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Item Caracterização farmacognóstica e atividade antimicrobiana da folha e casca do caule da Myrcia rostrata DC(Universidade Federal de Goiás, 2012-02-17) Alcântara, Guizelle Aparecida de; Paula, José Realino de; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4727958Y2; Verde, Giuliana Muniz Vila; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4702170Z2; Paula, Joelma Abadia Marciano de; http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4797707D6The family Myrtaceae in Brazil is one of the most important families, comprising about 23 genera and 130 species. The specie Myrcia rostrata DC. popularly known as "folha miúda" or "guamirim chorão" is commonly found in South American forests and in some units that are part of the Federation Cerrado, as in Goias, Distrito Federal, Mato Grosso and other states. The aim of this study was to establish parameters pharmacognostic for quality control of M. rostrata and analyze the antimicrobial activity of the leaves and stem bark of this species. For this, the macroscopic description and implementation of the sections for microscopic analysis, the plant material was used fresh. As for the post microscopy, determination of volatile substances, total ash and acid insoluble, research and quantification of constituent phytochemicals, obtaining of crude ethanol extract and fractions and essential oil extraction, the shells were dried in an oven with forced circulation at 40 ° C and leaves outdoors. The gas chromatography coupled to mass spectrometry (GC / MS) was used to characterize the chemistry composition of essential oils, the test of serial broth microdilution for antimicrobial activity and Minimal Inhibitory Concentration (MIC) and High Performance Liquid Chromatography (HPLC) to obtain the chromatograms of the aqueous fractions (FAqC) and dichloromethane (FDC) from the stem bark of M. rostrata. The leaves of this species are simple menbranacea consistency, with shiny dark green on the adaxial surface dark green and opaque in the abaxial. Microscopically hypostomaticare present numerous unicellular trichomes have secretory cavities and idioblasts with prismatic crystals. The shells are curved stem and appearance of the outer surface is characterized as thick, fissured and striatum of which have dark-brown color. When examined microscopically is possible to visualize the periderm, sclereids and crystal series. Were detect in the phytochemistry essential oil, tannins, flavonoids and terpenes both the leaves and the bark of the stem. The total phenols content, tannins that precipitate proteins, hydrolysable tannins and flavonoids in the leaves were 7,53% ± 0,14, 4,65% ± 0, 65,39% ± 1,70 and 2,83% ± 0, for the stem bark were 10,06% ± 0,06, 9,60% ± 0,60, 29,53% ± 0,52 and 0,38% ± 0,009. In the analysis of essential oils from six constituencies identified spathulenol (51.39%) and globulol (6.88%) were the major components in the shell, together with the -Caryophyllene these compounds also predominated in the leaves, which were identified 32 constituents. Therefore, the sesquiterpene hydrocarbons and oxygenated sesquiterpenes predominated in the essential oils from leaves and bark of M. rostrata. In the analysis of the antimicrobial activity of essential oil extracted from leaves of M. rostrata showed moderate antibacterial activity with minimum inhibitory concentration (MIC) of 250 mg / mL for Gram (-) Enterobacter aerogenes ATCC 13048 and for all Gram (+) tested, the crude extract of leaves inhibited fungi with MIC 31.25 mg / mL for the species Candida parapsilosis ATCC 22019, Candida parapsilosis 11-a, 02 Candida albicans and Cryptococcus gattii L1, Cryptococcus neoformans ATCC 28957 and Cryptococcus neoformans L2 CIM was 15.62 mg / mL. Fractions of the leaves and stem bark tested showed the lowest minimum inhibitory concentration was FAqC against Cryptococcus neoformans ATCC 28957 (7.81 mg / mL) and Cryptococcus gattii L1 (15.62 mg / mL) and the FDC against Gram (-) Enterobacter aerogenes ATCC 13 048 (23.43 mg / mL) and against Gram (+) Bacillus subtilis ATCC 6633 (93.75 mg / mL).The results contribute to the identification of the species M. rostrata and demonstrate its potential for treating diseases caused by micro-organisms.Item Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno(Universidade Federal de Goiás, 2014-04-25) Alencar, Rodrigo Gomes de; Marreto, Ricardo Neves; http://lattes.cnpq.br/6127043775208484; Marreto, Ricardo Neves; Araújo, Adriano Antunes de Souza; Taveira, Stephânia FleuryKetoprofen is a nonsteroidal anti-inflammatory drug used for the treatment of mild to moderate pain in chronic inflammatory conditions. Due to its superior potency ketoprofen can be used in the treatment of inflammatory bowel disease (IBD). The treatment of IBD becomes safer and more effective when the drug is incorporated into colon-specific drug delivery systems. Pellets are multiparticulate solid dosage forms extensively investigated as colon-specific drug delivery systems. Pellets can be introduced into capsules or compressed into tablets. The industrial production of tablets containing pellets has several advantages when compared to the production of capsules. However, the compression of the pellets should not affect the release of the drug and the tablets should quickly disintegrate following administration. Therefore, the aim of this study was to develop tablets containing ketoprofen coated pellets for colon-specific drug release. For this, pellets were produced by extrusion and spheronization technique containing 40% (w / w) ketoprofen. Ketoprofen pellets obtained were coated with two different pH - dependent polymers derived from methacrylic acid (Opadry ® k 94 or Eudragit ® FS 30D) with weight gains of 10 or 20% (w / w). The coated pellets were then compressed under different pellets’ amounts and different compression forces. An extra- granular mixture of lactose and microcrystalline cellulose was used as compression aid. The in vitro release of ketoprofen from the systems obtained was evaluated in Bio Dis ® apparatus. The morphological and physical properties of pellets and tablets were assessed. The Eudragit ® FS 30 D coated pellets with weight gains of 10 or 20% showed higher efficiency of colon-specific delivery (94 %), however, the drug was released slowly and incompletely in conditions mimicking the pH of the colonic region. After compression of the pellets, the efficiency of colon – specific drug delivery was lowered after compression (between 20% and 61%, depending on the formulation). The lowest decrease of colon specific efficiency was observed in formulations containing lower amount of pellets, which also produced disintegrating matrices with potential for use in the topical treatment of IBD.Item Desenvolvimento de complexos de inclusão sólidos contendo carvedilol e ciclodextrina pelas técnicas de leito fluidizado e spray drying(Universidade Federal de Goiás, 2016-03-31) Alonso , Ellen Cristine Pineze; Marreto , Ricardo Neves; http://lattes.cnpq.br/6127043775208484; Marreto, Ricardo Neves; http://lattes.cnpq.br/6127043775208484; Cunha Filho, Marcílio Sérgio Soares da; Martins, Felipe TerraIntroduction: Cyclodextrins have been used in several industries segments, mainly in the pharmaceutical industry. This material has been employed in the complexation of poorly soluble drugs with the aim to increase bioavailability and effect. Carvedilol (CARV) is a poor soluble drug used in the treatment of hypertension and congestive heart failure. Its oral bioavailability is reduced to β5%, due to their low aqueous solubility and first pass effect. Because of this, it is an excellent choice to form inclusion complexes with cyclodextrins. However, the use of cyclodextrins have some limitations, once it is necessary to use a large amount in the formulation and it can cause dilution of the drug and it can result in a solid oral form with inappropriate dimensions. Therefore, different strategies have been used to enhance complexation efficiency and reduce the amount of cyclodextrin, like the combination of the effect of drug ionization and inclusion complexes. In addition, the choice of the technique used to produce inclusion complexes is very important, because it is necessary to develop economic and effective techniques, which have been easily scalable to produce inclusion complexes in the industry. Spray drying technique have been extensively studied in cyclodextrin complexation, but this method is very expensive and presents lower efficiency. On the other hand, fluid-bed granulation has been widely used in the production of solid dosage forms but the use of this technique to produce cyclodextrin inclusion complexes is not described in the literature. Objective: The purpose of this study is to produce and characterize inclusion complexes containing carvedilol and cyclodextrin, using spray drying and fluidized bed techniques, with the aim to enhance drug dissolution rate. Material and methods: Phase solubility studies were performed using various cyclodextrins, in pH 1,β and 6,8, at room temperature, during 48 hours. Binary complexes were produced by spray drying and fluidized bed techniques. FTIR spectroscopy, DSC analysis, morphology, particle size, flowability and dissolution studies were performed to characterize the inclusion complexes. Results and discussion: Hidroxypropyl--cyclodextrin Cavitron W7 HP7 had the better solubility results. Thus, binary complexes CARV: HPCD prepared by spray drying and fluidized bed techniques in pH β,β showed better results and dissolution rate was 7 and 6 folds, respectively. However, solid dispersion prepared by fluid-bed presented better flowability indicating that this technique is the most appropriate for a large-scale production of solid dosage forms. Additionally, complexes containing HPȖCD showed good dissolution rate and could be considered as one more option for CARV complexation with great performance of inclusion complex formation in solid state.Item Administração transdérmica de cloridrato de raloxifeno encapsulado em nanopartículas lipídicas: estudos de pré-formulação para seleção dos lipídeos e tensoativos(Universidade Federal de Goiás, 2017-09-26) Alves, Guilherme Liberato; Taveira, Stephânia Fleury; http://lattes.cnpq.br/0382450621383005; Taveira, Stephânia Fleury; Marreto, Ricardo Neves; Gelfuso, Guilherme MartinsIntroduction: Raloxifene hydrochloride (RLX) is a widely prescribed drug for the treatment of osteoporosis and breast cancer. However, RLX presents a low oral bioavailability (2%), being an excellent candidate for transdermal drug delivery. The aim of this work was to develop nanostructured lipid carriers (NLC) containing RLX for transdermal drug delivery. In order to choose proper excipients, a compatibility study was performed. Methodology: Compatibility study was performed with differential scanning calorimeter (DSC), thermogravimetric anaysis (TGA), derivative thermogravimetry (DTG), isothermal stress testing (IST) and solubility study. RLX quantification was performed by high performance liquid chromatography (HPLC). After choosing the excipients, CLN were obtained by the microemulsion technique. Characterization was performed for mean diameter, polidispersivity index (PdI), zeta potential, entrapment efficiency (EE%) and stability. In vitro release and permeation studies were performed in Franz diffusion cells. Results and discussion. Conclusions: Drug-excipient compatibility studies allowed the development of stable and monodisperse CLN, capable of controlling drug release and increase its permeation in the skin when compared to the non-encapsulated drug in the control formulation.Item Estudo da composição química, de atividades biológicas e microencapsulação do óleo essencial dos frutos de Pterodon emarginatus Vogel - Fabaceae ("sucupira")(Universidade Federal de Goiás, 2012-02-28) ALVES, Suzana Ferreira; CONCEIÇÃO, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; BARA, Maria Teresa Freitas; http://lattes.cnpq.br/3914164125498267The present work aimed to do the study of chemical variability, evaluating biological activities and microencapsulate the essential oil of the fruits of Pterodon emarginatus Vogel (Fabaceae). Chapter 1 presents the study of the chemical variability of essential oil from fruits of sucupira of 11 individual of the Brazilian savanna, collected from five different populations, and were identified as its chemical composition by gas chromatography coupled to mass spectrometry (GC/MS), used for data analysis to multivariate statistical tool that indicated compounds β caryophyllene and α copaene as the main discriminant of the samples studied, both of which are of greater significance. Chapter 2 describes the antimicrobial activity and chemical composition of total oil of the fruits of sucupira, four samples being analyzed, three of the city of Jussara GO and one of region of Jaciara MT. The oils tested showed good antimicrobial activity against bacteria Gram positive (Gram (+)) and moderate activity against Enterobacter aerogenes ATCC 13048. Chapter 3 describes the process of obtaining microcapsules containg essential oil (OE) of sucupira employing the technique of spray drying and the development and validation methodology for quantification of the compound β caryophyllene. Were used gum Arabic and maltodextrin as wall material and prepared five different dispersions (Emulsion 1-E1, Emulsion 2-E2, Emulsion 3-E3, Emulsion 4-E4 and Emulsion 5-E5) which then were atomized in spray dryer. The results show that the drying condition most appropriate was sprinkler beak of 1,2 mm of diameter, power flow the emulsion in system of 4 mL/min, inlet temperature of 160ºC, air flow of 40 L/min e and pressure of 60 psi. Among the emulsions, E2 was standardized with adequate proportion of essential oil and wall materials, by presenting microcapsules (MOE) for having thick-walled, with a pronounced retention of essential oil, spherical morphology and low hygroscopicity. The method developed and validated proved to be linear, precise, acuurate and robust. Chapter 4 presents the evaluation of biological activities of antimicrobial essential oil of PES-01 employing the technique of broth microdilution and antinociceptive and anti-inflamatory activities performed to the microcapsules with the essential oil. The models of pain induced by formalin and hot plate were used to assess the antinociceptive activity and the model of carrageenan-induced pleurisy and Evans blue for evaluation of anti-inflamatory activity. The OE has weak antimicrobial activity (500 μg mL-1) against bacteria Gram (+) and against the fungi of the genus Cryptococcus was inactive against S. aureus ATCC 25923, against bacteria Gram (-) and against the fungi of the genus Candida. OE reduced by 61,54% (300 mg kg-¹) of the reactivity to pain. The MOE reduced 40,87% (1,0 g kg-¹) and 41,57% (2,0 g kg-¹) in first phase of the test formalin-induced pain, suggesting, anti-nociceptive activity. The 2nd phase of the test, the essential oil inhibited 52,35% of the pain related to inflammatory mediators and the microcapsules decreased from 25,86% - 55,60% of the pain. MOE at a dose of 1,0 g kg-¹ showed anti-nociceptive activity in hot plate model, suggestion central analgesic activity. In the arrageenaninduced pleurisy the MOE reduced 25,44% of the complete migration of leukocytes and significantly decreased the concentration of Evans blue in 24,18%, which demonstrates important anti-inflamatory activity.Item Desenvolvimento de modelos de QSAR e análise quimioinformática da sensibilização e permeabilidade da pele(Universidade Federal de Goiás, 2014-03-17) Alves, Vinícius de Medeiros; Andrade, Carolina Horta; http://lattes.cnpq.br/2018317447324228; Andrade, Carolina Horta; Ferreira, Elizabeth Igne; Camargo, Ademir J.Repetitive exposure to a chemical agent can induce an immune reaction in inherently susceptible individuals that leads to skin sensitization. Although many chemicals have been reported as skin sensitizers, there have been very few reports analyzing the relationships between their molecular structure and the sensitization potential including the connection to skin permeability, which is widely considered to be mechanistically implicated in sensitization. In this study, we have compiled, curated, and integrated the largest publicly available datasets related to chemically-induced skin sensitization and skin permeability. Unexpectedly, no correlation between sensitization and permeability has been found. Predictive QSAR models have been developed and validated for both skin sensitization and skin permeability using a standardized workflow fully compliant with the OECD guidelines. The classification accuracies of QSAR models discriminating sensitizers from non-sensitizers were 0.68-0.88 when evaluated on several external validation sets. When compared to the predictions generated by the OECD QSAR Toolbox skin sensitization module, our models had significantly higher prediction accuracy for the same sets of external compounds as evaluated by Positive Predicted Rate and Negative Predicted Rate as well as Correct Classification Rate. We have also developed QSAR models of skin permeability measured quantitatively. Cross-species correlation between human and rodent permeability data was found to be low (r²=0.44); thus, skin permeability models were developed using human data only and their external accuracy was q²ext = 0.87 (for 62% of external compounds found within the model applicability domain). Skin sensitization models have been employed to identify putative chemical hazards in the Scorecard database of possible skin or sense organ toxicants that should be regarded as primary candidates for the experimental validation.Item Avaliação da atividade antioxidante, hipotensora e vasodilatadora da Jabuticaba, Myrciaria cauliflora Berg.(Universidade Federal de Goiás, 2014-09-30) Andrade, Daniela Medeiros Lobo de; Rocha, Matheus Lavorenti; http://lattes.cnpq.br/7459866708740096; Rocha, Matheus Lavorenti; Bonaventura, Daniella; Bara, Maria Teresa FreitasThe research and the use of medicinal plants as therapeutic agents has been increasing in recent years and the jabuticaba (Myrciaria cauliflora) has occupied a favorable place in this segment by presenting biological properties due to their high antioxidant activity due to the presence of phenolic compounds. The aim of this study was to investigate the phytochemical characterization of EHAJ, evaluate the antioxidant potential of HAEJ and evaluate the influence of HAEJ on hemodynamic parameters in rat (in vivo) and the mechanisms involved in variation in vascular tone caused by HAEJ in aortas isolated of rat (in vitro). The quantification of the phenolic compounds in HAEJ was performed by a method that is based on the complexation of phenolic compounds present in the solution of ferric chloride (FeCl3) as measured by a spectrophotometer and ellagic acid quantitation was performed by analysis high performance liquid chromatography (HPLC). The phytochemical characterization of HAEJ was evaluated considering only one methodologie (mass spectrometry - ESI-MS) and antioxidant activity of HAEJ was evaluated considering two different methodologies (DPPH and differential pulse voltammetry - DPV). To achieve the experimental protocols in vivo, were inserted with the animals anesthetized, catheters in the right femoral vein and artery, and flow probes around the aorta for infusion of EHAJ, check blood pressure, heart rate and aortic blood flow, respectively. Besides the pressure was checked the vasorelaxant effect of HEAJ in preparations of isolated rat aorta pre-contracted with vasopressor agents. The concentration of nitric oxide produced by the endothelial cells in the presence of HEAJ was also evaluated by flow cytometry. Intravenous infusion of HEAJ (0.12 to 0.96 mg / kg) produced dose-dependent increase in aortic blood flow hypotension. In isolated arteries pre-contracted with contractile agonist, HEAJ induced concentration-dependent relaxation which was potentiated in preparations with intact endothelium (E+) (120μg/ml) as compared with preparations devoid of endothelium (E-) (1.92 mg / mL). And preparations pretreated with L-NAME, ODQ and MDL-12,330A reduced the relaxation caused by HEAJ, whereas pretreatment with diclofenado, atropine and propranolol did not alter the activity of HEAJ. In E- preparations pretreated with TEA, 4-AP, glibenclamide and ODQ, relaxation caused by HEAJ was reduced, while the clotrimazole pretreatment with CPA and does not alter the activity of HEAJ. Furthermore, HEAJ was able to decrease phenylephrine and KCl induced contractions. These findings suggest that the hypotension associated with HEAJ induces vascular relaxation; also suggests the involvement of such pathways cGMP / sGC and cAMP / AC and finally the involvement of potassium channels and calcium channels, this relaxation.Item Investigação da atividade antitumoral in vitro e in vivo da Eugenia dysenterica DC. (MYRTACEAE)(Universidade Federal de Goiás, 2011-08-30) ANDRADE, Wanessa Machado; PAULA, José Realino de; http://lattes.cnpq.br/3191837532986128; BOZINIS, Marize Campos Valadares; http://lattes.cnpq.br/6157755243167018Item Determinação de fármacos fenólicos em produtos farmacêuticos utilizando um biossensor de polifenoloxidase, obtida de extrato bruto do fruto da jurubeba (Solanum paniculatum L.)(Universidade Federal de Goiás, 2018-03-05) Antunes, Rafael Souza; Gil, Eric de Souza; http://lattes.cnpq.br/3218622824233303; Lopes, Flávio Marques; http://lattes.cnpq.br/1423301895802989; Lopes, Flávio Marques; Santiago, Mariângela Fontes; Alves, Virgínia FariasThe use of plant enzymes for analytical purposes is increasing every day, especially in the field of biotechnology linked to the development of new and more specific analytical instruments. In this way, the development of biosensors has been increasing since these allow the measurement of the analyte of interest to be performed by the selective transduction of a parameter of the target-analyte reaction that can be monitored. For this reason, the biological element that makes up the instrument, becomes an essential component for its construction. Polyphenoloxidase is an enzyme that catalyzes the conversion of a phenolic compound to a quinone, which can be reduced electrochemically and thus allows the detection (quantification) of the analyte of interest. This enzyme is widely distributed in plants and is widely used in the production of biosensors and the selective evaluation of phenolic drugs in pharmaceutical formulations and total phenols in industrial effluents. The polyphenoloxidases in this specific work were extracted from the fruit of Jurubeba (Solanum paniculatum L.) and used in the development of carbon paste electrochemical biosensors in the determination of phenolic drugs, such as paracetamol, ascorbic acid, salicylic acid and or methyldopa. Under experimental conditions the effect of the amount of enzymatic extract in the carbon paste ranging from 50 to 200 μL and the optimum pH of 3.0 to 9.0 using the differential pulse voltammetry technique was investigated. After optimization, the intermediate precision of the biosensor was tested through its reproducibility through the tests of repeatability, time of conditioning, stability and linearity. Soon after, used in the determination of the drugs, obtaining a better response in the detection of paracetamol, in this way, the calibration curve was realized and consequently applied in the determination of paracetamol of commercial samples in tablets. The biosensor had a linearity in the range of 5 to 245 μM, with a detection limit of 3 μM. The polyphenoloxidase extracted from the fruit of Jurubeba showed peculiar characteristics that it provided in the technological development of biosensors with application in the quality control of phenolic drugs, exhibiting high sensitivity, satisfactory selectivity, good repeatability and adequate stability.Item Desenvolvimento e avaliação de pellets contendo extrato de Pothomorphe umbellata (pariparoba) via extrusão esferonização(Universidade Federal de Goiás, 2011-08-31) Araújo Júnior, César Aparício de; Marreto, Ricardo Neves; Lima, Eliana Martins; http://lattes.cnpq.br/7248774319455970; Lima, Eliana Martins; Cunha Filho, Marcílio Sérgio Soares da; Marreto, Ricardo Neves; Taveira, Stephânia FleuryPothomorphe umbellata (L.) Miq. Piperaceae is known in Brazil as "caapeba", "caapeba North" or "Pariparoba" being widely used as an analgesic, anti-inflammatory and antispasmodic. According to scientific studies, 4-nerolidylcatechol (4-CN) is the main secondary metabolite of P. umbellata, has antioxidant activity greater than that of vitamin E. The incorporation of the extracts of P. umbellata (L.) Miq. in solid dosage forms is an interesting strategy to enable its use as an oral antioxidant and stabilizing its active labile 4-NC. Pellets are oral dosage forms which have good flow properties due to their spherical shape, narrow size distribution, in addition, the pellets allow to obtain uniform dispersion of doses of drug and incorporation of large amounts of active substances incompatible in the same pharmaceutical form. The objective of this study was to obtain an extract of P. umbellata, develop and characterize a multi-particulate solid dosage form and evaluate the stability of the developed formulations containing 4-NC. The roots of the plant material of P. umbellata was subjected to analysis of content, residual moisture, determination of swelling index, total ash content and granulometric determination. The identification of plant constituents of the sample was made by thin layer chromatography (TLC). Obtaining the hydroalcoholic extract was made by percolation. Quantitation of 4-NC was performed by High Performance Liquid Chromatography (HPLC-UV-Vis). The analytical method was validated for the parameters required in Resolution N°. 899, ANVISA. The determination of antioxidant activity of the isolated 4-NC and the percolated was evaluated using UV-Vis spectrophotometer using a technique that measures the activity of scavenging free radical 2,2-diphenyl-1-picril-hydrazyl (DPPH •). The pellets were produced by extrusion technique / spheronisation using granulation liquid consisting of the percolated, colloidal silicon dioxide and polysorbate 80. The excipients were microcrystalline cellulose, lactose and hydroxypropyl methylcellulose (HPMC). The drying of the pellets was done in an oven and fluidized bed coating. HPMC, povidone and copolymer (polyvinyl alcohol polyethylene glycol graft copolymer) were tested in the polymer coating. Accelerated photostability study was performed according to standards described by the ICH International Conference on Harmonisation evaluating 4-NC degradation in the extraction solution (percolated) and the solid dosage form (uncoated and coated pellets). The pellets were characterized by size distribution, morphology and friability. The external morphology of the pellets was evaluated through a stereomicroscope and the thickness of the coating was observed by Scanning Electron Microscopy (SEM). The result obtained for the moisture content was 6.33 ± 0.305% for total ash content: 8.25% ± 0.61 and swelling index of 3.30 ± 0.87mL and an average particle size of the powder was 170.26μm. The analytical method for 4-NC was linear in the range 10 to 200µg/mL. LQ and LD were calculated 1.42 and 0.42 µg/mL. The accuracy showed less than 5.0% relative standard deviation (RSD). The percolation process was efficient in the extraction of 4-NC. The production of pellets from the extrusion technique/spheronisation was presenting a satisfactory product was uniform with an average size of 1000 μm. In the study of antioxidant activity, the effective concentration (EC50) value found for the isolated 4-NC and present in the percolated was about two times more potent than vitamin E. In the study of photostability of 4-NC present in the coated pellets, the copolymer coating was used in which offered more protection to the active 4-NC against photodegradation. Given the impossibility of obtaining solid dosage forms with pure active, the use of the extract containing the 4-NC is considered more advantageous since the pharmaceutical technology can improve the stability of the asset against degradation.Item Perfil epidemiológico e fatores associados à síndrome respiratória aguda grave em Goiás, no período de 2013-2018(Universidade Federal de Goiás, 2020-09-02) Araujo, Kamilla Lelis Rodrigues de; Silva, Lara Lívia Santos da; http://lattes.cnpq.br/3374527511007494; Ternes, Yves Mauro Fernando; http://lattes.cnpq.br/3417780592064501; Silva, Lara Lívia Santos da; Reis, Angela Adamski da Silva; Siqueira Júnior, João BoscoSevere Acute Respiratory Syndrome (SARS) is a condition that, in addition to classic symptoms of influenza, shows signs of worsening with high morbidity and mortality. Thus, is a major concern for public health, being a disease of epidemiological importance, thatmust be notified and investigated. Therefore, the aim of this study was analyze the epidemiological profile and associated factors of SARS reported in the state of Goiás, between 2013 to 2018. This is a retrospective cohort study, with data obtained from the National disease notification system - Influenza Web. Logistic regression analysis was performed to verify the association between death and ICU admission and exposure variables by using the SPSS 25.0 statistical package program. Between 2013 and 2018, 4,832 cases of SARS were reported in Goiás. During the analyzed period, the majority of cases was attributed to Influenza virus (A or B), mainly Influenza A (22.3%), with predominance of pandemic H1N1 Influenza 2009 subtype H1N1pdm09 (17,9%). Among the variablesrelated to ICU admission, longer time to start antiviral treatment in days wasassociated with an increase in hospitalization while the absence of previousinfluenza vaccination, longer time to start antiviral treatment and older age wereassociated with deaths. Thus, this study showed a high frequency of SARS in the state of Goiás between the years 2013 and 2018, with the Influenza A virus(H1N1pdm09) being the main etiological agent. Among the factors related toadmission to the ICU and death, the time of initiation of treatment with antiviral, vaccination status and age of the patientwere observed, which highlights theneed for constant monitoring of the epidemiological situation of this disease, inorder to adopt public health measures for prevention and control.Item Biotransformação in vitro de novos candidatos a protótipos de fármacos antitumorais N-fenilpirazóis(Universidade Federal de Goiás, 2014-02-28) Araujo, Kelly Carolina Frauzino; Oliveira, Valeria de; http://lattes.cnpq.br/6300240031300604; Oliveira, Valéria de; Vaz, Boniek Gontijo; Santos, Pierre Alexandre dos; Menegatti, RicardoThe "Microbial Models of Mammalian Metabolism" represents an alternative to use of animals on metabolism studies. Introduced in the 70s this model, also called biotranformation, has several advantages for their application as low cost, reduction of animals for experimentation and and higher number and range of metabolites produced. 1-(4-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)piperazin-1-yl)ethanone (LQFM030) and 4-((1-(4-chlorophenyl)-1H-pyrazol-4-il)methyl)piperazin-1-ethyl carboxylate (LQFM018) compounds were synthesized by molecular simplification of a series of compounds with chronic myeloid leukemia antiproliferative activity already described, the Nutlins prototypes. This study aims to produce a probable human metabolites of LQFM 030 and LQFM 018 by microbial biotranformation with filamentous fungi. To do so, analytical methodologies were developed by thin layer chromatography and high performance liquid chromatography in order to monitor metabolites production. After perform a screening of tem microorganisms Mortierella isabellina NRRL 1757 strain was selected to obtain metabolites on a larger scale. Incubations were carried out with 100 mL of glucose culture medium in each flask . At the end of incubation (96 h) extraction and purification of possible metabolites was performed . In an independent assay with LQFM 030, ketoconazole (10, 20 and 30 mg) was added to inhibit P450 cytochrome . In another test 1 mL of ethanol was added every 24 hours to induce cytochrome totaling 96 hours of incubation. To evaluate the best time to finalize incubation , an experiment was conducted in 168 hours with different concentrations of the substrate, 0.25 mg / mL and 50 mg / mL. A possible role of CYP 3A was evidenced by the inhibition caused by ketoconazole addition, that can inhibit the formation of N-oxide metabolite in LQFM 030 biotransformation. Ethanol addition does not induce LQFM 030-N-oxide production, but was able to induce other metabolites formation. The best time to end LQFM 030 incubation was defined as 168 hours and 0.25 mg/mL concentration.Item Perfil farmacoterapêutico de adolescentes usuários de um centro de atenção psicossocial álcool e drogas infanto juvenil do estado de Goiás(Universidade Federal de Goiás, 2017-05-30) Araújo, Sandra Hernandez Morais de; Lopes, Flavio Marques; http://lattes.cnpq.br/1423301895802989; Dewulf, Nathalie de Lourdes Souza; http://lattes.cnpq.br/1244479719591748; Dewulf, Nathalie de Lourdes Souza; Garrote, Clévia Ferreira Duarte; Cunha, Luiz Carlos; Ferreira, Tatyana Xavier Almeida Matteuci; Santos, Thalyta Renata AraújoIntroduction: The use of Psychoactive Substances (PS) brings problems in several areas of the subject's life such as: health, psychological and social. Epidemiological studies show that it is in the passage from childhood to adolescence that the use begins. In Brazil, the treatment is preferentially done in the Centers of Psychosocial Care and in them are offered psychosocial and pharmacological interventions and the combination of them. Pharmacological interventions can be used to stabilize, detoxify, ameliorate withdrawal symptoms and prevent relapse. The pharmacist plays an important role in the safe and effective use of medicines in children and adolescents, since it can prevent identifying, evaluating and intervening in problems related to pharmacotherapy. Objective: to analyze the use of drugs by users of the Psychosocial Care Center Alcohol and Drugs Infanto Juvenil 24 hours (CPCAD adi III). Methodology: an analytical and quantitative cross-sectional study, carried out by reviewing medical records. The medical records of users who were younger than 18 years of age and with prescription of medicines were included and the medical records that were not filled out were excluded. Potential drug interactions (PDI) were analyzed using the Micromedex® and Medscape® database. Descriptive and bi-and multivariate logistic regression analyzes were performed considering a statistically significant relationship p≤0.5. Results: Of the 159 records used in the study, 71.7% were male subjects with mean age of 16 ± 1.9 years, incomplete elementary schooling (88%) and the search for treatment occurred in 55, 3% by judicial measure. Among the diagnostic hypotheses, the most frequent were mental and behavioral disorders due to the use of multiple drugs and the use of other psychoactive substances (F19) 34.9% and mental and behavioral disorders associated with the use of cannabinoids (F12) With 17.2%. The age of first use of SP was on average 12.4 ± 1.90 years. The most used PS was Cannabis (37.2%). The most prescribed drugs were the N03A (antiepileptic) 39.94% and N05A (antipsychotic) 34.83%% groups. A total of 815 PDI were found per type of interaction, 352 drugcannabis, 139 drug-ethanol, 125 drug-foods, 99 drug-tobacco, 83 drug-drug, and 17 drug-cocaine. Regarding the severity of the PDI found, 59.4% were moderate, 23.8% were secondary, 15.7% were serious and 1.1% were contraindicated. The drugs that presented the most PDI were chlorpromazine (32.3%) and diazepam (19.6%). Conclusion: the adolescents were the majority of males, the diagnostic hypothesis that had the highest frequency was that of mental and behavioral disorder due to the use of SPA (F-19). The use of PS was on average at 12 years of age and the most consumed PS was marijuana. The most commonly prescribed drugs were valproic acid (30.63%) and chlorpromazine (20.72%). It was found of 815 PDI with 59.4% classified as moderate. The factor involved in polypharmacy was total PDI and among the factors involved in the occurrence of total PDI were: being studying and the amount of diagnostic hypothesis. In view of the high PDI index, the relationship with polypharmacy and a high number of diagnostic hypotheses, it is necessary to increase the attention of health professionals regarding the topic and the development of protocols to support decision making.Item Ação da formulação mucoadesiva contendo Bidens pilosa L (Asteraceae) sobre a mucosite intestinal induzida por 5- fluorouracil em camundongos(Universidade Federal de Goiás, 2013-08-27) Ávila, Paulo Henrique Marcelino de; Valadares, Marize Campos; Bozinis, Marize Campos Valadares; Fuiza, Tatiana de Sousa; Mendonça , Elismauro Francisco deThe gastrointestinal mucositis is a side effect caused by anti-cancer chemotherapy. Among the drugs used in antineoplastic therapy 5-fluorouracil (5-FU) deserves special attention since the incidence of intestinal mucositis is 80% on treated patients. Despite many studies on intestinal mucositis induced by chemotherapy has been carried out, there aren't effective methods for treating intestinal mucositis, only palliative measures. Moreover, several studies reported anti-inflammatory and immunomodulatory activity of Bidens Pilosa L (BPL). Objective: To investigate the action of BPL in intestinal mucositis induced by 5-FU in mice. Methods: in this study, male Swiss mice were given doses of BPL (75, 100 and 125 mg / kg) and vehicle formulation administered orally (gavage) for 6 days, while doses of 5-FU (200 mg / kg ) were administered (intraperitoneal) from the 4th to 6th day (except in the groups treated with vehicle and formulation of BPL). On day 7, the mice were euthanized and the portion instestinal of each animal was extracted to perform the histomorformetria; expression analysis of Bax, Bcl2 p53 and Ki67 by immunohistochemistry analysis of the inflammatory process through the activity of the enzyme myeloperoxidase (MPO), and evaluation lipid peroxidation by determination of levels malondialdehyde (MDA). It is importantly to note that only the dose of BPL 100 mg/kg which showed better results in the analysis weight and histomorphometric , was chosen to make the immunohistochemistry, MDA and MPO assays.Results:The doses of BPL 75, 100 and 125 mg / kg showed reduce damage triggered by 5-FU in the intestinal mucositis. However the dose of 100 mg / kg was presented the best results in terms of reduction in body mass, as well as morphometric and histological changes induced by 5-FU. Furthermore it was found that treatment with only 3 doses of BPL (75, 100 and 125 mg / kg) caused no toxicological change. It was also found that the expression rate between Bax and Bcl2 were lower in the 100 mg / kg of BPL. Moreover, the dose of 100 mg / kg of BPL showed proliferative effect with increased expression of Ki67 and reduction of inflammatory infiltrate and lipid peroxidation intestinal tissue Conclusion: The results demonstrated that BPL reduced overall damage by 5-FU in intestinal mucositis induced in mice.Item AVALIAÇÃO DA TOXICIDADE PRÉ-CLINICA DO LÁTEX E DO EXTRATO ETANÓLICO DAS FOLHAS E DE Synadenium umbellatum PAX.(Universidade Federal de Goiás, 2008-03-12) AZEREDO, Flaubertt Santana de; CUNHA, Luiz Carlos da; http://lattes.cnpq.br/6349547031976679Item Estudo do efeito antinociceptivo e/ou anti-inflamatório das folhas de Spiranthera odoratissima A. St.-Hil. (Manacá). -Possível mecanismo envolvido(Universidade Federal de Goiás, 2010-08-30) BARBOSA, Daniela Borges Marquez; COSTA, Elson Alves; http://lattes.cnpq.br/2607893423583912Spiranthera odoratissima A. St.-Hil. is popularly known as Manacá and it is a native plant of the Brazilian Savanna Cerrado, and it can be found in the states of Mato Grosso, Goiás, Minas Gerais and Bahia. In the folk medicine this plant is used as an appetite stimulant and to treat rheumatism, abdominal pain, headache, muscle pain, stomach and liver dysfunction, kidney infections and urinary retention. The hydromethanolic fraction was obtained from the ethanolic extract of Spiranthera odoratissima leaves. According to phytochemical screening this fraction contains anthraquinones, tannins, flavonoids and coumarins. This fraction showed antinociceptive activity in the acetic acid-induced writhing method and the involvement of central antinociceptive mechanisms was discarded with the hot plate test, since the reduction in the latency to pain was not observed. The major subfraction isolated from the hydromethanolic fraction (sub-Fr10-28) showed antiinflammatory activity in different methodologies. Both hydromethanolic fraction and sub-Fr10-28 contain tannins able to inhibit the activity of phospholipase A2 enzyme, and subsequently inhibiting the production of arachidonic acid and preventing the production of eicosanoids such as prostaglandins, thromboxanes and leukotrienes by lipoxygenase and cyclooxygenase enzymes participation. These eicosanoids are important mediators for the maintenance of inflammatory process. Concluding, the analgesic effect of this plant may be due to an anti-inflammatory action, and this antiinflammatory action could be the result from the blockage of the phospholipase A2 enzyme.Item Utilização do óleo obtido de resíduos agroindustriais de goiaba (Psidium guajava L.) na nutrição de poedeiras comerciais(Universidade Federal de Goiás, 2014-10-31) Barbosa, Nathalia Pedroso; Stringhini, Jose Henrique; http://lattes.cnpq.br/8505634095383289; Mello, Heloísa Helena de Carvalho; http://lattes.cnpq.br/5510965166352073; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Conceição, Edemilson Cardoso da; Bara, Maria Teresa Freitas; Café, Marcos BarcellosPsidium guajava L. is a plant originated in Mexico, belonging to mytarceae family. The guava fruit is growth in economic value for the production of derivatives in the Brazilian agribusiness. However the use of guava pulp generates waste discarded in the environment, without the correct use, ie an environmental liability. The guava residue consists of pulp, peel, but mainly seeds. Yet is not described in the literature depth studies on its chemical composition or a suitable waste recovery. Thus, this study aimed to characterize the dust of organic residues of guava (donated by Food Predilecta ® - Matão, São Paulo), followed by obtaining the ethanol extract of the percolation method. The ethanol extract was characterized as the fatty acid profile, density and acid number and came to be known as: Powder oil waste processing Guava (OWG) from the OWG obtained the volatile fraction by hydrodistillation and characterization was carried out by gas chromatography coupled to mass spectrometry (GC / MS), followed by characterization of β-caryophyllene marker for high performance liquid chromatography (HPLC) and the identification of ORG constituents by GC / MS. We evaluated the antioxidant potential by free radical trapping methods 2,2-diphenyl-1- picryl hydrazyl (DPPH) and the capture of ferrous sulfate (FRAP). And finally, evaluated the implementation of the OWG, in laying hens Bovans White to verify the performance, posture, egg quality, digestibility and chemical composition of eggs and lipid oxidation of gems. The analysis of the volatile fraction of the OWG by GC / MS resulted in the identification of 25 compounds having as the major, the β-caryophyllene with 21.15%. Thus, an analytical HPLC method was revalidated in accordance with the criteria of Resolution 899/03 of ANVISA for quantification of β-caryophyllene (26.26%) in the OWG, to then be used for monitoring and characterization of OWG. Moreover, GC / MS, were identified in OWG, vitamin E and phytosterols such as α- tocopherol and the β-tocopherol, β-sitosterol and campesterol. OWG showed potential antioxidant activity, with EC50 31.24 mg / mL for the capture of DPPH and a content of 3,67.10-6 mM of ferrous sulfate per gram of capture OWG. Performance reviews and posture did not differ between treatments. The eggs of the birds supplemented with ORG and BHT had favored characteristics in relation to egg weight, yolk weight, White egg weight, suggesting the replacement of BHT, a commercial antioxidant with potential carcinogen by OWG. In supplementation in the diet digestibility analysis of OWG and BHT favored the absorption of protein and feed lipids, suggesting that because the oil antioxidant potential in preserving the laying of the power of nutritional constituents as well as to preserve the moisture content, low value caloric albumen and the lipid content in the yolks. The results showed an egg production with superior quality compared to conventional production. The work generates natural antioxidant additive application alternatives that results in improved quality, productivity and reduction in production costs. Moreover favors the export in view of the new requirements of importing countries products of Brazilian poultry.Item Caracterização eletroquímica e estudos mecânico-quânticos para obtenção de propriedades eletrônicas de parabenos(Universidade Federal de Goiás, 2011-02-28) BARBOSA, Núsia Luísa; GIL, Eric de Souza; http://lattes.cnpq.br/3218622824233303Parabens are antimicrobial preservatives widely used in the pharmaceutical, cosmetic and food industries. The alkyl side chain connected to the ester group defines some important physicochemical characteristics of these compounds, including the partitioning coefficient and redox properties. The voltammetry and computational analysis were carried out in order to evaluate the redox behavior of these compounds and other phenolic analogues. Correlations between chemical substituents inductive effects of parabens with potential shifts were observed. Using cyclic voltammetry and glassy carbon working electrode, in aqueous, only one single irreversible anodic peak was observed around 0.8 V for methylparaben (MP), etylparaben (EP), propylparaben (PP), butylparaben (BP), benzylparaben (BzP) and phenolic analogues. The positive inductive effect of alkyl groups was demonstrated by the anodic oxidation potential shift to lower values as the carbon number increases and, therefore the parabens (and other phenolic analogues) oxidation processes to the quinoninic forms showed great dependence of substituent pattern. It was further evaluated the influence of pH and composition of supporting electrolyte in voltammetric profile of parabens.Item Estudo fitoquímico e avaliações da toxicidade aguda e atividades biológicas da raiz do vetiver (Vetiveria zizanioides L. Nash) Poaceae(Universidade Federal de Goiás, 2009-03-23) BARROS, Gilvana Cristina de; BARA, Maria Teresa Freitas; http://lattes.cnpq.br/3914164125498267The use of medicinal plants in controlling the diseases has shown its potential for the discovery of new medicines. Among the plant species used in the Hospital de Medicina Alternativa (HMA / SES-GO) highlights the vetiver (Vetiveria zizanioides L. Nash), an aromatic plant of the family Poaceae, used as a mild anti-hypertensive and diuretic. In this work it was investigated the chemical composition of the hydroalcoholic extract of vetiver, the freeze-dried aqueous extract and the essential oil from the roots of V. zizanioides. In the hydroalcoholic extract were found terpenoids compounds and / or saponins, flavonoids and phenolic acid. In the freeze-dried aqueous extract was observed the presence of flavonoids and phenols. In the essential oil 38 compounds were identified, and khusimol, palustrol, khusimona, zizanona and epi-α-vetivona were the major constituents. In the assessment of the acute toxicity of the hydroalcoholic extract and the freeze-dried aqueous extract of root of V. zizanioides, it was concluded that these extracts showed no toxicity at a dose of 2000 mg / kg. The freeze-dried aqueous extract of the roots of V. zizainoides showed no statistically significant diuretic action in the doses tested. In the investigation of antimicrobial activity, the essential oil of the root of V. zizanioides showed potent activity to inhibiting the growth of Staphylococcus aureus with MIC of 0.15 mg / mL. The crude ethanolic extract showed an antimicrobial activity with MIC of 0.19 mg / mL for Bacillus cereus and Micrococcus roseus and 0.39 mg / mL for Micrococcus luteus, S. aureus and Bacillus subtilis. The hexane fraction showed stronger antimicrobial activity against strains of M. luteus, M. roseus, S. aureus and B. cereus. This study could prove that the essential oil, the crude ethanol extract and hexane fraction from roots of V. zizanioides showed antimicrobial potential.Item Efeitos da formulação mucoadesiva de Bidens pilosa L. (Asteraceae) e Curcuma longa L. (Zingiberaceae) no tratamento da mucosite intestinal(Universidade Federal de Goiás, 2014-04-11) Bastos, Carla Caroline Cunha; Valadares, Marize Campos; http://lattes.cnpq.br/6157755243167018; Valadares, Marize Campos; Costa, Nádia do Lago; Sacono, Nancy TomokoIntestinal mucositis is a limiting factor in anticancer therapies by causing gastrointestinal cell destruction reaching the majority of patients undergoing chemotherapy/radiotherapy and is often responsible for treatment discontinuation. Although several studies have already been conducted to treat this disease, there are still no universally accepted and standardized protocols of treatment. Plant species with anti-inflammatory and antioxidant properties have been considered for the treatment of mucositis, among them Bidens pilosa L. (BP) (Asteraceae) and Curcuma longa L. (CL) (Zingiberaceae). In this study, the effects of a formulation containing plant extracts of Bidens pilosa L. (BP) and Curcuma longa L. (CL), both with pharmaceutical technology of mucoadhesion in mice intestinal mucositis induced by 5-fluoruoacil (5-FU) were studied. This formulation was administered orally (gavage) for 6 days in each group of mice at doses of 75mg/kg + BP 3.75 mg / kg CL 100 mg / kg BP + 7.5 mg / kg or 125 mg CL / BP kg + 15 mg / kg CL. The treatment with the formulations occurred during six days, and in parallel with mucositis induction was performed with 5-FU (200 mg / kg, intraperitoneally) from day 4 to day 6. On day 7, the mice were euthanized and the duodenal portion of the intestine of each animal was extracted to perform the histomorphometry technique. From this analysis, the dose of 125 mg/kg mucoadhesive formulation showed best effectiveness results and was then chosen for the realization of the other tests: histopathology analysis, expression of Bax, Bcl-2, p53 and Ki-67 analysis via immunohistochemistry technique; analysis of the activity of myeloperoxidase (MPO) enzyme, and determination of malondialdehyde (MDA) levels. Furthermore, analysis of weight change and hematologic parameters were performed. To prove safety of the formulation, an oral toxicity test of mucoadhesive formulation, and effect evaluation of the plant extracts on the animals’intestine not submitted to mucositis were performed. The mucoadhesive formulation was able to assuage the histopathological damage caused by 5-FU; reduced weight loss, reduced levels of MPO and MDA; stimulated cell proliferation by increasing the expression of Ki-67; besides decreasing apoptosis observed by analyzing the expression of Bax and Bcl-2. The formulation at a dose of 2000mg/kg showed no signs of toxicity. It can be concluded that the formulation under study exerts preventive and/or therapeutic effects to intestinal mucositis with potential to be used with associated to anticancer treatment.