Design and evaluation of co-processed gelatin - guar gum as binder/disintegrant in high drug-loading paracetamol tablet
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Abstract
Background: Balancing mechanical strength and rapid disintegration required for high drug-loading immediate release tablets remain a formulation challenge especially with natural excipients.
Objectives: This study investigated the effect of co-processed gelatin - guar gum on compaction and drug release properties of paracetamol tablets.
Methods: Five batches (A-E) of paracetamol granules were formulated with 0:1, 4:1, 4:0.5, 5:1, and 5:0 % gelatin to guar gum using extended wet granulation. The granules were evaluated for pre-compression properties, and compressed to tablets. The tablets were evaluated for physicochemical parameters.
Results: Increasing the proportion of gelatin over guar gum improved some of the granules' and tablets' 2 properties, peaking in Batch D with granules of < 22.35 ° angle of repose and linear consolidation relationship (R > 0.95), and tablets of tensile strength > 12.88 kg/cm², disintegration time < 6.23 min, drug release > 85 % after 30 min, -6 and permeability (P ) > 1 x 10 cm/s after 3 hr. app
Conclusion: Balanced combination of gelatin and guar gum produced tablets with good mechanical resilience and immediate drug release properties. Further studies are needed to optimize gelatin-guar gum ratio for high drugloading immediate-release formulations.
Résumé
Contexte: L'équilibre entre la résistance mécanique et la désintégration rapide, requis pour les comprimés à libération immédiate à forte teneur en principe actif, demeure un défi de formulation, en particulier avec les excipients naturels.
Objectifs: Cette étude a examiné l'effet d'un coprocédé gélatine-gomme guar sur les propriétés de compactage et de libération du médicament des comprimés de paracétamol.
Méthodes: Cinq lots (A à E) de granulés de paracétamol ont été formulés avec des proportions de gélatine et de gomme de guar de 0:1, 4:1, 4:0.5, 5:1 et 5:0 % par rapport à la gomme de guar, par granulation humide prolongée. Les propriétés des granulés avant compression ont été évaluées, puis ils ont été comprimés en comprimés. Les paramètres physico-chimiques des comprimés ont ensuite été analysés.
Résultats: L'augmentation de la proportion de gélatine par rapport à la gomme guar a amélioré certaines propriétés des granulés et des comprimés, avec des performances optimales observées pour le lot D, présentant des granulés avec un angle de repos < 22.35° et une relation linéaire de consolidation (R² > 0.95), ainsi que des comprimés avec une résistance à la traction > 12.88 kg/cm², un temps de désintégration < 6.23 min, une libération du médicament > 85 % après 30 min, et une perméabilité apparente (Papp ) > 1 x 10-6 cm/s après 3 heures.
Conclusion: The balanced combination of gelatin and guar gum resulted in tablets with good mechanical resistance and immediate release of the active ingredient. Further studies are needed to optimize the gelatin/guar gum ratio to obtain immediate-release formulations with high concentrations of the active ingredient.
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