A Novel Application of an Effervescent Agent in Naproxen Liqui-Pellets for Enhanced Drug Release

摘要

Liqui-Pellet formulations have been introduced as a technology to improve the dissolution rate of poorly water-soluble drugs. This study aimed to incorporate sodium bicarbonate (NaHCO3) into the Liqui-Pellet formulation to explore the potential impact on the drug release rate. Naproxen Liqui-Pellet formulations containing 5%, 12%, 22%, 32%, and 42% w/w of NaHCO3 were successfully produced and their physicochemical properties were investigated and compared with a physical mixture pellet formulation. Incorporation of such a large amount of functional excipient is impossible or near impossible in the classical liquisolid formulation due to weight and size limitations, particularly for high-dose drugs. The results showed that NaHCO3 is an effective functional excipient to enhance the drug dissolution rate. The Liqui-Pellet formulation with 42% w/w NaHCO3 released 76.4% of drug after 2 hours at pH 1.2, which was 14 times faster than the physical mixture pellet (5.5% drug release in 2 h). In general, a faster dissolution rate was observed with increasing NaHCO3 concentration; however, there was a limit to this effect. Above a certain limit, the influence of NaHCO3 on the dissolution rate lessened. The flowability test showed that all formulations have good to excellent flowability. Overall, this study demonstrates the flexibility of Liqui-Pellets in terms of formulation design, which in turn further supports the potential of Liqui-Pellets as the next generation oral dosage form.