ABSTRACT

Racecadotril is primarily used to treat diarrhoea which acts as a peripherally acting enkephalinase inhibitor. Racecadotril gets rapidly converted to thiorphan which interacts specifically with active site of enkephalinase to produce potent blockade of enzyme, thereby preventing inactivation of endogenous opioid peptides, resulting in fast disintegration and enhanced drug release. Sublimation method was used to prepare orally disintegrating tablets of formulations F1 to F11. The preliminary trials were done using the super disintegrant avidone and sublimating agent camphor. Optimization of racecadotril orally disintegrating tablets (F1 to F11) were done by optimizing independent variables such as concentration of super disintegrant and sublimating agent (avidone as 0.5, 2.75 and 5% and camphor as 5, 10 and 15%) and dependent variables like disintegration time, percent friability and percent drug release. Optimization was done using Design export 13 software by Central composite design from Response surface methodology. ANOVA elucidates the impact of independent variables on dependent variables. In preliminary studies, it was found that, apart from avidone, formulations containing avidone and camphor combinations shown fast disintegration and increased percent drug release. The optimized formulation F6 (using Design expert software) having 5% avidone and 15% camphor showed disintegration time of 4 sec, percent friability of 0.63% and 99.31% drug release. The optimized formulations were characterized using Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Powder X-Ray diffraction (PXRD) studies which showed that there was no interaction between drugand excipients of formulation. Based on disintegration and dissolution studies, the optimized formulations were subjected to stability studies and had indicated good stability. Keywords: Sublimation, Disintegration, Optimization, Quality by design (QbD), Central Composite design, Friability
Publication date: 01/07/2024

https://ijbpas.com/pdf/2024/July/MS_IJBPAS_2024_8166.pdf

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https://doi.org/10.31032/IJBPAS/2024/13.7.8166