A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property significantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was significantly improved. The effect of the SD carrier polymers on blocking efflux pump can be an important approach to improve the bioavailability of AZT

A novel dosage form for buccal administration of bupropion

A bupropiona é um antidepressivo utilizado no tratamento do tabagismo. O objetivo deste trabalho foi a preparação de filmes hidrogelatinosos de liberação controlada para administração bucal de bupropiona. Os filmes foram preparados utilizando carboximetilcelulose sódica ultrapurificada, hidroxipropilmetilcelulose K4M e quitosana de média viscosidade. As características físico-químicas dos filmes foram avaliadas por microscopia eletrônica de varredura, teor de bupropiona, resistência mecânica (perfuração, relaxação, resiliência e tração) e citotoxicidade. Os resultados mostraram que os filmes em bicamada apresentaram teor de bupropiona de 121 mg por 9 cm2 de filme e que a bupropiona modifica a resistência mecânica dos filmes, sem, no entanto, inviabilizar o uso desta forma farmacêutica. Os estudos de citotoxicidade mostraram que as formulações dos filmes contendo bupropiona não causam dano celular. Este estudo mostrou que a bupropiona veiculada na forma de filme hidrogelatinoso pode ser uma alternativa útil no tratamento do tabagismo.Bupropion is an antidepressant used in the treatment of smoking. The purpose of this study was to prepare controlled-release hydrogel films for buccal administration of bupropion and investigate its physicochemical and cytotoxic properties. The films were prepared from ultrapure sodium carboxymethylcellulose, hydroxypropylmethylcellulose K4M, and medium-viscosity chitosan. Evaluation of film physicochemical characteristics was based on scanning electron microscopy, bupropion content, mechanical strength (burst strength, relaxation, resilience, and traction), and cytotoxicity. Bupropion content in bilayer films was 121 mg per 9 cm2. The presence of bupropion modified film mechanical strength, but did not compromise the use of this pharmaceutical form. As shown by the cytotoxicity results, films containing bupropion did not cause cellular damage. Bupropion administration in the form of hydrogel films is a potentially useful alternative in the treatment of smoking

Supercritical fluid and pharmaceutical applications. Part I: Process classification

The supercritical fluid technology has been target of many pharmaceuticals investigations in particles production for almost 35 years. This is due to the great advantages it offers over others technologies currently used for the same purpose. A brief history is presented, as well the classification of supercritical technology based on the role that the supercritical fluid (carbon dioxide) performs in the process.FAPESP (São Paulo, Brazil – project 2012/01333-0) for financial suppor

Polyphenols isolated from pomegranate juice (Punica granatum L.): Evaluation of physical-chemical properties by FTIR and quantification of total polyphenols and anthocyanins content / Isolamento de polifenóis do suco da romã (Punica granatum L.): Avaliação das propriedades físico-química por FTIR e quantificação do teor total de polifenóis e antocianinas

Pomegranate (Punica granatum L.) is a polyphenols source, such as anthocyanins, punicalagin, ellagitannins and tannins. Polyphenols are antioxidant compounds present in foods as cereals, fruits (peels, seeds and juice), vegetables, wine, and among others. Polyphenols are responsible to protect cells and to limit the risks of degenerative and tumoral diseases, as well as, to prevent cardiovascular diseases, neuronal diseases, and present important anti-inflammatory effects. The purpose of this study was to isolate polyphenols from pomegranate juice using solvents without heating. The solvents used were ultrapure water, ethanol, ethanol 70% and methanol. The samples were characterized by FTIR to evaluate the physical-chemical properties, the total polyphenols content was quantified by Folin-Ciocalteau method, using gallic acid as standard equivalent, and the total anthocyanins content was quantified by pH-differential method, using anthocyanins (cyanidin-3-glucoside) as standard equivalent. FTIR spectra showed the main characteristic groups of polyphenols, as hydroxyl group and stretching vibration of benzene rings. And the characteristic groups of solvents were CH2 ou CH3, hydroxyl, carboxyl e carbonyl group. For the quantification of total polyphenols and anthocyanins content, the best results were found to the pomegranate juice: ultrapure water samples. According to the data obtained it was possible to conclude, who the process employed was effective to isolate the polyphenols from pomegranate juice and the use of different types of solvent influenced in the achievement of these results. 

Polyphenols isolated from pomegranate juice (Punica granatum L.): Evaluation of physical-chemical properties by FTIR and quantification of total polyphenols and anthocyanins contente / Isolamento de polifenóis do suco da romã (Punica granatum L.): Avaliação das propriedades físico-química por FTIR e quantificação do teor total de polifenóis e antocianinas

Pomegranate (Punica granatum L.) is a polyphenols source, such as anthocyanins, punicalagin, ellagitannins and tannins. Polyphenols are antioxidant compounds present in foods as cereals, fruits (peels, seeds and juice), vegetables, wine, and among others. Polyphenols are responsible to protect cells and to limit the risks of degenerative and tumoral diseases, as well as, to prevent cardiovascular diseases, neuronal diseases, and present important anti-inflammatory effects. The purpose of this study was to isolate polyphenols from pomegranate juice using solvents without heating. The solvents used were ultrapure water, ethanol, ethanol 70% and methanol. The samples were characterized by FTIR to evaluate the physical-chemical properties, the total polyphenols content was quantified by Folin-Ciocalteau method, using gallic acid as standard equivalent, and the total anthocyanins content was quantified by pH-differential method, using anthocyanins (cyanidin-3-glucoside) as standard equivalent. FTIR spectra showed the main characteristic groups of polyphenols, as hydroxyl group and stretching vibration of benzene rings. And the characteristic groups of solvents were CH2 ou CH3, hydroxyl, carboxyl e carbonyl group. For the quantification of total polyphenols and anthocyanins content, the best results were found to the pomegranate juice: ultrapure water samples. According to the data obtained it was possible to conclude, who the process employed was effective to isolate the polyphenols from pomegranate juice and the use of different types of solvent influenced in the achievement of these results. 

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"

Caracterização física de Cateteres Centrais de Inserção Periférica (CCIP)

Cateteres centrais de inserção periférica (CCIP) são amplamente utilizados em neonatos internados em Unidades de Terapia Intensiva Neonatal (UTIN). O objetivo do presente estudo foi avaliar as características físicas de CCIP, por meio da aplicação das normas ABNT NBR ISO 10555-1: 2003 e ABNT NBR ISO 105553: 2003, e comparar os resultados produzidos na análise de CCIP no início de seu processo de produção (somente catéteres extrusados) com os obtidos na análise do produto acabado. Testes experimentais foram realizados em CCIP fabricados por um fabricante nacional entre os anos de 2011 e 2012. Os dados foram coletados a partir de testes realizados em ambos os catéteres que foram apenas extrusados, ou seja, sem pintar as demarcações, cortes e outros processos relacionados com garantia de qualidade, e catéteres após a conclusão do processo geral de fabricação. No presente estudo, incluiram-se todos os estágios do processo de produção do catéter que podem gerar algum tipo de modificação no produto que poderia gerar riscos aos pacientes que necessitam utilizá-los. Os catéteres foram analisados quanto à resistência à ruptura, radiopacidade, características de fluxo, vazamento de fluido sob pressão e ocorrência de vazamento de ar na montagem do tubo de sucção, conforme preconizado pelas normas NBR ISO 10555-1: 2003 e NBR ISO 10555-3: 2003. Os resultados obtidos foram satisfatórios em todas as análises realizadas, com exceção da resistência à ruptura, que não atendeu às especificações preconizadas pelos padrões para catéteres de silicone. Examinaram-se também catéteres feitos de poliuretano, que por sua vez cumpriram os padrões no que diz respeito à resistência à ruptura. Como as normas não especificam pontos importantes a serem levados em conta para a realização de testes inequivocamente, foram feitas sugestões para a revisão dessas normas. Palavras-chave: Teste mecânico. Teste de tensão. Refletividade de raios X. Deformação. Propriedades elásticas. Polímero

Self-Emulsifying Drug Delivery Systems (SEDDS) in pharmaceutical development

Lipid-based formulations, such as Self-Emulsifying Drug Delivery Systems (SEDDS), are an important tool for lipophilic drugs and offer the potential for enhancing drug absorption and oral bioavailability. SEDDS are a promising approach for the formulation of drug compounds with poor aqueous solubility. These systems are easily manufactured and physically stable mixtures of oil, surfactants, co-surfactants and solubilized drug substances that are administered orally in soft or hard gelatin capsules. In the gastrointestinal tract environment, these systems spontaneously emulsify. This review focuses on SEDDS formulations, describes their different types and presents case studies in which enhanced bioavailability were demonstrated in vivo using this formulation system53CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQCOORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPESFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESPsem informaçã

Design and development of self-emulsifying drug delivery systems novel cardioactive n-acylhydrazone compound

In this study, the emphasis is placed on a strategy for enhancing the drug/carrier interaction for improved drug solubility, drug-loading capacity, self-emulsification and stability.Preliminary solubility of L294 was determined in various oils, surfactants and cosurfactants. A ternary phase diagram was constructed to identify the self-emulsifying region for the selected systems, using series concentrations of Labrafac PG, Labrasol and Transcutol HP. Self-emulsifying properties, particle size, polydispersibility, and zeta potential were studied after dilution of formulations in water.The results demonstrated the development of a self-emulsifying formulation of L294 in liquid form, which upon contact with aqueous media spontaneously forms a clear nanoemulsion having a small droplet size (around 100 nm). The zeta potential of the selected SEDDS formulation was between −11.09 and −20.50 with a viscosity around 40-60 cP. The optimum formulation consisted of a mixture of Labrafac PG, Labrasol and Transcutol HP.The L294 showed extremely low water solubility (0,006 mg.mL-1), and when formulated in SEDDS, its solubility increased over than 33,000 fold.This study demonstrate that SEDDS can be considered as a very good candidate to optimize the peroral administration of L2944112CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQCOORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPESFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESPsem informaçã