Science and Technology Indonesia
Vol. 7 No. 2 (2022): April

Preparation and Evaluation of Antihypercholesterolemic Activity of Atorvastatin Calcium-Maleic Acid Co-Amorphous Solids

Yudi Wicaksono (Drug Modification Research Group, Faculty of Pharmacy, University of Jember, Jember, 68121, Indonesia)
Shofiatul Izzah Al Amaliyah (Drug Modification Research Group, Faculty of Pharmacy, University of Jember, Jember, 68121, Indonesia)
Finas Rahmayanti (Drug Modification Research Group, Faculty of Pharmacy, University of Jember, Jember, 68121, Indonesia)
Viddy Agustian Rosidi (Drug Modification Research Group, Faculty of Pharmacy, University of Jember, Jember, 68121, Indonesia)
Lina Winarti (Drug Modification Research Group, Faculty of Pharmacy, University of Jember, Jember, 68121, Indonesia)
Dwi Setyawan (Faculty of Pharmacy, Airlangga University, Surabaya, 60286, Indonesia)



Article Info

Publish Date
19 Apr 2022

Abstract

Atorvastatin calcium is a statin drug used for antihypercholesterolemic. The oral bioavailability of atorvastatin calcium is relatively low because it is poorly soluble in water. The low oral bioavailability of the drug causes a decrease in its therapeutic effectiveness. This study aimed to increase the solubility of atorvastatin calcium through the formation of co-amorphous solids and evaluate its activity as antihypercholesterolemic. Atorvastatin calcium was prepared into co-amorphous solids with a maleic acid coformer using the spray drying method. Solids characterization was carried out using Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transforms Infra Red (FTIR), and Scanning Electronic Microscopy (SEM). The solubility test was carried out using the shaking method, while the evaluation of antihypercholesterolemic was carried out in vivo in experimental animals. The results of the analysis of diffractograms, thermograms, FTIR spectra, and micrograph images showed that the atorvastatin calcium-maleic acid solids prepared by spray drying were a co-amorphous solid. The atorvastatin calcium-maleic acid co-amorphous solids had a greater solubility in water (p<0.05) when compared to pure atorvastatin calcium. However, the in vivo antihypercholesterolemic activity results in experimental animals showed that the cholesterol-lowering activity of the atorvastatin calcium-maleic acid co-amorphous solidswas not significantly different (p>0.05) with pure atorvastatin calcium. This phenomenon is thought to be because atorvastatin calcium from co-amorphous solids in solution is more present as a charged fraction, affecting the permeability and absorption process.

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Journal Info

Abbrev

JSTI

Publisher

Subject

Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Environmental Science Materials Science & Nanotechnology Physics

Description

An international Peer-review journal in the field of science and technology published by The Indonesian Science and Technology Society. Science and Technology Indonesia is a member of Crossref with DOI prefix number: 10.26554/sti. Science and Technology Indonesia publishes quarterly (January, April, ...