Raina et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):250-254
ISSN: 2250-1177 [250] CODEN (USA): JDDTAO
Available online on 15.03.2019 at http://jddtonline.info
Journal of Drug Delivery and Therapeutics
Open Access to Pharmaceutical and Medical Research
© 2011-18, publisher and licensee JDDT, This is an Open Access article which permits unrestricted
non-commercial use, provided the original work is properly cited
Open Access Research Article
Design, development and optimization of immediate release tablet of
deflazacort
Raina Binu
1
*, Shrivastava Birendra
2
, Bhargava Anurag
1
, Sharma Shailesh
3
, Sharma Abhimanyu Rai
1
,
Bajwa Prabhjot Singh
1
1
Ch. Devi Lal College of Pharmacy, Jagadhri, Yamuna Nagar, Haryana, India
2
School of Pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan, India,
3
Department of Pharmaceutics, Amar Shaheed Baba Ajit Singh Jujhar Singh Memorial College of Pharmacy, Bela, Punjab, India
ABSTRACT
The objective of the present study was to prepare immediate release tablets (IRTs) of deflazacort by direct compression method. Two types of
superdisintegrants i.e. sodium starch glycolate (SSG) and Ac-Di-sol were used in the formulation of tablets. Twelve preliminary batches were
prepared by varying the concentration of superdisintegrants. It was found that formulation containing Ac-Di-Sol disintegrated in less time as
compared to formulation containing sodium starch glycolate. Values of friability was found to be more in case of formulation containing Ac-Di-
Sol. Attempts were also made to prepare the tablets containing superdisintegrants in combination and these resulted in the formulation with
improved values of disintegration time and friability. On the basis of preliminary studies optimization of IRT was done employing 3
2
full factorial
design using design expert 7. The optimized batch of IRTs showed friability and disintegration time values of 0.598 and 64.17±3.50 respectively.
It was also found that 96.26±1.82% of drug was released within 5 min.
Keywords: Immediate release tablets, deflazacort, Rheumatoid arthritis, Sodium starch glycolate, Ac-Di-Sol, 3
2
full factorial design
Article Info: Received 31 Jan 2019; Review Completed 04 March 2019; Accepted 09 March 2019; Available online 15 March 2019
Cite this article as:
Raina B, Shrivastava B, Bhargava A, Sharma S, Sharma AR, Bajwa PS, Design, development and optimization of immediate
release tablet of deflazacort, Journal of Drug Delivery and Therapeutics. 2019; 9(2):250-254
http://dx.doi.org/10.22270/jddt.v9i2.2411
*Address for Correspondence:
Binu Raina, Ch. Devi Lal College of Pharmacy, Jagadhri, Yamuna Nagar, Haryana, India E-mail: binuraina407@gmail.com
INTRODUCTION
Oral route is the preferred route of administration for
administering therapeutic agents. Rate of absorption of drug
is controlled by rate of dissolution. Rate of dissolution can be
increased by various methods. In present study IRTs were
formulated that disintegrate in less time delivering fine
suspension of particles of drug with large surface area,
resulting in increased rate of dissolution
1
. Deflazacort was
chosen as the model drug. Solubility of deflazacort is low
thus making its dissolution controlled by disintegration.
Deflazacort is a corticosteroid which is an oxazoline
derivative of prednisolone, characterized by a high binding
affinity to tissue glucocorticoid receptors and exert anti-
inflammatory and immunosuppressive effects. Deflazacort
significantly inhibits both the proliferation of mononuclear
cells derived from human peripheral blood, and the release
of inflammatory cytokines by these cells. Thus deflazacort is
rapidly effective in symptoms and objective indices of
disease activity in rheumatoid arthritis
2
. RA is a chronic
disorder in which, the body's own immune system starts to
attack body tissues, reasons of which are unknown. This
disorder is accompanied with swelling, stiffness and pain. In
this disorder the attack is not only directed at the joint but to
many other parts of the body. In RA, the joint lining and
cartilage gets more damaged which eventually results in
erosion of two opposing bones. Based on the studies, it has
been reported that deflazacort could be used in treatment of
RA. It is as efficacious as prednisolone with less adverse
effects as compared to other corticosteroids
3
.
In the formulation of immediate release tablets basic
approach is to use superdisintegrants. In the present study
two types of superdisintegrants (sodium starch glycolate and
Ac-Di-Sol) were used. Concentration of both
superdisintegrants was optimized by employing 3
2
full
factorial design.
MATERIALS AND METHOD
Materials
Deflazacort and Avicel pH101 was obtained from Oscar
Remedies Pvt. Ltd. Haryana, India. Sodium starch glycolate,
talc and magnesium stearate was obtained from Nice
Chemicals Pvt. Ltd. Kerala, India. Ac-Di-Sol was obtained
from Optica Pharmaceuticals, Haryana, India.