Back to Search Start Over

Sustained-release tablets of indomethacin-loaded microcapsules: preparation, in vitro and in vivo characterization.

Authors :
Lu B
Wen R
Yang H
He Y
Source :
International journal of pharmaceutics [Int J Pharm] 2007 Mar 21; Vol. 333 (1-2), pp. 87-94. Date of Electronic Publication: 2006 Oct 06.
Publication Year :
2007

Abstract

Indomethacin (IDM) was encapsulated in gelatin-cellulose acetate phthalate (CAP) microcapsules (A) by complex coacervation method and in CAP microcapsules (B) by simple coacervation method. Microcapsules A and B, having mean diameters of 38.24 and 35.74 microm, respectively, were used to prepare sustained-release tablets A and B. The activation energy of thermal degradation for tablets A and B was calculated based on differential scanning calorimetry (DSC) to be 258.9 and 284.8 kcal/mol, respectively. In vitro release profiles showed no burst effect and release t(1/2) of the two sustained-release tablets were found to be 41.30+/-1.86 and 33.25+/-2.84 min, respectively, while that of IDM plain tablets C was 6.30+/-0.39 min (P<0.01). In vitro release of IDM from tablets A and B could be described by Higuchi equation and zero-order kinetics, respectively. After per os (po) administration with physiological saline, their irritation to rat stomach was obviously reduced in comparison with tablets C. Pharmacokinetic study in rabbits showed that t(max) was delayed and C(max) lowered compared with tablets C and the values of AUC(0-24 h) of the three tablets were very close.

Details

Language :
English
ISSN :
0378-5173
Volume :
333
Issue :
1-2
Database :
MEDLINE
Journal :
International journal of pharmaceutics
Publication Type :
Academic Journal
Accession number :
17081709
Full Text :
https://doi.org/10.1016/j.ijpharm.2006.10.002