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1.
Foods ; 13(15)2024 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-39123536

RESUMO

This project studied the use of lentil protein (LP) and quinoa protein (QP) in their native and modified states as carrier material in the encapsulation process by the ionic gelation technique of annatto seed extract. Soy protein (SP) was used as a model of carrier material and encapsulated bioactive compounds, respectively. The plant proteins were modified by enzymatic hydrolysis, N acylation, and N-cationization to improve their encapsulating properties. Additionally, the secondary structure, differential scanning calorimetry (DSC), solubility as a function of pH, isoelectric point (pI), molecular weight (MW), the content of free thiol groups (SH), the absorption capacity of water (WHC) and fat (FAC), emulsifier activity (EAI), emulsifier stability (ESI), and gelation temperature (Tg) were assessed on proteins in native and modified states. The results obtained demonstrated that in a native state, LP (80.52% and 63.82%) showed higher encapsulation efficiency than QP (73.63% and 45.77%), both for the hydrophilic dye and for the annatto extract. Structural modifications on proteins improve some functional properties, such as solubility, WHC, FAC, EAI, and ESI. However, enzymatic hydrolysis on the proteins decreased the gels' formation, the annatto extract's encapsulated efficiency, and the hydrophilic dye by the ionic gelation method. On the other hand, the modifications of N-acylation and N-cationization increased but did not generate statistically significant differences (p-value > 0.05) in the encapsulation efficiency of both the annatto extract and the hydrophilic dye compared to those obtained with native proteins. This research contributes to understanding how plant proteins (LP and QP) can be modified to enhance their encapsulating and solubility properties. The better encapsulation of bioactive compounds (like annatto extract) can improve product self-life, potentially benefiting the development of functional ingredients for the food industry.

2.
Foods ; 11(19)2022 Oct 06.
Artigo em Inglês | MEDLINE | ID: mdl-36230192

RESUMO

Given consumer trends propelling a movement toward using plant protein in the food industry and searching for alternative protein ingredients by the industry, this study aimed to assess the influence of factors such as protein concentration, medium pH, and the presence of a divalent ion (Ca2+) upon the rheological properties such as viscosity change and gel formation of dispersion proteins extracted from quinoa, black beans, and lentils. A solution of each protein was prepared by varying its concentration (2.5%, 5.0%, and 10%), the pH (5.0, 7.0, and 9.0), and the incorporation of calcium chloride (0.0% and 1.0%). Each obtained solution was subjected to rheological tests to determine the parameters: consistency index (K), flow behavior (n), the storage (G') and loss (G'') modules, and the phase shift angle (δ). The results demonstrate that the incorporation of Ca2+, the shift in protein levels, and the decrease in pH modified the rheological behaviors of proteins, which were also influenced by the structural characteristics of each protein studied. However, thermal treatment and protein concentrations caused the most significant impact on proteins' rheological behavior, forming gels independently of other conditions. It was possible to study and interpret the studied proteins' rheological variations according to the environment's conditions.

3.
J Food Sci Technol ; 59(5): 1665-1676, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35531395

RESUMO

Sonicated protein isolates were recovered from Chenopodium quinua, Phaseoulus vulgaris and Lens culinaris to develop a functional matrix by assessing the physicochemical and functional properties. The plant protein isolates were prepared from powdered materials followed by sonication in alkaline medium using a Box-Behnken design. pH (6-10), a buffer-to-material ratio (5:1 to 15:1) and sonication time (0-20 min) were taken as independent variables, whereas protein yield was taken as the dependent variable. A pH of 9, 20 min treatment, and a buffer-to-material ratio of 5:1 were the optimal extraction conditions for quinoa and black beans, whereas a 1:10 ratio was suitable for lentils. Sonication in alkaline medium caused partial protein unfolding and these isolates; in turn, the molecular weight affected the emulsifying activity and stability. Moreover, sonication had a strong effect on the gelation temperature, emulsifying activity, the water, and oil sorption. Sonication improved protein yield and exposed amino acids such as glutamic acid, aspartic acid, leucine and glycine. In turn, thiol groups were responsible for the increased in gelation temperature. The better gelling property coupled with high emulsifying property of these proteins show potential application as protein emulsifiers in the production of gels, sausages, and pet foods.

4.
Polymers (Basel) ; 14(9)2022 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-35566922

RESUMO

The addition of polymers in construction is a new tendency and an important step toward the production of structures with better functional properties. This work investigates the addition of polyurea (PU) as a polymeric material in mortars. Polymer mortars were manufactured with the addition of polyurea retained in different sieves (T50 and T100) and different concentrations (2% and 5%). The characterization of the, polyurea (PU)control mortar (PU0%) and manufactured polyurea mortars (PU2%T50, PU5%T50, PU2%T100, and PU5%T100) was conducted by means of morphological analysis, SEM, XRF, TGA, and a compressive strength test of hydraulic mortars. The results show that mortars with polyurea retained in sieve 100 with a particle size of 150 µm exhibit better thermal behavior and a greater resistance to compression with a concentration of 5% polyurea with respect to the other samples. The present work reveals that polyurea retained in sieve 100 can be considered as a polymeric additive for mortars, indicating that it could be a candidate for applications such as construction.

5.
Molecules ; 26(9)2021 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-33921948

RESUMO

Clove essential oil (CEO) is known for having excellent antioxidant and antimicrobial properties, but the poor stability of its components to light and temperature compromise this activity. The aim of this study is to evaluate the textural, antioxidant, antimicrobial and microstructural properties of matrixes produced with representative natural waxes and CEO. Thus, waxy emulsifiers, such as beeswax, candelilla wax, carnauba wax, and ozokerite wax, were employed to create such matrixes. The thermal, microstructural, textural, wetting, antioxidant, antimicrobial and infrared characteristics of the matrixes were then studied. The diverse chemical composition (long-chain wax esters in carnauba wax and short-chain fatty acids and hydrocarbons in beeswax and ozokerite wax, respectively) explained the differences in wetting, texture, melting, and crystallization characteristics. Crystal forms of these matrix systems varied from grainy, oval, to needle-like shape, but keeping an orthorhombic allomorph. The alignment and reorganization of beeswax and ozokerite wax into needle-like crystals increased the matrix strength and adhesion force compared to those of carnauba and candelilla matrixes, which showed weak strength and grainy morphology. The former two waxes and their matrixes also showed the largest plasticity. These lipidic matrixes show potential use for topical applications having acceptable antioxidant and textural properties.


Assuntos
Óleo de Cravo/química , Óleo de Cravo/farmacologia , Lipídeos/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Fenômenos Químicos , Fenômenos Mecânicos , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-Atividade , Ceras/química , Difração de Raios X
6.
Data Brief ; 31: 106014, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32715043

RESUMO

Traditionally, oil structuring has been conducted merely in vegetable oils. Alternatively, essential oil structuring provides a great opportunity to develop the topical application of these oils without causing allergic contact dermatitis and improving the sensory properties. The thermal, rheological and microstructure data collection of lipidic matrices produced with representative gelators such as carnauba wax, stearic acid, glyceryl monostearate and hydroxyethyl cellulose in lemon essential oil were carried out by DSC, rheology and phase contrast microscopy measurements. This dataset is valuable to researchers interested in characterizing lipidic matrices produced with several gelators, once incorporated in different topical formulations. These data can be used for quality control of topical formulations having several textural features.

7.
Antioxidants (Basel) ; 9(4)2020 Apr 13.
Artigo em Inglês | MEDLINE | ID: mdl-32294926

RESUMO

This study aimed to assess the thermal stability of the bioactive compounds from annatto seed extract, encapsulated by ionic gelation using quinoa proteins, lentil proteins, soy proteins, and sodium caseinate as carrying materials. The 10.0% aqueous dispersions of the different proteins (carriers) were prepared and mixed with the annatto seed extract. The dispersions were then extruded into a calcium chloride solution to induce the extract encapsulation. The capsules were characterized by encapsulation efficiency, particle size, infrared transmission spectroscopy, confocal microscopy, and scanning electron microscopy (SEM). The antioxidant and antimicrobial activities, the polyphenol compounds, and bixin content from the free and encapsulated extract were assessed once stored for 12 d at different temperatures (4 °C, 25 °C, and 65 °C). The results demonstrated the ability of the proteins to encapsulate the annatto extract with encapsulation efficiencies ranging from 58% to 80%, where the protein structure and amino acid content were the relevant factors to obtain high encapsulation efficiencies. The free extracts stored at 65 °C for 12 d experienced a degradation of bixin and polyphenol compounds, respectively. Conversely, the encapsulated extract had degradations from ~34.00% to ~4.05% for polyphenol compounds and ~20.0% for bixin, respectively. These proteins have a potential encapsulation capacity of annatto extract by ionic gelation.

8.
Pharmaceuticals (Basel) ; 13(1)2020 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-31936208

RESUMO

A promising strategy to improve the effectivity of anticancer treatment and decrease its side effects is to modulate drug release by using nanoparticulates (NPs) as carriers. In this study, methotrexate-loaded chitosan-polyanion nanoparticles were produced by polyelectrolyte complexation assisted by high-intensity sonication, using several anionic polymers, such as the sodium and potassium salts of poly(maleic acid-alt-ethylene) and poly(maleic acid-alt-octadecene), here named PAM-2 and PAM-18, respectively. Such NPs were analyzed and characterized according to particle size, polydispersity index, zeta potential and encapsulation efficiency. Likewise, their physical stability was tested at 4 °C and 40 °C in order to evaluate any change in the previously mentioned particle parameters. The in vitro methotrexate release was assessed at a pH of 7.4, which simulated physiological conditions, and the data were fitted to the heuristic models of order one, Higuchi, Peppas-Sahlin and Korsmeyer-Peppas. The results revealed that most of the MTX-chitosan-polyanion NPs have positive zeta potential values, sizes <280 nm and monodisperse populations, except for the NPs formed with PAM-18 polyanions. Further, the NPs showed adequate physical stability, preventing NP-NP aggregation. Likewise, these carriers modified the MTX release by an anomalous mechanism, where the NPs formed with PAM-2 polymer led to a release mechanism controlled by diffusion and relaxation, whereas the NPs formed with PAM-18 led to a mainly diffusion-controlled release mechanism.

9.
Polymers (Basel) ; 11(12)2019 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-31817917

RESUMO

Cancer is one of the most serious public health problems that affect humanity. Diverse delivery systems of anticancer drugs have been developed to enhance the treatment effectiveness and patient compliance. Thus, drug delivery systems from polymeric films could be an interesting and promising alternative, especially for skin chemotherapeutics. In this work, polymeric films based on glutathione-chitosan conjugates with degrees of thiolation of 4.4%, 5.1% and 7.0% were synthetized by casting-evaporation method and subsequent loading with methotrexate. The surface properties of these films were evaluated by contact angle and spreading rate measurements. The sessile drop methods along with the thermodynamic parameter of work of adhesion were determined using the Young-Dupré semi-empirical model. The in vitro methotrexate release was assessed at a pH of 4.5 and 7.4 simulating physiological conditions. Data from the resulting profiles were fitted to the order one, Higuchi, Peppas-Sahlin and Korsmeyer-Peppas kinetic models. The results suggest a strong relationship between the thiolation degree and hydrophilic surface properties such as contact angle and water spreading rate, whereas the work of adhesion was not significantly affected. Further, these polymer films could control the methotrexate release through diverse mechanisms such as diffusion and relaxation depending on the thiolation degree and the aqueous medium employed. In fact, as thiolation degree increased, the release mechanism shifted from a primary diffusional type towards a predominant relaxation-driven mechanism. These polymer films could be used as modified systems for anticancer local delivery.

10.
Polymers (Basel) ; 11(11)2019 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-31731554

RESUMO

Recently, one of the promising strategies to fight sensitive and resistant bacteria, and decrease the morbidity and mortality rates due to non-nosocomial infections, is to use antibiotic-loaded nanoparticles. In this study, ampicillin-loaded chitosan-polyanion nanoparticles were produced through the techniques of ionic gelation and polyelectrolyte complexation assisted by high-intensity sonication, using several crosslinking agents, including phytic acid (non-polymeric polyanion), sodium and potassium salts of poly(maleic acid-alt-ethylene) and poly(maleic acid-alt-octadecene) (polymeric polyanions). These nanoparticles were analysed and characterised in terms of particle size, polydispersity index, zeta potential and encapsulation efficiency. The stability of these nanosystems was carried out at temperatures of 4 and 40 °C, and the antimicrobial effect was determined by the broth microdilution method using sensitive and resistant Staphylococcus aureus strains. The results reveal that most of the nanosystems have sizes <220 nm, positive zeta potential values and a monodisperse population, except for the nanoparticles crosslinked with PAM-18 polyanions. The nanometric systems exhibited adequate stability preventing aggregation and revealed a two-fold increase in antimicrobial activity when compared with free ampicillin. This study demonstrates the potential application of synthesised nanoparticles in the field of medicine, especially for treating infections caused by pathogenic S. aureus strains.

11.
Antioxidants (Basel) ; 8(2)2019 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-30736339

RESUMO

This study deals with the extraction, optimization, and evaluation of the antioxidant and antimicrobial activities of bioactive compounds obtained from the seeds of annatto using microwave-assisted extraction as compared to leaching. Annatto seeds were subjected to a microwave treatment of 2450 MHz and power of 700 watts using a response surface design involving four factors: pH (4⁻11), solvent concentration (ethanol) (50⁻96 %), solvent-to-seed ratio (2⁻10), and microwave exposure time (0⁻5 min). The contents of polyphenol compounds and bixin were taken as response variables. Subsequently, the antioxidant and antimicrobial activities were assessed at the optimal processing conditions predicted by the experimental design. Microwaves, solvent concentration, and the solvent-to-seed ratio showed a statistically significant effect for the extraction of polyphenol compounds and bixin. Thus, microwaves accelerated the extraction of those compounds and the slight increase in temperature caused some degradation of the polyphenol compounds. The microwave-assisted extraction increased the contents of polyphenols and bixin along with their antioxidant activity as compared to leaching extraction. However, this technique does not significantly improve the antimicrobial activity against Bacillus cereus and Staphylococcus aureus.

12.
Vitae (Medellín) ; 25(1): 6-7, 2018.
Artigo em Inglês | LILACS, COLNAL | ID: biblio-994899

RESUMO

Proteins are macromolecules exhibiting amphiphilic properties, good biocompatibility, biodegradability, high nutritional value, and show strong interactions with several types of active compounds via hydrogen bonding and electrostatic interactions (1). These plant or animal-derived macromolecules differ in their molecular size depending on the number of amino acids present in their structure, which in turn, are linked by peptide bonds between the carbonyl (-CO-) and amino groups (-NH) (2).


Assuntos
Humanos , Proteínas , Biodegradação Ambiental , Aminoácidos , Valor Nutritivo
13.
Vitae (Medellín) ; 22(2): 73-73, 2015. Ilustraciones
Artigo em Inglês | LILACS, COLNAL | ID: biblio-987836

RESUMO

One of the most important features of foodstuffs and plant extract-based products is related to their fragile stability, especially when exposed to several ambient factors such as air, light radiation, heat and water vapour. The latter may contribute to the increase of free or bound water associated to the product. In this scenario, these variables may lead to different phenomena such as self-oxidation and hydrolysis of functional compounds and thus, a considerable inconsistency of products where these substances are part of occurs.


Assuntos
Humanos , Liofilização , Extratos Vegetais , Produção de Alimentos , Hidrólise
14.
Rev. latinoam. bioét ; 14(2): 28-37, jul.-dic. 2014. ilus, tab
Artigo em Espanhol | LILACS | ID: lil-724983

RESUMO

Este documento muestra los resultados parciales de la investigación "Responsabilidad social y ambiental de la industria manufacturera en la localidad de Puente Aranda en la ciudad de Bogotá como alternativa al desarrollo humano integral sustentable", realizados dentro del marco de trabajo del grupo de investigación Girsa. El estudio se basó en el análisis de la dinámica poblacional, ambiental y económica de la dicha localidad, a través de la metodología de la matriz de Vester. Con este instrumento se logró identificar las relaciones e interacciones dinámicas de todos los actores locales en el tiempo y en el espacio. Dentro de los problemas críticos que se encontraron en la localidad de Puente Aranda se encontró el agotamiento de fuentes hídricas, poca conciencia y educación ambiental de la población, una mala disposición de basuras, la no disponibilidad de servicios públicos para los nuevos asentamientos y altos niveles de emisión de partículas contaminantes.


This paper shows the partial results of the research "Social and environmental responsibility of the manufacturing industry in the locality of Puente Aranda in Bogotá as an alternative to integrated sustainable human development" carried out within the framework of the research group GIRSA. The study was based on the analysis of population, environmental and economic dynamics of the locality, through the methodology of matrix Vester. This matrix allows the identification and determination of the causes and consequences in a problematic situation. With this instrument it was possible to identify relationships and dynamic interactions of all local actors in time and space, in turn seven critical problems found two indifferent problems, a liability problem and five active problems present in the City Bridge Aranda. Among the critical issues depletion water sources, low environmental awareness and education of this population in the locality, poor waste disposal, non- availability of public services for new settlements and high emissions of particulate pollutants found.


Este documento apresenta os resultados parciais da pesquisa "Responsabilidade social e ambiental na indústria manufatureira na localidade de Puente Aranda na cidade de Bogotá como uma alternativa para o desenvolvimento humano integral sustentável", realizados no âmbito de trabalho do grupo de pesquisa Girsa. O estudo baseou-se na análise da dinâmica populacional, ambiental e econômica de dita localidade, através da metodologia da matriz Vester. Com este instrumento foi possível identificar as relações e interações dinâmicas de todos os atores locais no tempo e no espaço. Entre os problemas críticos que foram encontrados na localidade de Puente Aranda encontrou-se o esgotamento das fontes de água, falta de consciência e educação ambiental na população, coleta de lixo deficiente, falta de disponibilidade de serviços públicos para novos assentamentos e altos níveis de emissão de partículas poluentes.


Assuntos
Bioética , Responsabilidade Social , Ecologia , Princípio do Poluidor-Pagador
15.
Rev. ciênc. farm. básica apl ; Rev. ciênc. farm. básica apl;34(1)mar. 2013.
Artigo em Inglês | LILACS | ID: lil-672211

RESUMO

Os excipientes são materiais amplamente utilizados para formular fármacos através de compressão direta. No entanto, as propriedades do pó e compressão desses materiais são afetadas pela presença de lubrificantes e ingredientes ativos. Este estudo utilizou uma metodologia para avaliar a eficácia destes materiais como agentes de compressão direta. O efeito de três lubrificantes (estearato de magnésio, ácido esteárico e talco) na compressibilidade e compactação dos materiais foi avaliado pelo índice de compressibilidade e sensibilidade do lubrificante, respectivamente. Da mesma forma, a capacidade da diluição foi avaliada com um fármaco pouco compressível como o acetaminofeno. Finalmente, a recuperação elástica dos comprimidos foi avaliada aos cinco dias após a produção. Todos os lubrificantes aumentaram a compressibilidade destes materiais e a sua fluidez. No entanto, os lubrificantes hidrofóbicos, tais como o estearato de magnésio tem um efeito negativo sobre a compactação, em especial em materiais plásticos com uma superfície lisa, como o amido 1500. O amido de arroz e de mandioca e ácido algínico apresentaram a maior recuperação elástica (> 5%), indicando uma elevada tendência para a laminação. Além disso, os materiais plásticos com alta deformação, tais como o sorbitol, e polivinilpirrolidona (PVP-K30), exibiram a melhor potencial de diluição (~10%), enquanto que o ácido algínico mostrou um valor muito elevado (~ 70%). Em termos de desempenho, o sorbitol, o PVP-K30, alginato de sódio, Avicel PH-101, e de amido pré-gelatinizado são os materiais mais adequados para a compressão direta de fármacos.


Excipients are widely used to formulate solid drug forms by direct compression. However, the powder-forming and tableting properties of these excipients are affected by the presence of lubricants and active ingredients. In this study, a screening methodology was employed to test the performance of an excipient for direct compression. The effects of three lubricants (magnesium stearate, stearic acid and talc) on the compressibility and compaction of these excipients were assessed by the compressibility index and lubricant sensitivity ratio, respectively. Likewise, the dilution potential in blends with a poorly compactible drug such as acetaminophen was also assessed. Finally, the elastic recovery of tablets was evaluated five days after production. All lubricants increased the compressibility of these excipients and improved their flowability. However, hydrophobic lubricants such as magnesium stearate had a marked negative effect on compactibility, especially in plastic-deforming and more regularly-shaped materials with a smooth surface such as Starch 1500. Alginic acid, rice and cassava starches had the largest elastic recovery (>5%), indicating a tendency to cap. Moreover, highly plastic deforming materials such as sorbitol and polyvinylpyrrolidone (PVP-K30) exhibited the best dilution potential (~10%), whereas alginic acid showed a very high value (~70%). In terms of performance, sorbitol, PVP-K30, Avicel PH-101, sodium alginate and pregelatinized starch were the most appropriate excipients for the direct compression of drugs.


Assuntos
Diluição , Excipientes Farmacêuticos/análise , Preparações Farmacêuticas , Ligantes
16.
Drug Dev Ind Pharm ; 38(10): 1159-70, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22966909

RESUMO

It is necessary to have excipients with excellent functional properties to compensate for the poor mechanical properties and low aqueous solubility of the emerging active ingredients. Therefore, around 80% of the current drugs are not suitable for direct compression and more advanced excipients are required. Further, conventional grades of excipients cannot accommodate the technologically advanced high speed rotary tablet presses which require a powder with excellent flow, good compressibility, compactibility, particle size distribution and homogeneity of the ingredients. Co-processed excipients have been created to enhance the functional properties of the excipients and reduce their drawbacks. Co-processing is defined as the combination of two or more excipients by a physical process. Co-processed excipients are adequate for direct compression since they become multifunctional and thus, their dilution potential is high eliminating the need for many excipients in a formulation. In some cases, they are able to hold up to 50% of the drug in a formulation rendering compacts of good tableting properties. This study describes and discusses the functionality enhancement of commercial and investigational excipients through co-processing.


Assuntos
Química Farmacêutica/métodos , Excipientes/química , Comprimidos/química , Tecnologia Farmacêutica/métodos , Força Compressiva , Tamanho da Partícula , Pós/química , Solubilidade
17.
AAPS PharmSciTech ; 13(4): 1054-62, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22899380

RESUMO

Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose II (MCCII) were conducted. The effect of those disintegrants on the tensile strength, disintegration time and dissolution rate of spironolactone-based compacts was evaluated using a factorial design with three categorical factors (filler, lubricant, and disintegrant). The swelling values, water uptake and water sorption studies of these disintegrants all suggested that MCCII compacts disintegrate by a wicking mechanism similar to that of crospovidone, whereas a swelling mechanism was dominant for sodium starch glycolate and croscarmellose sodium. The disintegration time of MCCII and sodium starch glycolate remained unchanged with magnesium stearate. However, this lubricant delayed the disintegration time of crospovidone and croscarmellose sodium. MCCII presented the fastest disintegration time independent of the medium and lubricant employed. The water sorption ratio and swelling values determined sodium starch glycolate followed by croscarmellose sodium as the largest swelling materials, whereas crospovidone and MCCII where the least swelling disintegrants. The swelling property of sodium starch glycolate and croscarmellose sodium was strongly affected by the medium pH. The disintegration time of spironolactone compacts was faster when starch was used as a filler due to the formation of soft compacts. In this case, the type of filler employed rather than the disintegrant had a major effect on the disintegration and dissolution times of spironolactone.


Assuntos
Carboximetilcelulose Sódica/química , Celulose/química , Povidona/química , Espironolactona/química , Amido/análogos & derivados , Absorção , Química Farmacêutica/métodos , Excipientes/química , Solubilidade , Amido/química , Resistência à Tração , Água/química
18.
Chem Pharm Bull (Tokyo) ; 60(5): 603-11, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22689398

RESUMO

The effect of silicification on the tableting performance of microcrystalline cellulose II (MCCII) was assessed through coprocessing with fumed silica via spray drying and wet granulation at the 98:2, 95:5, 90:10 and 80:20 ratios. Compacts produced by spray drying and wet granulation rendered better tensile strength than MCCII. The Kawakita and Heckel models implied that silicification increased compressibility and decreased the plastic deforming behavior and densification by die filling at the early stage of compression for MCCII. It also decreased the sensitivity to hydrophobic lubricants such as magnesium stearate, especially for the spray-dried products due to the competing effect with magnesium stearate. Further, silicification decreased the high elastic recovery typical of MCCII due to the increase in specific surface area and fragmenting behavior which contributed to the formation of stronger compacts. Moreover, silicification did not affect the fast disintegrating properties and release rates of poorly soluble drugs such as griseofulvin formulated in tablets compared to those of Prosolv® SMCC 50 and Prosolv® SMCC 90. The new silicified materials are appropriate to formulate fast disintegrating tablets by direct compression.


Assuntos
Celulose/química , Composição de Medicamentos , Excipientes/química , Comprimidos/química , Ácidos Esteáricos/química , Resistência à Tração
19.
J Adv Pharm Technol Res ; 2(3): 144-50, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22171310

RESUMO

Microcrystalline cellulose (MCCI) has been widely used as an excipient for direct compression due to its good flowability, compressibility, and compactibility. In this study, MCCI was obtained from agricultural by-products, such as corn cob, sugar cane bagasse, rice husk, and cotton by pursuing acid hydrolysis, neutralization, clarification, and drying steps. Further, infrared spectroscopy (IR), X-ray diffraction (XRD), optical microscopy, degree of polymerization (DP), and powder and tableting properties were evaluated and compared to those of Avicel PH101, Avicel PH102, and Avicel PH200. Except for the commercial products, all materials showed a DP from 55 to 97. Particles of commercial products and corn cob had an irregular shape, whereas bagasse particles were elongated and thick. Rice and cotton particles exhibited a flake-like and fiber-like shape, respectively. MCCI as obtained from rice husk and cotton was the most densified material, while that produced from corn cob and bagasse was bulky, porous, and more compressible. All products had a moisture content of less than 10% and yields from 7.4% to 60.4%. MCCI as obtained from bagasse was the most porous and compressible material among all materials. This product also showed the best tableting properties along with Avicel products. Likewise, all MCCI products obtained from the above-mentioned sources showed a more rapid disintegration time than that of Avicel products. These materials can be used as a potential source of MCCI in the production of solid dosage forms.

20.
Braz. j. pharm. sci ; 47(3): 483-493, July-Sept. 2011. ilus, graf
Artigo em Inglês | LILACS | ID: lil-602665

RESUMO

Metformin hydrochloride is an antidiabetic agent which improves glucose tolerance in patients with type 2 diabetes and reduces basal plasma levels of glucose. In this study, a simplex centroid experimental design with 69 runs was used to select the best combination of some hydrophilic polymers that rendered a 24 h in-vitro release profile of metformin.HCl. The Korsmeyer-Peppas model was used to model the dissolution profiles since it presented the best fit to the experimental data. Further, a cubic model predicted the best formulation of metformin.HCl containing polyvinyl pyrrolidone, ethyl cellulose, hydroxypropyl methyl cellulose, carrageenan, sodium alginate, and gum arabic at 6.26, 68.7, 6.26, 6.26, 6.26 and 6.26 percent levels, respectively. The validation runs confirmed the accuracy of the cubic model with six components for predicting the best set of components which rendered a once-a-day modified release hydrophilic matrix tablet in compliance with the USP specifications.


O cloridrato de metformina é um agente antidiabético que melhora a tolerância à glicose em pacientes com diabetes tipo 2 e reduz os níveis plasmáticos basais de glicose. Neste estudo, um projeto experimental do tipo "centróide simplex" com 69 tomadas foi usado para selecionar a melhor combinação de alguns polímeros hidrofílicos que gerou um perfil de liberação da metformina.HCl de 24 horas. O modelo Korsmeyer-Peppas foi usado para modelar os perfis de dissolução, uma vez que apresentou os melhores ajustes aos dados experimentais. Além disso, um modelo cúbico previu a melhor formulação de metformina.HCl sendo aquela contendo polivinilpirrolidona, etilcelulose, hidroxipropilmetil celulose, carragena, alginato de sódio e goma arábica nos níveis 6.26, 68.7, 6.26, 6.26, 6.26 e 6.26 por cento, respectivamente. As corridas de validação confirmaram a precisão do modelo cúbico com os seis componentes para prever o melhor conjunto de componentes que originou uma libertação do tipo "uma vez ao dia" em conformidade com as especificações da USP, a partir de comprimidos matriciais.


Assuntos
Bioensaio , Química Farmacêutica , Metformina/farmacocinética , Polímeros/farmacologia , Sistemas de Liberação de Medicamentos/estatística & dados numéricos , Análise de Variância , Composição de Medicamentos , /tratamento farmacológico
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