Lipid-Based Pastillation: A Promising Strategy to Enhance Solubility and Bioavailability of Rosuvastatin Calcium

Abstract

Objectives: Rosuvastatin calcium, a Biopharmaceutics Classification System (BCS) Class II drug used to manage various conditions, is known for its low solubility, which results in slow dissolution and reduced bioavailability. This study focused on developing an advanced method to enhance its solubility. One of the latest and most innovative approaches for improving a substance’s solubility, dissolution rate, and consequently its bioavailability is pastillation. Materials and Methods: Rosuvastatin calcium pastilles were prepared using a laboratory-scale pastillation technique and optimized through a 32 factorial design. Formulations were evaluated for practical yield, drug content, dissolution behavior, Fourier transform infrared (FTIR) compatibility, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, and accelerated stability studies. All experiments were performed in triplicate (n = 3). Results: Pastilles of Rosuvastatin calcium were manufactured using Gelucire 50/13 and polyethylene glycol (PEG) 6000, following the selection of the polymer based on solubility tests. After the production was validated by FT-IR analysis, the pastilles were evaluated for their yield, solubility, drug
content, and dissolution performance. Conclusion: Rosuvastatin calcium pastilles were created with Gelucire 50/13 and PEG 6000, selected based on solubility assessments. Following validation of their production through
FT-IR analysis, the pastilles were examined for yield, drug content, solubility, and dissolution characteristics.