Development of a Sustained Release Solid Dispersion Using Swellable Polymer by Melting Method

Pharm Res. 2016 Jan;33(1):102-9. doi: 10.1007/s11095-015-1767-2. Epub 2015 Aug 12.

Abstract

Purpose: This study is to design a sustained release solid dispersion using swellable polymer by melting method.

Methods: Polyethylene glycol 6000 (PEG 6000) and hydroxypropyl methylcellulose 4000 (HPMC 4000) were used in solid dispersion for not only enhancing drug dissolution rate but also sustaining drug release. HPMC 4000 is a common swellable polymer in matrix sustained release dosage form, but could not be used in preparation of solid dispersion by melting method. However, the current study utilized the swelling capability of HPMC 4000 accompanied by the common carrier PEG 6000 in solid dispersion to accomplish the goal.

Results: While PEG 6000 acted as a releasing stimulant carrier and provided an environment to facilitate the swelling of HPMC 4000, this swellable polymer could act as a rate-controlling agent. This greatly assisted the dissolution enhancement by changing the crystalline structure of drug to more amorphous form and creating a molecular interaction.

Conclusions: These results suggested that this useful technique can be applied in designing a sustained release solid dispersion with many advantages.

Keywords: poorly water-soluble drug; solid dispersion; sustained release; swellable polymer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations*
  • Drug Design*
  • Hypromellose Derivatives / chemistry*
  • Polyethylene Glycols / chemistry
  • Solubility
  • Tablets
  • X-Ray Diffraction

Substances

  • Delayed-Action Preparations
  • Tablets
  • Polyethylene Glycol 6000
  • Hypromellose Derivatives
  • Polyethylene Glycols