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Formulation Design of Self-Microemulsifying Drug Delivery Systems for Improved Oral Bioavailability of Celecoxib

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Title Formulation Design of Self-Microemulsifying Drug Delivery Systems for
Improved Oral Bioavailability of Celecoxib
 
Creator Subramanian, Natesan
Ray, Subhabrata
Ghosal, Saroj Kumar
Bhadra, Ranjan
Moulik, Satya Priya
 
Subject Chemistry
 
Description Celecoxib is a hydrophobic and highly permeable drug belonging to class II of biopharmaceutics classification
system. Low aqueous solubility of celecoxib leads to high variability in absorption after oral administration.
Cohesiveness, low bulk density and compressibility, and poor flow properties of celecoxib impart complications
in it’s processing into solid dosage forms. To improve the solubility and bioavailability and to get faster onset of
action of celecoxib, the self-microemulsifying drug delivery system (SMEDDS) was developed. Composition of
SMEDDS was optimized using simplex lattice mixture design. Dissolution efficiency, t85%, absorbance of diluted
SMEDDS formulation and solubility of celecoxib in diluted formulation were chosen as response variables. The
SMEDDS formulation optimized via mixture design consisted of 49.5% PEG-8 caprylic/capric glycerides, 40.5%
mixture of Tween20 and Propylene glycol monocaprylic ester (3 : 1) and 10% celecoxib, which showed signifi-
cantly higher rate and extent of absorption than conventional capsule. The relative bioavailability of the
SMEDDS formulation to the conventional capsule was 132%. The present study demonstrated the suitability of
mixture design to optimize the compositions for SMEDDS. The developed SMEDDS formulations have the potential
to minimize the variability in absorption and to provide rapid onset of action of celecoxib.
 
Date 2004
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/508/1/BIOLOGICAL_%26_PHARMACEUTICAL_BULLETIN%2C__27(12)%2C__1993%2D1999_[4].pdf
Subramanian, Natesan and Ray, Subhabrata and Ghosal, Saroj Kumar and Bhadra, Ranjan and Moulik, Satya Priya (2004) Formulation Design of Self-Microemulsifying Drug Delivery Systems for Improved Oral Bioavailability of Celecoxib. Biol. Pharm. Bull. , 27 (12). pp. 1993-1999.
 
Relation http://dx.doi.org/10.1248/bpb.27.1993
http://www.eprints.iicb.res.in/508/