Preparação e avaliação de cápsulas gastro-resistentes de diclofenaco de sódio

Cápsulas resistentes ao trato gastrintestinal são freqüentemente usadas com diversos propósitos. Estas cápsulas promovem eficácia farmacológica e farmacocinética de substâncias que são instáveis, ou irritantes para a mucosa gástrica. O diclofenaco de sódio é um antiinflamatório não-esteróide, que, por ser muito utilizado, despertou o interesse do setor magistral para sua manipulação. Porém, o fármaco é irritante para a mucosa gástrica, havendo necessidade de se empregar substâncias capazes de proteger o meio gástrico da ação do medicamento e uma alternativa para o setor magistral é a manipulação de cápsulas gastro-resistentes. Estas cápsulas devem resistir, sem alteração, à ação do suco gástrico, mas desagregar-se rapidamente no suco intestinal. O objetivo deste trabalho foi preparar cápsulas na concentração de 50 mg/cápsula de diclofenaco de sódio formiladas ou revestidas com acetoftalato de celulose ou com Eudragit L100 na máquina de revestimento entérico “Enteric Coating Machine” PCCA ou manualmente. Foram analisados os resultados considerando o perfil de dissolução das formulações. Observou-se que as cápsulas revestidas na máquina com Eudragit L100 e com acetoftalato em acetona revestidas na máquina e manualmente mostraram bons resultados quanto à dissolução, porém, não apresentaram boa aparência no caso das cápsulas de cor vermelha. Quanto às cápsulas revestidas com formol, estas apresentam boa aparência, mas não deram bons resultados no teste de dissolução.

Relacionamento com médicos como estratégia de marketing da indústria farmacêutica

O marketing de relacionamento (MR) é uma das principais formas de melhoria no gerenciamento das relações das empresas com seus clientes e também parceiros. Definido como um conjunto de atividades com o objetivo de desenvolver e dar continuidade às relações entre a empresa e seus clientes, o MR trata da criação de uma base de relacionamento e integração em todas as fases do relacionamento. Na indústria farmacêutica, caracterizada por estratégias mercadológicas particulares, entre as quais se destaca a mudança de foco do consumidor final para o médico (que prescreve o medicamento), o MR é utilizado de forma constante, sendo disponibilizados altos investimentos nesta área. Com base neste contexto, este trabalho busca investigar a relação entre os incentivos da indústria farmacêutica, caracterizados pelas práticas de MR, e a quantidade de receitas prescritas pelos médicos. Assim, o objetivo central da pesquisa é identificar se o investimento desta indústria em MR junto aos médicos faz com que receite mais o produto. Para tanto, foi realizada uma pesquisa exploratória, utilizando dados secundários de um grande laboratório farmacêutico de nível mundial. Estes dados referem-se a uma amostra de 98 médicos de uma determinada especialidade que foram atendidos pelo Laboratório. Foram testadas as variáveis referentes às práticas de MR – visitas, amostras, congressos, coquetéis e outros, utilizando-se testes de regressão linear. Os resultados comprovaram que os médicos que recebem mais incentivos prescrevem mais receitas. Também foi verificado que existe uma relação positiva entre as práticas de MR e a quantidade de receitas prescritas, sendo que a concessão de inscrições em congressos influencia este resultado de forma mais significativa.

Desenvolvimento e validação de métodos analíticos para determinação do cloridrato de epinastina em comprimidos revestidos

O cloridrato de epinastina é um agente não sedativo, antagonista H1 da histamina, utilizado no tratamento da asma ou como anti-histamínico, comercializado no Brasil na forma farmacêutica comprimido revestido com o nome de Talerc ®. Embora, seja um medicamento amplamente comercializado não há referências relativas aos métodos de análise da forma farmacêutica. Este trabalho teve como objetivos o desenvolvimento e a validação de métodos analíticos para o controle de qualidade do cloridrato de epinastina nos comprimidos revestidos, bem como a realização de estudos preliminares de estabilidade térmica e de fotoestabilidade e determinação da cinética de reação do anti-histamínico em estudo.A análise qualitativa do cloridrato de epinastina foi realizada por ressonância magnética nuclear de próto n, determinação da faixa de fusão, espectrofotometria na região do infravermelho e do ultravioleta, cromatografia em camada delgada e por cromatografia a líquido de alta eficiência. Para análise quantitativa, foram validados os métodos por espectrofotometria na região do ultravioleta derivada de primeira ordem e por cromatografia a líquido de alta eficiência. A validação foi efetuada de acordo com as guias de validação disponíveis na literatura. No estudo preliminar de estabilidade térmica utilizou-se a forma farmacêutica submetida a temperatura de 80 °C por 10 dias. A fotoestabilidade foi realizada em câmara de luz ultravioleta de 254 nm por um período de 18 horas. Os métodos qualitativos foram úteis para identificação do cloridrato de epinastina. Os métodos quantitativos propostos foram validados de acordo com os parâmetros analíticos preconizados, podendo ser perfeitamente intercambiáveis. O estudo preliminar de estabilidade térmica não apresentou degradação da amostra nas condições de análise empregadas. O estudo de fotoestabilidade apresentou degradação intensa obedecendo uma cinética de reação de primeira ordem.

Arte, prazer e bisturi: construção corporal através da body modification

In view of a field research carried out by a team connected to the universe of body modification, it is possible to discern some uses and meanings linked to these forms of body interventions. Body modification or body change is part of the circuit of piercings and tattoos, although they are socially less thinned and more extreme, like scarifications, subcutaneous implants, bifurcated tongues, surfaces and body suspensions. The aim of this paper is to cast an anthropological glance on these practices, joining at the same context all the subjects involved with these techniques, placing them inside the same relational focus and capturing their journeys and trajectories. The discussions are concentrated on the notion of body building and urban life style. Ideas as personal distinctness and prestige imitation are also present in this universe, as well as matters attached to genre, pleasure, art, and to the so-called alternative circuit . This way, the ethnography so far presented here, reveals the complex and contemporaneous character of these practices of body markings in which the body appears as the central element in the experiences of the subjects of this study

Efeito da salinidade da água do mar no rendimento, composição e atividades biológicas de frações polissacarídicas da Chlorophyta Caulerpa cupressoides var. flabellata

Seaweeds sulfated polysaccharides have been described as having various pharmacological activities. However, nothing is known about the influence of salinity on the structure of sulfated polysaccharides from green seaweed and pharmacological activities they perform. Therefore, the main aim of this study was to evaluate the effect of salinity of seawater on yield and composition of polysaccharides-rich fractions from green seaweed Caulerpa cupressoides var. flabellata, collected in two different salinities beaches of the coast of Rio Grande do Norte, and to verify the influence of salinity on their biological activities. We extracted four sulfated polysaccharides-rich fractions from C. cupressoides collected in Camapum beach (denominated CCM F0.3; F0.5; F1.0; F2.0), which the seawater has higher salinity, and Buzios beach (denominated CCB F0.3; F0.5; F1.0; F2.0). Different from that observed for other seaweeds, the proximate composition of C. cupressoides did not change with increased salinity. Moreover, interestingly, the C. cupresoides have high amounts of protein, greater even than other edible seaweeds. There was no significant difference (p>0.05) between the yield of polysaccharide fractions of CCM and its CCB counterparts, which indicates that salinity does not interfere with the yield of polysaccharide fractions. However, there was a significant difference in the sulfate/sugar ratio of F0.3 (p<0.05) and F0.5 (p<0.01) (CCM F0.3 and CCB F0.5 was higher than those determined for their counterparts), while the sulfate/sugar ratio the F1.0 and F2.0 did not change significantly (p>0.05) with salinity. This result suggested that the observed difference in the sulfate/sugar ratio between the fractions from CCM and CCB, is not merely a function of salinity, but probably also is related to the biological function of these biopolymers in seaweed. In addition, the salinity variation between collection sites did not influence algal monosaccharide composition, eletrophoretic mobility or the infrared spectrum of polysaccharides, demonstrating that the salinity does not change the composition of sulfated polysaccharides of C. cupressoides. There were differences in antioxidant and anticoagulant fractions between CCM and CCB. CCB F0.3 (more sulfated) had higher total antioxidant capacity that CCM F0.3, since the chelating ability the CCM F0.5 was more potent than CCB F0.5 (more sulfated). These data indicate that the activities of sulfated polysaccharides from CCM and CCB depend on the spatial patterns of sulfate groups and that it is unlikely to be merely a charge density effect. C. cupressoides polysaccharides also exhibited anticoagulant activity in the intrinsic (aPTT test) and extrinsic pathway (PT test). CCB F1.0 and CCM F1.0 showed different (p<0,001) aPTT activity, although F0.3 and F0.5 showed no difference (p>0,05) between CCM and CCB, corroborating the fact that the sulfate/sugar ratio is not a determining factor for biological activity, but rather for sulfate distribution along the sugar chain. Moreover, F0.3 and F0.5 activity in aPTT test was similar to that of clexane®, anticoagulant drug. In addition, F0.5 showed PT activity. These results suggest that salinity may have created subtle differences in the structure of sulfated polysaccharides, such as the distribution of sulfate groups, which would cause differences in biological activities between the fractions of the CCM and the CCB

Avaliação do estresse oxidativo induzido por superfícies de titânio

Commercially pure Titanium (cp Ti) is a material largely used in orthopedic and dental implants due to its biocompatibility properties. Changes in the surface of cp Ti can determine the functional response of the cells such as facilitating implant fixation and stabilization, and increased roughness of the surface has been shown to improve adhesion and cellular proliferation. Various surface modification methods have been developed to increase roughness, such as mechanical, chemical, electrochemical and plasma treatment. An argon plasma treatment generates a surface that has good mechanical proprieties without chemical composition modification. Besides the topography, biological responses to the implant contribute significantly to its success. Oxidative stress induced by the biomaterials is considered one of the major causes of implant failure. For this reason the oxidative potential of titanium surfaces subjected to plasma treatment was evaluated on this work. CHO-k1 cells were cultivated on smooth or roughed Ti disks, and after three days, the redox balance was investigated measuring reactive oxygen species (ROS) generation, total antioxidant capacity and biomarkers of ROS attack. The results showed cells grown on titanium surfaces are subjected to intracellular oxidative stress due to hydrogen peroxide generation. Titanium discs subjected to the plasma treatment induced less oxidative stress than the untreated ones, which resulted in improved cellular ability. Our data suggest that plasma treated titanium may be a more biocompatible biomaterial.

Análise da estabilidade genética de células-tronco mesenquimais humanas

Human multipotent mesenchymal stromal cells (MSCs), also known as mesenchymal stem cells, have become an important and attractive therapeutic tool since they are easily isolated and cultured, have in vitro expansion potential, substantial plasticity and secrete bioactive molecules that exert trophic effects. The human umbilical cord as a cell source for cell therapy will help to avoid several ethical, political, religious and technical issues. One of the main issues with SC lines from different sources, mainly those of embryonic origin, is the possibility of chromosomal alterations and genomic instability during in vitro expansion. Cells isolated from one umbilical cord exhibited a rare balanced paracentric inversion, likely a cytogenetic constitutional alteration, karyotype: 46,XY,inv(3)(p13p25~26). Important genes related to cancer predisposition and others involved in DNA repair are located in 3p25~26. Titanium is an excellent biomaterial for bone-implant integration; however, the use can result in the generation of particulate debris that can accumulate in the tissues adjacent to the prosthesis, in the local bone marrow, in the lymph nodes, liver and spleen. Subsequently may elicit important biological responses that aren´t well studied. In this work, we have studied the genetic stability of MSC isolated from the umbilical cord vein during in vitro expansion, after the cryopreservation, and under different concentrations and time of exposition to titanium microparticles. Cells were isolated, in vitro expanded, demonstrated capacity for osteogenic, adipogenic and chondrogenic differentiation and were evaluated using flow cytometry, so they met the minimum requirements for characterization as MSCs. The cells were expanded under different concentrations and time of exposition to titanium microparticles. The genetic stability of MSCs was assessed by cytogenetic analysis, fluorescence in situ hybridization (FISH) and analysis of micronucleus and other nuclear alterations (CBMN). The cells were able to internalize the titanium microparticles, but MSCs preserve their morphology, differentiation capacity and surface marker expression profiles. Furthermore, there was an increase in the genomic instability after long time of in vitro expansion, and this instability was greater when cells were exposed to high doses of titanium microparticles that induced oxidative stress. It is necessary always assess the risks/ benefits of using titanium in tissue therapy involving MSCs, considering the biosafety of the use of bone regeneration using titanium and MSCs. Even without using titanium, it is important that the therapeutic use of such cells is based on analyzes that ensure quality, security and cellular stability, with the standardization of quality control programs appropriate. In conclusion, it is suggested that cytogenetic analysis, FISH analysis and the micronucleus and other nuclear alterations are carried out in CTMH before implanting in a patient

Efeito do tratamento térmico do titânio sobre a proliferação de células pré-osteoblásticas

Titanium is a biomaterial widely employed in biomedical applications (implants, prostheses, valves, stents). Several heat treatments are usually used in order to obtain physical properties required to different applications. This work studied the influence of the heat treatment on microstructure of commercial pure titanium, and their consequences in growth and proliferation of MC3T3-E1 cells. Discs of titanium were treated in different temperatures, and characterized by optical microscopy, image analysis, wettabillity, roughness, hardness and X-ray diffraction. After the heat treatment, significant modifications in these properties were observed. Pattern images of titanium, before and after the cell culture, were compared by overlapping to analyze the influence of microstructure in microstructure and preferences guidance cells. However, in general, titanium discs that showed a higher residual strength also presented an increase of cells numbers on surface

Síntese e caracterização do poli(ácido láctico) para potencial uso em sistemas de liberação controlada de fármacos

With the advances in medicine, life expectancy of the world population has grown considerably in recent decades. Studies have been performed in order to maintain the quality of life through the development of new drugs and new surgical procedures. Biomaterials is an example of the researches to improve quality of life, and its use goes from the reconstruction of tissues and organs affected by diseases or other types of failure, to use in drug delivery system able to prolong the drug in the body and increase its bioavailability. Biopolymers are a class of biomaterials widely targeted by researchers since they have ideal properties for biomedical applications, such as high biocompatibility and biodegradability. Poly (lactic acid) (PLA) is a biopolymer used as a biomaterial and its monomer, lactic acid, is eliminated by the Krebs Cycle (citric acid cycle). It is possible to synthesize PLA through various synthesis routes, however, the direct polycondensation is cheaper due the use of few steps of polymerization. In this work we used experimental design (DOE) to produce PLAs with different molecular weight from the direct polycondensation of lactic acid, with characteristics suitable for use in drug delivery system (DDS). Through the experimental design it was noted that the time of esterification, in the direct polycondensation, is the most important stage to obtain a higher molecular weight. The Fourier Transform Infrared (FTIR) spectrograms obtained were equivalent to the PLAs available in the literature. Results of Differential Scanning Calorimetry (DSC) showed that all PLAs produced are semicrystalline with glass transition temperatures (Tgs) ranging between 36 - 48 °C, and melting temperatures (Tm) ranging from 117 to 130 °C. The PLAs molecular weight characterized from Size Exclusion Chromatography (SEC), varied from 1000 to 11,000 g/mol. PLAs obtained showed a fibrous morphology characterized by Scanning Electron Microscopy (SEM)

Desenvolvimento de uma formulação cólon específica visando o tratamento da colite ulcerativa

Micro and nanoparticulate systems as drug delivery carriers have achieved successful therapeutic use by enhancing efficacy and reducing toxicity of potent drugs. The improvement of pharmaceutical grade polymers has allowed the development of such therapeutic systems. Microencapsulation is a process in which very thin coatings of inert natural or synthetic polymeric materials are deposited around microsized particles of solids or around droplets. Products thus formed are known as microparticles. Xylan is a natural polymer abundantly found in nature. It is the most common hemicellulose, representing more than 60% of the polysaccharides existing in the cell walls of corn cobs, and is normally degraded by the bacterial enzymes present in the colon of the human body. Therefore, this polymer is an eligible material to produce colon-specific drug carriers. The aim of this study was to evaluate the technological potential of xylan for the development of colon delivery systems for the treatment of inflammatory bowel diseases. First, coacervation was evaluated as a feasible method to produce xylan microcapsules. Afterwards, interfacial cross-linking polymerization was studied as a method to produce microcapsules with hydrophilic core. Additionally, magnetic xylan-coated microcapsules were prepared in order to investigate the ability of producing gastroresistant systems. Besides, the influence of the external phase composition on the production and mean diameter of microcapsules produced by interfacial cross-linking polymerization was investigated. Also, technological properties of xylan were determined in order to predict its possible application in other pharmaceutical dosage forms

Investigação farmacoepidemiológica do uso do clonazepam no distrito sanitário leste em Natal-RN

Prescription errors are the most serious type of medication errors found in the health system. The main purpose of this study was to evaluate the quality of clonazepam prescriptions. A descriptive and observational study with retrospective data collection was conducted at 30 community pharmacies in Natal/RN, Brazil, after informed consent was obtained from the pharmacists. A sample of 313 prescription notifications was randomly collected in October 2009. They were analyzed for legible handwriting and completeness. During the study, one researcher, two pharmacists, and one pharmacy undergraduate student evaluated patient and purchaser identification, pharmaceutical form, dosing regimen, administration route, and prescription by generic name. This research was approved by the institutional Ethics Committee. Among the 313 collected notifications, only 44.1% were legible. A total of 55.91% (175/313) had at least one illegible item, 100% contained incomplete information, and 97.12% (304/313) contained one or more abbreviations. The proportion of illegible handwriting related to the patient s identification (p=0.0001) was statistically significantly greater than that related to the drug purchaser s identification (p=0.0004). Contrary to legal requirements, prescriptions with the generic name accounted for 13.42% (42/313) of the total. All the examined notifications were handwritten. Prescription errors, which potentially can have serious consequences, have been evaluated worldwide, although little is known about this subject as it relates to community pharmacies. This study showed high percentages of prescribing problems, which justifies the development of future research about medication errors in community pharmacies and education activities for prescribers

Caracterização de superfícies de titânio modificado por oxidação à plasma

Recent years have seen a significant growth in surface modifications in titanium implants, resulting in shorter healing times in regions with low bone density. Among the different techniques, subtraction by chemical agents to increase oxidation has been applied for surface treatment of dental implants. However, this technique is generally unable to remove undesirable oxides, formed spontaneously during machining of titanium parts, raising costs due to additional decontamination stages. In order to solve this problem, the present study used plasma as an energy source to both remove these oxides and oxidize the titanium surface. In this respect, Ti disks were treated by hollow cathode discharge, using a variable DC power supply and vacuum system. Samples were previously submitted to a cleaning process using an atmosphere of Ar, H2 and a mixture of both, for 20 and 60 min. The most efficient cleaning condition was used for oxidation in a mixture of argon (60%) and oxygen (40%) until reaching a pressure of 2.2 mbar for 60 min at 500°C. Surfaces were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), atomic force microscopy (AFM), adhesion and cell proliferation. SEM showed less cell spreading and a larger number of projections orfilopodia in the treated samples compared to the control sample. AFM revealed surface defects in the treated samples, with varied geometry between peaks and valleys. Biological assays showed no significant difference in cell adhesion between treated surfaces and the control. With respect to cell proliferation, the treated surface exhibited improved performance when compared to the control sample. We concluded that the process was efficient in removing primary oxides as well as in oxidizing titanium surfaces

Superfícies de titânio modificadas termoquimicamente por plasma : avaliação da resposta biológica

This laboratory study involves the participation of a group with professionals from different areas that had contributed to the construction of a multidisciplinary knowledge, about biological response of titanium surfaces modified through thermochemical treatment by plasma. Thus, the crystalline phase was previously characterized in relation to the topography, roughness, molhability and nitrogen concentration in the samples surface. It s indispensable that materials implanted can influence in a good cellular response as well as promotes a bacteria action. Surfaces modified by plasma were exposed to different cultures such as: cellular (human osteoblastic) and bacteria (Staphylococcus epidermidis ATCC35984 and Pseudomonas aeruginosa ATCC 27853) in order to evaluate the biological response. It was evaluated the adhesion, proliferation, morphology and cellular preference of human ostheoblastic cells (HOST), as well as the formation of a biofilm and bacteria proliferation. It was still analyzed the bacteria selectivity ability in relation to the surfaces. The software Image Pro Plus was used to the counting of cells and bacteria adhered to the surface of disks. The results were submitted to the variance analysis (ANOVA), and then, by the Kruskal-Wallis test, using GraphPad Instat ® software, version 3.5 to Windows. The nitrided samples in spite of show a higher roughness and molhability showed a smaller bacteria growing and higher cellular proliferation, when compared to non treated samples, indicating that the treated material present a high efficiency to biomedical implants

Avaliação da publicidade de medicamentos veiculada nas principais emissoras de rádio de Natal-RN

Drugs advertising is one of the most important marketing resources used by the pharmaceutical industry to induce people to buy these products although they do not have the real necessity to use them. The purpose of this article is to evaluate drugs advertisings transmitted on radio stations in Natal/RN, from October 2007 to September 2008. Were collected 228 advertising pieces, where, 21 were different among themselves and corresponded to 15 drugs. The results showed that 73,3% of the drugs ads were announced on AM station and 26,7% on FM station. The majority of the drugs were constituted of analgesics (26%), following by antiacids, vitamins, phitotherapics (13% each). The legal analysis showed that each advertising had some kind of infraction. The omission of the registration number happened in each advertising, following by the totally lack of contraindications (95,2%) and contraindications DCB/DCI (76,2%). In 42,9% advertisements were observed the relation between drugs use and physique/intellectual/emotional/sexual performance and/or beauty and 33% of them had abusive exploration of illnesses. The obligatory warning was omitted in 28,6% and the offer of financial bonus happened in 9,5% cases. The content analysis demonstrated that the most persuasion and convincing elements observed were indicatives of consumption appeal (34,2%). The study indicates the necessity of the topic drugs advertisements to be treated in a wide context, that is, to be discussed as a public health concern. Although the advertising regulation and inspection is the State responsibility , this should be shared with the advertising agency, pharmaceutical industry and media. Furthermore, it is indispensable to inform and to conscience the population of their rights in such mistaken situation