The functionality of a co-processed excipient is usually derived from its composition and the proportion of each excipient that is incorporated to yield a composite excipient. The aim of this study was to assess the impact of binder as a formulation variable on the material and tableting properties of developed co-processed excipients containing gelatin (SGS) and microcrystalline cellulose (SMS) as binders respectively in the same proportion. Two co-processed excipients, SGS and SMS were generated by combining tapioca starch (90%), gelatin or microcrystalline cellulose (7.5%) and colloidal silicon dioxide (2.5%) using the co-fusion method. Particle size analysis and morphological assessment were carried out by light microscopy and scanning electron microscopy (SEM) respectively. DSC analysis was performed to evaluate the thermal behaviour of both materials and flow properties were assessed by measuring parameters like angle of repose, bulk and tapped densities, Carr's index and Hausner's ratio. Compaction behaviour of both materials was determined using Heckel and Walker equations and the compressibility-tabletability-compactibility (CTC) profile for each material was obtained. Particulate and bulk-level properties of SGS and SMS revealed spherical-shaped, free-flowing powders characterized by a glass transition event typical of amorphous polymers. Compaction analysis demonstrated greater degree of plastic deformation with SMS resulting in better tableting properties with respect to tensile strength and disintegration time. The outcome of the study shows that the choice of binder used in the formulation of a co-processed excipient plays a crucial role in defining the material and tableting properties of the co-processed excipient.
Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature for 24 h prior to evaluation. The results revealed that cogranulated co-processed excipient (SAS-CG) gave relatively better properties in terms of flow, compressibility, dilution potential, deformation, disintegration, crushing strength and friability. This study has shown that the method of coprocessing influences the powder and tableting properties of the co-processed excipient.
Objetivo: El objetivo de este estudio fue evaluar el rendimiento del almidón de maíz como excipiente multifuncional en la formulación de comprimidos de metronidazol. Métodos: Metronidazol Tabletas En Honorario preparado por granulación húmeda que contiene almidón de maíz como diluyente (40%), desintegrante (10%) y aglutinante (5%) y en comparación con una formulación de referencia que contiene lactosa como diluyente (40%), almidón de maíz como desintegrante (10%) y Acacia como aglutinante (5%). Los gránulos se analizaron para el tamaño de partícula, propiedades de flujo, compresibilidad y contenido de humedad. Las tabletas con un peso de 500 mg fueron comprimidas para ambas formulaciones en una simple Punch Tablet Press usando un punzón de 12 mm de cara plana en 57,5 MPa. Los comprimidos se mantuvieron durante 24 h para permitir la recuperación elástica y evaluar el peso y el contenido uniformidad, espesor, resistencia a la trituración, friabilidad, tiempo de desintegración y in vitro liberación de drogas. Resultados: Las propiedades del gránulo revelaron diferencias en el tamaño medio del gránulo, el ángulo de reposo, las densidades a granel y roscado para ambas formulaciones. Los comprimidos de Batch I dieron lugar a mejores propiedades de comprimidos en comparación con los comprimidos de lote II. Conclusión: Este estudio confirma la idoneidad del almidón de maíz como excipiente multifuncional en la formulación de comprimidos.
Superdisintegrants are a special class of excipients used in a tablet formulation to aid disintegration and possibly enhance the release kinetics of a drug. The intragranular and extragranular effect of sodium starch glycolate (SSG) or croscarmellose sodium (CCM) as superdisintegrants on tableting properties of metronidazole granules were investigated. The granules were characterized for particle size analysis, angle of repose, bulk and tapped densities as well as Carr's index (CI) and Hausner's ratio (HR). Tablets were prepared from each batch of granules weighing 500 mg on a single punch tablet press using 12 mm flat-faced punches and compressed at 57.5 MPa. The tablets were kept at 25 ± 2 °C/75 % RH for 24 h to allow for elastic recovery and the properties of weight variation, content uniformity, thickness, crushing strength (CS), disintegration time (DT), and drug-release were evaluated. The results showed that all the batches of granules exhibited good flow based on angle of repose < 30° , CI < 20 %, and HR ≤ 1.2. The evaluated tablet properties demonstrated that intragranular addition of either SSG or CCM lowered the CS and DT when compared to the extragranular effect. This indicates that the incorporation mode of superdisintegrant in a tablet formulation exerts an influence on tablet properties.
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