Influence of compression forces on tablets disintegration by AC Biosusceptometry

Analysis of physical phenomena that occurs during tablet disintegration has been studied by several experimental approaches; however none of them satisfactorily describe this process. The aim of this study was to investigate the influence of compression force on the tablets by associating the AC Biosusceptometry with consolidated methods in order to validate the biomagnetic technique as a tool for quality control in pharmaceutical processes.Tablets obtained at five compression levels were submitted to mechanical properties tests. For uncoated tablets, water uptake and disintegration force measurements were performed in order to compare with magnetic data. For coated tablets, magnetic measurements were carried out to establish a relationship between physical parameters of the disintegration process. According to the results, differences between the compression levels were found for water uptake, force development and magnetic area variation measurements. ACB method was able to estimate the disintegration properties as well as the kinetics of disintegration process for uncoated and coated tablets. This study provided a new approach for in vitro investigation and validated this biomagnetic technique as a tool for quality control for pharmaceutical industry. Moreover, using ACB will also be possible to test these parameters in humans allowing to establish an in vitro/in vivo correlation (IVIVC). (C) 2007 Elsevier B.V. All rights reserved.

Propolis effect on streptozotocin-induced diabetic rats

Propolis is one of the hive products that has been used extensively in folk medicine, due to its several biological and pharmacological properties. Besides, propolis-containing products have been intensely marketed by the pharmaceutical industry and health-food stores. This work was carried out in order to investigate whether propolis treatment could revert the metabolic alterations of streptozotocin-induced diabetic rats. Animals were kept in metabolic cages and diabetes was induced by a single dose of streptozotocin (35 mg/kg, IV). After a week, rats with glycemia higher than 230 mg/dL were divided into two groups and treated with ethanolic extract of propolis (10 and 90 mg/kg, PO) for seven days. Glycemia and free fatty acids were determined, as well as food and water intake, body weight and urine volume were registered weekly. Data showed no significant differences in the analyzed variables. Based on these results, one may conclude that propolis had no effects after diabetes establishment, in our conditions assays. Further assays with different concentrations of propolis and periods of administration should be carried out in order to evaluate its therapeutic potential in this disease.

Propolis: Is there a potential for the development of new drugs?

Introduction: Propolis has plenty of biological and pharmacological properties and its mechanisms of action have been widely investigated in the last years, using different experimental models in vitro and in vivo. Researchers have been interested in the investigation of isolated compounds responsible for propolis action; however, there is lack of clinical research on the effects of propolis.Strategy and objectives: Since propolis-containing products have been marketed and humans have used propolis for different purposes, the goal of this review is to discuss the potential of propolis for the development of new drugs, by comparing data from the literature that suggest candidate areas for the establishment of drugs against tumors, infections, allergy, diabetes, ulcers and with immunomodulatory action.Conclusions: The efficacy of propolis in different protocols in vitro and in vivo suggests its therapeutic properties, but before establishing a strategy using this bee product, it is necessary to study: (a) the chemical nature of the propolis sample. (b) Propolis efficacy should be compared to well-established parameters, e.g. positive or negative controls in the experiments. Moreover, possible interactions between propolis and other medicines should be investigated in humans as well. (c) Clinical investigation is needed to evaluate propolis potential in patients or healthy individuals, to understand under which conditions propolis may promote health. Data point out the importance of this research field not only for the readers and researchers in the scientific community waiting for further clarification on the potential of propolis but also for the pharmaceutical industry that looks for new drugs. (C) 2010 Elsevier B.V. All rights reserved.

Acerola: importance, culture conditions, production and biochemical aspects

Origin and importance. Acerola, or Malpighia emarginata D. C., is native to the Caribbean islands, Central America and the Amazonian region. More recently, it has been introduced in subtropical areas (Asia, India and South America). The vitamin C produced by acerola is better absorbed by the human organism than synthetic ascorbic acid. Exportation of acerola crops is a potential alternative source of income in agricultural businesses. In Brazil, the commercial farming of acerola is quite recent. Climatic conditions. Acerola is a rustic plant. It can resist temperatures close to 0 degrees C, but it is well adapted to temperatures around 26 degrees C with rainfall between (1200 and 1600) mm per year. Fruit characteristics. Acerola fruit is drupaceous, whose form can vary from round to conic. When ripe, it can be red, purple or yellow. The fruit weight varies between (3 and 16) g. Maturation. Acerola fruit presents fast metabolic activity and its maturation occurs rapidly. When commercialised in ambient conditions, it requires fast transportation or the use of refrigerated containers to retard its respiration and metabolism partially. Production and productivity. Flowering and fruiting are typically in cycles associated with rain. Usually, they take place in 25-day cycles, up to 8 times per year. The plant can be propagated by cuttings, grafting or seedlings. Harvest. Fruits produced for markets needs to be harvested at its optimal maturation stage. For distant markets, they need to be packed in boxes and piled up in low layers; transportation should be done in refrigerated trucks in relatively high humid conditions. Biochemical constituents. Acerola is the most important natural source of vitamin C [(1000 to 4500) mg.100(-1) g of pulp], but it is also rich in pectin and pectolytic enzymes, carotenoids, plant fibre, vitamin B, thiamin, riboflavin, niacin, proteins and mineral salts. It has also shown active anti-fungal properties. Products and market. Acerola is used in the production of juice, soft drinks, gums and liqueurs. The USA and Europe are great potential markets. In Europe, acerola extracts are used to enrich pear or apple juices. In the USA, they are used in the pharmaceutical industry. Conclusions. The demand for acerola has increased significantly in recent years because of the relevance of vitamin C in human health, coupled with the use of ascorbic acid as an antioxidant in food and feed. Acerola fruit contains other significant components, which are likely to lead to a further increase in its production and trade all over the world.

Planejamento racional de fármacos baseado em produtos naturais

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Development of a bioassay to quantify the ricin toxin content of castor bean (Ricinus communis L.) seeds

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Morfoanatomia e histoquímica de Brosimum gaudichaudii Trécul (Moraceae)

Brosimum gaudichaudii, conhecida como mamacadela, é espécie comum nos cerrados, com grande valor na medicina popular e na indústria de medicamentos. A casca da raiz e do caule é empregada no tratamento do vitiligo, sendo o bergapteno e psoraleno, duas furanocumarinas, responsáveis pela ação farmacológica. Neste trabalho são apresentadas a caracterização morfoanatômica e a histoquímica de órgãos vegetativos de B. gaudichaudii, com informações sobre o embrião e o desenvolvimento pós-seminal. Amostras foram processadas segundo técnicas usuais em anatomia e ultra-estrutura vegetal. O embrião é do tipo total e invaginado, a plântula cripto-hipogéia e o sistema radicular do tirodendro é composto por raiz primária pouco desenvolvida em relação às raízes laterais. Plantas adultas apresentam raízes gemíferas longas, plagiotrópicas originando ramos caulinares aéreos; tais raízes possuem periderme com súber desenvolvido e floema secundário abundante em relação ao xilema, sendo facilmente destacados quando manipulados. O caule jovem e a folha apresentam epiderme unisseriada, grande densidade de tricomas tectores unicelulares e tricomas glandulares. Laticíferos não-articulados ramificados ocorrem em todos os órgãos, podendo invadir os elementos de vaso. Idioblastos fenólicos ocorrem em abundância em todos tecidos e órgãos analisados. O valor das características anatômicas observadas no controle de qualidade da droga é discutido.

Lições para a história das ciências no Brasil: Instituto Pasteur de São Paulo

Este artigo pretende mostrar a importância e o papel do Instituto Pasteur de São Paulo (1903-16) no desenvolvimento da ciência microbiológica no Brasil e no surgimento da indústria farmacêutica de capital nacional.

Saúde pública e as empresas químico-farmacêuticas

O artigo trata da formação da indústria farmacêutica brasileira. Aborda algumas questões de história econômica e social, tais como o surgimento do sistema de saúde pública, as práticas de combate às doenças infecciosas, desde as desinfecções e produção de substâncias químicas pela indústria, à soroterapia e produção de soros e vacinas nas instituições de pesquisa científica públicas e nas empresas farmacêuticas privadas. Toma para análise da indústria farmacêutica privada nacional, a empresa Instituto Pinheiros - Produtos Terapêuticos S.A., enfatizando as relações entre seus cientistas, no desenvolvimento de produtos, de tecnologia e da própria discussão científica com as instituições públicas de pesquisa criadas no âmbito da política de saúde pública pelo estado de São Paulo.

Isolamento de fungos produtores de ácido γ-linolênico de solo da Estação Ecologica de Juréia-Itatins, SP

Fungi producing γ-linolenic acid (GLA) were isolated from soil of the Ecological Station of Juréia-Itatins, SP. This essential fatty acid has aroused great interest due to its increasing by applications in pharmaceutical industry. The GLA production by zygomycetous fungi is an alternative way of comparing seed extraction. Thirty-two zygomycetous strains of Mucorales were isolated, most of them belonging to Mucor genus. The GLA production was evaluated after 4 days of incubation at 25°C on a rotary shaker at 150 rpm in medium containing 2% glucose, and 1% yeast extract, following new medium addition (20%) and incubation for an additional period of 3 days at 12°C, without agitation. The GLA production varied according to the microorganism and the strain.

Reflexão sobre o ensino farmacêutico

This paper aims to discuss the directions of pharmaceutical education based on the new curriculum guidelines from MEC (Ministry of Education - Brazil). In the recent past, Brazilian pharmaceutical faculties prioritized the formation of professional resources in specific modalities in detriment of pharmacist's private field: the prescription filling and delivery at the drugstore. In order to avoid repeating the same mistake it is necessary to develop new competence, allowing the graduates to develop skills to connect the scientific and technological knowledge to Brazilian social context. The new curriculum guidelines are about to finish a time when the undergraduate studies seemed to split the pharmacist into two different professionals: one for the clinical analysis and other for the pharmaceutical industry. The previous educational model, which supposedly allows for pharmaceutical care without providing a broad integral knowledge of health sciences, cannot be repeated in the new curriculum. However, teaching subjects in a superficial and segmented manner, replete of predictable and repetitive technical practices and without a skilled teaching staff, will give no improvement in pharmacists education care. It is clear that the return of the formation of specific human resources in the field won't happen in short time.

Chorismate synthase: An attractive target for drug development against orphan diseases

The increase in incidence of infectious diseases worldwide, particularly in developing countries, is worrying. Each year, 14 million people are killed by infectious diseases, mainly HIV/AIDS, respiratory infections, malaria and tuberculosis. Despite the great burden in the poor countries, drug discovery to treat tropical diseases has come to a standstill. There is no interest by the pharmaceutical industry in drug development against the major diseases of the poor countries, since the financial return cannot be guaranteed. This has created an urgent need for new therapeutics to neglected diseases. A possible approach has been the exploitation of the inhibition of unique targets, vital to the pathogen such as the shikimate pathway enzymes, which are present in bacteria, fungi and apicomplexan parasites but are absent in mammals. The chorismate synthase (CS) catalyses the seventh step in this pathway, the conversion of 5-enolpyruvylshikimate-3-phosphate to chorismate. The strict requirement for a reduced flavin mononucleotide and the anti 1,4 elimination are both unusual aspects which make CS reaction unique among flavin-dependent enzymes, representing an important target for the chemotherapeutic agents development. In this review we present the main biochemical features of CS from bacterial and fungal sources and their difference from the apicomplexan CS. The CS mechanisms proposed are discussed and compared with structural data. The CS structures of some organisms are compared and their distinct features analyzed. Some known CS inhibitors are presented and the main characteristics are discussed. The structural and kinetics data reviewed here can be useful for the design of inhibitors. © 2007 Bentham Science Publishers Ltd.

Estudos de medicamentos biosimilares

In Brazil, the registration of new drugs is carried out only when the regulatory agency (Anvisa, acronym in Portuguese) is fully satisfied with the evidence of their quality, efficacy and safety, presented by a pharmaceutical industry that strive for this registration. With the patent expiration, pharmaceutical companies are attracted to produce biological medicines called biosimilar or biogenerics or simply generics, whose approval may result in reduced treatment costs. But it is necessary that the biosimilar be, at least, equally efective and safe and without contaminants in relation to the original. Recent consensus guidelines aim to establish criteria for efcacy and safety of these medicines. Preclinical studies in vitro and in vivo, the origin of raw materials and clinical studies phase I, II and III are recommended for biosimilar medicine registration in the international market. Low molecular weight heparins are found in this situation. In this review we specifcally addressed this type of medicine, which could serve as a benchmark for other biosimilar medicines.

Ampolas de Vidro: Riscos e Benefícios

Background and objectives: Glass ampoules have been widely used in packaging injection drugs. Glass has important characteristics that allow it to be widely used in fabrication of recipients for drugs and other sterile substances. However, contamination of solutions with glass microparticles on breaking open glass ampoules, the presence of metals, percutaneous injury, and biological contamination justify the need of educational materials to orient the manipulation of ampoules. Contents: Glass microparticles generated in the snap-opening of ampoules, as well as metals that contaminate their contents can be aspirated and injected through several routes. Exogenous contaminations by glass and metals can reach several sites in the organism. They trigger organic reactions that may give rise to injuries. Opening ampoules can expose professionals to the risk of percutaneous injuries. These lesions increase the biological risk as they are the gateway for viruses and bacteria. Ampoules opening systems (VIBRAC and OPC) have been developed to reduce the incidence of such accidents. Alternative materials to glass may represent an interesting strategy to increase safety. The use of prefilled syringes may represent an evolution regarding safety. Conclusions: Team training and information provided by the pharmaceutical industry on the use of ampoules are fundamental in the prophylaxis of accidents and contaminations. The search for safer materials to replace glass is also important. © 2011 Elsevier Editora Ltda.

Caracterização radiométrica de ácidos fosfóricos e seus produtos industriais

The addition of phosphoric acids and their (by)products became a common practice in areas like metal treatment, detergent production, water and effluent treatment, as well by food, beverage and pharmaceutical industries. The phosphoric acids exhibit different radionuclides activity concentration, being important to evaluate the implications for the human and animal health. The 238U concentration in almost all raw acid phosphoric are within the worldwide range and the mean exposure rate for the filtration cake is 10 nGy/h, which is mainly attributed to 40K. The results obtained for total and (bio)available uranium concentration in filtration cake indicate that only 40% is (bio)available for plants. The radionuclides present in phosphoric acid food grade and filtration cake do not raise their concentration in human food chain or soils to harmful levels, consequently, not offering hazard to the ecosystem and animal or human health.