Enhanced dissolution rates of glibenclamide through solid dispersions on microcrystalline cellulose and mannitol, combined with phosphatidylcholine

Drug Dev Ind Pharm. 2024 Apr;50(4):297-305. doi: 10.1080/03639045.2024.2321388. Epub 2024 Feb 27.

Abstract

Objective: This study aimed to investigate the impact of physical solid dispersions of spray-dried glibenclamide (SG) on the surface of microcrystalline cellulose (MC) and mannitol (M) surfaces, as well as their combination with phosphatidylcholine (P), on enhancing the dissolution rate of glibenclamide (G).

Methods: Solid dispersions were prepared using varying proportions of 1:1, 1:4, and 1:10 for SG on the surface of MC (SGA) and M (SGM), and then combined with P, in a proportion of 1:4:0.02 using spray drying. The particle size, specific surface area, scanning electron microscopy (SEM), X-ray diffraction (XRD), and dissolution rate of SGA and SGM were characterized.

Results: SEM analysis revealed successful adhesion of SG onto the surface of the carrier surfaces. XRD showed reduced crystalline characteristic peaks for SGA, while SGM exhibited a sharp peaks pattern. Both SGA and SGM demonstrated higher dissolution rates compared to SG and G alone. Furthermore, the dissolution rates of the solid dispersions of SG, MC and P (SGAP), and SG, M, and P (SGMP) were sequentially higher than that of SGA and SGM.

Conclusions: The study suggests that physical solid dispersions of SG on MC and M, along with their combination with P, can effectively enhance the dissolution rate of G. These findings may be valuable in developing of oral solid drug dosage forms utilizing SGA, SGM, SGAP, and SGMP.

Keywords: Solid dispersion; crystalline; dissolution rate; mannitol; microcrystalline cellulose; phosphatidylcholine; surface.

MeSH terms

  • Calorimetry, Differential Scanning
  • Cellulose*
  • Glyburide*
  • Mannitol*
  • Phosphatidylcholines
  • Solubility
  • X-Ray Diffraction

Substances

  • Mannitol
  • Glyburide
  • microcrystalline cellulose
  • Phosphatidylcholines
  • Cellulose