ABSTRACT The subcutaneous administration of insulin has been the treatment of millions of diabetics in the world. However, for such via insulin is invasive and not mimics the physiological action causing side effects. The oral route would be the most physiological and comfortable option, but the oral bioavailability of insulin is low by proteolytic activity and reduced permeability of the gastrointestinal tract. The aim of the study was to develop a nanostructured system integrating biomaterials for oral insulin delivery. Cashew gum (CG) is a polysaccharide extracted from the exudate of the plant Anacardium occidentale. It is a biopolymer composed of simple sugars and glucuronic acid and it can be used in nanostructured systems for the incorporation of molecules. The exudate was isolated, dissolved in water, filtered, precipitated in ethanol and purified. The CG was characterized by infrared spectroscopy and molecular weight by size exclusion chromatography. Nanoparticles were prepared through ionotropic gelation integrating cashew gum, dextran sulfate and poloxamer containing insulin stabilized with chitosan, poly(ethyleneglycol) and coated with albumin. The particles were analyzed for particle size, zeta potential and insulin entrapment efficiency. The FTIR spectrum for CG showed a band at 3395 cm-1 due to the stretching vibration of O-H, a band at 2926 cm-1 of C-H vibrations; absorption at 1639 cm-1 of O-H type from bound water molecules and bands at 1143, 1073 and 1024 cm-1 due vibrations of the C-O-C from glycosidic bonds and O-H of alcohols. The peak molar mass of GC was 2.35 × 104 g/mol. The particles had a size of 156 nm and after coating, size of 5387 nm with 92% insulin entrapment efficiency and zeta potential of -51 mV indicating electrostatic stabilization. The results suggest an innovative cashew gum base system for oral insulin administration.

Devido ao crescente interesse da população pelos tratamentos naturais, as argilas representam uma boa alternativa para a aceleração da cicatrização durante o tratamento de feridas. Dentre as argilas, a paligorsquita, uma argila piauiense, devido à sua composição com silício e alumínio, demonstra certa aplicabilidade farmacêutica como agente cicatrizante. O objetivo deste artigo é avaliar a ação cicatrizante da paligorsquita piauiense em sua forma natural e organofilizadas por meio da análise comparativa da macroscopia e dos exames histológicos em feridas cutâneas de ratos machos e fêmeas Wistar adultos com 2 meses de idade. Para tanto, foram realizadas tricotomia circular no corno dorsal dos ratos para verificar os efeitos dos tratamentos realizados com solução salina 0,9%, colagenase, paligorsquita natural, paligorsquita organofilizada por cloreto de cetiltrimetilamônio e paligorsquita organofilizada por cloreto de alquildimetilbenzilamônio. Para todas as argilas testadas foi feita a avaliação microbiológica pelo método de plaqueamento em profundidade e do método de estrias em superfície, bem como foi realizada após tratamento, a análise macroscópica das feridas cutâneas por meio organoléptico, medição em paquímetro e análise histológica. Por meio da avaliação microbiológica foi detectada a necessidade de esterilização da argila para posterior incorporação na forma farmacêutica. A análise macroscópica sugere que houve cicatrização da área lesionada, bem como a análise histológica demonstrou efeito benéfico após o uso tópico do material argiloso. Nossos dados sugerem que a paligorsquita pode exercer um maior efeito cicatrizante em relação aos demais tratamentos, embora após o término deste tratamento, todos os animais analisados apresentaram a mesma reparação tecidual.

In view of growing interest in natural treatments, clays would appear to be a good alternative for speeding up the healing process during the treatment of wounds. Of the various clays, palygorskite, a clay from the Brazilian State of Piauí, composed of silicon and aluminum, has shown itself to be pharmaceutically useful as a healing agent. The aim of this article is to evaluate the effect on the healing of wounds of Piauí palygorskite, both in its natural state and when organophilic, by way of comparative analysis of macroscopic and histological tests on skin wounds in adult male and female two-month-old Wistar rats. To this end, a circular trichotomy of the dorsal cornus of the rats was carried out to confirm the effects of treatments involving 0.9% saline solution, collagenase, natural palygorskite, organophilic palygorskite with cetyltrimethylammonium chloride, and organophilic palygorskite with alkyldimethylbenzylammonium chloride. The testing of all the clays involved microbiological evaluation using the depth of plaque and surface striation methods, along with post-treatment macroscopic analysis of skin wounds by way of organoleptics, pachymetry and histological analysis. Microbiological evaluation revealed the need for sterilization of the clay prior to incorporation in the pharmaceutical form. Macroscopic analysis suggests that healing of the wounded area occurred, and histological analysis showed the beneficial effect of the topical use of clay material. Our data suggest that palygorskite may be more powerful than other healing agents, although, on completing treatment, all the animals studied showed the same degree of tissue repair.

This study describes unpublished research on improving the solubility of benznidazole by the formation of an inclusion complex. The cyclodextrins selected were αCD, βCD, γCD, HPβCD, RMβCD and SBβCD. All complexes were obtained in solution, presenting 1:1 stoichiometry according to the phase solubility diagram. The highest association constants were obtained with RMβCD and SBβCD, being selected for attainment of solid state complexes. These were characterized using XRD, SEM and dissolution test. The data obtained suggest the formation of complexes and indicate that these may provide a promising alternative way of developing solid doses of drug with suitable biopharmaceutical properties.

O efavirenz é um inibidor não análogo de nucleosídeo da transcriptase reversa, utilizado no tratamento da infecção por HIV. Um método simples, por cromatografia líquida de alta eficiência, foi desenvolvido e validado para quantificação do efavirenz em comprimidos. O desenvolvimento do método levou em consideração as características físico-químicas do efavirenz. O método foi validado seguindo os parâmetros da USP 29. A análise foi realizada por meio de detector ultravioleta, utilizando um comprimento de onda de 252 nm, com coluna de fase reversa (C18, 250 mm x 3.9 mm, 10 μm) e fase móvel isocrática contendo acetonitrila/água/ácido ortofosfórico (70: 30: 0.1). Os critérios usados para validação foram: seletividade, linearidade, precisão, exatidão, robustez e limites de detecção e quantificação do método. Foi utilizado método estatístico em todas as etapas do processo de validação. Os resultados obtidos mostraram que o método é uma alternativa para quantificação do efavirenz em comprimidos, tornando viável seu uso na rotina industrial e laboratórios analíticos.

Efavirenz is a reverse transcriptase non analog nucleoside inhibitor used to treat HIV infections. A simple assay method by high performance liquid chromatography was developed and validated for efavirenz tablets. The physical chemical characteristics of efavirenz were investigated to developing the method. The method was validated observing the parameters described in USP 29. Analyses were performed by an ultraviolet detector at a 252 nm wavelength, on a reverse-phase column (C18, 250 mm x 3.9 mm, 10 μm), using an isocratic mobile phase containing acetonitrile/water/orthophosphoric acid (70:30:0.1). The validation parameters used were: selectivity, linearity, precision, accuracy, robustness, detection and quantification limits, and all resulting data were treated by a statistical method. The results obtained confirmed an alternative assay method for efavirenz tablets adequate for routine industrial use.

An UV-Vis spectrophotometry analytical method for quantifying Efavirenz was developed and validated as an alternative to replace the HPLC current method. The report method presents sample concentration of 10 μg mL-1, dissolved in a solution ethanol:water (60:40, v/v), economic and technically adequate for the purpose adopted. The results and the statistical treated proved that the method being considered an precise and accurate analytical low cost alternative for laboratory routine. The adaptability of this method in product and other analytical methods development has been challenged by mathematical calculation of drug extinction coefficient in water and methanol and practical experiments, showing interesting results.

This work aimed the development and validation of a new dissolution test for ornidazole coated tablets. The dissolution conditions were determined after testing Sink conditions, dissolution medium, apparatus, stirring speed, 24 h stability and medium filtration influence. The best conditions were paddle at a stirring speed of 75 rpm and 900 mL of 0.1 M HCl. A new HPLC quantification method was developed and validated. The dissolution test and quantification method showed to be adequate for their purposes and could be applied for quality control of ornidazole coated tablets, since there is no official monograph.

O trabalho teve como objetivo a verificação das possíveis interferências dos excipientes utilizados na obtenção do comprimido de liberação imediata à base de benznidazol por meio do processo de compressão direta e realização de estudo comparativo entre os comprimidos obtidos e o medicamento de referência Rochagan®, obtido por meio da granulação por via úmida. Sete lotes de bancada (LB) foram produzidos e aspectos, tais como compressibilidade, fluxo do pós, peso médio, friabilidade, desintegração, dureza, teor, dissolução, uniformidade de conteúdo, cinética de liberação in vitro (dissolução) e compatibilidade físico-química fármaco/excipiente foram avaliados. Diante dos resultados obtidos pode-se verificar que os pós analisados apresentaram características adequadas para o processo da compressão direta, além da comprovação da não existência de interação de natureza físico-química entre o fármaco e os excipientes testados. Os comprimidos obtidos a partir do LB I e III foram escolhidos para o estudo comparativo frente ao medicamento de referência, demonstrando semelhança com os resultados observados, tratados estatisticamente. Torna-se, assim, uma alternativa para a produção de medicamento destinado ao tratamento da doença de Chagas com um custo reduzido e qualidade satisfatória.

This work aimed to verify the interferences caused by the use of excipients for immediate release tablets based on benznidazole obtained by direct compression and the accomplishment of a comparative study between the tablets developed and the reference medicine RochaganTM, obtained by wet granulation. Seven small-scale batches (SSB) were developed and aspects such as compressibility, powder flow, mean weight, friability, disintegration, hardness, assay, content uniformity, kinetic of release in vitro (dissolution) and drug/excipients physical-chemical compatibility were evaluated. Based on the obtained results it can be verified that the analyzed powders presented adequated characteristics for the direct compression process, beyond the inexistent evidence of a physical-chemical interaction between the drug and the tested excipients. The tablets obtained from SSB I and III were chosen for the comparative study with the reference medicine, demonstrating similarity with the statistically treated obtained results, becoming an alternative option of a medicine product for the treatment of Chagas' disease with reduced cost and satisfactory quality.