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Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs.
- Source :
- Pharmaceutical Development & Technology; Aug2011, Vol. 16 Issue 4, p415-421, 7p
- Publication Year :
- 2011
-
Abstract
- The main purpose of this work was to develop a supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of carbamazepine (CBZ). S-SMEDDS of CBZ was prepared and drug precipitation behavior, dissolution rate in vitro and particle size distribution were evaluated. The relative bioavailability of S-SMEDDS formulation of CBZ was evaluated in beagle dogs compared with a commercial tablet. The results showed that the presence of a small amount of polymeric precipitation inhibitor (PVP) effectively sustained the supersaturated state by retarding precipitation kinetics. The mean particle size of S-SMEDDS formulation after dispersion was about 33.7 nm and the release rate from S-SMEDDS was significantly higher than the commercial tablet in vitro. In pharmacokinetic parameters of S-SMEDDS formulation, AUC<subscript>0∼∼t</subscript> and C<subscript>max</subscript> were 9.83 ±± 2.47 μμg··ml<superscript>−−1</superscript>··h and 4.96 ±± 1.16 μμg··ml<superscript>−−1</superscript>, compared to the conventional tablet which were 1.67 ±± 1.19 μμg··ml<superscript>−−1</superscript>··h and 0.74 ±± 0.19 μμg··ml<superscript>−−1</superscript>, respectively. AUC<subscript>0-t</subscript> of S-SMEDDS increased nearly five times compared to the market tablet with the same administration dose of 200 mg. On the other hand, AUC<subscript>0--t</subscript> of S-SMEDDS with a dose of 50 mg was about 85.9% compared to the commercial tablet with a dose of 200 mg. Thus, it was concluded that S-SMEDDS provide an effective approach for improving the extent of absorption of CBZ with a low surfactant level. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 10837450
- Volume :
- 16
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- Pharmaceutical Development & Technology
- Publication Type :
- Academic Journal
- Accession number :
- 62541214
- Full Text :
- https://doi.org/10.3109/10837451003774419