations of furosemide for the determination of parameters of pharmacological kinetics were analyzed by high-performance liquid chromatographic method (HPLC). The in vitro study accomplished through physiochemical analyses demonstrated that the formulas of the furosemide tablets attained the pharmaceutical requirements in agreement with USP 23 and the Brazilian Pharmacopoeia. The evaluation accomplished in dogs with UFPE-tablets given in only dose demonstrated uniformity in blood levels indicating stability in maintenance of the pharmaceutical formulation and efficiency in absorption of the active compound. These values are not significantly different in relation to the 5% confidence limit. Regarding maximum concentration (Tmax) time and global bioavaibility assessed by AUC means, there were no considerable differences as well. UFPE-furosemide displayed 743.492µg/mL.h as AUC average value whereas LAFEPE-furosemide had an average of 537.284µg/mL.h.

O extrato de tubérculos de Operculina macrocarpa (Jalapa do Brasil) é um produto fitoterápico, com eficácia no tratamento de constipação, como laxante. A resina quantificada é extraída com solução hidroalcóolica apresentando constituintes orgânicos e inorgânicos, podendo ser dividida em duas frações principais: uma solúvel em éter, chamada de jalapina e outra, mais polar, ainda pouco estudada, denominada convolvulina. O interesse principal deste trabalho foi propor uma otimização da metodologia gravimétrica para doseamento da resina descrita na Farmacopéia Brasileira primeira edição e sua validação com o objetivo de diminuir os custos e o tempo de partição das fases. Os resultados obtidos na validação foram tratados estatisticamente por análise de variância one-way (ANOVA) e teste t de Student. O método demonstrou atender aos requisitos de boas práticas em laboratórios exigidos pela legislação brasileira em vigor, RE n° 899 de 29 de maio de 2003 da Agência Nacional de Vigilância Sanitária, sendo, portanto, sensível, exato e preciso para o doseamento do extrato de Operculina macrocarpa, conhecida popularmente como Jalapa-do-Brasil.

The tubercle extract of Operculina macrocarpa (Jalap of Brazil) is a phytomedicine, with effectiveness in the treatment of constipation, as laxative. The quantified resin is extracted with hydro-alcoholic solution, presenting organic and inorganic constituents, separable in two main fractions: one soluble in ether, called jalapina and other, more polar, still little studied, called convolvulina. The main objective of this work was to consider the optimization of the gravimetrical methodology for assay of the resin described in the Brazilian Pharmacopeia, First Edition and its validation, with the objective to diminish the costs and the partition time of the phases. The results achieved in the validation had been statistically treated by one-way Variance Analysis (ANOVA) and t test of Student. The method demonstrated to attend to the Good Manufacture Practice requirements for laboratories, demanded by actual brazilian law, RE n° 899 of May 29th of 2003 from the National Agency of Sanitary Vigilance, being therefore, sensible, accurate and precise for the assay of the Operculina macrocarpa extract, known popularly as Jalap of Brazil.

This study aimed to analyze the final fermentation culture of Bacillus sphaericus 2362, standardize it and develop an active tablet formulation for use in urban mosquito breeding sites. It was performed in three phases: analysis and standardization of a B. sphaericus fermented culture; physical, chemical, and biological analysis of the active powder (solubility, residual humidity, particle size, resting angle, flowing off time, compacted density, and biological activity against Culex quinquefasciatus larvae); and the development of fast-disintegrating tablets. Five formulations with differing compositions were developed and a UV protector was added to the selected formulation. The formulation products with or without UV protector, as well as the active powder caused 100% larval mortality from 1 day to 2 months after a single treatment under simulated field conditions. These results show that the UV protector does not affect the initial larvicide activity of B. sphaericus, nor its persistence over a period of two months.

O Lapachol é uma naftoquinona isolada de várias espécies de plantas da família Bignoniáceas, encontrado facilmente nas regiões norte e nordeste do Brasil. Conhecido por suas propriedades anticancerígenas, possui ainda antiinflamatória, analgésica, antibiótica, antimalária antitripanossoma, e antiulcerogênica. O LAFEPE® em parceria com o Departamento de Antibióticos da Universidade Federal de Pernambuco - UFPE disponibiliza o Lapachol na forma de cápsulas de 250 mg e pretende, com este trabalho, apresentar uma revisão bibliográfica sobre a segurança e eficácia do Lapachol na terapêutica de modo a proporcionar uma maior difusão de conhecimentos na sua prescrição e torná-lo medicamento de referência dentro da política de genéricos do país.