In-Vivo Pharmacokinetic Study of Ranolazine Liquisolid Systems

Abstract

The present study aimed to develop and characterize liquisolid systems of Ranolazine to overcome its poor aqueous solubility and enhance dissolution and bioavailability. Ranolazine, a BCS Class II drug, exhibits low solubility and limited oral absorption. Liquisolid compacts were formulated using propylene glycol as a non-volatile solvent, microcrystalline cellulose (Avicel PH102) as the carrier, and colloidal silicon dioxide (Aerosil 200) as the coating material. The optimized formulation (F4) demonstrated superior flowability, mechanical strength, and rapid disintegration. In vivo pharmacokinetic studies in Wistar rats revealed significantly improved absorption and bioavailability compared to conventional tablets, while accelerated stability studies confirmed excellent physical and chemical stability under ICH Q1A(R2) conditions. The results validate the liquisolid technique as a cost-effective and scalable approach for improving oral delivery of poorly soluble drugs.

Introduction: pharmaceutical study focused on utilizing Liquisolid Technology to improve the therapeutic efficacy of poorly water-soluble BCS Class II drugs. Subsequent trials with Ranolazine, however, yielded a substantial increase in solubility, confirming the viability of the technique for this specific drug candidate. Researchers then employed a full factorial design to systematically optimize the Ranolazine formulation to maximize drug release and overall solubility. The final optimized system was validated through in-vivo pharmacokinetic testing, which demonstrated superior bioavailability by achieving a 44% higher peak plasma concentration in rats compared to the pure drug. Collectively, the results successfully establish the liquisolid system as an effective strategy for enhancing the delivery and absorption of Ranolazine, a critical antianginal agent.

Conclusion: The liquisolid technique significantly enhanced Ranolazine's solubility, dissolution, and bioavailability. The optimized formulation showed excellent physical properties, rapid release, and improved pharmacokinetic performance. Characterization confirmed drug compatibility and partial amorphization, contributing to the enhanced solubility. The final product also demonstrated robust stability, validating the liquisolid system as an effective strategy for improving BCS Class II drug delivery.