A New Multi-Component Solid of Atorvastatin Calcium with a Dipicolinic Acid Coformer for Improving the Water Solubility

Abstract

Atorvastatin calcium is a potent active pharmaceutical ingredient that reduces blood cholesterol levels. However, oral bioavailability is low because it is difficult to dissolve in water. Therefore, further research to increase the solubility of the drug is needed to improve its bioavailability properties. This research aimed to increase the solubility of atorvastatin calcium through the formation of a multi-component solid. Furthermore, the drug was formed into a multi-component solid with dipicolinic acid as a coformer using the solvent evaporation-quenching method. A powder X-ray diffractometer (PXRD), Fourier transform infrared (FTIR) spectrometer, differential scanning calorimeter (DSC), and scanning electron microscope (SEM) was used to characterize the solid. Also, the shake-flask method was used to analyze the solubility of the solid in distilled water. The results showed that atorvastatin calcium and dipicolinic acid formed a new multi-component solid of cocrystal type. The solubility of the atorvastatin calcium from the multi-component solid was 344.31 ± 37.09 mg/L, which was a significant increase of about 2.7-fold compared to the pure form. 

Keywords

• atorvastatin calcium
• dipicolinic acid
• multi-component solid
• solubility properties