ABSTRACT

Atorvastatin calcium is used to lower the amount of cholesterol in the blood and to prevent stroke, heart attack and angina (chest pain). It is also called as HMG CoA reductase inhibitors which is a competitive inhibitor and inhibits 3 hydroxy-3-methylglutaryl-coenzyme reductase which is the rate determining enzyme located in hepatic tissue which produces mevalonate an early step in cholesterol biosynthesis. 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 Ac Di Sol and sublimating agent menthol. Optimization of atorvastatin calcium orally disintegrating tablets (F1 to F11) were done by optimizing independent variables such as concentration of super disintegrant and sublimating agent (Ac Di Sol as 0.5, 2.75 and 5% and menthol as 2.5, 8.75 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 Ac Di Sol, formulations containing Ac Di Sol and menthol combinations shown fast disintegration and increased percent drug release. The optimized formulation F8 (using Design expert software) having 5% Ac Di Sol and 8.75% menthol showed disintegration time of 14 sec, percent friability of 0.88% and 98.6% 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 drug and excipients of formulation. Based on disintegration and dissolution studies, the optimized formulations were subjected to stability studies and had indicated good stability. Keywords: Disintegration, sublimation, optimization, characterization, friability, percent drug release
Publication date: 01/07/2024

https://ijbpas.com/pdf/2024/July/MS_IJBPAS_2024_8167.pdf

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https://doi.org/10.31032/IJBPAS/2024/13.7.8167