| dc.description.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
solids was 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. | en_US |
