Papel del farmacéutico comunitario costarricense en quimioterapia preventiva de parasitosis intestinal. Estudio exploratorio / Role of the Costa Rican community pharmacist in preventive chemotherapy of intestinal parasitosis. Exploratory study

Objetivo: Identificar intervenciones farmacéuticas, en quimioterapia preventiva de parasitosis intestinal, que promuevan la prevención de esta enferme-dad y el uso efectivo y seguro de los antiparasitarios. Método: Estudio de opinión exploratorio, descriptivo transversal y multicéntrico donde se entrevistó, de forma presencial mediante un instrumento diseñado para tal fin, a 49 farmacéuticos comunitarios. Resultado: De la totalidad de los farmacéuticos comunitarios entrevistados, un 89.80% (n=44) comentó ofertar el servicio de indicación farmacéutica en caso de quimioterapia preventiva de parasitosis intestinal. Como parte de las intervenciones realizadas destacaron: derivación al médico u otro profesional de salud según criterios específicos (100.00%), dispensación de un medicamento antiparasitario (93.18%) y brindar recomendaciones higiénicas y dietéticas (79.55%). El albendazol y la nitazoxanida fueron los principales medicamentos indicados y dispensados. Conclusión: Se evidencia la importancia del papel del farmacéutico comunitario costarricense, en quimioterapia preventiva de parasitosis intestinal, para la muestra estudiada, cuyas acciones favorecen el uso racional de antiparasitarios y la prevención de las parasitosis. (AU)

Objective: To identify pharmacist interventions, in preventive chemotherapy for intestinal parasitosis that promote the prevention of intestinal parasito-sis and the effective and safe use of antiparasitic drugs. Method: It was carried out an exploratory, descripti-ve, cross-sectional and multicentre opinion study in which 49 community pharmacists were interviewed in person, using an instrument designed for this purpose. Result: Overall, 89.80% (n=44) of the community pharmacists interviewed reported offering the mi-nor ailments service in the case of preventive che-motherapy for intestinal parasitosis. Interventions included: referral to a physician or other health care provider according to criteria (100.00%), dispensing of an antiparasitic agent (93.18%) and hygiene and dietary recommendations (79.55%). Albenda-zole and nitazoxanide were the main medications dispensed. Conclusion: The importance of the role of the Costa Rican community pharmacist in preventive chemotherapy of intestinal parasitosis is evident according to the sample analyzed because his/her actions promote rational use of antiparasitic agents and the prevention of parasitosis.(AU)

Trypanocidal treatment of Chagas disease.

Chagas disease is a neglected parasitosis caused by the protozoan parasite Trypanosoma cruzi. This infection is present in most Latin American countries, although, due to migratory movements, it is a growing cause for concern in non-endemic countries. The only two drugs currently available for its treatment-benznidazole and nifurtimox-were marketed 50 years ago. While they are very effective for acute and recent infection, and for the prevention of maternofoetal transmission, their efficacy declines in people who have chronic infection, especially those older than 18 years of age. In the presence of visceral involvement, parasiticidal treatment is of little or no value. The safety profile of both drugs is far from ideal, with frequent adverse events and high rates of drug discontinuation, mainly in adults. So far, new drugs and new strategies have not been shown to improve the results of the current nitroimidazoles, although the results are promising. In this review, we focus on the aspects that allow clinicians to make the best use of currently available drugs. In addition, we discuss new therapeutic options and ongoing research in the field.

Trypanocidal treatment of Chagas disease / Tratamiento tripanocida de la enfermedad de Chagas

Chagas disease is a neglected parasitosis caused by the protozoan parasite Trypanosoma cruzi. This infection is present in most Latin American countries, although, due to migratory movements, it is a growing cause for concern in non-endemic countries. The only two drugs currently available for its treatment—benznidazole and nifurtimox—were marketed 50 years ago. While they are very effective for acute and recent infection, and for the prevention of maternofoetal transmission, their efficacy declines in people who have chronic infection, especially those older than 18 years of age. In the presence of visceral involvement, parasiticidal treatment is of little or no value. The safety profile of both drugs is far from ideal, with frequent adverse events and high rates of drug discontinuation, mainly in adults. So far, new drugs and new strategies have not been shown to improve the results of the current nitroimidazoles, although the results are promising. In this review, we focus on the aspects that allow clinicians to make the best use of currently available drugs. In addition, we discuss new therapeutic options and ongoing research in the field.(AU)

La enfermedad de Chagas es una parasitosis desatendida causada por el parásito protozoico Trypanosoma cruzi. Esta infección está presente en la mayoría de los países de América Latina aunque, debido a los movimientos migratorios, es un motivo de creciente preocupación en los países no endémicos. Los 2 únicos fármacos disponibles en la actualidad para su tratamiento (benznidazol y nifurtimox) se comercializaron hace 50 años. Aunque son muy eficaces para las infecciones agudas y recientes, así como para la prevención de la transmisión maternofetal, su eficacia disminuye en las personas que padecen infecciones crónicas, especialmente en mayores de 18 años. En presencia de afectación visceral, el tratamiento parasiticida tiene poco o ningún valor. El perfil de seguridad de ambos fármacos dista mucho de ser ideal, con efectos adversos frecuentes y altas tasas de abandono del tratamiento, especialmente en adultos. Hasta ahora no se ha demostrado que los nuevos medicamentos y las nuevas estrategias mejoren los resultados de los nitroimidazoles actuales, aunque los resultados son prometedores. En esta revisión nos centramos en los aspectos que permiten a los médicos hacer el mejor uso de los medicamentos disponibles en la actualidad. Además, analizamos las nuevas opciones terapéuticas y las investigaciones en curso en este campo.(AU)

Mass treatment as a strategy to control intestinal parasites does not reduce the prevalency of infections in Guarani indigenous schoolchildren in Brazil / TRATAMENTO EM MASSA COMO ESTRATÉGIA DE CONTROLE DE PARASITAS INTESTINAIS NÃO REDUZ A PREVALÊNCIA DE INFECÇÕES EM ESCOLARES INDÍGENAS GUARANIS NO BRASIL

The high frequency of intestinal parasites is favored by environmental and socio-cultural conditions of indigenous populations, and is still a neglected public health problem. Mass administration of broad-spectrum drugs aims to reduce the prevalence and intensity of the infections. The prevalence of intestinal parasites in school-children in an indigenous Guarani village was evaluated before and after the mass treatment of the population with albendazole. In the first phase of collection of stool samples, 81.4% of them were positive for enteroparasites and in the second phase, after two doses of antiparasitic medication, 87.5% were positive. Although the prevalence of infections by some helminths has reduced after treatment, many parasites remained frequent in the studied population, showing a change in the epidemiological profile in the distribution of these diseases in the population. The prevalence of intestinal parasites in indigenous schoolchildren proved to be high even after mass treatment with albendazole.

A alta frequência de parasitoses intestinais é favorecida por condições ambientais e socioculturais das populações indígenas, sendo ainda um problema de saúde pública negligenciado. A administração em massa de medicamentos de amplo espectro busca reduzir o número e a intensidade das infecções. Avaliou-se a prevalência de parasitoses intestinais em escolares de uma aldeia indígena Guarani, antes e após o tratamento em massa da população com o albendazol. Na primeira fase de coleta das amostras de fezes, 81,4% delas apresentaram-se positivas para enteroparasitos e na segunda fase, após duas doses de antiparasitário, 87,5% apresentaram-se positivas. Embora a prevalência de infecções por alguns helmintos tenha reduzido após o tratamento, muitos parasitos continuaram frequentes na população estudada, mostrando uma mudança no perfil epidemiológico na distribuição dessas doenças na população. A prevalência de enteroparasitoses nos escolares indígenas mostrou-se elevada mesmo após o tratamento em massa com albendazol.

Resistance of bovine gastrointestinal nematodes to four classes of anthelmintics in the semiarid region of Paraíba state, Brazil / Resistência de nematódeos gastrintestinais de bovinos à quatro classes de anti-helmínticos no semiárido do Estado da Paraíba, Brasil

Abstract The effectiveness of four anthelmintic classes on cattle gastrointestinal nematodes in the semi-arid region of Paraiba State, Brazil, was evaluated. Twenty farms were used, testing 40 animals in each one, totaling 800 animals. Cattle were divided into four groups composed with ten animals: I, treated with albendazole sulfoxide 15%; II, treated with ivermectin 1%; III, treated with closantel 25%; IV, treated with levamisole hydrochloride 7.5%. All treatments were administered subcutaneously. For the Fecal Egg Count Reduction Test (FECRT), individual fecal samples were collected on days 0 and 14, and sent for analysis of egg count per gram of feces (EPG) and larval cultures. It was observed that multiresistance was present in 95% (19/20) of the farms. Resistance to ivermectin and albendazole was observed in 95% (19/20), to closantel in 75% (15/20) and to levamisole in 20% (4/20). The most used management system was semi-intensive (75%; 15/20) and the ivermectin was the most reported drug for controlling helminths (65%; 13/20). Haemonchus spp. was the most prevalent helminth genus. It was concluded that the anthelmintic resistance of bovine gastrointestinal nematodes is high in the semi-arid of Paraíba State, Brazil, with multiresistance observed mainly to ivermectin, albendazole and closantel.

Resumo Avaliou-se a eficácia de quatro classes de anti-helmínticos sobre nematódeos gastrintestinais de bovinos na região semiárida da Paraíba, Brasil. Foram utilizadas 20 fazendas, sendo testados 40 animais em cada uma, totalizando 800 animais. Os bovinos foram distribuídos em quatro grupos compostos por dez animais: I, tratado com sulfóxido de albendazol 15%; II, tratado com ivermectina 1%; III, tratado com closantel 25%; IV, tratado com cloridrato de levamisole 7,5%. Para o Teste de Redução da Contagem de Ovos Fecais (TRCOF), amostras fecais individuais foram coletadas nos dias 0 e 14 e enviadas para análises de contagem de ovos por grama de fezes (OPG) e coproculturas. Observou-se que a multirressistência estava presente em 95% (19/20) das fazendas. Foi observada resistência à ivermectina e ao albendazol, em 95% das fazendas (19/20); ao closantel, em 75% (15/20) e, ao levamisole, em 20% (4/20). O sistema de manejo mais utilizado foi o semi-intensivo (75%; 15/20) e a ivermectina foi o fármaco mais relatado para controle de verminose (65%; 13/20). O gênero de helminto mais prevalente foi Haemonchus spp. (76,7%). Conclui-se que é alta a resistência anti-helmíntica por nematódeos gastrintestinais de bovinos no Semiárido da Paraíba, Brasil, com multirressistência observada principalmente à ivermectina, ao albendazol e ao closantel.

Practices employed by veterinary practitioners for controlling canine gastrointestinal helminths and ectoparasites / Práticas realizadas por veterinários para controle de helmintos gastrintestinais e ectoparasitos de cães

Abstract The present study attempted to evaluate the practical experience and methods employed by Brazilian veterinary practitioners for control of parasites. Twenty-one questions were asked of 403 veterinary practitioners based in different climatic zones with reference to parasite epidemiology from the country. Administration of a combination of drugs at three-month intervals was the most common regime recommended for prophylaxis against gastrointestinal helminths, with a single treatment repeated after 15 days. Routine prophylaxis against dog ectoparasites was recommended by 82.4% veterinary practitioners, and 46.6% changed the drug compound used. Monthly prophylaxic treatments for ectoparasites, using systemic, topical and/or collar-impregnated drugs, was recommended by 21.5% veterinary practitioners. Side-effects of ectoparasiticide-impregnated collars were suspected by 58% of the veterinary practitioners. Isoxazolines were the most frequently used chemical group to treat ectoparasites in dogs. Poor efficacy of fipronil in controlling ticks was suspected by 79.5% of the veterinary practitioners. The isoxazolines and combination of anthelmintic compounds are the most common drugs to prevent or treat ectoparasites and gastrointestinal nematodes, respectively. The suspect of the inefficacy of antiparasitic drugs is shared among the veterinary practitioners from part of Brazil. Guidelines are needed, specifically for the control of gastrointestinal helminths and ectoparasites in Brazilian dogs.

Resumo O presente estudo avaliou os métodos de controle empregados por médicos veterinários clínicos para o controle de parasitos de cães no Brasil. Vinte e uma perguntas foram feitas a 403 veterinários de diferentes regiões do país. O uso de associações de compostos ativos em intervalos de três meses foi o mais recomendado para profilaxia de helmintos gastrointestinais, repetido após 15 dias. A profilaxia de rotina contra ectoparasitos foi recomendada por 82,4% dos veterinários, e 46,6% mudam rotineiramente o composto indicado. Tratamentos profiláticos mensais para ectoparasitos, com produtos sistêmicos, tópicos e / ou impregnados com colar, foram recomendados por 21,5% dos veterinários. Os efeitos colaterais das coleiras impregnadas com ectoparasiticidas foram relatados por 58% dos médicos veterinários. As isoxazolinas foram o grupo químico mais utilizado para tratar ectoparasitos em cães. A baixa eficácia do fipronil no controle de carrapatos foi suspeitada por 79,5% dos médicos veterinários. As isoxazolinas e a associação de compostos anti-helmínticos são os medicamentos mais comuns para prevenir ou tratar ectoparasitos e nematoides gastrointestinais, respectivamente. A suspeita da ineficácia dos antiparasitários é compartilhada entre os médicos veterinários de algumas regiões do Brasil. Orientações são necessárias, especificamente para o controle de helmintos e ectoparasitos gastrointestinais em cães no Brasil.

Trypanocidal treatment of Chagas disease.

Chagas disease is a neglected parasitosis caused by the protozoan parasite Trypanosoma cruzi. This infection is present in most Latin American countries, although, due to migratory movements, it is a growing cause for concern in non-endemic countries. The only two drugs currently available for its treatment-benznidazole and nifurtimox-were marketed 50 years ago. While they are very effective for acute and recent infection, and for the prevention of maternofoetal transmission, their efficacy declines in people who have chronic infection, especially those older than 18 years of age. In the presence of visceral involvement, parasiticidal treatment is of little or no value. The safety profile of both drugs is far from ideal, with frequent adverse events and high rates of drug discontinuation, mainly in adults. So far, new drugs and new strategies have not been shown to improve the results of the current nitroimidazoles, although the results are promising. In this review, we focus on the aspects that allow clinicians to make the best use of currently available drugs. In addition, we discuss new therapeutic options and ongoing research in the field.

Berberina, curcumina y quercetina como potenciales agentes con capacidad antiparasitaria

Introducción: El uso indiscriminado de agentes antiparasitarios ha resultado en el establecimiento de resistencia a ellos. Por lo cual es necesario el desarrollo de nuevas alternativas de tratamiento. Los productos naturales poseen diversas cualidades como posibles coadyuvantes en terapias contra distintos agentes etiológicos, entre los que destaca sus efectos antiparasitarios. Objetivo: Evaluar la actividad antiparasitaria, antioxidante, citotóxica y citoprotectora de Berberina (Ber), Curcumina (Cur) y Quercetina (Qr). Metodología: Se prepararon soluciones de Ber, Cur y Qr grado analítico y se realizaron alícuotas a diferentes concentraciones para su evaluación en contra de: Entamoeba histolytica, Trichomonas vaginalis y Strongyloides venezuelensis, paraello, se determinó la concentración inhibitoria media (IC50), además se determinó la capacidad antioxidante (CE50) mediante la prueba de DPPH, ambos por la prueba de Probit. Mediante la técnica de hemólisis se determinó la actividad citotóxica y citoprotectora, se aplicó Anova y la prueba de Tukey para determinar la diferencia de las medias en los tratamientos evaluados. Resultados: Ber, Cur y Qr, presentaron actividad en contra de E. histolytica, T. vaginalis y S. venezuelensis in-vitro. Ber presentó IC50 de 1.7, 1.2 y 1.9 μM respectivamente siendo más efectivo en comparación de Cur con IC50 de 55.3, 40.6 y 13.7 μM o Qr con IC50 de 147.2, 93.2 y 110.9 μM, sin embargo, la mejor actividad antioxidante (EC50 = 1.1 μg/ml), citoprotectora y menos hemolítica, fue presentada por Qr (P < 0.001) en comparación con el control evaluado. Conclusiones: Los metabolitos de origen natural berberina, curcumina y quercetina, poseen actividad en contra de trofozoítos de E. histolytica, T. vaginalisy larvas de S. venezuelensis en dosis bajas comparables con los fármacos de referencia para el caso de Ber. Además, estos productos de origen natural, no sintético podrían ser objeto de futuras investigaciones para coadyuvar al tratamiento de parasitosis, ya que, en dosis bajas, mostraron actividad antioxidante sin mostrar hemólisis considerable en eritrocitos humanos.

Introduction: The indiscriminate use of antiparasitic agents has resulted in the establishment of resistance to them. Therefore, the development of new treatment alternatives is necessary. Natural products have various qualities as possible adjuvants in therapies against different etiological agents, among which its antiparasitic effects stand out. Objective: To evaluate the antiparasitic, antioxidant, cytotoxic, and cytoprotective activity of Berberine (Ber), Curcumin (Cur), and Quercetin (Qr). Methods: Analytical grade Ber, Cur, and Qr solutions were prepared, and aliquots were made at different concentrations for their evaluation against Entamoeba histolytica, Trichomonas vaginalis, and Strongyloides venezuelensis. To do this, the mean inhibitory concentration (IC50) was determined, and the antioxidant capacity (EC50) was also determined by the DPPH assay, both using the Probit statistical test. The cytotoxic and cytoprotective activity was determined by the hemolysis technique, Anova and Tukey's test were applied to determine the difference in the means in the treatments evaluated. Results: Ber, Cur, and Qr, showed activity against E. histolytica, T. vaginalis, and S. venezuelensisin-vitro. Ber presented IC50 of 1.7, 1.2, and 1.9 μM respectively, being more effective compared to Cur with IC50 of 55.3, 40.6, and 13.7 μM, or Qr with IC50 of 147.2, 93.2, and 110.9 μM, however, the best antioxidant activity (EC50 = 1.1 μg/ml), cytoprotective and less hemolytic, was presented by Qr (P < 0.001) compared to the evaluated control. Conclusions: The metabolites of natural origin berberine, curcumin, and quercetin, have activity against trophozoites of E. histolytica, T. vaginalis and larvae of S. venezuelensis in low doses comparable to the reference drugs in the case of Ber. Furthermore, these non-synthetic products of natural origin could be the subject of future research to help treat parasitosis, since in low doses, they showed antioxidant activity without showing considerable cytotoxicity in human erythrocytes.

Compostos carbonílicos α, ß-insaturados e hidrazonas sintéticas como antiparasitários / α, ß-Unsaturated carbonyl compounds and Synthetic hydrazones as antiparasitics

Apesar da grande relevância médica e social, e por serem responsáveis por grande parte das mortes em países subdesenvolvidos e em desenvolvimento as doenças negligenciadas (DN), ainda, não apresentam terapêutica eficaz. Dentre as diversas DN, doenças como a doença de Chagas, a Leishmaniose visceral e a malária, se destacam no cenário nacional, por terem alta incidência e prejuízos sociais. Os fármacos disponíveis para o tratamento destas parasitoses, apresentam alta toxicidade e, em alguns casos, resistência por parte dos parasitas. Assim sendo, faz-se necessário o planejamento e desenvolvimento de novos agentes quimioterápicos mais seguros e eficazes. Dentre as diferentes estratégias de planejamento de fármacos, selecionamos o planejamento de fármacos baseado na estrutura do ligante - LBDD (Ligand-Based Drug Design) - como base para desenvolvimento deste trabalho. Nesta estratégia, utiliza-se o conhecimento de moléculas (ligantes) e de suas atividades biológicas conhecidas previamente determinadas experimentalmente, como protótipos para a busca de novas entidades químicas com atividade biológica semelhante ou melhorada. Sendo assim, o presente trabalho teve como objetivo a síntese e avaliação biológica de moléculas bioativas para o tratamento de doenças parasitárias. Baseando-se no conhecimento prévio da atividade antiparasitária de compostos carbonílicos α,ß-insaturados e hidrazonas, foram sintetizados séries de compostos destas classes químicas na busca de novos agentes quimioterápicos. Os compostos obtidos foram avaliados contra a forma epimastigota de Trypanosoma cruzi, promastigota de Leishmania donovani, amastigota de Leishmania infantum e, também, determinou-se o seu grau de citotoxicidade (CC50) frente a células de macrófago humanos diferenciado (THP-1). As 31 moléculas obtidas foram caracterizadas por técnicas de ponto de fusão, RMN 1H e RMN 13C e avaliada sua pureza por HPLC. Os compostos da classe da cinamoil-hidrazonas apresentaram-se como promissores antiparasitários, mostrando atividade frente a forma promastigota (Leishmania donovani), 4 dos 12 compostos foram ativos (IC50= 1,27 - 13,68 µM) e frente a forma amastigota (Leishmania infantum), 10 dos 12 compostos apresentaram atividade (9,09 - 63,5 µM). Mesmo apresentando citotoxicidade moderada (CC50 = 8,83 - 87,47 µM), os compostos obtiveram valores inferiores ao fármaco de referência (doxorubicina: CC50 = 0,26 µM). Diante do exposto, o planejamento de fármacos realizado por LBDD mostrou-se bem-sucedido, pois a classe de cinamoil-hidrazonas mostrou-se promissora como antiparasitários, visto sua atividade na escala de baixo micromolar e moderada citotoxicidade em células humanas. Esses resultados assinalam que a classe de compostos descrita está passível a continuar sendo investigada no intuito de aprimorar os protótipos obtidos na busca de novos agentes quimioterápicos antiparasitários e desvendar os mecanismos de ação leishmanicida

Despite to the great medical and social relevance and the amount of deaths in underdeveloped and developing countries, neglected diseases (ND) still do not have an effective therapy. Among the various ND, illnesses such as Chagas disease, visceral leishmaniasis and malaria holds a great importance in the Brazilian scenario due to high incidence and social damage. The drugs available for the treatment of these parasitosis present high toxicity and, in some cases, resistance by the pathogens. Thus, the planning and development of new, safer and more effective chemotherapeutic substances are urgent needed. Among the different drug planning strategies, we selected ligand-based drug design (LBDD) as the basis for the development of this work. In this strategy, we use the knowledge of molecules (ligands) and their known biological activities previously determined experimentally, as prototypes to search for new chemical entities with similar or improved biological activity. Therefore, the present work aimed the synthesis and biological evaluation of bioactive molecules for the treatment of parasitic diseases. Based on previous knowledge of the antiparasitic activity of α,ß-unsaturated and hydrazone carbonyl compounds, series of compounds of these chemical classes were synthesized in search of new chemotherapeutic agents. The compounds obtained were evaluated against the epimastigote form of Trypanosoma cruzi, Leishmania donovani promastigote, Leishmania infantum amastigote and their cytotoxicity (CC50) against differentiated human macrophages (THP-1). The 31 molecules obtained were characterized by melting point, 1 H NMR and 13C NMR techniques and their purity were characterized by HPLC. The cinnamoyl hydrazone class compounds showed promising antiparasitic activity, showing activity against promastigote form (L. donovani), 4 of 12 compounds were active (IC50 = 1.27 - 13.68 µM) and amastigote form (L. infantum), 10 of the 12 compounds showed activity (9.09 - 63.5 µM). Even presenting moderate cytotoxicity (CC50 = 8.83 - 87.47 µM), the compounds had values below the reference drug (doxorubicin: CC50 = 0.26 µM). Considering the results, LBDD drug planning proved to be successful and the class of cinnamoyl hydrazones were promising as antiparasitics due to its activity in low micromolar scale and moderate cytotoxicity in human cells. These results indicate that the described class of compounds can be further investigated in order to improve the prototypes obtained in the search for new antiparasitic chemotherapeutic agents and to unravel the mechanisms of action of leishmanicidal molecules

Resultados académicos en Farmacología de estudiantes de Enfermería Universidad Kmpa Vita. Uíge, Angola / Academic results in Pharmacology obtained by Nursing students. Kimpa Vita University. Uíge, Angola

Introducción: Los conocimientos en Farmacología tienen un lugar destacado en el ejercicio de la Enfermería. Es imprescindible que el estudiante de Enfermería en lo académico pueda asimilar todos los aspectos de la Farmacología durante la formación universitaria. Objetivo: Describir los resultados académicos en Farmacología de los estudiantes de Enfermería de la Universidad Kimpa Vita de Uíge en Angola. Materiales y Métodos: Estudio retrospectivo de los estudiantes de tercero, cuarto y quinto años de Licenciatura en Enfermería. La Farmacología se impartió por el programa de estudio de 2008 de Cuba, y se utilizó el sistema de evaluación establecido en Angola. Se revisaron las actas de examen y se aplicó una pregunta de respuesta simple para evaluar el nivel de conocimientos en el tema fármacos antimicrobianos y antiparasitarios. Resultados: Los resultados en Farmacología I fueron fundamentalmente:suficiente (74,83 por ciento), y en Farmacologia II: suficiente (61,57 por ciento) y bien (34,01 por ciento). Los resultados del tema evaluado fueron principalmente en los estudiantes de tercer año: suspensos (41,75 por ciento), cuarto año: suficiente (45,10 por ciento), y en quinto año: suficiente (32,58 por ciento) y bien (37,08 por ciento). Conclusiones: Los resultados en Farmacología se obtienen por el progreso en los métodos de estudio, la atencion individualizada al estudiante y la integración de sus contenidos en las disciplinas propias de la profesión(AU)

Introduction: The knowledge of Pharmacology has a significant importance in the practice of Nursing. It is indispensable that the Nursing student achieves the assimilation of knowledge of all the aspects of Pharmacology from the academic point of view during the university formation. Objectives: To describe the academic results in Pharmacology obtained by Nursing students of the Kimpa Vita University of Uíge in Angola. Materials and Methods: A retrospective study was carried out with third, fourth and fifth year Nursing students. Pharmacology was taught according to the Cuban curriculum of 2008, and the evaluation system established in Angola was used. Official documents were reviewed, and a question with a simple answer was applied to evaluate the level of knowledge of antimicrobial and anti-parasitic drugs. Results: The results in Pharmacology I were mainly satisfactory (74.83 percent); and in Pharmacology II they were satisfactory (61.57 percent) and good (34.01 percent). The results of the evaluation related to the topics were: third-year students: failed (41.75 percent); fourth-year students: satisfactory (45.10 percent), and fifth-year ones: satisfactory (32.58 percent and good (37, 08 percent). Conclusions: The results in Pharmacology are achieved by the progress in the study methods, the individualized attention to the student, and the integration of their contents to the disciplines related to the profession(AU)

Desenlaces clínicos en una cohorte colombiana de pacientes con síndrome de flujo vaginal tratadas con antimicóticos y antibióticos / Clinical outcomes in a Colombian cohort of patients with vaginal discharge syndrome treated with antifungals and antibiotics

Resumen Objetivo: Reportar el desempeño clínico de dos medicamentos indicados para tratamiento del síndrome de flujo vaginal (fluconazol, secnidazol y terconazol, clindamicina) y comparar el efecto clínico. Materiales y métodos: Estudio observacional, comparativo y analítico de cohortes al que se incluyeron pacientes con diagnóstico de síndrome de flujo vaginal susceptibles de ser tratadas con fluconazol-secnidazol o terconazol-clindamicina en 12 ciudades de Colombia, con seguimiento de 8 días (± 3 días). Este proyecto fue aprobado por un comité de ética en investigación con seres humanos. Resultados: Se incluyeron 176 pacientes, pero solo 153 (87%) completaron el seguimiento. Los límites de edad fueron 18 y 67 años; 134 (76%) iniciaron con fluconazol-secnidazol y 42 (24%) con terconazol-clindamicina. Por lo que se refiere a la comparación en disminución de los síntomas, fluconazol-secnidazol y terconazol-clindamicina: flujo (p = 0.0000), prurito (p = 0.002), irritación (p = 0.0000), mal olor (p = 0.001) y dispareunia (p = 0.4). Conclusión: La prescripción de la combinación fluconazol-secnidazol fue más frecuente. El apego al tratamiento fue de 86%. La proporción de disminución de los síntomas tuvo límites de 15 y 40%; para el flujo vaginal fue superior a 70% (fluconazol-secnidazol: 115 de 121 y terconazol-clindamicina: 29 de 41).

Abstract Objective: To know the real life clinical performance of the prescription of two drugs for the treatment of vaginal discharge syndrome (Fluconazole-Secnidazole and Terconazole-Clindamycin) and to compare the clinical outcomes. Materials and methods: An analytical cohort study was conducted. We included women older than 18 years with a diagnosis of vaginal discharge syndrome who were candidates to be treated with Fluconazole-Secnidazole or Terconazole-Clindamycin with 8 days (±3) of follow-up, in 12 cities of Colombia. This project was approved by a research with human being's ethics committee. Results: 176 patients were included, 153 (86.9%) completed the follow-up, their age ranged between 18 and 67 years. 134 (76.1%) started treatment with Fluconazole-Secnidazole and 42 (23.8%) Terconazole-Clindamycin. Symptoms improvement was compared (Enrollment vs. Control), finding for Fluconazole-Secnidazole and Terconazole-Clindamycin: discharge (p=0.0000), pruritus (p=0.002), irritation (p=0.0000), bad smell (p=0.001) and dyspareunia (p=0.4). Conclusions: The prescription of the combination Fluconazole-Secnidazole was more frequent. The adherence to treatment was 86%. The proportion of improvement in symptoms ranged between 15% and 40%, however, for the case of vaginal discharge it was greater than 70% (Fluconazole-Secnidazole: 115/121 and Terconazole-Clindamycin: 29/41).

Blastocystis sp. en humanos: actualización y experiencia clínico-terapéutica

Blastocystis sp. es uno de los parásitos del humano más frecuentemente identificados en el laboratorio clínico durante el estudio parasitológico de las muestras de heces. En esta revisión se actualizan los aspectos relativos a la diversidad genética y especificidad del huésped, la taxonomía, caracterización molecular, formas clínicas y experiencia terapéutica en pacientes inmuno-competentes y comprometidos, sintomáticos y asintomáticos, de la consulta de la Sección de Geohelmintiasis del Instituto de Medicina Tropical de la Facultad de Medicina de la Universidad Central de Venezuela, proponiendo el secnidazol como droga de primera elección. Se analiza la presencia de Blastocystis como patógeno humano o como comensal, formando parte de la microbiota intestinal. Se considera la tendencia actual entre los diferentes grupos de investigación a mirar la blastocistosis como un problema de salud pública en lugar de una entidad clínica frecuente y se incluyen elementos que pudieran reforzar esta visión. Se incluyen las medidas que pudieran contribuir a prevenir la parasitosis. Dado que la investigación sobre este parásito progresa rápidamente, se recomienda realizar revisiones frecuentes para mantener actualizados los conceptos relacionados con su epidemiología, diagnóstico, tratamiento y prevención en el paciente inmunocompetente así como en el inmunosuprimido.

Blastocystis sp. is one of the human parasites most frequently identified in the clinical laboratory during the parasitological study of stool samples. This review updates the aspects related to genetic diversity and host specificity, taxonomy, molecular characterization, clinical forms and therapeutic experience in symptom free and symptomatic immune-competent and compromised patients who attended to the Soil Transmitted Helminth Section of the Institute of Tropical Medicine of the Faculty of Medicine of the Central University of Venezuela, proposing secnidazole as the drug of first choice. The presence of Blastocystis as human pathogen or as part of the gut microbiota, are analyzed. The current trend among the different research groups is to look at Blastocystosis as a public health problem rather than a common clinical entity and include elements that could reinforce this view. Measures that could help prevent parasitic disease are also included. Since research on this parasite is progressing rapidly, frequent reviews are recommended to keep the concepts related to its epidemiology, diagnosis, treatment and prevention updated in the immunocompetent as well as the immunosuppressed patient.

Tratamento da fase crônica da Doença de Chagas: revisão sistemática / Treatment of chronic phase of Chagas Disease: systematic review

A tripanossomíase americana, mais conhecida como Doença de Chagas (DC), tem por agente causal o Trypanosoma cruzi (T. cruzi). Para efeitos práticos, o tratamento da DC pressupõe uma terapêutica específica e sintomática, embora haja divergências quanto às porcentagens de cura no tratamento etiológico da DC. Objetivo: Realizar uma revisão sistemática da literatura avaliando a eficácia do tratamento durante a fase crônica da DC. Métodos: Revisão sistemática da literatura nas bases de dados: Medline, Lilacs, Cochrane e SciELO, para identificar estudos relevantes, utilizando os descritores "Chagas disease AND treatment", "trypanossomiasis AND treatment", "Chagas disease AND benzonidazole" e "trypanossomiasis AND benzonidazole", onde foram avaliados os artigos publicados nos últimos dez anos. Para avaliação da qualidade metodológica dos ensaios clínicos randomizados controlados utilizou-se o escore Jadad, e para estudos observacionais, o instrumento de avaliação crítica utilizado foi a escala de avaliação Newcastle-Ottawa. Resultados: Foram encontrados 1.645 artigos nas diferentes bases de dados, sendo quatro incluídos para análise (dois ensaios clínicos randomizados e dois estudos caso controle). Conclusão: Os resultados demonstram que o tratamento etiológico da DC pode trazer benefícios durante a progressão clínica da doença e fornecer melhor prognóstico para os pacientes, particularmente quando administrados na forma indeterminada da doença

Tecnologias que empregam fármacos antiparasitários para tratamento da doença Chagas / Technologies using antiparasitic drugs to treat Chagas disease / Tecnologías que utilizan medicamentos antiparasitarios para tratar laenfermedad de Chagas

Com o aumento de diagnósticos da doença de Chagas, surge a necessidade de desenvolvimento de fármacos que tenham maior efeito contra os parasitas. O presente artigo objetiva apresentar um mapeamento tecnológico dos documentos de patentes relacionadas a tecnologias que empregam fármacos antiparasitários para tratamento da doença Chagas, por intermédio do banco de patentes do United States Patent andTrademark Office – USPTO. A primeira patente das 117 analisadas foi depositada nessa base em 1976. Os resultados demonstram que os estudos sobre o tratamento da doença de Chagas por meio de fármacos antiparasitários estão em desenvolvimento, focados na prevenção da doença, e são subsidiados em sua maioria por iniciativas particulares. Há pouco interesse da indústria farmacêutica no desenvolvimento de novos fármacos para tratamento e as universidades não têm incentivo para desenvolvimento de pesquisas sobre esse tema...

Con el aumento del diagnóstico de la enfermedad de Chagas, hay una necesidad de desarrollar fármacos quetengan un mayor efecto contra parásitos. Este artículo tiene como objetivo presentar un mapeo tecnológico dedocumentos de patentes relacionadas con las tecnologías que emplean fármacos antiparasitarios para tratarla enfermedad de Chagas, a través del United States Patent and Trademark Office – USPTO. Se analizaron117 patentes; la primera patente había sido presentada en esa base en 1976. Los resultados muestran que losestudios sobre el tratamiento de la enfermedad de Chagas a través de medicamentos antiparasitarios estánen desarrollo, centrados en la prevención de la enfermedad, y la mayoría es subvencionada por iniciativasprivadas. Hay poco interés por parte de la industria farmacéutica para desarrollar nuevos fármacos para eltratamiento y las universidades no tienen incentivos para desarrollar la investigación en esta área...

With increasing diagnostic Chagas disease, it is necessary to develop drugs that have a greater effect againstparasites. This article aims to present a technological mapping of patent documents related to technologiesemploying antiparasitic drugs to treat Chagas disease, through the patent database United States Patentand Trademark Office - USPTO. 117 patents were analyzed, and the first patent was filed on that basis in1976. The results show that studies of the treatment of Chagas disease through antiparasitic drugs are in development,focused on preventing the disease, and most of them are subsidized by private initiatives. Thereis little interest from the pharmaceutical industry to develop new drugs for treatment and universities haveno incentive to develop research in this area...

Interações entre antiparasitários e alimentos / Interactions between antiparasitic drugs and food

O uso, por vezes indiscriminado, de antiparasitários pode levar a consequências importantes na saúde do indivíduo, principalmente relacionadas a alterações no sistema gastrointestinal. As interações entre fármacos e nutrientes podem ocorrer quando um alimento ou nutriente altera a resposta esperada de um medicamento ou quando este interfere sobre o estado nutricional do indivíduo. Essa alteração da eficácia pode resultar em falha no tratamento ou até mesmo na toxicidade do fármaco. A fim de conhecer, identificar e prevenir interações indesejáveis entre antiparasitários e alimentos, o presente artigo de revisão aborda os principais fármacos e alimentos ou nutrientes envolvidos, bem como as consequências que tais interações podem acarretar ao indivíduo. O estado nutricional é de suma importância nas infecções parasitárias, pois é o determinante entre uma maior carga de parasitos ou a resistência total contra a infecção. De forma geral, indivíduos parasitados são inapetentes e emagrecidos, o que em crianças pode comprometer o desenvolvimento físico e intelectual. Portanto, o conhecimento e uma correta orientação médica, farmacêutica e nutricional levam a um tratamento bem sucedido...

The often indiscriminate use of antiparasitic drugs can lead to serious consequences for the health of the individual, mainly related to alterations in the gastrointestinal system. Interactions between drugs and nutrients may occur when a food or nutrient changes the expected response of a drug or when a medicine interferes with the individual's nutritional status. These changes may result in treatment failure or even toxicity of the drug. As an aid to the detection, identification and prevention of undesirable interactions between foods and antiparasite drugs, in this review we discuss the major drugs and foods or nutrients involved and the consequences that these interactions can have for the individual. Nutritional status is important in parasitic infections, as it is a factor determining the parasite load level or the total resistance against infection. Generally, individuals infected by parasites have a poor appetiteand are emaciated, which in children can damage physical and intellectual development. Therefore, knowledge of the parasite and proper medical, pharmaceutical and nutritional guidance lead to a more successful treatment...

Antiparasitic antibodies occur with similar frequency in patients with clinically established multiple sclerosis with or without oligoclonal bands in the cerebrospinal fluid / Anticorpos antiparasitarios ocorrem com frequencia semelhante em pacientes com esclerose multipla quando ha e quando nao ha bandas oligoclonais no liquido cefalorraquidiano

The "hygiene hypothesis" postulates an inverse relationship between the prevalence of parasitic infections and the frequency of multiple sclerosis (MS). Objective: It was to study whether antibodies against parasites could be demonstrated more frequently in blood serum from MS patients with oligoclonal bands (OCB) than from MS patients without OCB. Methods: We studied serum samples from 164 patients who had previously been analyzed to investigate OCB. Parasitic antibodies were studied through unidimensional electrophoresis of proteins on polyacrylamide gel against Taenia antigens, searching for antiparasitic specific low molecular weight antibodies and also for antiparasitic nonspecific high molecular weight antibodies. Results: Two of the 103 patients with no evidence of OCB had antibodies of low molecular weight and 59 of them had antibodies of high molecular weight. Of the 61 patients with evidence of OCB, one showed antibodies of low molecular weight and 16 showed antibodies of high molecular weight. Conclusion: Antiparasitic antibodies are detected with similar frequency in MS patients with OCB and in MS patients without OCB.

A "hipótese da higiene" postula haver relação inversamente proporcional entre a prevalência de infecções por parasitas e a frequência da esclerose múltipla (EM). Objetivo: Foi verificar se em pacientes com EM aparecem anticorpos antiparasitários mais frequentemente no grupo com bandas oligoclonais (BOC) do que no grupo sem BOC. Métodos: Foram estudadas amostras de sangue de 164 pacientes previamente analisadas para investigar BOC. Foi feita eletroforese unidimensional de proteínas em gel de poliacrilamida contra antígenos de Taenia para pesquisa de anticorpos específicos de baixo peso molecular e também de anticorpos inespecíficos de alto peso molecular. Resultados: Dois dos 103 pacientes em que não havia BOC apresentaram anticorpos de baixo peso molecular, e 59 apresentaram anticorpos de alto peso molecular. Dos 61 pacientes em que não havia BOC, um apresentou anticorpos de baixo peso molecular e 16, anticorpos de alto peso molecular. Conclusão: Anticorpos antiparasitários foram detectados com frequência semelhante em doentes com EM independentemente da presença ou não de BOC.

Diseño y preparación de formas farmacéuticas sólidas de Benznidazol para el tratamiento de la Enfermedad de Chagas / Design and Preparation fo Pharmaceutical Solid Dosage Forms of Benznidazole for the Treatment of Chagas Disease

INTRODUCCIÓN: En Argentina se emplea el benznidazolcomo terapéutica de primera línea para el tratamiento etiológico del Chagas. Desde su lanzamiento (hace más de 40 años), sólo se dispone de comprimidos convencionales de 100 mg; no se han desarrollado nuevas formas farmacéuticas que aumenten la eficacia y seguridad, ni alternativas con dosis pediátricas. OBJETIVOS: Desarrollar formas farmacéuticas de benznidazol que ofrezcan ventajas farmacoterapéuticas. MÉTODOS: Preformulación y diseño de nuevas formulaciones de benznidazol, con caracterización físico-química y selección de las formulaciones más favorables. Frente a la discontinuidad de producción del ingrediente activo benznidazol, se desarrolló una metodología de extracción a partir de 8520/8520/nica alternativa comercial disponible. RESULTADOS: Se obtuvieron nuevas formulaciones de comprimidos de 50 y 100 mg debenznidazol, con una rápida disolución del producto de referencia. Además, se obtuvieron formulaciones masticables de 50 mg bajo la forma de hidrogeles azucarados, con un efectivo enmascaramiento del mal sabor. Todas las formulaciones cumplieron los ensayos de evaluación de las propiedades farmacotécnicas y biofarmacéuticas, superando los perfiles de referencia. CONCLUSIONES: Se desarrollaron nuevas alternativas farmacéuticas de benznidazol de rápida disolución, que podrían mejorar el tratamiento etiológico de la enfermedad(especialmente en pediatría) y convertirse en herramientas aptas para su explotación comercial

INTRODUCTION: In Argentina, benznidazole is the drug of choice for the etiological treatment of Chagas disease. Since it was launched (more than 40 years ago), there are only 100 mg tablets available; the development included neither new pharmaceutical forms improving efficacy and safety, nor a pediatric dosage option. OBJECTIVES: To develop pharmaceutical form sof benznidazole with pharmacotherapeutic advantages. METHODS: Preformulation and design of new formulation sof benznidazole, with physicochemical characterization and selection of the most favorable formulations. Due to the discontinuity in the production of the active ingredient benznidazole, a specific methodology was developed in order to obtain it from the only commercially available alternative. RESULTS: New benznidazole tablet formulations were obtained (50 and 100 mg), with a rapid dissolution of the reference product, as well as chewable formulation sof 50 mg as sugar hydrogels featuring an effective taste masking. All formulations passed the evaluation tests for pharmacotechnical and biopharmaceutical properties, out performing the reference profiles. CONCLUSIONS:New fast-dissolving pharmaceutical dosage forms of benznidazole were developed, which could improve the etiological treatment of the disease (especially in the pediatric field) and become a proper tool for its commercial exploitation

Diseño y preparación de formas farmacéuticas sólidas de Benznidazol para el tratamiento de la Enfermedad de Chagas / Design and Preparation fo Pharmaceutical Solid Dosage Forms of Benznidazole for the Treatment of Chagas Disease

INTRODUCCION: En Argentina se emplea el benznidazolcomo terapéutica de primera línea para el tratamiento etiológico del Chagas. Desde su lanzamiento (hace más de 40 años), sólo se dispone de comprimidos convencionales de 100 mg; no se han desarrollado nuevas formas farmacéuticas que aumenten la eficacia y seguridad, ni alternativas con dosis pediátricas. OBJETIVOS: Desarrollar formas farmacéuticas de benznidazol que ofrezcan ventajas farmacoterapéuticas. METODOS: Preformulación y diseño de nuevas formulaciones de benznidazol, con caracterización físico-química y selección de las formulaciones más favorables. Frente a la discontinuidad de producción del ingrediente activo benznidazol, se desarrolló una metodología de extracción a partir de 8520/8520/nica alternativa comercial disponible. RESULTADOS: Se obtuvieron nuevas formulaciones de comprimidos de 50 y 100 mg debenznidazol, con una rápida disolución del producto de referencia. Además, se obtuvieron formulaciones masticables de 50 mg bajo la forma de hidrogeles azucarados, con un efectivo enmascaramiento del mal sabor. Todas las formulaciones cumplieron los ensayos de evaluación de las propiedades farmacotécnicas y biofarmacéuticas, superando los perfiles de referencia. CONCLUSIONES: Se desarrollaron nuevas alternativas farmacéuticas de benznidazol de rápida disolución, que podrían mejorar el tratamiento etiológico de la enfermedad(especialmente en pediatría) y convertirse en herramientas aptas para su explotación comercial (AU)

INTRODUCTION: In Argentina, benznidazole is the drug of choice for the etiological treatment of Chagas disease. Since it was launched (more than 40 years ago), there are only 100 mg tablets available; the development included neither new pharmaceutical forms improving efficacy and safety, nor a pediatric dosage option. OBJECTIVES: To develop pharmaceutical form sof benznidazole with pharmacotherapeutic advantages. METHODS: Preformulation and design of new formulation sof benznidazole, with physicochemical characterization and selection of the most favorable formulations. Due to the discontinuity in the production of the active ingredient benznidazole, a specific methodology was developed in order to obtain it from the only commercially available alternative. RESULTS: New benznidazole tablet formulations were obtained (50 and 100 mg), with a rapid dissolution of the reference product, as well as chewable formulation sof 50 mg as sugar hydrogels featuring an effective taste masking. All formulations passed the evaluation tests for pharmacotechnical and biopharmaceutical properties, out performing the reference profiles. CONCLUSIONS:New fast-dissolving pharmaceutical dosage forms of benznidazole were developed, which could improve the etiological treatment of the disease (especially in the pediatric field) and become a proper tool for its commercial exploitation (AU)

Avaliação in vitro de diferentes propriedades físico-químicas de medicamentos de uso infantil / In vitro evaluation of different physicochemical properties of pediatric medicines

Objetivo: Avaliar in vitro o pH endógeno, a Acidez Total Titulável (ATT) e o oBrix de medicamentos infantis. Metodologia: A amostra foi constituída por 22 diferentes medicamentos de 5 distintas classes: antibióticos, anti-histamínicos, antiparasitários, antiinflamatórios não esteróides e corticóides. As medidas do pH foram determinadas utilizando-se o potenciômetro, a acidez total foi realizada utilizando o método da A.O.A.C e o oBrix foi determinado por refratometria. Os dados foram expressos em médias e analisou-se a diferença entre os grupos, através da ANOVA. A significância utilizada foi de 0,05 com 95% de grau de confiança.Resultados: Verificou-se que 59,1% dos medicamentos apresentaram um pH menor que 5,5, sendo portanto potencialmente erosivo aos tecidos dentais. A menor e maior média do pH foram encontradas para o Benflogin (1,75) e para o Predsim (7,35), respectivamente. Em relação à ATT, a menor média foi verificada para o Cataflan (0,01%), enquanto o maior valor foi registrado para o Infectrin (0,98%). A avaliação do oBrix revelou que o Alersin apresentou a menor média (6,25%), enquanto o Cataflan mostrou o maior valor (74,33%). Não se verificou diferença estatisticamente significativa entre as variáveis pH e a classe de medicamento (P=0,950) e entre o °Brix e a classe de medicamento (P=0,477). Todavia, verificou-se diferenças estatisticamente significante em relação à acidez total e a classe de medicamento (P = 0,000), de modo que as diferenças maiores ficaram entre as médias dos antibióticos com: os antiinflamatórios (P=0,002), os antiparasitários (P=0,003) e os corticóides (P=0,005)...

Objective: To evaluate in vitro the endogenous pH, the total titratable acidity (TTA) and o Brix of pediatric medicines. Method: The sample consisted of 22 pediatric medicines belonging to five classes: antibiotics, antihistamines, anthelmintics, non-steroid antiinflammatory drugs and corticoids. The pH was measured with a potentiometer, total acidity was obtained by the AOAC method and oBrix was determined by refractometry. The data were expressed as means and the differences among the groups were analyzed by ANOVA. The significance level was set at 0.05 with a 95% confidence level. Results: As much as 59.1% of the medicines presented pH lower than 5.5, being therefore potentially erosive to the dental tissues. Benflogin (1.75) and Predsim (7.35) presented the lowest and the highest pH means, respectively. As for TTA, the lowest mean was obtained for Cataflan (0.01%) and the highest for Infectrin (0.98%). Evaluation of oBrix revealed that Alersin presented the lowest mean (6.25%) and Cataflan (74.33%) presented the highest mean. There was no statistically significant difference among the medicine classes regarding the pH (p=0.950) or regarding the o Brix (p=0.477). On the other hand, there were statistically significant differences among the medicine classes for TTA (p=0.000); the greatest differences were found between the antibiotics and the anti-inflammatory drugs (p=0.002), the anthelmintics (p=0.003) and the corticoids (p=0.005). Conclusion: The pediatric medicines may be considered as potentially erosive to the dental tissues. In view of the statistically significant differences among the medicine classes regarding the TTA, it is recommended that the control and follow up be directed to the erosive potential of each class. The antibiotics are the class of medicine with the highest pH and acidity, and so its intake should be followed by an adequate oral hygiene...

Assay and physicochemical characterization of the antiparasitic albendazole

The aim of this study was to characterize three batches of albendazole by pharmacopeial and complementary analytical techniques in order to establish more detailed specifications for the development of pharmaceutical forms. The ABZ01, ABZ02, and ABZ03 batches had melting points of 208 ºC, 208 ºC, and 209 ºC, respectively. X-ray diffraction revealed that all three batches showed crystalline behavior and the absence of polymorphism. Scanning electron microscopy showed that all the samples were crystals of different sizes with a strong tendency to aggregate. The samples were insoluble in water (5.07, 4.27, and 4.52 mg mL-1, respectively) and very slightly soluble in 0.1 M HCl (55.10, 56.90, and 61.70 mg mL-1, respectively) and additionally showed purities within the range specified by the Brazilian Pharmacopoeia 5th edition (F. Bras. V; 98% to 102%). The pharmacopeial assay method was not reproducible and some changes were necessary. The method was validated and showed to be selective, specific, linear, robust, precise, and accurate. From this characterization, we concluded that pharmacopeial techniques alone are not able to detect subtle differences in active pharmaceutical ingredients; therefore, the use of other complementary techniques is required to ensure strict quality control in the pharmaceutical industry.

O objetivo do trabalho foi caracterizar três lotes de albendazol com técnicas analíticas farmacopéicas e complementares a fim de estabelecer especificações mais detalhadas para o desenvolvimento de formas farmacêuticas. Os lotes ABZ01, ABZ02 e ABZ03 apresentaram fusão em 208 ºC, 208 ºC e 209 ºC. Foi possível evidenciar, por difração de raios X, que os três lotes apresentaram comportamento cristalino e ausência de polimorfismo. Através da microscopia eletrônica de varredura verificou-se que todas as amostras apresentaram cristais com diferentes tamanhos e forte tendência de agregação. As amostras foram insolúveis em água (5,07; 4,27 e 4,52 µg mL-1) e muito pouco solúveis em HCl 0,1M (55,10; 56,90 e 61,70 µg mL-1) e, ainda, apresentaram pureza dentro da faixa especificada pela F.Bras.V (98% a 102%). O método farmacopéico de doseamento não foi reprodutível, e algumas mudanças foram necessárias. O método foi validado e demonstrou ser seletivo, específico, linear, robusto, preciso e exato. A partir dessa caracterização, pode-se concluir que apenas técnicas farmacopéicas não são capazes de detectar diferenças sutis entre os ingredientes farmacêuticos ativos, necessitando, portanto, de uso de outras técnicas complementares para garantir um rígido controle de qualidade na indústria farmacêutica.