Preformulation study of fiber formation and formulation of drug-loaded microfiber based orodispersible tablets for in vitro dissolution enhancement

Int J Pharm. 2014 Dec 30;477(1-2):643-9. doi: 10.1016/j.ijpharm.2014.11.011. Epub 2014 Nov 6.

Abstract

Preformulation study of rotary spun hydroxypropyl cellulose fibers was carried out using the combination of textural characterization of gels in the concentration range of 42-60% w/w and optical microscopic evaluation of formed fibers. High adhesiveness values resulted in bead formation at lower polymer concentration, meanwhile fiber formation was hindered when high adhesiveness values were associated with high polymer content. The optimum gel concentration for fiber formation was given to 50% w/w. Drug loaded microfibers were prepared using a model drug of biopharmaceutical drug classification system class II. Fibers were milled, sieved and mixed with tableting excipients in order to directly compress orodispersible tablets. Hardness, friability, in vitro disintegration time values complied with the pharmacopoeial requirements. In vitro dissolution profiles obtained from three distinct dissolution media (pH 1.0; 4.5; 6.8) were quite differentiated compared to the compressed physical mixture of the same composition. Difference and similarity factors confirmed that the drug dissolution from microfiber based formula was almost independent from the pH value of the media. X-ray diffraction patterns indicated that the drug embedded in microfibers was in amorphous state, and the decrease of o-Ps lifetime values suggested that fiber formation enabled the development of a more ordered fibrous system.

Keywords: Dissolution enhancement; High-speed rotary spinning; Hydroxypropyl cellulose; Microfibers; Orodispersible tablet.

MeSH terms

  • Administration, Oral
  • Cellulose / analogs & derivatives*
  • Cellulose / chemistry
  • Chemistry, Pharmaceutical
  • Drug Carriers / chemistry*
  • Excipients / chemistry*
  • Gels
  • Hardness
  • Particle Size
  • Phase Transition
  • Solubility
  • Surface Properties
  • Tablets
  • Technology, Pharmaceutical / methods*

Substances

  • Drug Carriers
  • Excipients
  • Gels
  • Tablets
  • Cellulose
  • hydroxypropylcellulose