Bioavailability enhancement of baclofen by gastroretentive floating formulation: statistical optimization, in vitro and in vivo pharmacokinetic studies.
Summary of "Bioavailability enhancement of baclofen by gastroretentive floating formulation: statistical optimization, in vitro and in vivo pharmacokinetic studies."
Objectives: The study was aimed to improve bioavailability of baclofen by developing gastroretentive floating drug delivery system (GFDDS). Methods: Preliminary optimization was done to select various release retardants to obtain minimum floating lag time, maximum floating duration and sustained release. Optimization by 3(2) factorial design was done using Polyox WSR 303 (X(1)) and HPMC K(4)M (X(2)) as independent variables and cumulative percentage drug released at 6 h (Q6h) as dependent variable. Results: Optimized formulation showed floating lag time of 4-5 s, floated for more than 12 h and released the drug in sustained manner. In vitro release followed zero ordered kinetics and when fitted to Korsemeyer Peppas model, indicated drug release by combination of diffusion as well as chain relaxation. In vivo floatability study confirmed floatation for more than 6 h. In vivo pharmacokinetic studies in rabbits showed C(max) of 189.96 ± 13.04 ng/mL and T(max) of 4 ± 0.35 h for GFDDS. The difference for AUC((0-T)) and AUC((0-∞)) between the test and reference formulation was statistically significant (p > 0.05). AUC((0-T)) and AUC((0-∞)) for GFDDS was 2.34 and 2.43 times greater than the marketed formulation respectively. Conclusion: GFDDS provided prolonged gastric residence and showed significant increase in bi oavailability of baclofen.
Affiliation
Department of Pharmacy, TIFAC Centre of Relevance and Excellence in NDDS, Centre of PG Studies and Research,The M. S. University of Baroda , Fatehgunj, Vadodara, Gujarat , India.
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/22901056
- DOI: http://dx.doi.org/10.3109/03639045.2012.709249
Medical and Biotech [MESH] Definitions
Area Under Curve
A statistical means of summarizing information from a series of measurements on one individual. It is frequently used in clinical pharmacology where the AUC from serum levels can be interpreted as the total uptake of whatever has been administered. As a plot of the concentration of a drug against time, after a single dose of medicine, producing a standard shape curve, it is a means of comparing the bioavailability of the same drug made by different companies. (From Winslade, Dictionary of Clinical Research, 1992)
Models, Statistical
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Bibliometrics
The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)
Factor Analysis, Statistical
A set of statistical methods for analyzing the correlations among several variables in order to estimate the number of fundamental dimensions that underlie the observed data and to describe and measure those dimensions. It is used frequently in the development of scoring systems for rating scales and questionnaires.
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