Microencapsulation of a Hydrophilic Drug into a Hydrophobic Matrix Using a Salting‐Out Procedure. II. Effects of Adsorbents on Microsphere Properties

Abstract

Wax microspheres of the hydrophilic drug guaifenesin were prepared by the congealable disperse‐phase method using a salting‐out procedure. In order to improve the particle properties of the microspheres, adsorbents (colloidal silica, magnesium stearate, and talc) were used during preparation. The effects of adsorbents on microsphere properties such as the angle of repose (AR), compressibility index (CI), geometric mean diameter (GMD), loading efficiency (LE), and in vitro drug release (DR) were determined. The AR, CI, and GMD of the microspheres were significantly reduced in the presence of the adsorbents. Increase in the concentrations of colloidal silica and magnesium stearate led to lower LE and faster DR, while talc showed no effect, which could be due to the particle diameter and specific surface area of the adsorbents. The microspheres prepared with colloidal silica were chosen to be compressed into tablets since they were smaller, more uniform, and had better flow properties than those made with magnesium stearate and talc. The in vitro drug release profile of the microsphere tablets was compared with that of commercially available Mucinex®, sustained release guaifenesin matrix tablets. Similar release profiles were observed between the two tablets. Scanning electronic microscopy (SEM) studies of the broken tablets revealed that the deformation of the microspheres caused by compression was minimal.

Key Words:

• Guaifenesin
• Wax microspheres
• Salting‐out
• Adsorbents
• Tableted microspheres