Preparation and In Vitro/In Vivo Evaluation of Celecoxib Self-microemulsifying Drug Delivery Systems
10.3870/j.issn.1004-0781.2017.05.020
- VernacularTitle:塞来昔布自微乳化释药系统的制备及体内外评价
- Author:
Haichun LI
;
Min WANG
;
Peng XIE
;
Jingbo QI
;
Hui XIAO
- Keywords:
Celecoxib;
Self-microemulsifying drug delivery system;
Pseudo-ernary phase diagram;
Dissolution;
Bioavailability
- From:
Herald of Medicine
2017;36(5):549-553
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate celecoxib self-microemulsifying drug delivery system (CXB-SMEDDS) that was developed to increase the dissolution rate and oral bioavailability of celecoxib.Methods The formulation of CXB-SMEDDS was optimized by pseudo-ternary phase diagrams analysis.The appearance, morphology, particle size distribution and in vitro drug release behavior of CXB-SMEDDS were investigated after diluted by water.The bioavailability of CXB-SMEDDS was determined by oral administration to rats compared with CXB suspension.Results An optimized formulation was selected: Medium chain triglycerides as oil phase, Tween 20 as surfactant, Transcutol HP as cosurfactant.The ratio of oil phase, surfactant and cosurfactant was 2∶9∶9.Upon mixing with water, CXB-SMEDDS formed a clear and transparent microemulsion solution with homogeneous small spherical under transmission electron microscopy.For particle size of CXB-SMEDDS was found to be (57.6±14.2) nm.The in vitro dissolution test indicated a significant improvement in release characteristics of CXB.The AUC of CXB-SMEDDS and CXB suspension were (5.54±0.94) and (3.32±0.59) mg·L-1·h, respectively.The relative bioavailability was 166.9%.Conclusion The SMEDDS can significantly increase celecoxib dissolution in vitro and bioavailability in vivo.
