Melt Extrusion for a High Melting Point Compound with Improved Solubility and Sustained Release

Jiannan Lu, Sakae Obara, Fei Liu, Wanyi Fu, Wen Zhang, Shingo Kikuchi

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle size) was explored as the polymeric carrier, while hypromellose (HPMC, Metolose® SR) was chosen as the release rate control agent. GRF presented an HPMCAS grade-dependent solubility: AS-HMP > AS-MMP > AS-LMP. At 10 wt.% loading, the release of GRF was prolonged to 6 h with the incorporation of 10% HPMC 90SH-100SR, while its solubility was enhanced up to sevenfold. Fourier transform infrared spectroscopy (FT-IR) identified the H-bonding between drug and polymers. Element analysis utilizing X-ray photoelectron spectroscopy (XPS) discovered that less GRF aggregated on the surface of binary powders compared with ternary powders containing HPMC, indicating the relatively poor wettability of the latter one. The morphology of extrudates was observed by scanning electron microscopy (SEM) and atomic force microscopy (AFM), illustrating a much smoother and uniform surface of binary extrudates. Immediate release tablets including 10% super-disintegrant L-HPC were able to achieve identical dissolution profile as the powders of extrudates.

Original languageEnglish (US)
Pages (from-to)358-370
Number of pages13
JournalAAPS PharmSciTech
Issue number1
StatePublished - Jan 1 2018

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science


  • amorphous solid dispersion
  • hot melt extrusion
  • polymer blends
  • solubility enhancement
  • sustained release


Dive into the research topics of 'Melt Extrusion for a High Melting Point Compound with Improved Solubility and Sustained Release'. Together they form a unique fingerprint.

Cite this