Formulation of Gelucire®-Based Solid Dispersions of Atorvastatin Calcium: In Vitro Dissolution and In Vivo Bioavailability Study

Atorvastatin (ATV) is a poorly water-soluble drug that exhibits poor oral bioavailability. Therefore, present research was designed to develop ATV solid dispersions (SDs) to enhance the solubility, drug release, and oral bioavailability. Various SDs of ATV were formulated by conventional and microwave-induced melting methods using Gelucire®48/16 as a carrier. The formulated SDs were characterized for different physicochemical characterizations, drug release, and oral bioavailability studies. The results obtained from the different physicochemical characterization indicate the molecular dispersion of ATV within various SDs.

The drug polymer interaction results showed no interaction between ATV and used carrier. There was marked enhancement in the solubility (1.95–9.32 folds) was observed for ATV in prepared SDs as compare to pure ATV. The drug content was found to be in the range of 96.19% ± 2.14% to 98.34% ± 1.32%. The drug release results revealed significant enhancement in ATV release from prepared SDs compared to the pure drug and the marketed tablets. The formulation F8 showed high dissolution performance (% DE₃₀ value of 80.65 ± 3.05) among the other formulations.

Optimized Gelucire®48/16–based SDs formulation suggested improved oral absorption of atorvastatin as evidenced with improved pharmacokinetic parameters (C_max 2864.33 ± 573.86 ng/ml; AUC_0-t 5594.95 ± 623.3 ng/h ml) as compared to ATV suspension (C_max 317.82 ± 63.56 ng/ml; AUC_0-t 573.94 ± 398.9 ng/h ml) and marketed tablets (C_max 852.72 ± 42.63 ng/ml; 4837.4 ± 174.7 ng/h ml). Conclusively, solid dispersion-based oral formulation of atorvastatin could be a promising approach for enhanced drug solubilization, dissolution, and subsequently improved absorption.

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Article information: Aldosari, B.N., Almurshedi, A.S., Alfagih, I.M. et al. Formulation of Gelucire®-Based Solid Dispersions of Atorvastatin Calcium: In Vitro Dissolution and In Vivo Bioavailability Study. AAPS PharmSciTech 22, 161 (2021). https://doi.org/10.1208/s12249-021-02019-5