In the present work, fast dissolving tablets of fexofenadine HCl were designed with a view to enhance patient compliance by direct compression method. The present work studied the effect of superdisintegrants on release rate of fexofenadine HCl in the form of fast disintegrating tablet. For the present study range of superdisintegrants in their different concentrations, were used. The superdisintegrants used were crosscarmellose sodium, crosspovidone and kyron        T-314. The blends were prepared by direct compression technique. The tablets were evaluated for hardness, thickness, friability, drug content, weight variation and in-vitro drug release studies in pH 6.8. Keywords: Fexofenadine hydrochloride, fast dissolving tablets, crosscarmellose sodium, crospovidone, kyron T-31

Bankar, V H

desale, kuldeep yogendra

Gaikwad, P D

Pawar, S P

Advanced Research Journals

  
 
International Journal of Drug Delivery 4 (2012) 82-88 
http://www.arjournals.org/index.php/ijdd/index 
 
Original Research Article 
             
Formulation and Characterization of Fexofenadine hydrochloride Fast Dissolving Tablet 
by using various Superdisintegrants. 
K Y Desale1, P D Gaikwad1, V H Bankar1, S P Pawar1 
 
*Corresponding author: 
 
KY Desale 
 
1P S G V P MÊs 
College of Pharmacy, Shahada, 
Dist:Nandurbar 425 409, 
Maharashtra, India.. 
 
 
 
 
 
 
 
 
A b s t r a c t  
In the present work, fast dissolving tablets of fexofenadine HCl were designed with a view to 
enhance patient compliance by direct compression method. The present work studied the effect of 
superdisintegrants on release rate of fexofenadine HCl in the form of fast disintegrating tablet. For 
the present study range of superdisintegrants in their different concentrations, were used. The 
superdisintegrants used were crosscarmellose sodium, crosspovidone and kyron        T-314. The 
blends were prepared by direct compression technique. The tablets were evaluated for hardness, 
thickness, friability, drug content, weight variation and in-vitro drug release studies in pH 6.8. 
Keywords: Fexofenadine hydrochloride, fast dissolving tablets, crosscarmellose sodium, 
crospovidone, kyron T-314. 
Introduction 
Many patients have difficulty to swallow tablets and hard gelatin 
capsules and thus does not comply with prescription, which 
results in high incidence of non-compliance and ineffective 
therapy. It is estimated that 50% of the population is affected by 
this problem. Recent advances in Novel Drug Delivery Systems 
(NDDS) aim to enhance safety and efficacy of drug molecule by 
formulating a convenient dosage form for administration and to 
achieve better patient compliance. One such approach is „Fast 
Dissolving Tablets (FDT) [1-5].  
According to European Pharmacopoeia, the FDT should 
disperse/disintegrate in less than three minutes. The basic 
approach used in development of FDT is the use of 
superdisintegrants like cross linked carboxymelhylcellulose 
(croscarmellose), sodium starch glycolate (Primogel, Explotab), 
polyvinylpyrrolidone (Polyplasdone) etc. which provide 
instantaneous disintegration of tablet after putting on tongue, 
thereby releasing the drug in saliva. Their growing importance 
was underlined recently when European pharmacopoeia adopted 
the term „Orodispersible tablet‰ as a tablet that to be placed in the 
mouth where it disperses rapidly before swallowing. The 
bioavailability of some drugs may be increased due to absorption 
of drug in oral cavity and also due to pregastric absorption of 
saliva containing dispersed drugs that pass down into the 
stomach. More ever, the amount of drug that is subjected to first 
pass metabolism is reduced as compared to standard tablet. The 
technologies used for manufacturing fast-dissolving tablets are 
freeze-drying, spray-drying, tablet molding, sublimation, sugar-
based excipients, tablet compression, and disintegration addition. 
As a result of increased life expectancy, the elderly constitute a 
large portion of the worldwide population today [6-7]. These 
people eventually will experience deterioration of their 
physiological and physical abilities. fexofenadine HCl  is a non-
sedating anti-histamine used in systemic relief of allergic 
conditions including seasonal allergic rhinitis and urticaria [8]. 
Fexofenadine HCl was preferred as a model drug for formulation 
development. fexofenadine HCl is biopharmaceutical classification 
system type II as it possesses low solubility and high permeability. 
This depicts its good bioavailability which in turn suggests its ideal 
candidature for fast disintegrating drug delivery system.  It is 
indicated for the relief of symptoms associated with seasonal 
allergic rhinitis in adults and children 2 years of age and older and 
for treatment of uncomplicated skin manifestations of chronic 
idiopathic urticaria in adults and children 6 months of age and 
older. These conditions are commonly found in pediatric patients, 
where palatability is of main concern. In case of conventional 
ISSN: 0975-0215 
  
This work is licensed under a Creative Commons Attribution 3.0 License.  
Desale et al. International Journal of Drug Delivery 4 (1) 82-88 [2012] 
 
PAGE | 83 |
 
 
tablets there is problem of swallowing of tablet particularly in 
pediatric patient.  
In many orally disintegrating tablet technologies based on direct 
compression, the addition of superdisintegrants principally affects 
the rate of disintegration and hence the dissolution. The presence 
of other formulation ingredients such as water-soluble excipients 
and effervescent agents further hastens the process of 
disintegration. Although superdisintegrants primarily affect the 
rate of disintegration, but when used at high levels they can also 
affect mouth feel, tablet hardness and friability [9]. 
In the present work an attempt was made to formulate fast 
disintegrating tablet of fexofenadine HCl which get disintegrate in 
saliva which overcome swallowing problem especially for pediatric 
patients. So, even elder people who have swallowing or chewing 
difficulties experience ease of administration. Moreover these 
tablets have sufficient mechanical integrity to withstand rigors of 
mechanical shocks during processing and shipment without 
breakage. 
Materials and methods 
Fexofenadine HCl was obtained from Aurobindo Pharmaceuticals, 
Hyderabad, India., crosscarmellose sodium, crosprovidone, 
pearlitol SD 200 was a gift from Signet Chemicals., Mumbai., 
kyron T-314was a gift from Corel Pharmachem., Ahemdabad., 
microcrystalline cellulose and aerosol was purchase from Modern 
Scientific, Nasik., aspartame and magnesium stearate was 
purchase from SD Fine Chemicals, Mumbai, India. 
Drug Polymer Compatibility Study 
In order to study possible incompatibilities between drug and 
superdisintegrants, IR spectrums fexofenadine HCl , kyron T-314 
and itÊs physical mixture were recorded in the stretching frequency 
range 400-4000 cm-1. The samples were prepared by KBr press 
pellet technique. 
Evaluation of Tablet Blend 
Tablet blend was evaluated by angle of repose, bulk density, 
tapped density, CarrÊs index and HausnerÊs ratios. Each analysis 
was carried out in triplicate.  
Preparation and compression of tablets 
Required quantity of each ingredient was taken for each specified 
formulation. All the ingredients were passed through mesh 60. 
The ingredients depicted in Table 1 were mixed homogenously 
and co grind in a mortar and pestle. Finally, magnesium stearate 
was added and mixed for 5 min. The mixed blend of drug and 
excipients was compressed using cadmach single punch tablet 
punching machine to produce convex faced tablets weighing 150 
mg each with a diameter of 8mm. 
Evaluation of Tablet 
The prepared tablets were evaluated for hardness, thickness, 
friability, weight variation, wetting time, disintegration time and 
drug content. 
In- vitro  drug release studies 
The developed formulations (n=3) were subjected to release 
studies using USP type II dissolution apparatus at 50 rpm with a 
constant temperature water bath at 37ĈCμ2ĈC. Dissolution 
medium used was pH 6.8 (900 ml) for 2, 4, 6, 8, 10, 12, 14, 16, 
18, 20 min. Withdraw 10 ml of samples at different time interval 
and replaced with an equivalent amount of fresh medium. The 
concentration of fexofenadine HCl was determined by measuring 
the absorbance at 222 nm.  
Wetting time  
The wetting time of tablets was measured using a simple 
procedure. A piece of tissue paper folded twice was placed in a 
small petri dish containing 10 ml of pH 6.8 buffer solution. A tablet 
having amaranth powder on the upper surface was placed on the 
filter paper. Time required to develop red color on the upper 
surface of tablet was recorded as wetting time. 
Result and Discussion 
Drug Polymer Compatibility Studies 
Fourier Transform Infra-Red Studies 
Drug polymer compatibility study was carried out by Fourier 
Transform Infra-Red Studies. The IR spectrum of pure drug, kyron 
T-314, and its physical mixture  are shown in Figure No.1-3. From 
the result, it was observed that there is no significant changes in 
material characteristics when fexofenadine HCl was used with 
kyron T-314. 
Characterization of Tablet Blend 
The formulations F1 to F9 were evaluated for angle of repose, 
bulk density, tapped density, CarrÊs index and HausnerÊs ratio. 
The results are shown in Table No.2. From the Table No.2, the 
angle of repose, bulk density, tapped density, CarrÊs index and 
HausnerÊs ratio were found to be within the limits. The 
compressibility index was the lowest for all the formulations which 
had good flow properties. Also, lower values for Hausner ratio 
indicate excellent flow properties of the formulations. 
Characterization of Formulation 
The hardness, thickness, friability, weight variation and drug 
content of all the formulations were determined and the results 
obtained are mentioned in the Table No.3-5. The tablets 
evaluated for the weight variation showed within the limit. The 
friability of the tablets was found to be less than 1% which was 
Desale et al. International Journal of Drug Delivery 4 (1) 82-88 [2012] 
 
PAGE | 84 |
 
 
considered within the limit. The drug content of the formulations 
was found to be within the limits. 
In-vitro  Drug Release Studies 
Effect of Crosscarmellose  
In order to investigate the effect of crosscarmellose on 
fexofenadine HCl, the formulation F1-F3 were prepared with 
crosscarmellose in the concentration range of 2, 3, 4 % w/w. The 
results of release profile are shown in Figure No.4. From the 
Figure No.4, it was observed that the formulation F1, F2 and F3 
showed drug release rate 93.12%, 94.09%, 94.84% in 20 min. 
From the results, it was observed that the disintegration time of 
tablet decreases as the concentration of the superdisintegrants 
increases. Other workers also reported the same result [10-11]. 
 
Effect of Crosspovidone 
In order to investigate the effect of crosspovidone on fexofenadine 
HCl, the formulation F4-F6 were prepared with crosspovidone in 
the concentration range of   2, 3, 4 % w/w. The results of release 
profile are shown in Figure No. 5. From the Figure No.5, it was 
observed that formulation F4, F5 and F6 showed drug release 
rate 94.15%, 95.29%, 96.26% in 20 min. This is because, as the 
concentration of superdisintegrants increases as the 
disintegration time decreases [12].The formulation prepared with 
crosspovidone showed more drug release as compared to the 
crosscarmellose. The reason behind this, crosscarmellose is 
generally used as a superdisintegrants but crosspovidone is used 
as a superdisintegrants as well as solubility enhancing agent 
[13].Because of this the formulation F4-F6 showed more drug 
release rate as and disintegrate fastly as compare to formulation 
prepared by crosscarmellose. Thus crosspovidone shows more 
release as compare to crosscarmellose. 
  
Effect of Kyron T-314 
In order to investigate the effect of kyron T 314 on fexofenadine 
HCl, the formulation F7-F9 were prepared with Kyron T-314 in the 
concentration range of 1, 2, 3% w/w. the result of release profile 
are shown in Figure No. 6. 
From the Figure No. 6, it was observed that formulation F7, F8, 
F9 shows drug release rate 95.58%, 96.32% and 97.46% in 20 
min. this indicates that as concentration of superdisintegrant 
increases the disintegration time decreases. The formulation 
prepared with kyron T-314 showed more drug release as 
compared to crosspovidone. This result might be because of it 
having high swelling index as compared to crosspovidone.[14] 
Conclusion 
From the study it is concluded that, fast dissolving tablet of 
fexofenadine HCl can be successfully prepared by direct 
compression techniques using selected superdisintegrants for 
better patient compliance and effective therapy. The formulation 
F9 which is prepared with kyron T-314 in the concentration of 3% 
is considered as a optimized batch. Disintegration studies 
indicated that disintegration time were decreased by increasing 
the concentration of superdisintegrants in following manner. 
  
Kyron T-314 < Crosspovidone < Crosscarmellose 
 
 Fast dissolving tablet of fexofenadine HCl of acceptable 
texture and sufficient structural integrity is successfully prepared 
by the cost effective direct compression technology. 
  
List of abbreviations 
              NDDS- Novel Drug Delivery Systems 
  FDT- Fast Dissolving Tablet 
  HCl  - Hydrochloric acid   
  FTIR- Fourier transform infrared spectroscopy 
AuthorÊs contributions 
Mr. K. Y. Desale - Carried out experimental part of study. 
Ms. P.D. Gaikwad and Dr.V.H. Bankar - Substantial contribution 
to conception and design, or acquisition of data, or analysis and    
interpretation of data, also involved in drafting                    
or revising it critically for important intellectual                    
content and given final approval of the version to                    
be published.  
Acknowledgment 
The authors are grateful to Dr. V. H. Bankar , as a guide and Dr. 
S.P. Pawar, Principal of P.S.G.V.P.MÊS College of Pharmacy, 
Shahada, Maharashtra , India, for providing technical assistance 
and support for this study. 
 
 
 
References 
[1]. Seager H. Drug delivery products 
and the zydis Fast dissolving dosage 
forms. J of Pharmacy and 
Pharmacology. 1998: 50: 375-382. 
[2]. Chang RK, Guo X, Burnside BA, 
Cough RA. Fast dissolving tablets. 
Pharm Tech 2000: 24(6): 52-58. 
[3]. Dobetti L. Fast-melting tablets: 
Developments and technologies. 
Pharma Tech 2001: 44-50. 
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[4]. Kuchekar BS, Arumugam V. Fast 
dissolving tablets. Indian J Pharm 
Educ 2001: 35: 150-152. 
[5]. Nagendra Kumar D, Raju SA, 
Shirsand SB. Formulation design of 
fast dissolving tablets of 
fexofenadine hydrochloride by 
sublimation Method. International J 
of Pharma and Bio Sciences. 2010: 
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[6]. Kaushik D, Saini TR, Dureja H. 
Development of melt in mouth 
tablets by sublimation technique. J  
Pharm. Res.2004: 3: 35-37. 
[7]. Kuchekar BS, Atul BC, Mahajan HS. 
Mouth dissolving tablets: A novel 
drug delivery system, 2003: Pharma 
Times 35: 7-9. 
[8]. Allen LV, Wang B. Particulate 
support matrix for making a rapidly 
dissolving tablet, 1997: US Patent 
5595761. 
[9]. Desale KY, Bankar VH, Gaikwad 
PD, Pawar SP.  Review on: Fast 
dissolving/disintegrating tablets. 
International J of Pharmaceutical 
Sciences Review and Research. 
2011: Volume 11, Issue 1, 152-158. 
[10]. Venkatalakshmi R, Swatr SC, 
Tejaswini G, Srujana D, Reddy G, 
Kumar J. Formulation and evaluation 
of granisetron hydrochloride mouth 
dissolving tablet. International J of 
Pharmaceutical Science. 2009: 
Volume 1, Issue 2, 336-341. 
[11]. Serasiya T, koradia S, Vaghani S, 
JivaniI NP. Design, optimization and 
in-vitro evaluation of orodispersible 
tablets of pheniramine maleate. 
International J of Pharma Research 
and Development, 2004: Volume 1, 
Issue10, 1-18. 
[12]. Kakade SM, Mannur VS, Ramani 
KB. Formulation and evaluation of 
mouth dissolving tablets of losartan 
potassium by direct compression 
techniques. International J of 
Research and Pharmaceutical 
Sciences, 2010: Volume 3, Issue 1, 
290-295.  
[13]. Rowe RC, Sheskey PJ, Owen SC. 
Handbook of pharmaceutical 
excipients, 5th edition, 
Pharmaceutical Press, London. 
2006: 209-211. 
[14]. Rowe RC, Sheskey PJ, Owen SC. 
Handbook of pharmaceutical 
excipients, 5th edition, 
Pharmaceutical Press, London. 
2006: 504-506.. 
 
 
 
 
Table No.1 Formulation Composition 
Ingredients F1 F2 F3 F4 F5 F6 F7 F8 F9 
Fexofenadine HCl 30 30 30 30 30 30 30 30 30 
Microcrystalline Cellulose 38 36.5 35 38 36.5 35 39.5 38 36.5 
Crosscarmellose 3 4.5 6 - - - - - - 
Crosprovidone - - - 3 4.5 6 - - - 
Kyron T-314 - - - - - - 1.5 3 4.5 
Pearlitol SD 200 68 68 68 68 68 68 68 68 68 
Aspartame 7 7 7 7 7 7 7 7 7 
Aerosil 2 2 2 2 2 2 2 2 2 
Magnesium stearate 2 2 2 2 2 2 2 2 2 
 
 
 
 
 
 
 
 
 
 
 
Desale et al. International Journal of Drug Delivery 4 (1) 82-88 [2012] 
 
PAGE | 86 |
 
 
Table No. 2. Results of Tablet Blend 
 
Formulations Angle of 
Repose 
Bulk Density 
(gms/cm3) 
Tapped Density 
(gms/cm3) 
CarrÊs Index 
(%) 
HausnerÊs Ratio
F1 38.04 μ0.21 0.766 μ0.03 0.894 μ0.04 14.31 1.16 
F2 35.53 μ0.39 0.777 μ0.01 0.905 μ0.03 14.21 1.16 
F3 36.02 μ0.33 0.719 μ0.04 0.888 μ0.02 19.05 1.23 
F4 33.69 μ0.24 0.733 μ0.02 0.855 μ0.01 14.33 1.16 
F5 36.86 μ0.29 0.695 μ0.05 0.850 μ0.03 18.23 1.22 
F6 34.82 μ0.47 0.714 μ0.02 0.882 μ0.05 18.98 1.23 
F7 32.47 μ0.18 0.690 μ0.01 0.844 μ0.04 18.29 1.22 
F8 34.28 μ0.25 0.755 μ0.02 0.888 μ0.02 15.00 1.17 
F9 31.75 μ0.19 0.733 μ0.04 0.855 μ0.01 14.26 1.16 
 
Table No 3. Results of Characterization of Formulations F1-F3 
 
Evaluation Parameter F1 F2 F3 
Weight Variation (mg) 149.33±0.37 149.10±0.17 150.11±0.09 
Thickness (mm) 2.21±0.4 2.23±0.06 2.20±0.15 
Hardness (kg/cm2) 4.2±0.2 3.9±0.3 3.4±0.4 
% Friability 0.52±0.01 0.69±0.03 0.49±0.02 
Content Uniformity (%) 99.21±0.5 99.0±0.2 99.14±0.3 
Wetting time (sec.) 42.67±0.35 33.57±0.77 26.30±0.63 
Disintegration time (sec.) 46.33±0.57 37.53±1.04 29.00±1.15 
                                   Mean ± SD, n=3    
                    
Table No 4. Results of Characterization of Formulations F4-F6 
 
 
Evaluation Parameter F4 F5 F6 
Weight Variation (mg) 151.00±0.96 149.93±0.12 148.22±0.96 
Thickness (mm) 2.23±0.05 2.20±0.27 2.22±0.29 
Hardness (kg/cm2) 3.8±0.5 3.5±0.4 3.4±0.2 
% Friability 0.56±0.04 0.77±0.05 0.590±0.02 
Content Uniformity (%) 99.13±0.4 99.42±0.4 99.01±0.3 
Wetting time (sec.) 42.27±1.23 29.31±1.64 24.14±0.77 
Disintegration time (sec.) 46.67±0.48 32.28±1.08 28.00±1.20 
                                   Mean ± SD, n=3 
                              
Table No 5. Results of Characterization of Formulations F7-F9 
 
Evaluation Parameter F7 F8 F9 
Weight Variation (mg) 151.11±0.22 150.20±0.04 151.12±0.09 
Thickness (mm) 2.21±0.54 2.24±0.33 2.22±0.28 
Hardness (kg/cm2) 4.1±0.3 3.9±0.5 3.7±0.3 
% Friability 0.66±0.01 0.64±0.04 0.71±0.05 
Content Uniformity (%) 99.21±0.2 99.13±0.4 99.19±0.5 
Wetting time (sec.) 36.40±0.93 33.60±1.22 19.20±0.72 
Disintegration time (sec.) 40.20±0.57 37.58±1.45 23.33±0.55 
                                   Mean ± SD, n=3 
 
 
Desale et al. International Journal of Drug Delivery 4 (1) 82-88 [2012] 
 
PAGE | 87 |
 
 
 
 
 
 
Figure No 1. FTIR Spectra of Fexofenadine HCl 
 
 
Figure No 2. FTIR Spectra of Kyron T-314 
 
Figure No 3. FTIR Spectra of Physical Mixture 
 
 
 
Desale et al. International Journal of Drug Delivery 4 (1) 82-88 [2012] 
 
PAGE | 88 |
 
 
 
Figure No 4. Results of in-vitro Drug Release Profile of F1- F3 
 
 
 
Figure No 5. Results of in-vitro Drug Release Profile of F4- F6 
 
 
 
Figure No 6. Results of in-vitro Drug Release Profile of F7- F9 
 
 
 


Formulation and Characterization of Fexofenadine hydrochloride Fast Dissolving Tablet by using various Superdisintegrants

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Formulation and Characterization of Fexofenadine hydrochloride Fast Dissolving Tablet by using various Superdisintegrants

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