Atorvastatin calcium formulation development followed by pharmacokinetic with in vitro and in vivo correlation (IVIVC) with employing soluplus and hydroxy propyl methyl cellulose with optimization

Abstract

Objectives The goal of this study was to evaluate different proportions of solid dispersions and formulations by employing various carriers in order to improve solubility of poorly soluble atorvastatin calcium. Materials and methods Solid dispersions can be created using the Solvent Evaporation technique. In comparison to pure drug, (Hydroxy propyl methyl cellulose) HPMC (1:1) indicated as (Solid dispersion) SD1, HPMC E5 (1:2), HPMC E5 (1:4), HPMC (1:1.5) designated as SD2, SD3, SD4, drug caffeine (1:0.5) and caffeine (1:1), denoted as SD5, SD6. The Design Expert software used to 2 level factorial design, the three independent components of X1: are ratios of solid dispersion equivalent (drug:HPMC:soluplus), X2:Superdisintegrant (Primellose), and X3:Surfactant (Sodium lauryl sulphate) was used to do analysis of variance (ANOVA), 3D surface plots, counter plots, optimization, and desirability. Fourier-transform infrared spectroscopy was used to investigate drug-excipient compatibility. Marketed tablets (uncoated tablets manufactured by ‘Revat Laboratories limited) with optimized tablet composition were used in the comparative trials (A2) and Pharmacokinetics. Results and discussion The solid dispersion approach greatly increased the amount of atorvastatin calcium released. The values of f1 and f2 were determined to be 1.89 and 77.78, respectively, and the dissolution profiles of the optimized formulation (A2) and the market tablet were found to be significance. The optimized formula did better on the desirability level (0.975), indicating that it was a good fit. To determine dose bioavailability and to see if there is an in-vitro-in-vivo link. Conclusion The formulations were successfully developed using factorial design, and can be further used for oral delivery of antilipidemic agents is atorvastatin calcium. The model’s predictability and validity were demonstrated when the experimental values matched the expected values. The in vitro-in vivo correlation was good in pharmacokinetic experiments, indicating a significant improvement.