COMPATIBILITY STUDY BETWEEN PRAVASTATIN AND EZETIMIBE, AND PHARMACEUTICAL EXCIPIENTS USED IN FIXED-DOSE COMBINATION TABLET

KANG MIN KIM

doi:10.22159/ajpcr.2021.v14i8.41793

Authors

KANG MIN KIM Department of Pharmaceutical Science and Technology, Kyungsung University, Busan, South Korea.

DOI:

https://doi.org/10.22159/ajpcr.2021.v14i8.41793

Keywords:

Fixed-dose combination tablet, Compatibility, Pravastatin, Ezetimibe

Abstract

Objective: The purpose of this study was to qualitatively predict drug-excipient binding interactions for stable drug formulation of a pravastatin and ezetimibe fixed-dose combination (FDC) tablet.

Methods: Drug impurity-excipient interactions under accelerated conditions (40°C/75% relative humidity) for 4 weeks were confirmed by high-performance liquid chromatography, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and thermogravimetric (TG) analysis.

Results: Pravastatin impurity was affected by four excipients under accelerated conditions for 4 weeks. Ezetimibe was affected by two excipients. Any other results were within the acceptance criteria. XRD analysis for physical stability revealed characteristic peaks of pravastatin and ezetimibe at a diffraction angle of 2θ (pravastatin: 4.1–24.4°, and ezetimibe: 13.62–29.59°) without a change in the crystalline form after 4 weeks. DSC and TG analysis showed evidence of stability in Alu-Alu foil.

Conclusion: Thus, the tested excipients were confirmed to be compatible with pravastatin and ezetimibe and can be used in FDC bi-layer tablets.

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