Raina et al Journal of Drug Delivery & Therapeutics.

2019; 9(2):250-254

Design, development and optimization of immediate release tablet of

deflazacort

INTRODUCTION 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
Deflazacort is a corticosteroid which is an oxazoline cartilage gets more damaged which eventually results in
derivative of prednisolone, characterized by a high binding erosion of two opposing bones. Based on the studies, it has
affinity to tissue glucocorticoid receptors and exert anti- been reported that deflazacort could be used in treatment of
inflammatory and immunosuppressive effects. Deflazacort RA. It is as efficacious as prednisolone with less adverse
significantly inhibits both the proliferation of mononuclear effects as compared to other corticosteroids3.
cells derived from human peripheral blood, and the release of
inflammatory cytokines by these cells. Thus deflazacort is In the formulation of immediate release tablets basic
rapidly effective in symptoms and objective indices of disease approach is to use superdisintegrants. In the present study
activity in rheumatoid arthritis2. RA is a chronic disorder in two types of superdisintegrants (sodium starch glycolate and
which, the body's own immune system starts to attack body Ac-Di-Sol) were used. Concentration of both
tissues, reasons of which are unknown. This disorder is superdisintegrants was optimized by employing 32 full
accompanied with swelling, stiffness and pain. In 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.

ISSN: 2250-1177 [250] CODEN (USA): JDDTAO

Raina et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):250-254

Methods mixing. Powdered mixture was passed through 60 # sieve and

blended properly using a mortar and pestle. The resultant
Preparation of immediate release tablets blend was lubricated with the addition of lubricant and
Based on composition of deflazacort IRT tablets with glidant and finally compressed into tablets (30 mg)
deflazacort IRT tablet depicted in table 1 6mg deflazacort and using 3 mm round flat punches. Machine settings were
excipients (except the lubricant; magnesium stearate and adjusted to get the desired hardness value, which gave an
glidant ; talc) were physically mixed by geometric intact tablet.

Evaluation
Table 5: Characterization of preliminary batch of compressed immediate release tablets
F. Weight variation Thickness (mm) Hardness Drug Friability Disintegration
Code (mg) (Mean±SD)*** (Mean±SD)*** (Kg/cm2) content (%)***** time (sec)******
****
F1 30.25±2.50 3.3449±0.089 3.166±.057 99.83 0.372 621.000±3.605
F2 29.6±2.258 3.5576±0.086 3.067±0.173 99.76 0.402 234.667±4.163
F3 31.15±1.579 3.6953±0.112 2.867±0.100 99.74 0.442 227.333±3.177
F4 31.4±2.627 3.8069±0.128 2.633±0.208 99.69 0.575 183.667±5.507
F5 28.15±2.998 3.4608±0.074 2.935±.058 99.87 0.398 147.667±2.516
F6 30.75±1.762 3.6313±0.097 2.8±0.153 99.82 0.447 114.000±4.582
F7 30.25±2.417 3.48±0.103 2.667±0.142 101.2 0.533 70.000±3.605
F8 29.6±2.208 3.520±.154 2.433±0.153 98.51 0.617 56.667±3.512
F9 31.15±2.852 3.510±.099 2.867±0.208 102.21 0.425 129.667±4.509
F10 30.4±2.577 3.59±0.087 2.767±0.058 97.71 0.614 60.000±3.605
F11 28.15±2.998 3.46±0.117 2.905±0.100 98.13 0.579 114.000±4.582
F12 32.75±1.162 2.70±0.094 2.533±0.153 101.82 0.898 49.000±4.358
*** Each value is average of twenty independent determinations; **** Each value is average of ten independent determinations,
*****Each value is average of 216 tablets, ****** Each value is average of six independent determinations.

Statistical and response surface analysis of models and Ac-Di-Sol disintegration time decreased (Patel et al.,
2015)14. The formulation (CT1-CT4) showed unaccepted
Statistical analysis
increase in disintegration time (106, 92, 78 and 87 s
It was found there was a wide variation in the values of respectively), that exceeded the limits specified for IRTs,
disintegration time and friability with change in which is less than 75 s (Dobetti 2012)15
concentration of two factors. Table 6 describes the effect of
In case of friability it was found that with increase in
SSG concentrations (2, 4, and 6%) and Ac-Di-Sol
concentration of SSG and Ac-Di-Sol friability value of IRTs
concentrations (6, 7 and 8%) on the characteristics of IRT.
also increased.
Results showed that with increase in concentration of SSG

ISSN: 2250-1177 [251] CODEN (USA): JDDTAO

Raina et al Journal of Drug Delivery & Therapeutics. 2019; 9(2):250-254

Response surface analysis

ISSN: 2250-1177 [252] CODEN (USA): JDDTAO