Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Formulation, in vitro evaluation and characterization of atorvastatin solid dispersion

Asif Iqbal¹, Md Shafayat Hossain^1,2 , Md Abdullah Shamim^1,3, Monirul Islam⁴, Md Abu Talha Siddique¹

¹Pharmacy Discipline, Life Science School, Khulna University, Khulna-9208; ²Veritas Pharmaceutical Ltd, Gazipur, Dhaka, People's Republic of Bangladesh; ³Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, Pomona, California-91766, USA; ⁴Department of Pharmacy, Pabna University of Science and Technology, Pabna, People's Republic of Bangladesh.

For correspondence:- Md Shafayat Hossain Email: shafayatbd@gmail.com

Accepted: 15 May 2020 Published: 30 June 2020

Citation: Iqbal A, Hossain M, Shamim M, Islam M, Siddique MT. Formulation, in vitro evaluation and characterization of atorvastatin solid dispersion. Trop J Pharm Res 2020; 19(6):1131-1138 doi: 10.4314/tjpr.v19i6.2

© 2020 The authors.
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Abstract

Purpose: To formulate a polymer-incorporated solid dispersion preparation for enhancing the dissolution and bioavailability of atorvastatin calcium trihydrate (ATV), while maintaining oral compatibility.

Method: Four different methods, i.e., physical mixing (PM), fusion (F), solvent evaporation (SE) and kneading (K), as well as three different excipients i.e. croscarmellose sodium (CCS), microcrystalline cellulose (MCC) and lactose (LAC) were used to formulate various drug-carrier combinations.

Results: In SE method, the rank order of magnitude of drug release was CCS > LAC > MCC, while in fusion and kneading methods, the rank order of release was MCC > CCS > LAC and MCC > CCS > LAC, respectively. Drug release of atorvastatin was maximum (103 %) in FM2 formulation. However, this formulation was non-compatible based on spectroscopic analysis. In contrast, SC2 formulations at 1:2 ratio were compatible in terms of cumulative drug release (99 %), and based on spectroscopic data, thermal analysis and microscopic evaluation.

Conclusion: These results confirm that CCS forms a superior interface with atorvastatin when SE formulation method is used. Thus, solid dispersion is a promising approach for enhancing the oral bioavailability of atorvastatin.

Keywords: Atorvastatin, Solid dispersion, Bioavailability, Solvent evaporation