Retarded dissolution of ibuprofen in gelatin microcapsule by cross-linking with glutaradehyde

Arch Pharm Res. 2006 Jun;29(6):520-4. doi: 10.1007/BF02969427.

Abstract

Ibuprofen-loaded gelatin microcapsule, a solid form of microcapsules simultaneously containing ethanol and ibuprofen in water-soluble gelatin shell was previously reported to improve the dissolution of drug. In this study, to retard the initial high dissolution of ibuprofen from gelatin microcapsule, the ibuprofen-loaded cross-linked gelatin microcapsule was prepared by treating an ibuprofen-loaded gelatin microcapsule with glutaraldehyde and its dissolution was evaluated compared to ibuprofen powder and gelatin microcapsule. The ibuprofen-loaded cross-linked microcapsule treated with glutaraldehyde for 10 and 60 sec gave significantly higher dissolution rates than did ibuprofen powder. Furthermore, the dissolution rate of ibuprofen from the cross-linked microcapsule treated for 10 sec was similar to that from gelatin microcapsule. However, the dissolution rate of ibuprofen from the cross-linked microcapsule treated for 60 sec decreased significantly compared to gelatin microcapsule, suggesting that the treatment of gelatin microcapsule with glutaraldehyde for 60 sec could cross-link the gelatin microcapsule. Furthermore, the cross-linking of gelatin microcapsule markedly retarded the release rate of ibuprofen in pH 1.2 simulated gastric fluid compared to gelatin microcapsule. However, the cross-linking of gelatin microcapsule with glutaraldehyde hardly changed the size of gelatin microcapsules, ethanol and ibuprofen contents encapsulated in gelatin microcapsule. Thus, the ibuprofen-loaded cross-linked gelatin microcapsule could retard the initial high dissolution of poorly water-soluble ibuprofen.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Capsules
  • Cross-Linking Reagents / chemistry*
  • Delayed-Action Preparations
  • Drug Compounding / methods
  • Gelatin / chemistry*
  • Glutaral / chemistry*
  • Ibuprofen / chemistry*
  • Particle Size
  • Powders
  • Solubility
  • Time Factors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Capsules
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Powders
  • Gelatin
  • Glutaral
  • Ibuprofen