Retarded dissolution of ibuprofen in gelatin microcapsule by cross-linking with glutaradehyde.
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.
Yong
Chul-Soon
CS
College of Pharmacy, Yeungnam University, Gyongsan, Korea.
Li
Dong-Xun
DX
Oh
Dong-Hoon
DH
Kim
Jung-Ae
JA
Yoo
Bong-Kyu
BK
Woo
Jong-Soo
JS
Rhee
Jong-Dal
JD
Choi
Han-Gon
HG
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002214:Capsules; D003432:Cross-Linking Reagents / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods; D005780:Gelatin / Q000737:chemistry*; D005976:Glutaral / Q000737:chemistry*; D007052:Ibuprofen / Q000737:chemistry*; D010316:Particle Size; D011208:Powders; D012995:Solubility; D013997:Time Factors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D011208:Powders; D005780:Gelatin; D005976:Glutaral; D007052:Ibuprofen