Enhanced Solubility of Albendazole in Cyclodextrin Inclusion Complex: A Molecular Modeling Approach and Physicochemical Evaluation.

BACKGROUND: Albendazole (ABZ) is the drug of choice for the treatment of a variety of human and veterinary parasites. However, it has low aqueous solubility and low bioavailability. Cyclodextrins (CD) are pharmaceutical excipients with the ability to modulate the solubilization property of hydrophobic molecules. OBJECTIVE: The aim of the study was to analyze through in vitro and in silico studies (Autodock Vina software and CycloMolder platform) the formation of inclusion complexes between ABZ, ß-cyclodextrin (ß-CD) and its derivatives Methyl-ß-cyclodextrin (M-ß-CD) and Hydroxypropyl-ß-cyclodextrin (HP-ß-CD). METHODS: The most stable inclusion complexes were produced by the kneading method and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), determination of the ABZ content and in vitro dissolution profile. RESULTS: Molecular modeling revealed that inclusion complexes between HP-ß-CD:ABZ (in the proportion 1:1 and 2:1) presented the lowest formation energy and the highest number of intermolecular interactions, showing that the use of more cyclodextrins does not generate gains in the stability of the complex. On the characterization tests, the complexes experimentally obtained by the kneading method demonstrated highly suggestive parameters, including ABZ in HP-ß-CD in both molar proportions, suppression of bands in the infrared spectrum, displacement of the drug's melting temperature in DSC, crystallinity halos instead of the characteristic peaks of ABZ crystals in the XRD and a release of more than 80% of ABZ in less than 5 minutes, dissolution efficiency of up to 92%. CONCLUSION: In silico studies provided a rational selection of the appropriate complexes of cyclodextrin, enabling the elaboration of more targeted complexes, decreasing time and costs for elaboration of new formulations, thereby increasing the oral biodisponibility of ABZ.

Development and validation of a method for phenobarbital in serum: anticonvulsant pharmacotherapy monitoring

The therapeutic drug monitoring (TDM) is an important strategy for the effectiveness and safety of long-term pharmacotherapy, such as the use of phenobarbital as an anticonvulsant drug in epilepsy. In this sense, HLPC has been presented as a technique for the measurement of phenobarbital in serum. However, the ideal conditions for carrying out the method must be established for each laboratory reality. An analytical method using HPLC was developed and validated in order to identify and quantify Phenobarbital in blood. The chromatographic conditions were C-18 column (Shimpack XR-ODS 50L x 3.0), acetonitrile-water mobile phase (30:70, v v-1), 0.2 mL min-1 flow and reading wavelength of 210 nm. Linearity was established in the range of 2.5 to 80 µg mL-1, the linear correlation coefficient was 0.9981. The average of the coefficient of variation of the precision was 5.30%. The relative standard error of the accuracy was -2.17% and of the recovery coefficient was 97.83%. In all eleven patients, phenobarbital concentrations were below the therapeutic range. The tested method was selective, linear, precise, accurate and showed good recovery.(AU)

Análise das demandas judiciais para aquisição de medicamentos no estado da Paraíba / Analysis of medicine procurement lawsuits in the state of Paraíba, Brazil

Resumo O objetivo deste estudo foi descrever os aspectos médico-científicos e sanitários dos mandados judiciais para fornecimento de medicamentos impetrados ao Tribunal de Justiça da Paraíba (TJ-PB) contra agentes públicos no estado da Paraíba. Teve caráter descritivo, transversal, e foi realizado no Tribunal de Justiça da Paraíba. Foram analisados processos de medicamentos julgados na segunda instância entre os anos de 2009 e 2010 com decisão definitiva. Quanto às evidências científicas da eficácia e segurança, os medicamentos foram avaliados por meio de revisões sistemáticas na base de dados do Centro Cochrane do Brasil. Os grupos de medicamentos solicitados com maior frequência foram os agentes neoplásicos, seguidos de insulinas e antagonistas da angiotensina II. Os custos com medicamentos antineoplásicos representaram 76% do gasto total com demandas judiciais, representando um custo aproximado de R$ 343 mil por mês. Desses, um item não tinha registro em orgão sanitário brasileiro. Os resultados apontam para um elevado número de demandas judiciais com prevalência de solicitações de medicamentos padronizados pelo Sistema Único de Saúde (SUS), dos quais os antineoplásicos obtêm destaque e reforçam a necessidade de revisão da Política Nacional de Assistência Farmacêutica tanto das estratégias de implantação como da premência em ampliar a relação de medicamentos disponibilizados pelo SUS.

Abstract This study aimed to describe the medical, scientific, and sanitary aspects of lawsuits for drug supply filed with the Court of Paraíba (TJ-PB) against public officials in the state of Paraíba, Brazil. It was a descriptive and cross-sectional study, which had as source the Information System of the Paraíba Court. Drug processes judged at the second instance between the years 2009 and 2010 with a final decision already made ​​at the time of consultation were analyzed. About the scientific evidences of efficacy and safety, drugs were evaluated through systematic reviews in the Brazilian Cochrane Centre database. The groups of drugs most frequently requested were the antineoplastic agents, followed by insulin and angiotensin II antagonists. The antineoplastic agents' costs accounted for 76% of the total spent on litigation, representing an approximate cost of R$ 343,000 per month, of which an item had no record in Brazilian sanitary organ. The results pointed to a high number of lawsuits with prevalence of requests for drugs standardized by the Brazilian Unified Health System (SUS), of which the antineoplastic agents are noteworthy and reinforce the need for revision of the National Pharmaceutical Assistance Policy, both regarding deployment strategies as the urgency to expand the list of drugs available through SUS.

Effect of alpha lipoic acid on the blood cell count and iron kinetics in hypertensive patients / Efecto del ácido lipoico en el recuento de sangre y el metabolismo de hierro en pacientes hipertensos

Introduction: The α-lipoic acid (ALA) has been used as a treatment to reduce oxidative damage in Systemic Arterial Hypertension (SAH), but there are no in vivo studies reporting the effect of its mechanism of action on iron metabolism. Objective: To evaluate the antioxidant effect of α-lipoic acid on Blood cell count (CBC) and iron metabolism in hypertensive subjects with or without anemia. Method: Double-blind, randomized, placebo-controlled clinical trial. The sample consisted of 60 hypertensive patients that were randomly divided into treatment group (n = 32), receiving 600 mg / day of ALA for twelve weeks and control group (n = 28), receiving placebo for the same period. Blood cell count, serum iron, ferritin, Latent Iron-Binding Capacity (LIBC), Total Iron-Binding Capacity (TIBC), Transferrin Saturation Index (TSI) and transferrin were assessed before and after intervention. To assess changes between groups, the Student t-test and ANOVA were used, adopting a significance level of 5%. Results: After intervention, ALA supplementation showed a statistically significant (p < 0.05) association with the reduction of total leukocytes, increase in the number of neutrophils and reductions in the serum levels of iron and TSI. Conclusion: Oral administration of ALA as a therapeutic adjuvant changes the hematologic response of white blood cells and reduces the absorption of iron. It is observed that the mechanism of metals chelation by lipoic acid may be responsible for these changes and, consequently, could trigger a condition of iron deficiency anemia in hypertensive individuals (AU)

Introducción: El Ácido α-Lipóico (ALA) ha sido utilizado como recurso terapéutico para reducir daño oxidativo en la Hipertensión Arterial Sistémica (HAS), pero aún no existen estudios in vivo que reporten sobre su mecanismo de acción en el metabolismo del hierro. Objetivo: Evaluar el efecto antioxidante del ácido Alfa- Lipóico sobre el hemograma y metabolismo del hierroen individuos hipertensos con o sin anemia. Métodos: Estudio clínico doble-ciego, randomizado y controlado con placebo. La muestra fue constituida por 60 individuos hipertensos, distribuidos aleatoriamente en grupo tratamiento (n = 32), que recibió 600 mg/día del ALA por doce semanas y grupo control (n = 28), que recibió el placebo por el mismo período. Fueron analizados antes y después de la intervención, los parámetros del hemograma, Hierro Sérico, Ferritina, Capacidad Latente de Enlace del hierro, Capacidad Total de Enlace del Hierro, Índice de Saturación de la Transferrina (ISI) y Transferrina. Para evaluar las alteraciones entre los grupos, se utilizó el teste t de Student y el análisis de varianza ANOVA, adoptándose el nivel de significación de 5%. Resultados: Después de la intervención, el suplemento con el ALA demostró una asociación estadísticamente significativa (p < 0,05) con la reducción de los leucocitos totales, aumento del número de neutrófilos y reducciones en los niveles de Hierro Sérico e ISI. Conclusión: La administración oral del ALA como un adyuvante terapéutico, altera la respuesta hematológica del leucograma y reduce la absorción del hierro. Cabe senãlar que el mecanismo de quelación de metales por el ácido lipoico puede ser responsable de estos cambios y, en consecuencia, podría desencadenar una condicion de anemia ferropénica en individuos hipertensos (AU)

Effect of alpha lipoic acid on the blood cell count and iron kinetics in hypertensive patients.

INTRODUCTION: The -lipoic acid (ALA) has been used as a treatment to reduce oxidative damage in Systemic Arterial Hypertension (SAH), but there are no in vivo studies reporting the effect of its mechanism of action on iron metabolism. OBJECTIVE: To evaluate the antioxidant effect of -lipoic acid on Blood cell count (CBC) and iron metabolism in hypertensive subjects with or without anemia. METHOD: Double-blind, randomized, placebo-controlled clinical trial. The sample consisted of 60 hypertensive patients that were randomly divided into treatment group (n = 32), receiving 600 mg / day of ALA for twelve weeks and control group (n = 28), receiving placebo for the same period. Blood cell count, serum iron, ferritin, Latent Iron-Binding Capacity (LIBC), Total Iron-Binding Capacity (TIBC), Transferrin Saturation Index (TSI) and transferrin were assessed before and after intervention. To assess changes between groups, the Student t-test and ANOVA were used, adopting a significance level of 5%. RESULTS: After intervention, ALA supplementation showed a statistically significant (p < 0.05) association with the reduction of total leukocytes, increase in the number of neutrophils and reductions in the serum levels of iron and TSI. CONCLUSION: Oral administration of ALA as a therapeutic adjuvant changes the hematologic response of white blood cells and reduces the absorption of iron. It is observed that the mechanism of metals chelation by lipoic acid may be responsible for these changes and, consequently, could trigger a condition of iron deficiency anemia in hypertensive individuals.

Introducción: El Ácido -Lipóico (ALA) ha sido utilizado como recurso terapéutico para reducir daño oxidativo en la Hipertensión Arterial Sistémica (HAS), pero aún no existen estudios in vivo que reporten sobre su mecanismo de acción en el metabolismo del hierro. Objetivo: Evaluar el efecto antioxidante del ácido Alfa- Lipóico sobre el hemograma y metabolismo del hierro en individuos hipertensos con o sin anemia. Métodos: Estudio clínico doble-ciego, randomizado y controlado con placebo. La muestra fue constituida por 60 individuos hipertensos, distribuidos aleatoriamente en grupo tratamiento (n = 32), que recibió 600 mg/día del ALA por doce semanas y grupo control (n = 28), que recibió el placebo por el mismo período. Fueron analizados antes y después de la intervención, los parámetros del hemograma, Hierro Sérico, Ferritina, Capacidad Latente de Enlace del hierro, Capacidad Total de Enlace del Hierro, Índice de Saturación de la Transferrina (ISI) y Transferrina. Para evaluar las alteraciones entre los grupos, se utilizó el teste t de Student y el análisis de varianza ANOVA, adoptándose el nivel de significación de 5%. Resultados: Después de la intervención, el suplemento con el ALA demostró una asociación estadísticamente significativa (p < 0,05) con la reducción de los leucocitos totales, aumento del número de neutrófilos y reducciones en los niveles de Hierro Sérico e ISI. Conclusión: La administración oral del ALA como un adyuvante terapéutico, altera la respuesta hematológica del leucograma y reduce la absorción del hierro. Cabe senãlar que el mecanismo de quelación de metales por el ácido lipoico puede ser responsable de estos cambios y, en consecuencia, podría desencadenar una condicion de anemia ferropénica en individuos hipertensos.

Uso de cosméticos por mulheres do município de Esperança, Paraíba, Brasil / Use of cosmetics for women of the city of Hope, Paraíba, Brazil

O aumento de vendas de produtos cosméticos e de higiene pessoal deve ser atentamente acompanhado pelos setores regulatórios competentes, uma vez que mais de oito mil matérias-primas são usadas na formulação destes produtos e muitas podem ocasionar efeitos adversos tóxicos ou mesmo alergias. Assim, este trabalho visou investigar quais as finalidades do uso de cosméticos entre mulheres, conhecer os mais utilizados e saber os locais de aquisição destes produtos. Tratou-se de um estudo transversal, descritivo e exploratório, tendo como instrumento de coleta de dados um questionário com perguntas objetivas, aplicado entre 102 mulheres. A higiene (65,7%) foi respondida como a principal finalidade de uso. Os produtos com maior frequência de utilização foram os perfumes e desodorantes (90,2%), maquiagens (74,5%), produtos para depilação (74,5%) e tinturas de cabelos (41,2%). A maior parte das mulheres (63,7%) relatou comprar os cosméticos em revistas. Diante dos resultados expostos, pode-se inferir que as mulheres utilizam variados tipos de cosméticos, com diferentes finalidades, o que pode implicar em risco para saúde.

The increasing sales of cosmetics and toiletries must be carefully monitored by competent regulatory sectors, as many of the more than eight thousand ingredients used to formulate cosmetics can have adverse effects, such as carcinogenicity, genotoxicity, phototoxicity, contact dermatitis, hives, hypopigmentation, hyperpigmentation, depigmentation, damage to hair and nails, etc. The aims of the present study were to investigate the reasons for the use of cosmetics by women and determine both the most frequently used products and where such products are acquired. For such, a cross-sectional study with an analytical approach was carried out. Data were collected through the use of a questionnaire with objective questions administered to 102 women. Hygiene (65.7%) was the main reason cited for using cosmetic products. The most frequently used products were perfumes and deodorants (90.2%), makeup (74.5%), hair removal products (74.5%) and hair dyes (41.2%). The majority (63.7%) reported to buying cosmetics from catalogues. The present findings demonstrate that women use many kinds of cosmetics for different purposes, which may imply health risks.

Indicadores de prescrição e de cuidado ao paciente na atenção básica do município de Esperança, Paraíba, 2007 / Prescription indicators and patient-care in public primary care in the municipality of Esperança, Paraíba, 2007

Objetivo: descrever aspectos da prescrição e cuidado a pacientes em Unidades Básicas de Saúde da Família (UBSF) do município de Esperança, estado da Paraíba, Brasil. Métodos: estudo descritivo, sobre indicadores de prescrição e cuidado ao paciente propostos pela Organização Mundial da Saúde; amostra de conveniência, composta por pacientes maiores de 18 anos atendidos em janeiro-agosto de 2007. Resultados: foram considerados 600 pacientes, com média de medicamentos/receita de 2,4, 74,6 por cento dos medicamentos prescritos pelo nome genérico e 85,3 por cento constantes da Relação Municipal de Medicamentos Essenciais (REMUME); 9,3 por cento das receitas continham ao menos algum antibiótico, 10,1 por cento algum psicofármaco e 2,97 por cento alguma medicação injetável; foram dispensados 48,0 por cento dos medicamentos prescritos; o tempo médio de dispensação foi de 49 segundos e o tempo médio de consulta, 7 minutos e 8 segundos. Conclusão: os prescritores seguem a relação de medicamentos padronizados embora a REMUNE necessite atualizá-la periodicamente para atender o perfil epidemiológico populacional.

Objective: to discribe aspects of prescription and patient-care at Healthcare Units of Family Health (HUFH) in the municipality of Esperança, state of Bahia, Brazil. Methods: a descriptive cross-sectional study on prescription and patient-care indicators proposed by the World Health Organization. Results: average for prescribed drugs were 2.4; 74.6 percent of the medicaments were prescribed by generic name; 85.3 percent were listed by the Municipal List of Essential Drugs (REMUME); 9.3 percent had at least one antibiotic; 10.1 percent had at least one psychotropic; and 2.97 percent, at least an injectable medication; 48.0 percent of the prescribed drugs were effectively dispensed; the average time of dispensation was 49 seconds, and the medical consultation time, 7 minutes and 8 seconds. Conclusion: prescription follows standard list recommended, but REMUME needs actualization to attend the epidemiologic profile of the population.

[Medical prescriptions: adequate orientation to medicine use?]. / Prescrição médica: orientações adequadas para o uso de medicamentos?

During physician's consultation, the lack of adequate information on medication to the patient is a major problem to reach the correct pharmacotherapy. This study aims at assessing the patient knowledge about prescribed drugs. In order to proceed the investigation, interviews were performed about type of medication, dosage, administration schedule, purpose, duration of treatment and side effects. From 199 patients interviewed after they had received a prescription, 53.8% didn't have any information about the medicine, 20.3% didn't know the dosage and 25.4% didn't know the medication schedule. The purpose of the medication was the information with the highest percentage of correct answers, with 75.1% of the patients showing good level of knowledge. Regarding to the duration of the treatment and side effects, 57.4% and 94.4% of the patients, respectively, didn't present any correct information. Results suggest that the majority of the patients didn't have sufficient and safe knowledge to the use of prescribed medication.

Prescrição médica: orientações adequadas para o uso de medicamentos? / Medical prescriptions: adequate orientation to medicine use?

O conhecimento insuficiente de informação dada ao paciente durante a consulta médica resulta em grandes dificuldades para a condução correta da terapêutica medicamentosa. Baseados nesse contexto, o estudo teve como objetivo avaliar o grau de conhecimento dos pacientes sobre os medicamentos prescritos na Atenção Básica no município de Esperança (PB). Para tal, foram entrevistadas 199 pessoas que, após consulta médica, receberam prescrição, tendo sido avaliado o nível de conhecimento desses pacientes em relação ao nome do medicamento, a dose, o horário, a finalidade, o tempo de uso e reações desagradáveis. Entre os entrevistados, 53,8 por cento evidenciaram desconhecer o nome do medicamento, 20,3 por cento a dosagem e 25,4 por cento o horário de utilização. O item em que se observou maior frequência de acerto foi finalidade do medicamento, tendo 75,1 por cento dos pacientes apresentado bom conhecimento. No que se refere ao tempo de uso e às reações desagradáveis, 57,4 por cento e 94,4 por cento dos pacientes, respectivamente, não possuíam nenhuma informação correta. Os resultados sugerem que a maioria dos pacientes não apresenta o conhecimento adequado e seguro para a utilização dos medicamentos prescritos.

During physician's consultation, the lack of adequate information on medication to the patient is a major problem to reach the correct pharmacotherapy. This study aims at assessing the patient knowledge about prescribed drugs. In order to proceed the investigation, interviews were performed about type of medication, dosage, administration schedule, purpose, duration of treatment and side effects. From 199 patients interviewed after they had received a prescription, 53.8 percent didn't have any information about the medicine, 20.3 percent didn't know the dosage and 25.4 percent didn't know the medication schedule. The purpose of the medication was the information with the highest percentage of correct answers, with 75.1 percent of the patients showing good level of knowledge. Regarding to the duration of the treatment and side effects, 57.4 percent and 94.4 percent of the patients, respectively, didn't present any correct information. Results suggest that the majority of the patients didn't have sufficient and safe knowledge to the use of prescribed medication.