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The aim of this study was to evaluate the physicochemical composition and antibacterial activity of Brazilian propolis extracts from different types, concentrations, and extraction solvents and from different regions in Brazil. A total of 21 samples were analyzed, comprising 14 samples from Apis mellifera (12 green, 1 brown, and 1 red) and 7 samples from stingless bees (3 mandaçaia, 2 jataí, 1 hebora, and 1 tubuna). The analyses performed were dry extract, total phenolic content (TPC) and antioxidant activity (DPPH and ABTS). The antibacterial activity was performed by Determination of Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC). The results showed that very low levels of phenolic compounds and antioxidant activity decreased the antimicrobial activity of the propolis extracts from tubuna and jataí. However, there was no correlation between the increase in propolis concentration in the extract, and the increase in antimicrobial activity. The highest TPC and antioxidant activity was obtained for green propolis extract made with 70% raw propolis that presented similar antibacterial activity to the samples formulated with 30% or less raw propolis. The aqueous propolis extract showed lower antimicrobial activity compared to the alcoholic extracts, indicating that ethanol is a better solvent for extracting the active compounds from propolis. It was observed that the MIC (0.06 to 0.2 mg/mL) and MBC (0.2 to 0.5 mg/mL) values for Gram-negative bacteria were higher compared to Gram-positive bacteria (MIC 0.001-0.2 mg/mL, and the MBC 0.02-0.5 mg/mL). The propolis extracts that exhibited the highest antimicrobial activities were from stingless bees hebora from the Distrito Federal (DF) and mandaçaia from Santa Catarina, showing comparable efficacy to samples 5, 6, and 7, which were the green propolis from the DF. Hence, these products can be considered an excellent source of bioactive compounds with the potential for utilization in both the pharmaceutical and food industries.

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The aim of this study was to evaluate the antibacterial activity of nanoemulsions of Baccharis dracunculifolia essential oil. The volatile compounds of the essential oil were identified using gas chromatography-mass spectrometry. The properties of the nanoemulsions (droplet size, polydispersity index, pH, and electrical conductivity) were determined. The antibacterial activities of the essential oil and its nanoemulsions were evaluated using MIC, MBC, and disk diffusion. The microorganisms used were: Gram-positive bacteria (Staphylococcus aureus ATCC 25923, Bacillus cereus ATCC 14579, Streptococcus mutans ATCC 25175, and Enterococcus faecalis ATCC 29212) and Gram-negative bacteria (Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC BAA-1706, Salmonella enterica ATCC 14028, and Escherichia coli ATCC 25922). The major volatile compounds of the B. dracunculifolia essential oil were limonene (19.36%), (E)-nerolidol (12.75%), bicyclogermacrene (10.76%), and ß-pinene (9.60%). The nanoemulsions had a mean droplet size between 13.14 and 56.84 nm. The nanoemulsions presented lower and statistically significant MIC values compared to the essential oil, indicating enhancement of the bacteriostatic action. The disk diffusion method showed that both the nanoemulsions and the essential oil presented inhibition zones only for Gram-positive bacteria, while there were no results against Gram-negative bacteria, indicating that B. dracunculifolia essential oil has a better antimicrobial effect on Gram-positive microorganisms.

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Tablet scoring is a controversial but common practice used to adjust doses, facilitate drug intake, or lower the cost of drug treatment, especially in children and the elderly. The risks of tablet scoring are mainly related to inaccuracies in the resulting dose and stability problems. The aim of this article is to provide an overview of worldwide guidelines regarding tablet scoring. We found that regulatory health agencies in Mercosur countries as well as other South American countries do not have published standards addressing tablet splitting. Among the surveyed health agencies, the Food and Drug Administration (FDA) in the United States is the only one to present standards, ranging from splitting instructions to regulation of the manufacturing process. The concept of functional scoring implemented by the FDA has introduced some level of guarantee as to the ability of tablets to be split. In conclusion, technical and scientific bases are still insufficient to guide health rules on this subject, making the decision on scoring, in certain situations, random and highly risky to public health. The need for more detailed regulation is vital to ensure the safety of tablet medications.

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RESUMO A partição de comprimidos é uma prática controversa no meio da saúde. Mesmo assim, é amplamente difundida, principalmente em tratamentos envolvendo crianças e idosos, para ajustar doses, facilitar a ingestão do medicamento ou baratear o custo do tratamento medicamentoso. Os riscos dessa prática estão relacionados principalmente à imprecisão na dosagem das frações e a problemas de estabilidade no medicamento partido. O objetivo deste trabalho foi traçar um panorama das bases sanitárias que norteiam esse tema no mundo. Constatamos que as agências regulatórias de saúde dos países que integram o Mercosul, além de outros países sul-americanos, não possuem normas publicadas que tratem de partição de comprimidos. Entre as agências sanitárias pesquisadas, a Food and Drug Administration (FDA), nos Estados Unidos, é a única a apresentar normas que abrangem desde instruções para orientar o fracionamento até a regulação do processo de fabricação. O conceito de sulco funcional implementado pela FDA estabelece algumas garantias quanto à capacidade do comprimido de ser fracionado. Pode-se concluir que ainda faltam bases técnicas e científicas para direcionar as normas sanitárias acerca desse tema, tornando a decisão sobre a partição de comprimidos, em determinadas situações, aleatória e de alto risco para a saúde pública. A necessidade de regulação mais pormenorizada é vital para garantir a segurança dos usuários de medicamentos.

ABSTRACT Tablet scoring is a controversial but common practice used to adjust doses, facilitate drug intake, or lower the cost of drug treatment, especially in children and the elderly. The risks of tablet scoring are mainly related to inaccuracies in the resulting dose and stability problems. The aim of this article is to provide an overview of worldwide guidelines regarding tablet scoring. We found that regulatory health agencies in Mercosur countries as well as other South American countries do not have published standards addressing tablet splitting. Among the surveyed health agencies, the Food and Drug Administration (FDA) in the United States is the only one to present standards, ranging from splitting instructions to regulation of the manufacturing process. The concept of functional scoring implemented by the FDA has introduced some level of guarantee as to the ability of tablets to be split. In conclusion, technical and scientific bases are still insufficient to guide health rules on this subject, making the decision on scoring, in certain situations, random and highly risky to public health. The need for more detailed regulation is vital to ensure the safety of tablet medications.

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A partição de comprimidos é uma prática controversa no meio da saúde. Mesmo assim, é amplamente difundida, principalmente em tratamentos envolvendo crianças e idosos, para ajustar doses, facilitar a ingestão do medicamento ou baratear o custo do tratamento medicamentoso. Os riscos dessa prática estão relacionados principalmente à imprecisão na dosagem das frações e a problemas de estabilidade no medicamento partido. O objetivo deste trabalho foi traçar um panorama das bases sanitárias que norteiam esse tema no mundo. Constatamos que as agências regulatórias de saúde dos países que integram o Mercosul, além de outros países sul-americanos, não possuem normas publicadas que tratem de partição de comprimidos. Entre as agências sanitárias pesquisadas, a Food and Drug Administration (FDA), nos Estados Unidos, é a única a apresentar normas que abrangem desde instruções para orientar o fracionamento até a regulação do processo de fabricação. O conceito de sulco funcional implementado pela FDA estabelece algumas garantias quanto à capacidade do comprimido de ser fracionado. Pode-se concluir que ainda faltam bases técnicas e científicas para direcionar as normas sanitárias acerca desse tema, tornando a decisão sobre a partição de comprimidos, em determinadas situações, aleatória e de alto risco para a saúde pública. A necessidade de regulação mais pormenorizada é vital para garantir a segurança dos usuários de medicamentos.

Tablet scoring is a controversial but common practice used to adjust doses, facilitate drug intake, or lower the cost of drug treatment, especially in children and the elderly. The risks of tablet scoring are mainly related to inaccuracies in the resulting dose and stability problems. The aim of this article is to provide an overview of worldwide guidelines regarding tablet scoring. We found that regulatory health agencies in Mercosur countries as well as other South American countries do not have published standards addressing tablet splitting. Among the surveyed health agencies, the Food and Drug Administration (FDA) in the United States is the only one to present standards, ranging from splitting instructions to regulation of the manufacturing process. The concept of functional scoring implemented by the FDA has introduced some level of guarantee as to the ability of tablets to be split. In conclusion, technical and scientific bases are still insufficient to guide health rules on this subject, making the decision on scoring, in certain situations, random and highly risky to public health. The need for more detailed regulation is vital to ensure the safety of tablet medications.

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The medicinal plant Maytenus ilicifolia is a commonly used phytomedicine for the treatment of gastritis. The high dose required and low density of these extracts make necessary a daily intake of several capsules, hindering adherence to the medication. The purpose of this work was to develop a suitable dosage form for the administration of Maytenus ilicifolia using effervescent granules. A 23 factorial design was used to study the physical characteristics of the granules (particle size distribution, repose angle, Carr index, scanning electron microscopy and disintegration time). Moisture stability was also determined. According to the experimental design, granule size is the most important factor in determining the flow characteristics of effervescent granules. In turn, the disintegration time is controlled by the content of sodium bicarbonate present in the effervescent mixture as well as the granule size. The stability of formulations when exposed to moisture is strongly influenced by the percentage of effervescent mixture present in the vegetal granules. Precautions in handling and storage should be taken to ensure the stability of these preparations. The effervescent granules produced from Maytenus ilicifolia met the pharmacopoeial quality parameters, with appropriate mechanical and physical characteristics and proved to be a promising vehicle for plant extracts.

A planta medicinal Maytenus ilicifolia é comumente empregada como fitoterápico no tratamento da gastrite. As elevadas doses requeridas e a baixa densidade dos extratos dessa planta levam à ingestão diária de várias cápsulas do medicamento, dificultando a adesão ao tratamento. A proposta desse trabalho foi desenvolver uma forma farmacêutica adequada para administração de Maytenus ilicifolia usando granulados efervescentes. Um desenho fatorial 23 foi empregado para estudar as características físicas dos granulados (distribuição dos tamanhos de partícula, ângulo de repouso, índice de Carr, microscopia eletrônica de varredura e tempo de desintegração). A higroscopicidade das preparações também foi estudada. De acordo com o desenho experimental, o tamanho de partícula é o fator mais importante para a determinação das características de fluxo dos granulados efervescentes. Em contrapartida, o tempo de desintegração é controlado pelo conteúdo de bicarbonato de sódio presente na mistura efervescente, assim como pelo tamanho do granulado. A estabilidade das formulações quando expostas à umidade é fortemente influenciada pelo percentual de mistura efervescente presente nos granulados. Precauções de manipulação e armazenamento devem ser tomadas para garantir a estabilidade dessas preparações. Os granulados efervescentes produzidos com Maytenus ilicifolia cumprem os requisitos farmacopeicos de qualidade, com adequadas características físicas e mecânicas, provando ser um veículo promissor para extratos vegetais.

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OBJECTIVES: Benznidazole (BNZ), the primary chemotherapy agent used to treat Chagas disease, has poor aqueous solubility, which results in low bioavailability. The purpose of this work was to develop stable effervescent tablets using an inclusion complex of BNZ with cyclodextrin (CD). METHOD: In the first phase, different CDs were evaluated according to their ability to improve the aqueous solubility of BNZ. Then, inclusion complexes of BNZ in the solid state were produced by the kneading method and the complexes were evaluated using several physical-chemical assays. Finally, effervescent tablets were prepared according to a complete 3(2) factorial design. The effects of the concentration of CD and effervescent mixture on the dissolution rate and physical stability of tablets were evaluated. KEY FINDINGS: Hydroxypropyl-ß-cyclodextrin produced the greatest improvement in the aqueous solubility of BNZ, almost 20-times greater than the water system. Solid systems produced with BNZ and CD showed physical-chemical interactions and increased the drug dissolution rate, suggesting the formation of a true solid inclusion complex. Moreover, the effervescent matrix of the tablets was effective in improving the dissolution behaviour of BNZ complexed with CD. CONCLUSIONS: Effervescent tablets produced using an inclusion complex of BNZ with CD suggest a possible improvement in the bioavailability of BNZ, and this could represent a relevant advance in Chagas therapy.

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