Physicochemical and dissolution profile characterization of pellets containing different binders obtained by the extrusion-spheronization process

Com a finalidade de se avaliar o comportamento de diferentes polímeros empregados como aglutinantes em pellets de pequeno diâmetro para uso oral foram preparadas formulações contendo paracetamol e um dos seguintes polímeros: PVP, PEG 1500, hidroxipropilmetilcelulose e metilcelulose por apresentarem diferentes propriedades aglutinantes. Os pellets foram obtidos pelo processo de extrusão/esferonização e secagem em leito fluidizado. Para avaliar a liberação do fármaco, empregou-se o método 3 da Farmacopeia Americana, também conhecido como Bio-Dis e o método preconizado pela mesma farmacopeia para comprimidos de paracetamol. Os pellets foram avaliados, ainda, com relação à granulometria, friabilidade, densidade verdadeira e teor. Os resultados indicaram que os diferentes aglutinantes empregados são capazes de afetar a produção e algumas das características físico-químicas dos pellets e o ensaio de dissolução revelou que as formulações comportam-se como produtos de liberação imediata. Os pellets obtidos apresentaram características de liberação favoráveis para a obtenção de comprimidos de liberação instantânea. O aparato 3 da Farmacopeia Americana demonstrou ser um método com melhor capacidade discriminatória entre as formulações, quando comparado com o método da cesta.With the purpose of evaluating the behavior of different polymers employed as binders in small-diameter pellets for oral administration, we prepared formulations containing paracetamol and one of the following polymers: PVP, PEG 1500, hydroxypropylmethylcellulose and methylcellulose, and we evaluated their different binding properties. The pellets were obtained by the extrusion/spheronization process and were subsequently subjected to fluid bed drying. In order to assess drug delivery, the United States Pharmacopeia (USP) apparatus 3 (Bio-Dis) was employed, in conjunction with the method described by the same pharmacopeia for the dissolution of paracetamol tablets (apparatus 1). The pellets were also evaluated for granulometry, friability, true density and drug content. The results indicate that the different binders used are capable of affecting production in different ways, and some of the physicochemical characteristics of the pellets, as well as the dissolution test, revealed that the formulations acted like immediate-release products. The pellets obtained presented favorable release characteristics for orally disintegrating tablets. USP apparatus 3 seems to be more adequate for discriminating among formulations than the basket method

Projeto e construção de um picnômetro a ar para caracterização de insumos e produtos farmacêuticos

This paper describes a project, construction and test of a low cost air pycnometer, developed to be used preferentially in pharmaceutical research. A complete discussion of the construction, test and calibration of this equipment is presented and some measurements are made using pharmaceutical powders and dry granulations. The equipment performance has been estimated through its calibration curve, and the obtained value to its volume resolution is about 1%. This equipment is accomplished at the Applied Nuclear Physics Laboratory of University of Sorocaba (LAFINAU) in Sorocaba, SP, Brazil and it was denominated "Picnômetro a Ar Uniso - PICNAU"

UVA and UVB formulation phototoxicity in a three-dimensional human skin model: photodegradation effect

In vitro three-dimensional human skin models are an innovative alternative to evaluate cytotoxicity and phototoxicity in the cosmetic industry. The aim of this study was to use a skin model to evaluate the potential toxicity of sunscreen formulations with or without exposure to UV radiation. In addition, the toxicity of these formulations was evaluated after exposure to photodegradation. The results showed toxicity with all formulations/conditions tested, including the control formulation, compared to PBS. Cell viability of photodegraded formulations - prior to the phototoxicity radiation process - was higher, indicating that some formulation components were degraded into products with reduced toxicity. The results also indicated that avobenzone was more unstable/toxic than octyl p-methoxycinnamate under the same test conditions. The sunscreens and their formulations were shown to be toxic to skin model cells to some extent, even when not exposed to UV irradiation; however the biological role of this toxicity is unclear. This result shows the importance of testing sunscreen formulations in real in-use conditions. Finally, since we used an in vitro assay based on a human cell model, this non-invasive technique represents a suitable alternative to animal models for phototoxicity tests in general and could have application in screening new sunscreen products

Sensory Priming: The olfaction as an attention inducer

In this study, we investigated the influence of the olfactive stimulus on visual attention. Two groups of 30 subjects participated in two experiments. Both experiments presented two arrays of fruits stimulus intercalated by an olfactive intervention. The stimulus was received in the form of images by the first group and in the form of words by the second group. An eye-tracking device monitored the timekeeping of visual attention dispensed in each stimulus. The results showed that olfactive priming influenced visual attention in both cases but with a greater degree in the images stimulus group. This study shows for the first time that image information is more susceptible to priming olfactive information than wording information. This effect may be associated with the formation of mental images in working memory, aroused by fragrances

<b>Desenvolvimento de formulações de comprimidos tamponados mastigáveis de didanosina com perfil de dissolução e capacidade neutralizante ácida otimizados</b>

Neste estudo buscou-se desenvolver formulações de comprimidos tamponados mastigáveis (CTM) de didanosina com eficiência de dissolução (ED%) e capacidade neutralizante ácida (CNA) otimizados, tendo como base o medicamento referência e especialidades farmacêuticas disponíveis no mercado nacional. Cinco formulações de CTM foram produzidas e avaliadas quanto a ED% e CNA, por meio de ensaio de dissolução e titulação ácido-base, respectivamente. Os resultados iniciais de CNA foram próximos aos encontrados para as especialidades farmacêuticas, aproximadamente 12 mEq HCl, porém distantes do medicamento referência (especialidade A, CNA = 17,93 mEq HCl). Já as formulações derivadas de CTM-4 conduziram à obtenção de comprimidos tamponados com CNA otimizada de aproximadamente 17,5 mEq HCl, o mesmo ocorrendo para ED%, (61,33% e 62,00%, CTM-4-2-1 e 3, respectivamente). Esse resultado mostra-se próximo ao valor de 59,33% da especialidade A, quando utilizado o mesmo método de dissolução, indicando haver equivalência entre estas formulações e o medicamento referência para estes parâmetros. Palavras-chave: Capacidade neutralizante ácida. Comprimidos tamponados mastigáveis. Didanosina. dissolução

Application of gastro-resistant coating on didanosine tablets using differents machines: conventional or perforated pan coater and fluid bed

Los comprimidos gastro-resistentes de didanosina fueron desarrollados utilizando diferentes equipos de recubrimiento. Cuatro formulaciones de núcleos fueron preparadas y evaluadas por medio del perfil de disolución y posteriormente la formulación seleccionada fue recubierta (3,5; 5,5 y 8,0 %, p/p) en bombo grageador convencional, tambor perforado y lecho fluido, siendo evaluada la gastro-resistencia. Todos los equipos y niveles de revestimiento resultaron en comprimidos gastro-resistentes; sin embargo, para el de mayor nivel de revestimiento no fue observada la permeación del líquido de disolución en los núcleos. No hubo diferencia en el revestimiento frente a los diferentes equipos utilizados, siendo las variaciones estructurales, funcionales y operacionales las razones para la preferencia del uso de cualquiera de ellos.Formulation of didanosine gastro-resistant tablets was devel- oped using different coating machines. Four core formulations were prepared and tested about drug dissolution. The selected formulation was coating (3.5, 5.5 and 8.0% w/w) in conventional and perforated coating machines and fluid bed equipment and assay about gastro-resistant properties. All coating equipments and levels of coating provided gastro-resistant tablets, however only for the bigger level of coating was not observed permeation of dissolution mean into the tablets. No difference was noted between the efficacy of coating equipments, therefore structural, functional and operational variations are the cause to preference one to another.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Gastro-resistant pellets of didanosine obtained by extrusion and spheronization: assessing the production process

The aim this work was develop gastro-resistant pellets of didanosine as well as study the impact on the pellets properties, regarding the way as the binder was added and drying process used. The pellets formation was accompanied by analysis of morphological parameters and didanosine dissolution. In the most cases, pellets showed diameter around 1.0 mm and shape parameters acceptable. The variations of the process did not interfere significantly in pellets size. In turn, drying in fluid bed favored the dissolution of didanosine, in contrast to binder addition on powder form that impaired. In another hand, this last resulted in the best aspect factor (about 1.1). Gastro-resistant pellets showed adequate dissolution, compatible with this type of dosage form. The variables of process studied enabled obtain pellets with characteristics of shape and dissolution just slightly different, indicating flexibility of the formulation for production of gastro-resistant pellets of didanosine.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Estudo de propriedades físico-químicas envolvidas no processo de compactação de uma formulação experimental contendo zidovudina

Estudo das propriedades físico-químicas envolvidos no processo de compactação de uma formulação experimental contendo como fármaco modelo a zidovudina. O objetivo foi caracterizar o comportamento físico-químico de comprimidos produzidos por compressão direta usando-se diferentes pressões de compactação. Nas análises foram empregadas metodologias convencionais e não convencionais. A metodologia não convencional foi o uso da técnica da atenuação de raios-gama na determinação da porosidade. As metodologias convencionais utilizadas foram os testes de friabilidade, dureza e dissolução. Os modelos teóricos utilizados para explicar o comportamento físico-químico da formulação sob compressão são os proposto por Heckel e Walker. Os estudos mostraram que o processo de densificação é governado principalmente por deformações do tipo plásticas e pressões em torno de 246MPa são suficientes para induzir deformação plástica e consolidação do sistema compactado. Os resultados da análise de Walker indicam que a formulação tem propriedades de compressão que podem ser melhoradas