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Comparative in vitro and in vivo evaluations of oral sustained-release formulations of diclofenac sodium in beagle dogs.
Pharmazie. 2009 Oct; 64(10):648-52.P

Abstract

PURPOSE

Two sustained release formulations (microspheres and Voltaren SR75) were evaluated for their drug release characteristics in dissolution (in vitro study) and after oral administration to beagle dogs (in vivo study) by HPLC.

METHODS

The dissolution study was carried out according to the paddle method and the pharmacokinetic study was conducted using HPLC analysis in a crossover design in six female beagle dogs after oral administration of 75 mg diclofenac sodium (DFS).

RESULTS

The dissolution profiles showed 45% release for Voltaren SR75 and around 95% for the microspheres. Oral administration of DFS resulted in AUC(0-24) and Cmax values of 20.4 microg h/mL and 3.04 microg/mL for microspheres and 33.5 microg h/mL and 5.59 microg/mL for Voltaren, respectively. The Tmax was 3.0 h for both formulations. A significant difference in AUC(0-24) and Cmax was observed for DFS absorption from microspheres and Voltaren.

CONCLUSIONS

The results from the dissolution assay demonstrated the faster release of diclofenac sodium from microspheres. The bioavailability of DFS in microspheres was about 61% that of Voltaren, for the parameters AUC and Cmax, and they are therefore not bioequivalent to Voltaren in relation to the extent of absorption. However, the rate of drug absorption (Tmax) was similar for the two formulations.

Authors+Show Affiliations

Medeiros DC
Departamento de Farmacologia, Centro de Ciências Biológicas, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brasil.
Mazon-Cardoso T
No affiliation info available
Lemos-Senna E
No affiliation info available
Poli A
No affiliation info available

MeSH

Administration, OralAnimalsAnti-Inflammatory Agents, Non-SteroidalArea Under CurveCalibrationChromatography, High Pressure LiquidDelayed-Action PreparationsDiclofenacDogsFemaleHalf-LifeHydrogen-Ion ConcentrationMicrospheresReproducibility of ResultsSolubilitySpectrophotometry, Ultraviolet

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19947166

Citation

Medeiros, D C., et al. "Comparative in Vitro and in Vivo Evaluations of Oral Sustained-release Formulations of Diclofenac Sodium in Beagle Dogs." Die Pharmazie, vol. 64, no. 10, 2009, pp. 648-52.
Medeiros DC, Mazon-Cardoso T, Lemos-Senna E, et al. Comparative in vitro and in vivo evaluations of oral sustained-release formulations of diclofenac sodium in beagle dogs. Pharmazie. 2009;64(10):648-52.
Medeiros, D. C., Mazon-Cardoso, T., Lemos-Senna, E., & Poli, A. (2009). Comparative in vitro and in vivo evaluations of oral sustained-release formulations of diclofenac sodium in beagle dogs. Die Pharmazie, 64(10), 648-52.
Medeiros DC, et al. Comparative in Vitro and in Vivo Evaluations of Oral Sustained-release Formulations of Diclofenac Sodium in Beagle Dogs. Pharmazie. 2009;64(10):648-52. PubMed PMID: 19947166.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparative in vitro and in vivo evaluations of oral sustained-release formulations of diclofenac sodium in beagle dogs. AU - Medeiros,D C, AU - Mazon-Cardoso,T, AU - Lemos-Senna,E, AU - Poli,A, PY - 2009/12/2/entrez PY - 2009/12/2/pubmed PY - 2010/1/22/medline SP - 648 EP - 52 JF - Die Pharmazie JO - Pharmazie VL - 64 IS - 10 N2 - PURPOSE: Two sustained release formulations (microspheres and Voltaren SR75) were evaluated for their drug release characteristics in dissolution (in vitro study) and after oral administration to beagle dogs (in vivo study) by HPLC. METHODS: The dissolution study was carried out according to the paddle method and the pharmacokinetic study was conducted using HPLC analysis in a crossover design in six female beagle dogs after oral administration of 75 mg diclofenac sodium (DFS). RESULTS: The dissolution profiles showed 45% release for Voltaren SR75 and around 95% for the microspheres. Oral administration of DFS resulted in AUC(0-24) and Cmax values of 20.4 microg h/mL and 3.04 microg/mL for microspheres and 33.5 microg h/mL and 5.59 microg/mL for Voltaren, respectively. The Tmax was 3.0 h for both formulations. A significant difference in AUC(0-24) and Cmax was observed for DFS absorption from microspheres and Voltaren. CONCLUSIONS: The results from the dissolution assay demonstrated the faster release of diclofenac sodium from microspheres. The bioavailability of DFS in microspheres was about 61% that of Voltaren, for the parameters AUC and Cmax, and they are therefore not bioequivalent to Voltaren in relation to the extent of absorption. However, the rate of drug absorption (Tmax) was similar for the two formulations. SN - 0031-7144 UR - https://www.unboundmedicine.com/medline/citation/19947166/Comparative_in_vitro_and_in_vivo_evaluations_of_oral_sustained_release_formulations_of_diclofenac_sodium_in_beagle_dogs_ DB - PRIME DP - Unbound Medicine ER -