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Sitagliptin is an inhibitor of the enzyme dipeptidyl peptidase-4, used for the treatment of type 2 diabetes mellitus. The crystal structure of active pharmaceutical solids determines their physical and chemical properties. The polymorphism, solvates and hydrates can influence the free energy, thermodynamic parameters, solubility, solid-state stability, processability and dissolution rate, besides directly affecting the bioavailability. Thus, the physicochemical characterization of an active pharmaceutical ingredient is required to guarantee the rational development of new dosage forms. In this context, we describe herein the solid-state characterization of three crystalline forms of sitagliptin: sitagliptin phosphate monohydrate, sitagliptin phosphate anhydrous and sitagliptin base form. The investigation was carried out using differential scanning calorimetry (DSC), thermogravimetry (TG)/derivative thermogravimetry (DTG), spectroscopic techniques, X-ray powder diffraction (XRPD) and morphological analysis by scanning electron microscopy. The thermal analysis revealed that during the dehydration of sitagliptin phosphate monohydrate (Tpeak = 134.43 °C, ΔH = −1.15 J g−1) there is a characteristic crystalline transition event, which alters the physicochemical parameters of the drug, such as the melting point and solubility. The crystalline behavior of sitagliptin base form differs from that of sitagliptin phosphate monohydrate and sitagliptin phosphate anhydrous, mainly with regard to the lower temperature of the fusion event. The melting point (Tpeak) values obtained were 120.29 °C for sitagliptin base form, 206.37 °C for sitagliptin phosphate monohydrate and 214.92 °C for sitagliptin phosphate anhydrous. In relation to the thermal stability, sitagliptin phosphate monohydrate and sitagliptin phosphate anhydrous showed a slight difference; however, both are more thermostable than the base molecule. Therefore, through this study it was possible to establish the most suitable crystalline form of sitagliptin for the development of a safe, effective and appropriate pharmaceutical dosage form.

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The aim of this study was to evaluate the chemical, antioxidant, and antimicrobial activity of the essential oils as well as the anatomy of the aerial parts from Baccharis aracatubaensis, Baccharis burchellii, and Baccharis organensis owing to the therapeutic potential of Baccharis. The volatile constituents were analyzed using GC/MS, the antioxidant activity was evaluated by oxygen radical absorbance capacity (ORAC FL ) and DPPH assays, and the antimicrobial activity by a microdilution technique. Of the 56 compounds identified, only seven (β-caryophyllene, γ-muurolene, bicyclogermacrene, β-germacrene, spathulenol, τ-muurolol, and α-cadinol) were common in the three specimens studied. Of these, γ-muurolene was found abundantly in B. aracatubaensis, while bicyclogermacrene was abundant in B. burchellii and B. organensis. The essential oils exhibited antioxidant activity in the ORAC FL (> 500.0 μmol TE g À 1 ) and DPPH assays. However, they did not exhibit any antimicrobial activity. Secretory ducts and flagelliform glandular trichomes were observed in the anatomical study of all the Baccharis species studied.

VEIGA, A.; ROSSA, L. S.; MURAKAMI, F. S. Avaliação da qualidade microbiológica de maquiagens de uso coletivo. Arq. Cienc. Saúde UNIPAR, Umuarama, v. 20, n. 3, p, 159-163, set./dez. 2016. RESUMO:O mercado de cosméticos destaca-se no Brasil por apresentar crescimento mesmo diante da crise econômica. Devido ao constante aumento na utilização desses produtos é necessário avaliar a segurança microbiológica, especialmente para produtos de uso coletivo e, portanto, com maior risco de contaminação. O objetivo do presente trabalho foi avaliar a qualidade microbiológica de amostras de cosmé-ticos para maquiagem, de uso coletivo, da cidade de Curitiba, Paraná. Foram analisadas quinze (15) amostras coletadas durante o período de janeiro a agosto de 2015. As análises microbiológicas foram realizadas segundo o Guia ABC de Microbiologia, objetivando a contagem de microrganismos viáveis totais e a pesquisa de patógenos. Quanto à contagem de microrganismos todas as amostras encontram-se dentro dos limites especificados pela legislação vigente. No entanto, três amostras apresentaram contaminação por microrganismo patogênico Staphylococcus coagulase positiva. Em indivíduos adultos saudáveis a utilização de cosméticos contaminados pode não representar sérios riscos, a menos que o organismo seja um patogênico primário, não sendo o caso do gênero Staphylococcus. Entretanto, pode representar perigo para pessoas com sistema imunológico fragilizado. Sendo assim, os conservantes utilizados para as preparações cosméticas permanecem eficazes mesmo após o seu uso coletivo, não apresentando sérios riscos a indivíduos adultos saudáveis. PALAVRAS-CHAVE: Avaliação Microbiológica; Cosméticos; Maquiagem; Uso coletivo. MICROBIOLOGICAL QUALITY EVALUATION OF PUBLIC USE MAKEUP ABSTRACT:The Brazilian cosmetics industry continues to grow despite the country's economic crisis. Due to the increasing use of these products, there is the need to evaluate their microbiological safety, especially for cosmetics of shared use regarding the risk of contamination. The aim of this study was to evaluate the microbiological quality of shared makeup samples in the city of Curitiba -Parana, Brazil. Fifteen samples were collected from January to August 2015. The microbiological investigation was performed according to ABC Microbiology Guide aiming at the total viable microorganism and pathogen count. Regarding the microorganism count, all samples were within the limits specified by law. However, tree samples were contaminated by positive coagulase Staphylococcus. This can pose danger to people with weakened immune systems. Thus, it can be concluded that the preservatives used in the preparation of cosmetics remain effective even after their shared use, and therefore, they do not present serious risk to healthy adults.

Background: Orodispersible Tablets (ODTs) are an option to facilitate the intake of pharmaceutical solid dosage forms, which dissolve in the mouth within 30 seconds releasing the drug immediately with no need for water intake or chewing. Objective: The main goal of our study is the technological development of lactose-free orodispersible tablets that contain ketoprofen. Methods: We assessed different variables during the pharmaceutical development of ODTs: compression techniques conducted after a wet granulation process, aiming to optimize the flow properties of the formulation, and a suspension freeze-drying molded in blisters. We developed three formulations for each method, each containing one of the superdisintegrants: croscarmellose, crospovidone, or starch glycolate. Result: During the production of ODTs, we performed quality control of the granulation process, since the production of pellets contributed to the enhancement of the disintegration time and content homogeneity. Quality control tests for ODTs produced by freeze-drying were also satisfactory, despite significant changes in the final physical aspect of these products when compared to that of ODTs produced by compression. In addition, the disintegration times of ODTs produced by freeze-drying were substantially higher. Furthermore, these tablets displayed greater friability and pose a challenge to the control of a standard individual weight. Conclusion: Among the superdisintegrants, croscarmellose contributed most significantly to reduce the disintegration time and to dissolve KTP effectively in 20 minutes.

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Natural products, especially plants, have been investigated as sources of new substances with antimicrobial properties. In this context, the Myrcia genus is extensively researched for presenting such activities. This work aims to evaluate the antifungal, antibacterial, and antioxidant properties of extracts and fractions of stems of Myrcia hatschbachii, also to characterize two phenolic compounds. The antibacterial and antifungal activities were assessed by using the broth microdilution method. The ethyl acetate fraction (FGA) inhibited the growth of Candida albicans at a Minimum Inhibitory Concentration (MIC) of 15.6 µg/mL, presented 40% of phenolic compounds in its composition, obtained the most significant results in antioxidant methods (DPPH, FRAP, ABTS), besides the identification of ellagic and 3-O-methyl ellagic acids by NMR. Considering the relevant antifungal activity revealed by the fraction, new studies can be carried out to encourage the continuous search for antifungal alternatives.