Melt Extrusion of High-Dose Co-Amorphous Drug-Drug Combinations : Theme: Formulation and Manufacturing of Solid Dosage Forms Guest Editors: Tony Zhou and Tonglei Li

Pharm Res. 2017 Dec;34(12):2689-2697. doi: 10.1007/s11095-017-2254-8. Epub 2017 Sep 19.

Abstract

Purpose: Many future drug products will be based on innovative manufacturing solutions, which will increase the need for a thorough understanding of the interplay between drug material properties and processability. In this study, hot melt extrusion of a drug-drug mixture with minimal amount of polymeric excipient was investigated.

Methods: Using indomethacin-cimetidine as a model drug-drug system, processability of physical mixtures with and without 5% (w/w) of polyethylene oxide (PEO) were studied using Differential Scanning Calorimetry (DSC) and Small Amplitude Oscillatory Shear (SAOS) rheometry. Extrudates containing a co-amorphous glass solution were produced and the solid-state composition of these was studied with DSC.

Results: Rheological analysis indicated that the studied systems display viscosities higher than expected for small molecule melts and addition of PEO decreased the viscosity of the melt. Extrudates of indomethacin-cimetidine alone displayed amorphous-amorphous phase separation after 4 weeks of storage, whereas no phase separation was observed during the 16 week storage of the indomethacin-cimetidine extrudates containing 5% (w/w) PEO.

Conclusions: Melt extrusion of co-amorphous extrudates with low amounts of polymer was found to be a feasible manufacturing technique. Addition of 5% (w/w) polymer reduced melt viscosity and prevented phase separation.

Keywords: Co-amorphous; HME; Hot melt extrusion; Processability; Rheology.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Calorimetry, Differential Scanning
  • Cimetidine / chemistry*
  • Crystallization
  • Drug Combinations
  • Drug Compounding / methods*
  • Drug Storage
  • Excipients / chemistry*
  • Histamine H2 Antagonists / chemistry*
  • Indomethacin / chemistry*
  • Polyethylene Glycols / chemistry*
  • Rheology
  • Viscosity

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Combinations
  • Excipients
  • Histamine H2 Antagonists
  • Polyethylene Glycols
  • Cimetidine
  • Indomethacin