Article Sidebar
Published:
Jun 26, 2013DOI:
10.4314/tjpr.v12i3.6Keywords:
Article Details
Submission of a manuscript to this journal is a representation that the manuscript has not been published previously and is not under consideration for publication elsewhere.
All authors named in each manuscript would be required to sign a form (to be supplied by the Editor) so that they may retain their copyright in the article but to assign to us (the Publishers) and its licensees in perpetuity, in all forms, formats and media (whether known or created in the future) to (i) publish, reproduce, distribute, display and store the contribution, (ii) translate the contribution into other languages, create adaptations, reprints, include within collections and create summaries, extracts and/or abstracts of the contribution, (iii) create any other derivative works(s) based on the contribution, (iv) to exploit all subsidiary rights in the contribution, (v) the inclusion of electronic links from the contribution to third party material where-ever it may be located, and (vi) license any thrid party to do any or all of the above.
Main Article Content
Formulation and In vitro/In vivo Evaluation of Sustained Release Diltiazem Matrix Tablets
Abstract
Purpose: To develop and optimise sustained release (SR) matrix tablets of diltiazem hydrochloride (DHL).
Methods: DHL tablets were prepared by direct compression and consisted of hydroxypropylmethylcellulose (HPMC), Kollidon SR and Eudragit RSPO. A 32 full factorial design was applied to study the effect of polymers used on drug release from the DHL. The tablets were also evaluated for physicochemical characteristics and release kinetics. In vivo (human) studies were carried out on the optimised formulation using a commercial sustained release product as a reference.
Results: The physicochemical characteristics of all prepared tablets were satisfactory. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the developed formulation was described by the Higuchi model. Mean time to attain peak drug concentration (Tmax) was 2.05 ± 0.52 and 2.30 ± 0.57 h for the optimized and commercial formulations, respectively, while mean maximum drug concentration (Cmax) was 501.74 ± 0.05 ng/ml and
509.65±0.06, ng/ml, respectively. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed based on linear regression analysis.
Conclusion: A fair correlation between in vitro dissolution and in vivo data was found for the optimized formulation of diltiazem. The results also indicate that the approach used could lead to a successful development of a sustained release formulation of the drug.
Keywords: Diltiazem, Matrix tablet, Hydroxypropyl methylcellulose, Eudragit, Optimization
