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<p>Lafutidine (LAFT), a histamine H2-receptor antagonist, is a promising drug for decreasing stomach acid secretion during both nocturnal and postprandial periods. BCS (Biopharmaceutical classification system) class II drug exhibits poor water solubility, which limits its dissolution and delays the achievement of its minimal effective concentration. This study focused on designing and developing liquisolid pellets as an innovative drug delivery system to enhance the dissolution rate of poorly water-soluble drug-lafutidine. This approach employs liquisolid technology alongside the benefits of multi-particulate dosage forms to tackle issues associated with oral drug delivery. A Plackett-Burman experimental design was employed to assess various non-volatile solvents, carrier materials, coating agents, and disintegrants, thereby identifying key factors that affect the efficiency of the formulation. Compatibility of drugs with excipients was further supported by Fourier Transform Infrared Spectroscopy. A 3² complete factorial design was used to determine the optimization of the impact of spheronizer speed (X<sub>1</sub>) and disintegrant (Sodium starch glcolate) concentration (X<sub>2</sub>) on the release percentage of the drug (Y<sub>1</sub>) and flow characteristics (Y<sub>2</sub>). The liquisolid pellets showed improved flow, releasing 99.7% of the drug within 12&#xa0;min in 0.1&#xa0;N HCl, which was remarkably more than the commercial product. The flow characteristics were excellent, having an angle of repose of 17.6°. A non-volatile solvent, Transcutol P allowed the pharmaceutical to dissolve well. Neusilin US2 enhanced flow properties and liquid absorption capability of the blend. Compared to the commercial formulation, liquid solid pellets had a greater drug release. It was found that 73.4% of the drug was released in the marketed formulation after 12&#xa0;min, compared to 98% in the liquid-solid formulation, the statistics show a considerable difference between the two formulations. Results show the innovative potential of liquisolid technology not only in improving the dissolution but also the bioavailability of poorly water-soluble pharmaceuticals. This work concentrates on a robust and scalable formulation method that enhances the solubility of lafutidine, serving as a model to address solubility issues in drug development. The proposed liquisolid pellet method offers an effective strategy to enhance therapy efficacy and patient adherence, showing its significance for modern drug delivery studies.</p>

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Optimization and Characterization of Lafutidine Liquisolid Pellets: A Novel Strategy for Improved Solubility and Drug Release

  • 期刊论文

  • 发表日期：

    2026年2月16日

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  • Jalpa S. Paun,
  • Sheetal Buddhadev,
  • Jigal Hirawala,
  • Prajal Christian,
  • Nilam Rathod,
  • Bhupendra Prajapati

摘要

Lafutidine (LAFT), a histamine H2-receptor antagonist, is a promising drug for decreasing stomach acid secretion during both nocturnal and postprandial periods. BCS (Biopharmaceutical classification system) class II drug exhibits poor water solubility, which limits its dissolution and delays the achievement of its minimal effective concentration. This study focused on designing and developing liquisolid pellets as an innovative drug delivery system to enhance the dissolution rate of poorly water-soluble drug-lafutidine. This approach employs liquisolid technology alongside the benefits of multi-particulate dosage forms to tackle issues associated with oral drug delivery. A Plackett-Burman experimental design was employed to assess various non-volatile solvents, carrier materials, coating agents, and disintegrants, thereby identifying key factors that affect the efficiency of the formulation. Compatibility of drugs with excipients was further supported by Fourier Transform Infrared Spectroscopy. A 3² complete factorial design was used to determine the optimization of the impact of spheronizer speed (X1) and disintegrant (Sodium starch glcolate) concentration (X2) on the release percentage of the drug (Y1) and flow characteristics (Y2). The liquisolid pellets showed improved flow, releasing 99.7% of the drug within 12 min in 0.1 N HCl, which was remarkably more than the commercial product. The flow characteristics were excellent, having an angle of repose of 17.6°. A non-volatile solvent, Transcutol P allowed the pharmaceutical to dissolve well. Neusilin US2 enhanced flow properties and liquid absorption capability of the blend. Compared to the commercial formulation, liquid solid pellets had a greater drug release. It was found that 73.4% of the drug was released in the marketed formulation after 12 min, compared to 98% in the liquid-solid formulation, the statistics show a considerable difference between the two formulations. Results show the innovative potential of liquisolid technology not only in improving the dissolution but also the bioavailability of poorly water-soluble pharmaceuticals. This work concentrates on a robust and scalable formulation method that enhances the solubility of lafutidine, serving as a model to address solubility issues in drug development. The proposed liquisolid pellet method offers an effective strategy to enhance therapy efficacy and patient adherence, showing its significance for modern drug delivery studies.