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

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A Correction to this article was published on 13 October 2022

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Abstract

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 (Cmax 2864.33 ± 573.86 ng/ml; AUC0-t 5594.95 ± 623.3 ng/h ml) as compared to ATV suspension (Cmax 317.82 ± 63.56 ng/ml; AUC0-t 573.94 ± 398.9 ng/h ml) and marketed tablets (Cmax 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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Acknowledgements

The authors would like to thank Nawal M. Almutairi (a Pharm D candidate) for her assistance in completing some of the experiments in this work. The authors extend their thanks to the Deanship of Scientific Research at King Saud University for the logistic support of this work through the Research Assistant Internship Program, Project no. (RAIP-2-20-215). The authors extend their sincere appreciation to theDeanship of Scientific Research at King Saud University forfunding this research work through the research groupproject number RG-1441-460.

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  1. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

    Basmah N. Aldosari, Alanood S. Almurshedi, Iman M. Alfagih, Bushra T. AlQuadeib, Mohammad A. Altamimi, Syed Sarim Imam, Afzal Hussain, Ehab Elzayat & Sultan Alshehri

  2. Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

    Faleh Alqahtani

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Basmah N. Aldosari and Alanood S. Almurshedi are co-first authors.

The original article has been updated to correct the author’s name from "Ehab Alzait" to "Ehab Elzayat”.

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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

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