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BACKGROUND: Patients often require adjustments to drug doses due to impaired renal function. Glomerular filtration rate (GFR) estimation using various equations can result in discrepancies, potentially leading to different dose adjustment recommendations. AIM: To determine the clinical significance of discrepancies observed between different equations used to estimate GFR for drug dose adjustments in a real-world group of patients over 65 years in primary care. METHOD: The Cockcroft-Gault (CG), Modification of Diet in Renal Disease (MDRD), Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI), and Berlin Initiative Study 1 equations were applied to estimate GFR in a group of patients over 65 years old attending a primary care center. Results were compared using Bland-Altman plots, and limits of agreement (LoA) and overall bias were calculated. Regression analyses were conducted to identify the null difference GFR and the slope of differences for each pairwise comparison. RESULTS: A total of 1886 patients were analyzed. Differences between patient-adjusted and body surface area (BSA)-normalized versions of the equations were not clinically relevant for dose adjustments, with LoAs below 20 mL/min. However, discrepancies among the original versions of several equations presented LoAs over 30 mL/min. Greater differences were found between CG and MDRD or CKD-EPI equations. CONCLUSION: Clinically relevant differences in GFR estimation were observed among different equations, potentially impacting drug dose adjustments. However, discrepancies were not considered significant when comparing patient-adjusted and BSA-normalized versions of the equations, particularly for patients with BSA close to the average.
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Insuficiência Renal Crônica , Insuficiência Renal , Humanos , Idoso , Taxa de Filtração Glomerular , Estudos Transversais , Insuficiência Renal Crônica/diagnóstico , Insuficiência Renal Crônica/epidemiologia , Tomada de Decisões , CreatininaRESUMO
BACKGROUND: Different questionnaires assess self-reported medication adherence and others quantify aspects of patients attitudes towards medication, but not together in a single instrument. Gathering these two aspects in a single instrument could reduce patients survey burden. AIM: The aim of this study was to develop the Medication Adherence Universal Questionnaire (MAUQ) using the Maastricht Utrecht Adherence in Hypertension short version (MUAH-16) factorial structure as the hypothesized model. METHOD: A multistep process started with the modification of the MUAH-16 to obtain the MAUQ. Patients using at least one antihypertensive medicine were recruited. The two questionnaires, the MUAH-16 and MAUQ, were applied. A confirmatory factor analysis (CFA) was performed using the initial MUAH-16 s-order 4-factor model. An additional bifactor model with four uncorrelated factors and an overall score was tested. The comparative fit index (CFI), root mean square error of approximation (RMSEA) with confidence intervals (CIs), and standardized root mean squared residual (SRMR) were used to assess both models. RESULTS: A sample of 300 hypertensive patients completed the instruments. The CFA with the second-order 4-factor solution resulted in similar results for the MUAH-16 and MAUQ: CFIs of 0.934 and 0.930, RMSEAs of 0.043 [CI 0.030-0.056] and 0.045 [CI 0.031-0.057] and SRMRs of 0.060 and 0.061, respectively. The CFA with the bifactor model showed slightly better results for both the MUAH-16 and MAUQ: CFIs of 0.974 and 0.976, RMSEAs of 0.030 [CI 0.005-0.046] and 0.028 [CI 0.001-0.044], and SRMRs of 0.043 and 0.044, respectively. CONCLUSION: CFA demonstrated that the MAUQ presented a better fit to both models than the MUAH-16, obtaining a robust universal free instrument to assess medicine-taking behaviour and four medicine beliefs components.
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Hipertensão , Adesão à Medicação , Humanos , Reprodutibilidade dos Testes , Inquéritos e Questionários , Anti-Hipertensivos/uso terapêutico , Hipertensão/diagnóstico , Hipertensão/tratamento farmacológico , Hipertensão/epidemiologia , PsicometriaRESUMO
Na página 9, Figura 2 onde se lê:73,53%Deverá ler-se:76,48%Artigo publicado com erros: https://www.actamedicaportuguesa.com/revista/index.php/amp/article/view/16892.
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INTRODUCTION AND OBJECTIVES: Patient knowledge about hypertension is an important patient-related determinant for poor blood pressure control and is a target for more effective interventions. We aimed to evaluate hypertensive patients' knowledge and awareness about hypertension and its influence on their beliefs about their medication and their adherence to antihypertensive therapy. METHODS: A cross-sectional study was conducted among adult patients attending one of the participating pharmacies and taking at least one antihypertensive drug. Data on personal and family history were collected, and Portuguese versions of the Hypertension Knowledge Test (HKT), Beliefs about Medicines Questionnaire (BMQ), and short version of the Maastricht Utrecht Adherence in Hypertension questionnaire (MUAH-16) were administered. RESULTS: A total of 240 patients were enrolled. The mean number of antihypertensive drugs used was 1.62±0.99, with 15.4% of patients treated with three or more drugs. More than 80% of patients knew the blood pressure therapeutic goals and identified overweight, sedentary lifestyle, and salt as risk factors for hypertension. Conversely, the majority of the patients were not aware of the asymptomatic characteristics of hypertension and believed that antihypertensive treatment had to be used for a limited time duration. Negative and significant correlations were found between the HKT and negative attitudes toward medication, but no association was found with positive attitudes. CONCLUSIONS: Hypertensive patients had good knowledge of hypertension risk factors but not of antihypertensive treatment. Increasing patient knowledge about hypertension may possibly reduce negative attitudes toward medication but will probably have no impact on positive attitudes.
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BACKGROUND: Symptomatic control is essential in palliative care, particularly in end-of-life, in which the pathophysiological changes that characterize this last phase of life strengthen the need to carry out an early therapeutic review. Hence, we aim to evaluate the prescribing pattern at a palliative care unit at two different time points: on admission and the day of the patient's death. METHODS: Quantitative, analytic, longitudinal, retrospective and observational study. Participants were adult patients who were admitted and died in a palliative care unit, in Portugal. Sociodemographic, clinical and pharmacological data were collected, including frequencies and routes of administration of schedule prescribed drugs and rescue drugs, from the day of admission until the day of death. RESULTS: 115 patients were included with an average age of 70.0 ± 12.9 years old, 53.9 were male, mostly referred by the Hospital Palliative Care Support Teams. The most common pathology was cancer, mainly in advanced stage. On admission, the median scheduled prescription was seven and "as needed" was three drugs. On the day of death, a decrease of prescriptions was observed. Opioids were always the most prescribed drugs. Near death, there was a higher tendency to prescribe butylscopolamine, midazolam, diazepam and levomepromazine. The most frequent route of drug administration was oral on admission and subcutaneous on the day of death. CONCLUSIONS: Polypharmacy is a reality in palliative care despite specialist palliative care teams. A reduction of prescribed drugs was verified, essentially due less comorbidity-oriented drugs. Further studies are required to analyse the importance of Hospital Palliative Care Support Teams.
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Enfermagem de Cuidados Paliativos na Terminalidade da Vida , Cuidados Paliativos , Adulto , Idoso , Idoso de 80 Anos ou mais , Morte , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Prescrições , Estudos RetrospectivosRESUMO
BACKGROUND: Cardiovascular disease (CVD) remains the leading cause of death worldwide. Assessing the patients' CVD risk, controlling the risk factors, and ensuring the guideline-adherent cardiovascular pharmacotherapy are crucial interventions to improve health outcomes. This study aimed to evaluate the potential of pharmacists to improve the adherence to pharmacotherapy guidelines and the achievement of risk factor goals among patients who attended a community pharmacy. METHODS: We conducted a single-center cross-sectional study. We performed in-pharmacy point-of-care testing, blood pressure and anthropometric measurements, and reviewed patients' pharmacotherapy, based on European Society of Cardiology guidelines. RESULTS: Of the 333 patients, 63.1% were in the high/very high risk category, 91.9% showed at least two modifiable risk factors, and in 61.9% of patients the cardiovascular pharmacotherapy was non-adherent to the current guidelines, failing to reach treatment goals. The lipid-lowering therapy was the least guideline adherent, with a suboptimal use of statins. However, we found no statistically significant difference between the guideline-adherent and the non-adherent group in terms of risk factor control. The pharmacist recommended 603 interventions to adhere to the guidelines. CONCLUSIONS: Community pharmacists are able to identify opportunities to optimize cardiovascular pharmacotherapy and support the patients to achieve cardiovascular risk factor goals, based on evidence-based guidelines, contributing to the improvement of CVD management.
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Doenças Cardiovasculares , Farmácias , Doenças Cardiovasculares/tratamento farmacológico , Doenças Cardiovasculares/prevenção & controle , Estudos Transversais , Fidelidade a Diretrizes , Humanos , Portugal , Fatores de RiscoRESUMO
INTRODUCTION: The purpose of medication reconciliation is to promote patient safety by reducing medication errors and adverse events due to medication discrepancies in transition of care. The aim of this pilot study of medication reconciliation at the time of hospital admission was to identify the necessary resources for its implementation in clinical practice. MATERIAL AND METHODS: Pilot study with 100 patients admitted to an Internal Medicine department between October and December 2019, aged 18 and over, and chronically taking at least one medicine. The best possible medication history was obtained systematically, with subsequent identification, classification and resolution of the discrepancies. RESULTS: The study sample, in general characterized by polypharmacy and by having multiple long-term conditions, presented a mean age of 77.04 ± 13.74 years, being 67.0% male. Overall, 791 discrepancies were identified. Intentional discrepancies were 95.7% and 50.9% of them were documented. The difficulties encountered were mainly related with the access and quality of therapeutic information and communication problems between different healthcare professionals. The key priority resources that were identified were related with the process, tools, and personnel categories. CONCLUSION: The data revealed weaknesses in the clinical records available at the primary/hospital care interface. Optimization of data sources, standardization and informatization of the process, multidisciplinary approach and definition of priority groups were identified as opportunities for optimization.
Introdução: A reconciliação terapêutica visa promover a segurança do doente por meio da redução de erros de medicação e eventos adversos decorrentes de discrepâncias de medicação na transição de cuidados. Foi nosso objetivo realizar um estudo-piloto de reconciliação terapêutica no momento da admissão hospitalar para, a partir dele, identificarmos os recursos necessários para a sua implementação na prática clínica.Material e Métodos: Estudo-piloto com 100 doentes admitidos num serviço de Medicina Interna entre outubro e dezembro de 2019, com mais de 18 anos e a tomar cronicamente pelo menos um medicamento. A melhor história farmacoterapêutica possível foi obtida sistematicamente, com posterior identificação, classificação e resolução das discrepâncias.Resultados: A amostra em estudo, em geral polimedicada e com múltiplas morbilidades, apresentou uma média de idades de 77,04 ± 13,74 anos, sendo 67,0% do sexo masculino. Foram identificadas 791 discrepâncias e as intencionais (95,7%) estavam documentadas em 50,9% das situações. As dificuldades encontradas relacionaram-se principalmente com o acesso e a qualidade da informação terapêutica e com a dificuldade de comunicação entre os diversos profissionais de saúde. Os principais recursos prioritários identificados relacionaram-se com as categorias de processo, ferramentas e pessoal.Conclusão: Os dados revelaram fragilidades nos registos clínicos disponíveis na interface dos cuidados primários/hospitalares. A otimização das fontes de dados, normalização e informatização do processo, atuação multidisciplinar e definição de grupos prioritários foram identificadas como oportunidades de otimização.
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Reconciliação de Medicamentos , Admissão do Paciente , Humanos , Masculino , Adolescente , Adulto , Pessoa de Meia-Idade , Idoso , Idoso de 80 Anos ou mais , Feminino , Projetos Piloto , Estudos Prospectivos , Erros de MedicaçãoRESUMO
The purpose of this review was to identify apps to support the HCV treatment and perform a quality assessment. A comprehensive search was conducted until February 2020 in Apple App Store (iOs) and Google Play Store (Android) using search term such "hepatitis", "hepatology", and "HCV". Two independent authors identified the apps and performed data extraction and quality assessment using Mobile App Rating Scale (MARS). Spearman's correlation analysis was used to analyze the relationships between user's star ratings found in the app stores and quality app defined by the MARS instrument. A total of 316 potential apps were identified, of which 12 apps fully met the eligibility criteria. Most apps were available in both App Stores and developed by commercial developers for healthcare provider. Almost all of apps were updated within the last two year and received 3.7 or above star ratings from users. Overall, only one app was considered with a good quality. The average scores for objective and subjective MARS quality of these apps were 3.54 (SD = 0.65) and 3.27 (SD = 0.76), respectively. Moreover, a majority of apps received objective scores between 3.29 and 4.37/5. However, MARS items such "interactivity", "visual appeal", "quality information", and "credibility" obtained minimum acceptable scores. MARS scores were not significantly correlation the user's star ratings. This systematic search found gaps in apps to support the HCV treatment; 12 apps were identified in this study and only one app achieved a good quality. There is a need that users use these apps cautiously as well as involve expert healthcare professionals in the development of new HCV apps.
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Hepatite C , Aplicativos Móveis , Atenção à Saúde , Hepatite C/tratamento farmacológico , HumanosRESUMO
BACKGROUND: Since the start of the new Coronavirus (COVID-19) outbreak in December 2019, pharmacists worldwide are playing a key role adopting innovative strategies to minimize the adverse impact of the pandemic. OBJECTIVES: To identify and describe core services provided by the pharmacist during the COVID-19 pandemic. METHODS: A literature search was performed in MEDLINE, Embase, Scopus, and LILACS for studies published between December 1st, 2019 and May 20th, 2020 without language restriction. Studies that reported services provided by pharmacists during the COVID-19 pandemic were included. Two independent authors performed study selection and data extraction with a consensus process. The pharmacist's intervention identified in the included studies were described based on key domains in the DEPICT v.2. RESULTS: A total of 1189 records were identified, of which 11 studies fully met the eligibility criteria. Most of them were conducted in the United States of America (n = 4) and China (n = 4). The most common type of publication were letters (n = 4) describing the workplace of the pharmacist in hospitals (n = 8). These findings showed the different roles of pharmacists during the COVID-19 pandemic, such as disease prevention and infection control, adequate storage and drug supply, patient care and support for healthcare professionals. Pharmacists' interventions were mostly conducted for healthcare professionals and patients (n = 7), through one-to-one contact (n = 11), telephone (n = 6) or video conference (n = 5). The pharmacists' main responsibility was to provide drug information for healthcare professionals (n = 7) as well as patient counseling (n = 8). CONCLUSIONS: A reasonable number of studies that described the role of the pharmacists during the COVID-19 pandemic were found. All studies reported actions taken by pharmacists, although without providing a satisfactory description. Thus, future research with more detailed description as well as an evaluation of the impact of pharmacist intervention is needed in order to guide future actions in this and/or other pandemic.
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COVID-19/terapia , Assistência Farmacêutica/organização & administração , Farmacêuticos/organização & administração , COVID-19/epidemiologia , Humanos , Papel ProfissionalRESUMO
INTRODUCTION: Obtaining the best possible medication history is the crucial step in medication reconciliation. Our aim was to evaluate the potential contributions of the main data sources available - patient/caregiver, hospital medical records, and shared electronic health records - to obtain an accurate 'best possible medication history'. MATERIAL AND METHODS: An observational cross-sectional study was conducted. Adult patients taking at least one medicine were included. Patient interview was performed upon admission and this information was reconciled with hospital medical records and shared electronic health records, assessed retrospectively. Concordance between sources was assessed. In the shared electronic health records, information was collected for four time-periods: the preceding three, six, nine and 12-months. The proportion of omitted data between time-periods was analysed. RESULTS: A total of 148 patients were admitted, with a mean age of 54.6 ± 16.3 years. A total of 1639 medicines were retrieved. Only 29% were collected simultaneously in the three sources of information, 40% were only obtained in shared electronic health records and only 5% were obtained exclusively from patients. The total number of medicines gathered in shared electronic health records considering the different time frames were 778 (three-months), 1397 (six-months), 1748 (nine-months), and 1933 (12-months). DISCUSSION: The use of shared electronic health records provides data that were omitted in the other data sources available and retrieving the information at six months is the most efficient procedure to establish the basis of the best possible medication history. CONCLUSION: Shared electronic health records should be the preferred source of information to supplement the patient or caregiver interview in order to increase the accuracy of best possible medication history of the patient, particularly if collected within the prior six months.
Introdução: A obtenção da melhor história farmacoterapêutica possível é uma etapa crucial da reconciliação da medicação. O objetivo foi avaliar as potenciais contribuições das principais fontes de informação disponíveis doente/cuidador, Processo Único, Plataforma de Dados da Saúde e para obter uma mais exacta melhor história farmacoterapêutica possível. Material e Métodos: Foi realizado um estudo transversal observacional. Incluíram-se doentes adultos a tomar pelo menos um medicamento. A entrevista com o doente foi realizada na admissão e os dados do Processo Único e da Plataforma de Dados da Saúde recolhidos retrospetivamente. A concordância entre as fontes de informação foi avaliada. Na plataforma de dados da saúde, os dados foram recolhidos em quatro janelas temporais: os últimos três, seis, nove e 12- meses. Os dados omitidos entre os diferentes tempos foram analisados. Resultados: Participaram 148 doentes, com uma idade média de 54,6 ± 16,3 anos. Foram recolhidos 1639 medicamentos. Destes, 29% foram obtidos simultaneamente nas três fontes de informação, 40% foram obtidos apenas na Plataforma de Dados da Saúde e 5% foram obtidos exclusivamente a partir do doente. O número total de fármacos recolhidos na Plataforma de Dados da Saúde nos diferentes tempos foi 778 (três meses), 1397 (seis meses), 1748 (nove meses) e 1933 (12 meses). Discussão: A consulta da Plataforma de Dados da Saúde permite obter dados omitidos nas outras fontes de informação e a recolha dos seis meses precedentes é o procedimento mais eficiente para constituir a base da melhor história farmacoterapêutica possível. Conclusão: A Plataforma de Dados da Saúde deve ser a fonte de informação preferencial para complementar a entrevista do doente/cuidador de forma a aumentar a exatidão da melhor história farmacoterapêutica possível, particularmente se a informação for recolhida em relação aos seis meses precedentes.
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Prontuários Médicos , Reconciliação de Medicamentos , Adulto , Idoso , Estudos Transversais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos RetrospectivosRESUMO
Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach's low pH, enzymatic content, and poor absorption in the gastrointestinal tract. Polymers with marine source like chitosan are commonly used in nanotechnology and drug delivery due to their biocompatibility and special features. This work focuses on the preparation and characterization of mucoadhesive insulin-loaded polymeric nanoparticles. Results showed a suitable mean size for oral administration (<600 nm by dynamic laser scattering), spherical shape, encapsulation efficiency (59.8%), and high recovery yield (80.6%). Circular dichroism spectroscopy demonstrated that protein retained its secondary structure after encapsulation. Moreover, the mucoadhesive potential of the nanoparticles was assessed in silico and the results, corroborated with ex-vivo experiments, showed that using chitosan strongly increases mucoadhesion. Besides, in vitro and in vivo safety assessment of the final formulation were performed, showing no toxicity. Lastly, the insulin-loaded nanoparticles were effective in reducing diabetic rats' glycemia. Overall, the coating of insulin-loaded nanoparticles with chitosan represents a potentially safe and promising approach to protect insulin and enhance peroral delivery.
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Adesão Celular , Insulina/administração & dosagem , Mucosa Bucal/metabolismo , Nanopartículas/química , Adesivos/química , Administração Oral , Animais , Células CACO-2 , Quitosana/análogos & derivados , Humanos , Insulina/farmacocinética , Masculino , Absorção pela Mucosa Oral , Ratos , Ratos WistarRESUMO
AIM: Parvifloron D is a natural diterpene with a broad and not selective cytotoxicity toward human tumor cells. In order to develop a targeted antimelanoma drug delivery platform for Parvifloron D, hybrid nanoparticles were prepared with biopolymers and functionalized with α-melanocyte stimulating hormone. Results/methodology: Nanoparticles were produced according to a solvent displacement method and the physicochemical properties were assessed. It was shown that Parvifloron D is cytotoxic and can induce, both as free and as encapsulated drug, cell death in melanoma cells (human A375 and mouse B16V5). Parvifloron D-loaded nanoparticles showed a high encapsulation efficiency (87%) and a sustained release profile. In vitro experiments showed the nanoparticles' uptake and cell internalization. CONCLUSION: Hybrid nanoparticles appear to be a promising platform for long-term drug release, presenting the desired structure and a robust performance for targeted anticancer therapy.
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Abietanos , Sistemas de Liberação de Medicamentos , Nanopartículas , Animais , Linhagem Celular Tumoral , Humanos , Melanoma/tratamento farmacológico , CamundongosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: A variety of plant polyphenols have been reported to have anti-inflammatory, frequently associated with erythema, edema, hyperplasia, skin photoaging and photocarcinogenesis. Cymbopogon citratus (DC). Stapf (Poaceae) is a worldwide known medicinal plant, used in traditional medicine in inflammation-related conditions. AIM OF THE STUDY: In this work, the anti-inflammatory potential of C. citratus infusion (CcI) and its polyphenols as topical agents was evaluated in vivo. MATERIALS AND METHODS: The plant extract was prepared and its fractioning led two polyphenol-rich fractions: flavonoids fraction (CcF) and tannins fraction (CcT). An oil/water emulsion was developed with each active (CcI, CcF+CcT and diclofenac), pH and texture having been evaluated. Release tests were further performed using static Franz diffusion cells and all collected samples were monitored by HPLC-PDA. In vivo topical anti-inflammatory activity evaluation was performed by the carrageenan-induced rat paw edema model. RESULTS: The texture analysis revealed statistically significant differences for all tested parameters to CcF+CcT, supporting its topical application. Release experiments lead to the detection of the phenolic compounds from each sample in the receptor medium and the six major flavonoids were quantified, by HPLC-PDA: carlinoside, isoorientin, cynaroside, luteolin 7-O-neohesperidoside, kurilesin A and cassiaoccidentalin B. The CcF+CcT formulation prompted to the higher release rate for all these flavonoids. CcI4%, CcI1% and CcF+CcT exhibited an edema reduction of 43.18, 29.55 and 59.09%, respectively. CONCLUSIONS: Our findings highlight that CcI, containing luteolin 7-O-neohesperidoside, cassiaoccidentalin B, carlinoside, cynaroside and tannins have a potential anti-inflammatory topical activity, suggesting their promising application in the treatment of skin inflammatory pathologies.
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Anti-Inflamatórios/farmacologia , Cymbopogon/química , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/farmacologia , Animais , Anti-Inflamatórios/química , Edema/tratamento farmacológico , Flavonoides/química , Flavonoides/farmacologia , Masculino , Medicina Tradicional/métodos , Extratos Vegetais/química , Plantas Medicinais/química , Ratos , Ratos Wistar , Taninos/farmacologiaRESUMO
Topical glucocorticosteroids were incorporated into nanocarrier-based formulations, to overcome side effects of conventional formulations and to achieve maximum skin deposition. Nanoparticulate carriers have the potential to prolong the anti-inflammatory effect and provide higher local concentration of drugs, offering a better solution for treating dermatological conditions and improving patient compliance. Nanoparticles were formulated with poly-ϵ-caprolactone as the polymeric core along with stearic acid as the fatty acid, for incorporation of betamethasone-21-acetate. Oleic acid was applied as the coating fatty acid. Improvement of the drug efficacy, and reduction in drug degradation with time in the encapsulated form was examined, while administering it locally through controlled release. Nanoparticles were spherical with mean size of 300 nm and negatively charged surface. Encapsulation efficiency was 90%. Physicochemical stability in aqueous media of the empty and loaded nanoparticles was evaluated for six months. Drug degradation was reduced compared to free drug, after encapsulation into nanoparticles, avoiding the potency decline and promoting a controlled drug release over one month. Fourier transform infrared spectroscopy and thermal analysis confirmed drug entrapment, while cytotoxicity studies performed in vitro on human keratinocytes, Saccharomyces cerevisiae models and Artemia salina, showed a dose-response relationship for nanoparticles and free drug. In all models, drug loaded nanoparticles had a greater inhibitory effect. Nanoparticles increased drug permeation into lipid membranes in vitro. Preliminary safety and permeation studies conducted on rats, showed betamethasone-21-acetate in serum after 48 h application of a gel containing nanoparticles. No skin reactions were observed. In conclusion, the developed nanoparticles may be applied as topical treatment, after encapsulation of betamethasone-21-acetate, as nanoparticles promote prolonged drug release, increase drug stability in aqueous media, reducing drug degradation, and increase drug permeability through lipid membranes.
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Anti-Inflamatórios , Betametasona , Portadores de Fármacos , Nanopartículas , Resinas Acrílicas/química , Administração Cutânea , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/sangue , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacocinética , Artemia/efeitos dos fármacos , Betametasona/administração & dosagem , Betametasona/sangue , Betametasona/química , Betametasona/farmacocinética , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Humanos , Queratinócitos/efeitos dos fármacos , Masculino , Nanopartículas/administração & dosagem , Nanopartículas/química , Ácido Oleico/química , Poloxâmero/química , Ratos Wistar , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/crescimento & desenvolvimento , Absorção CutâneaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Treatment of gastric ulcers with medicinal plants is quite common in traditional medicine worldwide. Cymbopogon citratus (DC) Stapf. leaves infusion has been used in folk medicine of many tropical and subtropical regions to treat gastric disturbances. The aim of this study was to assess the potential gastroprotective activity of an essential oil-free infusion from C. citratus leaves in acute gastric lesions induced by ethanol in rat. MATERIALS AND METHODS: The study was performed on adult male Wistar rats (234.0±22.7g) fasted for 24h but with free access to water. The extract was given orally before (prevention) or after (treatment) intragastric administration of absolute ethanol. Effects of dose (28 or 56mg/kg of body weight) and time of contact of the extract with gastric mucosa (1 or 2h) were also assessed. Animals were sacrificed, being the stomachs removed and the lesions were assessed by macroscopic observation and histopathology. RESULTS: C. citratus extract, given orally before or after ethanol, significantly (P<0.01) reduced gastric mucosal injury compared with control group (vehicle+ethanol). The effect does not appear to be dose-dependent. Results also suggested that the extract is more effective when the time of contact with gastric mucosa increases. CONCLUSIONS: The results of this assay confirm the gastroprotective activity of C. citratus extract on experimental gastric lesions induced by ethanol, contributing for the pharmacological validation of its traditional use.
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Antiulcerosos/uso terapêutico , Cymbopogon , Extratos Vegetais/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Animais , Etanol , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/patologia , Masculino , Fitoterapia , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologiaRESUMO
Cymbopogon citratus (lemongrass) leaf infusion, a commonly used ingredient in Asian, African and Latin American cuisines, is also used in traditional medicine for the treatment of several pathological conditions; however, little is known about their bioactive compounds. Recent studies revealed the crucial role of the phenolic compounds namely flavonoids and tannins on the infusion bioactivity. Flavonoids have already been characterized; however the tannin fraction of lemongrass infusion is still uncharted. The aim of the present work is to characterize this fraction, and to evaluate its contribution to the antioxidant potential of this plant. Chemical characterization was achieved by HPLC-DAD-ESI/tandem MS and the antioxidant activity was evaluated using DPPH, ABTS and FRAP assays. Hetero-dimeric flavan structures have been described for the first time in lemongrass consisting of apigeniflavan or luteoliflavan units linked to a flavanone, either naringenin or eriodictyol, which may occur as aglycone or glycosylated forms. The antioxidant capacity of the fraction containing these compounds was significantly higher than the infusion, indicating its potential as a source of natural antioxidants.
Assuntos
Antioxidantes/análise , Cymbopogon/química , Flavanonas/análise , Flavonoides/análise , Glicosídeos/análise , Folhas de Planta/química , Chás de Ervas/análise , Antioxidantes/química , Antioxidantes/isolamento & purificação , Apigenina/análise , Apigenina/química , Apigenina/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Etnofarmacologia , Flavanonas/química , Flavanonas/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Luteolina/análise , Luteolina/química , Luteolina/isolamento & purificação , Medicina Tradicional , Estrutura Molecular , Peso Molecular , Portugal , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem , Taninos/análise , Taninos/isolamento & purificaçãoRESUMO
O presente estudo teve como objetivos caracterizar a situação real do consumo de Plantas Medicinais (PM) numa amostra de pacientes com patologia cardiovascular e identificar potenciais interações entre as PM e a terapêutica farmacológica cardiovascular convencional.O estudo foi realizado numa Farmácia Comunitária em Portugal entre abril e junho de 2014. Dos 128 utentes abordados ao balcão que fazem uso da terapêutica cardiovascular, 65 (51%) faziam uso de PM, seja sob a forma de infusão, suplementos ou medicamentos à base de PM. Desses, 43 (66%) foram entrevistados, tendo 22 (34%) sido excluídos por não terem manifestado interesse em participar no estudo. Através da revisão da medicação efetuada para cada doente foram encontradas um total de 123 interações planta-medicamento, com uma média de 2,9 interações/doente, com potencial para diminuir o sucesso da terapêutica cardiovascular. O presente estudo demonstra como o serviço farmacêutico da revisão da medicação pode ser utilizado para otimizar a terapêutica dos doentes cardiovasculares quando estes tomam medicamentos e PM em simultâneo, o que evidencia a função do farmacêutico na sensibilização da população, no sentido de evitar situações prejudiciais para a saúde e bem estar do doente.
Assuntos
Humanos , Plantas Medicinais , Anormalidades Cardiovasculares/terapia , Ações Farmacológicas , Brasil , Uso de MedicamentosRESUMO
Indomethacin (IM), a non-steroidal anti-inflammatory drug, has the capacity to induce hepatic and renal injuries when administrated systemically. The aim of this study is to assess the IM absorption from complexed forms when orally administered to rats, by means of a comparative evaluation of its capacity to induce hepatic and renal injury in different forms, namely IM acid, IM sodium salt or IM complexed with hydroxypropyl-ß-cyclodextrin (HP-ß-CD), using freeze- and spray-drying methods. A total of 135 Wistar rats weighing 224.4 ± 62.5 g were put into 10 groups. They were allowed free access to water but were maintained on fast for 18 h before the first administration until the end of the experiment. Water and HP-ß-CD (control groups) and IM acid form, IM trihydrated-sodium-salt and IM-HP-ß-CD spray- and freeze-dried, at normal and toxic doses (test groups), were orally administered once/day for 3 days. Seventy-two hours after the first administration, the animals were sacrificed and a fragment of the liver and one kidney were collected and prepared for histopathological evaluation. Lesion indexes (rated 0/4 for liver and 0/3 for kidney) were developed and the type of injury scored according to the severity of damage. A statistical analysis of the severity and incidence of lesions was carried out. Animals administered with IM complexed forms showed similar hepatic and renal lesions, both in toxic and therapeutic doses, when compared with those observed in animals administered with IM acid or salt forms. This suggests that under the present experimental conditions, IM is equally absorbed from the gastrointestinal tract, independently of the administered IM form.
Assuntos
Anti-Inflamatórios não Esteroides/toxicidade , Indometacina/toxicidade , Rim/patologia , Fígado/patologia , beta-Ciclodextrinas/toxicidade , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Composição de Medicamentos , Avaliação Pré-Clínica de Medicamentos , Excipientes/administração & dosagem , Excipientes/farmacocinética , Excipientes/toxicidade , Feminino , Liofilização , Trato Gastrointestinal/fisiologia , Indometacina/administração & dosagem , Indometacina/química , Indometacina/farmacocinética , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Masculino , Modelos Animais , Distribuição Aleatória , Ratos , Ratos Wistar , Gastropatias/prevenção & controle , beta-Ciclodextrinas/administração & dosagem , beta-Ciclodextrinas/química , beta-Ciclodextrinas/farmacocinéticaRESUMO
This study aimed to evaluate the semicarbazide-sensitive amine oxidase (SSAO) activity in human arterial tissues and in serum of patients with type 2 diabetes. The SSAO activity, with (14)C-benzylamine as substrate, was measured in homogenates of human inferior mesenteric arteries obtained at surgery, from 10 patients with type 2 diabetes and 16 non-diabetic patients and in the serum of 39 patients with type 2 diabetes and 40 non-diabetic control patients. The SSAO activity in the homogenates of vascular tissue was significantly lower in the diabetics than in the non-diabetics (P = 0.001). The SSAO activity in the serum of patients with type 2 diabetes was higher when compared with control group (P = 0.0001). In conclusion, the SSAO activity increased in the serum and decreased in the arterial tissue. These findings suggest damage in the vascular tissue and support the hypothesis that serum SSAO may be a useful biochemical marker for diabetes.
Assuntos
Amina Oxidase (contendo Cobre)/metabolismo , Diabetes Mellitus Tipo 2/sangue , Artérias Mesentéricas/enzimologia , Idoso , Amina Oxidase (contendo Cobre)/sangue , Biomarcadores/sangue , Neoplasias Colorretais/cirurgia , Diabetes Mellitus/sangue , Diabetes Mellitus/enzimologia , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/enzimologia , Feminino , Humanos , Cinética , Masculino , Artérias Mesentéricas/cirurgia , Pessoa de Meia-Idade , Valores de ReferênciaRESUMO
Indomethacin (IM) is a non-steroidal anti-inflammatory drug which inhibits prostaglandin biosynthesis. It is practically insoluble in water and has the capacity to induce gastric injury. Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) is an alkylated derivative of beta-CD with the capacity to form inclusion complexes with suitable molecules. IM is considered to form partial inclusion complexes with HP-beta-CD by enclosure of the p-chlorobenzoic part of the molecule in the cyclodextrin channel, reducing the adverse effects. The aim of this paper is to evaluate the gastric damage induced by the IM inclusion complex prepared by freeze-drying and spray-drying. A total of 135 Wistar rats weighing 224.4 +/- 62.5 g were put into 10 groups. They were allowed free access to water but were maintained fasted for 18 h before the first administration until the end of the experiment. IM acid-form, IM trihydrated-sodium-salt and IM-HP-beta-CD spray and freeze-dried, at normal and toxic doses, were administered through gastric cannula once/day for 3 days. Seventy-two hours after the first administration, the animals were sacrificed and the stomachs collected and prepared for morphological study by using the haematoxylin-eosin technique. Lesion indexes (rated 0/4) were developed and the type of injury was scored according to the severity of damage and the incidence of microscopic evidence of harm. Microscopic assessment demonstrated levels of injury with index one on 10-25%. The type of complexation method had different incidence but the same degree. The results show that IM inclusion complexation protects against gastric injury, reducing the incidence and the maximum degree of severity from 4 to 1, with a better performance of the spray-dried complex.