Enhancing Solubility and Dissolution of BCS Class II Drug Pitavastatin Calcium by Solid Dispersion Technique Incorporating Second Generation Carriers - Development and characterization

Pitavastatin calcium is used for treatment of conditions like hypercholesterolemia by blocking and reducing cholesterol synthesis. It is a BCS class II drug with poor solubility which further effects the dissolution. The present research focuses on improving the solubility and dissolution of Pitavastatin Calcium by formulating solid dispersions (SD). The solid dispersions were prepared by fusion and kneading method, employing second generation carrier’s Polyethylene glycol 6000 (PEG 6000), Polyvinylpyrrolidone K30 (PVP K30) and Beta Cyclodextrin as hydrophilic polymeric materials in different ratios of drug and polymer (1:1, 1:2, 1:4, 1:6). The formulations were evaluated through FTIR (Fourier transform infrared spectroscopy), DSC (differential scanning Calorimetry), PXRD (Powder X-ray diffraction) and SEM (scanning electron microscopy) studies for major analysis. They were further evaluated for compatibility, solubility, micromeritic properties, In-vitro drug release, percentage yield, drug content and stability studies. The PXRD analysis directed that crystallinity of drug was reduced upon dispersing in carrier, which was visualized by enhanced solubility and dissolution of solid dispersions when compared to pure drug. SEM studies suggested the morphological changes of pure API which existed as rod shaped crystalline material to an reduced crystalline system. The outcomes specified solid dispersions prepared by kneading method exhibited improved properties in comparison to fusion method, particularly the SD comprising beta cyclodextrin PSD20 formulated by kneading method with 1:6 ratio produced high solubility and dissolution with 98.91% drug release in 30 min which was considered as best suitable formulation. It endorses that SD technique has considerably improved the solubility and dissolution rate of API which could be further formulated into suitable dosage form.