Formulation and In vitro/In vivo Evaluation of
Sustained Release Diltiazem Matrix Tablets
Dheeraj Baviskar1*, Rajesh Sharma2
and Dinesh Jain3
1Institute of Pharmaceutical
Education, Boradi, Tal-Shirpur, Dist-Dhule, 2School
of Pharmacy, D.A.V.V., Phashila Campus, Khandwa Road,
3College of Pharmacy, I.P.S. Academy,
Rajendra Nagar, Indore, India
*For correspondence:
Email:
baviskar@sancharnet.in; Tel: +91- 9850001942
Received: 8 April
2012
Revised accepted:
15 July 2013.
Tropical Journal of
Pharmaceutical Research, October 2013;
12(5): 679-684
http://dx.doi.org/10.4314/tjpr.v12i5.3
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 hydroxyprpoylmethyl
cellulose, 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 volunteer studies
were carried out on the optimised formulation with a
commercial sustained release product serving as
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 hours. The release profile of the developed
formulation was described by the Higuchi model. Mean
time of occurrence for maximum (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 concentration of drug (Cmax)
was 501.74 ± 0.05 and 509.65 ± 0.06, ng/ml respectively.
Good correlation between the dissolution profiles and
bioavailability was observed using the method of linear
regression analysis and correlation coefficient.
Conclusion:
A
fair correlation between in vitro dissolution and in
vivo data was found. The results obtained indicate
successful development of a sustained release
formulation of diltiazem.
Keywords: Diltiazem,
Matrix tablet, Hydroxypropyl methylcellulose Eudragit,
In vitro/in vivo correlation, Optimization
