Comparison of pharmacokinetics in beagle dogs of nimesulide bilayer tablets with dispersible tablets.
Summary of "Comparison of pharmacokinetics in beagle dogs of nimesulide bilayer tablets with dispersible tablets."
The purpose of this study was to compare the in vitro release and the in vivo pharmacokinetics of bilayer tablets with the conventional dispersible tablets of nimesulide. The tablets were administered to beagle dogs and the plasma levels of nimesulide were determined by high-performance liquid chromatography-MS/MS. The pharmacokinetic parameters were calculated using a noncompartmental model. The bilayer tablets showed a biphasic in vitro release pattern with initial burst release and sustained release following the quasi-Fickian diffusion-based release mechanism. The C(max), t(max), mean residence time (MRT), and area under the curve from 0 to 36 h were 10.8 ± 4.2 μg/mL, 2.3 ± 1.0 h, 6.7 ± 2.1 h, 81.5 ± 26.7 μg·h/mL for the bilayer tablets and 14.8 ± 5.8 μg/mL, 2.7 ± 0.8 h, 5.6 ± 0.9 h, 95.4 ± 44.2 μg·h/mL for the dispersible tablets. Compared with the dispersible tablets, the bilayer tablets have lower C(max), similar t(max), and longer MRT. The aforementioned pharmacokinetic parameters, especially the MRT demonstrated to be valuable for evaluating the biphasic characteristics. This study provides a promising in vivo evaluation method for the bilayer tablets with biphasic release pattern.
Affiliation
Beijing Institute of Pharmacology and Toxicology , Beijing , China.
Journal Details
This article was published in the following journal.
Name: Drug development and industrial pharmacy
ISSN: 1520-5762
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22397600
- DOI: http://dx.doi.org/10.3109/03639045.2012.662506
Medical and Biotech [MESH] Definitions
Anaerobiospirillum
A genus of gram-negative, spiral-shaped bacteria in the family SUCCINIVIBRIONACEAE. It has been isolated from the THROAT and COLON of beagle dogs and from human FECES.
Cross-cultural Comparison
Comparison of various psychological, sociological, or cultural factors in order to assess the similarities or diversities occurring in two or more different cultures or societies.
Tablets, Enteric-coated
Tablets coated with material that delays release of the medication until after they leave the stomach. (Dorland, 28th ed)
Canidae
A family of terrestrial carnivores with long snouts and non-retractable claws. Members include COYOTES; DOGS; FOXES; JACKALS; RACCOON DOGS; and WOLVES.
Staphylococcus Intermedius
A species of gram-positive bacteria in the family STAPHYLOCOCCACEAE. It is a zoonotic organism and common commensal in dogs, but can cause disease in dogs and other animals. It also can be associated with human disease.
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