ABSTRACT Introduction: Triathlon can be considered one of the most successful endurance sports worldwide due to the wide dissemination of information, expansion of the offer of competitions, and greater popularity. Objective: To analyze Brazilian triathletes’ sociodemographic, socioeconomic, and motivational profiles. Methods: 411 triathletes participated in the study, 127 women [37.87 ± 9.34 years] and 284 men [36.02 ± 9.23 years]. Three questionnaires were sent electronically to assess sociodemographic, socioeconomic, and motivational data. In addition, descriptive analyses and statistical tests were performed to compare motivation between age, sex, and technical level groups. Results: It was found that there is a prevalence of male triathletes, amateurs, aged between 30-40 years, employed and economically favored. Amateur athletes have running as a base sport for Triathlon, and professionals start their sports career through swimming. Among the most practiced distances are the sprint Triathlon and half Ironman. Regarding motivation, women differ in the dimensions of group activity (p=0.020), emotion (p=0.002), and technical competence (p=0.007). Professional triathletes had higher scores in the dimensions of social recognition (p=0.001) and competition (p=0.001) and lower scores in the physical fitness dimension (p=0.005). Triathletes aged between 35 and 49 years had lower averages in the social recognition dimension (p=0.007), (p=0.012) and (p=0.004) and competition (p=0.028), (p=0.008) and (p=0.044) when compared to athletes aged 20 to 29 years. Conclusion: the profile of Brazilian triathletes is diverse, and differences in sex, age, and technical level impacted the motivation of the evaluated triathletes. Level of Evidence III; Diagnostic studies - Investigation of a diagnosis test; Study of non-consecutive patients, with no uniformly applied “gold standard”.

RESUMEN Introducción: El triatlón puede considerarse uno de los deportes de resistencia de mayor éxito a nivel mundial debido a la gran difusión de información, ampliación de la oferta de competiciones y mayor popularidad. Objetivo: Analizar el perfil sociodemográfico, socioeconómico y motivacional de los triatletas brasileños. Métodos: Participaron en el estudio 411 triatletas, 127 mujeres [37,87 ± 9,34 años] y 284 hombres [36,02 ± 9,23 años]. Se enviaron electrónicamente tres cuestionarios para evaluar datos sociodemográficos, socioeconómicos y de motivación. Se realizaron análisis descriptivos y pruebas estadísticas para comparar la motivación entre grupos de edad, sexo y nivel técnico. Resultados: Se encontró que existe un predominio de triatletas masculinos, amateurs, con edades entre 30-40 años, empleados y económicamente favorecidos. Los deportistas aficionados tienen la carrera como deporte base para el Triatlón y los profesionales inician su carrera deportiva a través de la natación. Entre las distancias más practicadas se encuentran el Triatlón sprint y el medio Ironman. Respecto a la motivación, las mujeres difieren en las dimensiones actividad grupal (p=0,020), emoción (p=0,002) y competencia técnica (p=0,007). Los triatletas profesionales obtuvieron puntuaciones más altas en las dimensiones de reconocimiento social (p=0,001) y competición (p=0,001) y puntuaciones más bajas en la dimensión de condición física (p=0,005). Los triatletas con edades comprendidas entre 35 y 49 años tuvieron medias más bajas en la dimensión reconocimiento social (p=0,007), (p=0,012) y (p=0,004) y competición (p=0,028), (p=0,008) y (p=0,044) en comparación con atletas de 20 a 29 años. Conclusión: el perfil de los triatletas brasileños es diverso y las diferencias de sexo, edad y nivel técnico impactaron en la motivación de los triatletas evaluados. Nivel de Evidencia III; Estudios diagnósticos - Investigación de un diagnóstico prueba; Estudio de pacientes no consecutivos, sin un “patrón oro” aplicado uniformemente.

RESUMO Introdução: O Triathlon pode ser considerado um dos esportes endurance de maior sucesso mundialmente devido à grande disseminação de informações, ampliação da oferta de competições e maior popularidade. Objetivo: Analisar o perfil sociodemográfico, socioeconômico e motivacional de triatletas brasileiros. Métodos: Participaram da pesquisa 411 triatletas, sendo 127 mulheres [37,87 ± 9,34 anos] e 284 homens [36,02 ± 9,23 anos]. Foram enviados eletronicamente três questionários que avaliam dados sociodemográficos, socioeconômicos e a motivação. Foram realizadas análises descritivas e testes estatísticos para comparar a motivação entre grupos de idade, sexo e nível técnico. Resultados: Verificou-se que há prevalência de triatletas homens, amadores, com faixa etária entre 30-40 anos, empregados e economicamente favorecidos. Atletas amadores possuem a corrida como esporte de base para o Triathlon e profissionais iniciam sua carreira esportiva pela natação. Entre as distâncias mais praticadas estão o Triathlon sprint e meio Ironman. Sobre a motivação, mulheres diferem nas dimensões de atividade de grupo (p=0,020), emoção (p=0,002) e competência técnica (p=0,007). Triatletas profissionais apresentaram maiores pontuações nas dimensões de reconhecimento social (p=0,001) e competição (p=0,001) e menores pontuações na dimensão aptidão física (p=0,005). Triatletas com idades entre 35 a 49 anos obtiveram menores médias na dimensão reconhecimento social (p=0,007), (p=0,012) e (p=0,004) e competição (p=0,028), (p=0,008) e (p=0,044) quando comparados com atletas de 20 a 29 anos. Conclusão: o perfil de triatletas brasileiros é diverso e as diferenças de sexo, idade e nível técnico impactaram na motivação dos triatletas avaliados. Nível de Evidência III; Estudos diagnósticos - Investigação de um diagnóstico este; Estudo de pacientes não consecutivos, sem “padrão ouro” aplicado de maneira uniforme.

Abstract The objective of this study is to assess the efficiency of flood control measures implemented in the Audi-União District, located on the Iguaçu River floodplain in the city of Curitiba, Brazil, by the application of hydrological-hydraulic modeling using HEC-HMS and HEC-RAS software packages. The scenarios of the years of 2014, 2024 and 2034 with return periods of 10, 25, 50 and 100 years were analyzed. It was observed that the set of hydraulic structures located upstream of Audi-União District can reduce the peak flow at the beginning of the Iguaçu River by 31.4% and the flood area by 35.1%, considering the period of return of 100 years and the land use of 2014. Regarding the measures implemented directly by the Audi-União District, it was observed that the built levee can control floods in the area, except for a small area that is not protected by the levee, in both 2014 and future scenarios. The creation of the Iguaçu Environmental Protection Area and the relocation of families, which were non-structural measures implemented in the region, also proved to be efficient, considering that these areas would suffer from flooding even for rainfall events with a period of return of 10 years.

Resumo Este estudo teve como objetivo avaliar a eficiência das medidas implementadas para contenção de cheias na região denominada Bolsão Audi-União, localizada na planície de inundação do rio Iguaçu em Curitiba-PR, mediante a aplicação de modelagem hidrológica-hidráulica utilizando os programas HEC-HMS e HEC-RAS. Foram analisados os cenários referentes aos anos de 2014, 2024 e 2034, com tempos de recorrência de 10, 25, 50 e 100 anos. Verificou-se que o conjunto de obras realizadas a montante do Bolsão Audi-União conseguem reduzir em 31,4% a vazão de pico no início do rio Iguaçu e em 35,1% da mancha de inundação ao considerar o tempo de retorno de 100 anos, considerando uso e ocupação do solo do ano de 2014. No que se refere às medidas implementadas diretamente no Bolsão Audi-União, constatou-se que o dique construído consegue conter as inundações ocorridas no local, com exceção de uma pequena área que não é protegida pelo dique, tanto no cenário de 2014 como em cenários futuros. A criação da Área de Proteção Ambiental do Iguaçu e a realocação de famílias, que foram medidas não estruturais implementadas na região, também se mostraram eficientes, tendo em vista que estas áreas sofreriam com inundações até mesmo para eventos com tempo de retorno de 10 anos.

Abstract Piper nigrum (black pepper) is used in Indian traditional medicine and its main alkaloid, Piperine (PIP), presents antioxidant, antitumor and neuroprotective pharmacological properties. This substance is insoluble in aqueous media and can irritate the gastrointestinal tract. Aiming to avoid these inconvenient characteristics and enable PIP oral administration, this study suggested the PIP microencapsulation through the emulsion-solvent evaporation method and the preparation of microparticulated tablets by direct compression. An UV-spectroscopy method was validated to quantify PIP. Microparticles and microparticulated tablets were successfully obtained and the microparticles exhibited excellent flow. The scanning electron microscopy images showed that PIP microparticles were intact after compression. The in vitro release showed a controlled release of PIP from microparticles and PIP microparticles from tablets in comparison to PIP and PIP tablets. The release profiles of PIP microparticles and the microparticulated tablets were similar. Therefore, tablets containing PIP microparticles are promising multiparticulated dosage forms because a tablet allows microparticles administration and the intact ones promote a controlled release, decreasing its irritating potential on the mucosa.

Abstract The locust bean gum (LBG) is a polysaccharide with thickening, stabilizing and gelling properties and it has been used in the preparation of pharmaceutical formulations. Hydrogels (HGs) are obtained from natural or synthetic materials that present interesting properties for skin application. This study aimed to develop HGs from LBG using indole-3-carbinol (I3C) as an asset model for cutaneous application. HGs were prepared by dispersing LBG (2%, 3% and 4% w/v) directly in cold water. The formulations showed content close to 0.5 mg/g (HPLC) and pH ranging from 7.25 to 7.41 (potentiometry). The spreadability factor (parallel plate method) was inversely proportional to LBG concentration. The rheological evaluation (rotational viscometer) demonstrated a non-Newtonian pseudoplastic flow behavior (Ostwald De Weale model), which is interesting for cutaneous application. The HET-CAM evaluation showed the non-irritating characteristic of the formulations. The bioadhesive potential demonstrated bioadhesion in a concentration-dependent manner. Permeation in human skin using Franz cells showed that the highest LBG concentration improved the skin distribution profile with greater I3C amounts in the viable skin layers. The present study demonstrated the feasibility of preparing HGs with LBG and the formulation with the highest polymer concentration was the most promising to transport active ingredients through the skin.

Abstract Triathlon, composed of swimming, cycling and running, has shown an increase in its practice in the last few years. We are currently facing one of the biggest pandemics in the world due to the new coronavirus, which directly affected the training routine and preparation for triathlon competitions. The objective of this investigation, under a qualitative methodology, is to understand what are the motivational factors for the practice of Triathlon by Brazilian athletes. The results show three emerging categories: workout schedules, tests and competitions and the impacts of the COVID-19 pandemic. The article concludes that triathletes are motivated by different reasons and trace an intimate relationship between the practice of Triathlon and their respective sports trajectories.

Resumen El triatlón, compuesto por natación, ciclismo y carrera a pie, ha mostrado un incremento en su práctica en los últimos años. Actualmente nos enfrentamos a una de las pandemias más grandes del mundo debido al nuevo coronavirus, que afectó directamente a la rutina de entrenamiento y preparación para las competencias de los triatletas. El objetivo de esta investigación, bajo una metodología cualitativa, es comprender cuáles son los factores motivacionales para la práctica del Triatlón por parte de los atletas brasileños. Los resultados muestran tres categorías emergentes: hojas de entrenamiento, pruebas y competencias e impactos de la pandemia de COVID-19. El artículo concluye que los triatletas se motivan por diferentes motivos y trazan una íntima relación entre la práctica del Triatlón y sus respectivas trayectorias deportivas.

Resumo O Triathlon, composto por natação, ciclismo e corrida, evidenciou um crescimento da sua prática nos últimos anos. Atualmente enfrentamos uma das maiores pandemias mundiais devido ao novo coronavírus, o que afetou diretamente a rotina de treinos e preparação para competições de triatletas. O objetivo desta investigação, sob uma metodologia qualitativa, é compreender quais são os fatores motivacionais para a prática do Triathlon por atletas brasileiros. Os resultados mostram três categorias emergentes: planilhas de treinos, provas e competições e impactos da pandemia de COVID-19. O artigo conclui que triatletas são motivados por razões distintas e traçam íntima relação à prática do Triathlon com suas respectivas trajetórias esportivas.

Abstract Pyrostegia venusta (Ker Gawl.) Miers, popularly known as “Cipó-de São-João”, has been used in traditional medicine for its therapeutic properties. Nanotechnology is able to enhance the pharmacological activity of plant extracts. In this context, liposomes and polymeric nanoparticles containing P. venusta ethanolic extract were developed and then physico-chemically characterized to evaluate the mutagenic/antimutagenic effects of P. venusta. In addition, transaminases and serum creatinine were biochemically analyzed for liver and renal damage, respectively. The micronucleus test was performed with male Swiss mice treated orally for 15 consecutive days with free extracts and nanostructured with P. venusta, and then intraperitoneally with N-ethyl-N-nitrosurea (50 mg/kg) on the 15th day of treatment. Micronucleated polychromatic erythrocytes (MNPCE) were evaluated in bone marrow. There was a significant reduction in the frequency of MNPCE (LPEPV = 183% and NPEPV = 114%, p < 0.001), indicating antimutagenic potential of the nanostructured extracts with P. venusta. The groups treated with only nanostructured extract did not show an increase in MNPCE frequency, and biochemical analyzes showed no significant difference between treatments. The liposomes and polymeric nanoparticles containing Pyrostegia venusta ethanolic extract showed biological potential in preventing the first step of carcinogenesis under the experimental conditions.

Abstract In the current study, nanocapsules (NC) formulations containing a co-load of clotrimazole (C), a highly prescribed antifungal drug, and diphenyl diselenide [(PhSe)2], an organoselenium compound with a promising scope of pharmacological actions, were prepared. Formulations were characterized as well as the potential toxicity, antioxidant action, and antifungal effect were assessed using in vitro techniques. The NCs were prepared employing Eudragit® RS 100 as polymeric wall and medium chain triglycerides or virgin coconut oil (CO) as core. All NC suspensions had pH around acid range, compound content close to theoretical value (1 mg/mL/drug), average diameter in nanometric range, positive values of zeta potential as well as high encapsulation efficacy and mucoadhesive property. Physicochemical stability was performed over a 30-day period and showed no modification in the aforementioned parameters to all samples. Preliminary screening of toxicological potential performed by the hen’s egg test chorioallantoic membrane technique classified the formulations as non-irritant. The DPPH radical assay revealed that nanoencapsulated compounds had superior antioxidant action in comparison to their free forms (concentration range tested 1.0-25.0 µg/mL). Importantly, the formulation composed of CO and containing C and (PhSe)2 showed the highest antioxidant potential and was selected for further investigation regarding antifungal effect against some Candida spp strains. Results of in vitro antifungal assay demonstrated that the C and (PhSe)2 co-encapsulation had a minimum inhibitory concentration (MIC) values around 60. Thus, our study supplies additional data about advantages achieved by encapsulating active compounds.

Resumo O objetivo deste trabalho foi apresentar dados sobre a eficácia de anti-helmínticos em rebanhos ovinos no Rio de Janeiro, Brasil, e discutir a interpretação do teste de redução da contagem de ovos nas fezes (TRCOF) para cada gênero de nematoide. A contagem de ovos fecais (OPG) e coprocultura pré e pós-tratamento foram realizadas para avaliar a eficácia e a prevalência geral do parasito, respectivamente. Um teste de eficácia adicional foi realizado na Fazenda # 1 após um ano do teste inicial. Resistência anti-helmíntica grave foi encontrada, não havendo sensibilidade no TRCOF em nenhuma das 22 fazendas avaliadas. No entanto, na análise das larvas infectantes observou-se que algumas drogas foram eficazes contra certos gêneros parasitários; por exemplo, o levamisol foi mais eficaz contra Haemonchus spp. e a moxidectina contra Trichostrongylus spp. No TRCOF adicional realizado na Fazenda 1, a moxidectina e o nitroxinil foram ineficazes separadamente, mas quando aplicados em combinação, foram altamente eficazes devido à sua eficácia contra Haemonchus spp. (nitroxinil) e Trichostrongylus spp. (moxidectina), respectivamente. O TRCOF visando às espécies de nematoides parasitas prevalentes nas fazendas pode possibilitar a escolha de anti-helmínticos mais eficazes.

Abstract The aim here is to present data on the efficacy of anthelmintics in sheep flocks in Rio de Janeiro, Brazil, and to discuss the interpretation of the fecal egg count reduction test (FECRT) for each nematode genus. Fecal eggs counts and pre- and post-treatment coprocultures were performed, the former to evaluate the efficacy of and the latter to determine the overall parasite prevalence. An additional efficacy test was performed at Farm # 1 a year after the initial test. Severe anthelmintic resistance was found for the flocks, with no FECRT sensitivity at any of the 22 farms evaluated. However, an analysis of the infective larvae showed that some drugs were effective against certain parasitic genera; i.e., levamisole was more effective against Haemonchus spp. and moxidectin against Trichostrongylus spp. In the additional FECRT performed at Farm # 1, moxidectin and nitroxynil were ineffective separately, but when applied in combination they were highly effective due to their efficacy against Haemonchus (nitroxynil) and Trichostrongylus (moxidectin), respectively. The use of the FECRT targeting the parasitic nematode species prevalent on farms may make it possible to choose more effective anthelmintics.

RESUMO O gladíolo é uma importante flor de corte cultivada em todo o mundo, muito apreciada para uso em arranjos florais. A crescente preocupação com a contaminação ambiental e a busca pela produção com maior qualidade, tem resultado no aumento dos estudos com o uso de insumos orgânicos e microrganismos na floricultura, destacando-se o vermicomposto e o Trichoderma sp. O presente trabalho foi conduzido com o objetivo avaliar o desenvolvimento e a qualidade de hastes florais de gladíolo em função do uso de vermicomposto e de Trichoderma sp. aplicados ao substrato. O experimento foi conduzido em casa de vegetação, de agosto a dezembro de 2015. Foram utilizados quatro tratamentos: T1 = substrato controle (50% solo e 50% substrato comercial Carolina Soil®, T2 = vermicomposto (40%) e substrato controle (60%); T3 = Trichoderma sp. adicionado ao substrato controle; T4 = Trichoderma sp. adicionado ao vermicomposto (40%) e substrato controle (60%). A variedade de gladíolo utilizada foi a Peter's Pears. As variáveis analisadas foram: altura da planta principal, índice de clorofila Falcker, comprimento e diâmetro da haste principal, comprimento do pendão, número de floretes da haste principal, proporcionalidade entre pendão e haste e tempo até o início da floração. Concluiu-se que o desenvolvimento e a qualidade das hastes florais de gladíolo foram favorecidos pelo uso do vermicomposto na concentração de 40%, adicionado ao substrato.

ABSTRACT The gladiolus is an important cut flower that is cultivated in all parts of the world, and it is very appreciated to be used in floral arrangements. The growing concern with the environmental contamination and the look for production with higher quality have resulted in increasing the number of studies on the use of organic inputs and microorganisms in floriculture, in particular, the vermicompost and the Trichoderma sp. This work was conducted with the objective to evaluate the development and the quality of gladiolus floral stems in function of the use of vermicompost and Trichoderma sp. applied to the substrate. The experiment was conducted in a greenhouse during the period of August to December of 2015. It was done by utilizing four treatments: T1 = control substrate (50% soil and 50% commercial substrate Carolina Soil); T2 = vermicompost (40%) and control substrate (60%); T3 = Trichoderma sp. added to the control substrate; T4 = Trichoderma sp. added to the vermicompost (40%) and control substrate (60%). The gladiolus variety used was the Peter's Pears. The variables analyzed were main plant height, Falker chlorophyll index, length and diameter of the main stem, tassel length, quantity of main stem florets, proportionality between tassel and stem, and time until the start of flowering. It was concluded that the development and the quality of the gladiolus floral stem were favored by the use of vermicompost in the concentration of 40% added to the substrate.

ABSTRACT Polymeric stabilizers have received attention in the preparation of nanostructured systems due to their ability to enhance formulation stability. Considering this, the objective of this work was to prepare poly(ε-caprolactone) nanocapsules using the pullulan as a polymeric stabilizer. The nanocapsules were prepared using the interfacial deposition method of preformed polymers and they were characterized in terms of pH, average diameter, polydispersity index, zeta potential, beclomethasone dipropionate content, encapsulation efficiency, photostability and drug release profiles. The formulations showed physicochemical characteristics consistent with nanocarriers for drug delivery such as: average diameter lower than 270 nm, polydispersity indexes lower than 0.2, negative zeta potential (-22.7 to -26.3 mV) and encapsulation efficiencies close to 100%. In addition, the nanocapsules were able to delay the beclomethasone dipropionate photodegradation under UVC radiation and by the dialysis bag diffusion technique, the nanocapsules were able to prolong the drug release. Thus, pullulan could be considered an interesting excipient to formulate polymeric nanocapsules.

resumo Um método simples de CLAE-FR/UV indicativo de estabilidade foi validado para a determinação do dipropionato de beclometasona (BD) em suspensões de nanocápsulas. As condições cromatográficas foram: coluna C18 fase reversa (250 mm x 4,60 mm, 5 µm, 110 Å), usando como fase móvel metanol e água (85:15 v/v) a 1,0 mL/min, com detecção UV a 254 nm. A curva de calibração foi linear no intervalo de 5,0-25,0 µg/mL com coeficiente de correlação >0,999. A precisão foi demonstrada por um desvio padrão relativo menor que 2,0%. A exatidão foi avaliada pelo teste de recuperação do BD a partir das nanocápsulas (98,03% a 100,35%). O teste de especificidade não mostrou interferência dos componentes das nanocápsulas e nem dos produtos de degradação derivados de condições ácidas, básicas e fotolíticas. Em conclusão, o método é adequado para ser aplicado na avaliação do BD puro e em nanocápsulas e pode ser empregado para o estudo de estabilidade e degradação cinética.

abstract A simple stability-indicating RP-HPLC/UV method was validated for determination of beclomethasone dipropionate (BD) in nanocapsule suspensions. Chromatographic conditions consisted of a RP C18column (250 mm x 4.60 mm, 5 µm, 110 Å), using methanol and water (85:15 v/v) as mobile phase at 1.0 mL/min with UV detection at 254 nm. The calibration curve was found to be linear in the concentration range of 5.0-25.0 µg/mL with a correlation coefficient > 0.999. Precision was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of BD from nanocapsules (98.03% to 100.35%). Specificity showed no interference from the components of nanocapsules or from the degradation products derived from acid, basic and photolytic conditions. In conclusion, the method is suitable to be applied to assay BD in bulk drug and in nanocapsules, and it can be employed to study stability and degradation kinetics.

<p>O alendronato de sódio é um fármaco da classe dos bisfosfonatos, comumente utilizado no tratamento da osteoporose pós-menopausa. Entretanto, sua administração oral está associada à baixa biodisponibilidade e irritação gastroesofágica. Este trabalho objetivou o desenvolvimento de comprimidos contendo micropartículas de alendronato de sódio por compressão direta, a fim de obter uma forma segura e eficaz. Os parâmetros avaliados foram peso médio, dureza, espessura e teor de fármaco. Estudos de liberação <italic>in vitro</italic> foram realizados utilizando fluído gástrico e intestinal simulado e o perfil de liberação foi analisado pelos modelos matemáticos de Korsmeyer-Peppas, mono- e biexponencial. Os comprimidos apresentaram peso médio adequado, espessura, dureza e teor próximo a 100%. Além disso, a formulação liberou menos de 11% do fármaco em fluído gástrico, mostrando uma boa gastrorresistência. Em pH 6,8, em torno de 100% do fármaco foram liberados em 12 h, apresentando liberação prolongada. A modelagem matemática indica que os resultados seguem a equação biexponencial. Pela análise do expoente de liberação obtido no modelo de Korsmeyer-Peppas sugere-se que a dissolução do fármaco ocorre por transporte anômalo. Concluindo, a preparação dos comprimidos microparticulados pode ser considerada uma alternativa promissora para a liberação oral do alendronato de sódio.</p>

<p>Sodium alendronate is an antiresorptive drug used for the treatment of postmenopausal osteoporosis. However, its oral administration is associated with low bioavailability and gastroesophageal irritation. This work aimed at developing tablets containing sodium alendronate-loaded microparticles by direct compression to achieve a safe and effective form. The parameters evaluated were average weight, hardness, thickness and drug content. <italic>In vitro</italic> release tests were carried out using simulated gastric and intestinal fluids, and the profiles were analyzed through the Korsmeyer-Peppas mono- or biexponential dependent approaches. Tablets presented adequate average weight, thickness, good mechanical properties and drug content close to 100%. Moreover, the formulation released less than 11% of sodium alendronate in gastric fluid, exhibiting a good gastroresistance. At pH 6.8, almost 100% of the drug was released in 12h, showing a prolonged profile. The mathematical modeling indicated that the experimental data was better fitted to the biexponential equation. Furthermore, a good correlation coefficient was obtained for the Korsmeyer-Peppas model and the release exponent suggested that the drug dissolution was driven by anomalous transport. In conclusion, the microparticulated tablets can be considered a promising alternative for oral delivery of sodium alendronate.</p>

Neste trabalho relata-se a preparação de comprimidos pela compressão direta de micropartículas contendo alendronato de sódio, utilizando o pullulan como diluente. As propriedades dos comprimidos de pullulan foram comparadas com as de comprimidos de celulose microcristalina e de lactose. Os comprimidos de pullulan mostraram baixa variação no peso médio, espessura e teor. Por outro lado, estes apresentaram altos valores de dureza comparados aos preparados com os outros excipientes. Através dos estudos de liberação in vitro pode-se observar que apenas o pullulan foi capaz de manter a gastrorresistência e as propriedades de liberação das micropartículas, o que se deve à sua capacidade de proteger as partículas do dano causado pela força de compressão. Dessa forma, o pullulan foi considerado um excipiente vantajoso para a preparação de comprimidos microparticulados.

This work reports the preparation of tablets by direct compression of sodium alendronate-loaded microparticles, using pullulan as filler. The tableting properties of pullulan were compared with those of microcrystalline cellulose and lactose. Pullulan tablets showed low variations in average weight, thickness and drug content. Moreover, these tablets exhibited a higher hardness compared to the other excipients. In vitro release studies showed that only pullulan was capable to maintain gastroresistance and release properties of microparticles, due to its ability to protect particles against damage caused by compression force. Thus, pullulan was considered an advantageous excipient to prepare tableted microparticles.

The hydrophilic drug sodium alendronate was encapsulated in blended microparticles of Eudragit® S100 and Methocel® F4M or Methocel® K100LV. Both formulations prepared by spray-drying showed spherical collapsed shape and smooth surface, encapsulation efficiencies of 85 and 82% and mean diameters of 11.7 and 8.4 µm, respectively. At pH 1.2, in vitro dissolution studies showed good gastro-resistance for both formulations. At pH 6.8, the sodium alendronate release from the microparticles was delayed and was controlled by Fickian diffusion. In conclusion, the prepared microparticles showed high encapsulation efficiency of sodium alendronate presenting gastro-resistance and sustained release suitable for its oral administration.