FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

NAGADANI SWARNALATHA; VIDYAVATHI MARAVAJHALA

doi:10.22159/ijap.2021v13i5.41558

Authors

NAGADANI SWARNALATHA Department of Pharmaceutics, Sri Venkateshwara College of Pharmacy, Hyderabad 500014, India
VIDYAVATHI MARAVAJHALA Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam, Tirupathi 517502, India

DOI:

https://doi.org/10.22159/ijap.2021v13i5.41558

Keywords:

Gum karaya, ODT, t90%, Q10, AUC, tmax

Abstract

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride.

Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t _90%), and % drug dissolved in 10 min (Q10) as significant parameters.

Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (t_max), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t_1/2)and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation.

Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased t_max to which stability studies were conducted which were found to be stable.

Downloads

Download data is not yet available.

References

Sreenivas SA, Dandagi PM, Gadad AP. Orodispersible tablets: new-fangled drug delivery system-a review. Ind J Pharm Educ Res 2005;39:177–80.

Setty CM, Prasad DV, Gupta VRM. Development of fast dispersible Acelofenac tablets: effect of the functionality of superdisintegrants. Ind J Pharm Sci 2008;70:180–5.

Raghaendra RNG, Ketan T, Sumanji B. Formulation and evaluation of fast dissolving tablet of metoprolol tartrate. Int J Pharm Clin Res 2010;2:40–5.

Shweta SG, Tapar KK, Borse MD, Ghuge RA. Taste masking and characterization of diphenhydramine hydrochloride by spray-drying technique. Int J Pharm Res Dev 2010;1:1-7.

Karthikeyan M, Mukhthar UAK, Megha M, Shadeer HP. Formulation of diclofenac tablets for rapid pain relief. Asia Pacific J Trop Dis 2012;2:308–11.

Kawano Y, Ito A, Sasatsu M, Machida Y, Onishi H. Preparation and evaluation of taste-masked orally disintegrating tablets with granules made by the wet granulation method. Yakugaku Zasshi 2010;130:1737-42.

Liew KB, Tan YTF, Peh KK. Characterization of oral disintegrating film containing Donepezil for Alzheimer's disease. AAPS PharmSciTech 2012;13:134-42.

Auda SH, Elbadry M, Ibrahim MA. Design, formulation, and characterization of fast dissolving films containing dextromethorphan. Dig J Nanomater Bios 2014;9:133-41.

Naresh Kumar K, Sandeep D. Formulating taste-masked orally disintegrating tablets of a bitter drug Ibuprofen. Int Res J Pharm 2013;4:71-8.

Preethi GB, Sayan B, Shivakumar NH, Ravi Kumar M. Formulation of fast-dissolving tablets of doxazosin mesylate drug by direct compression method. Int J Appl Pharm 2017;9:22-8.

United States Pharmacopeia Convention. United States Pharmacopeia and National Formulary (USP 34-NF29) United States Pharmacopeia Convention; 2011.

Shah D, Shah Y, Rampradhan M. Development and evaluation of controlled release diltiazem hydrochloride microparticles using cross-linked polyvinyl alcohol. Drug Dev Ind Pharm 1997;23:567-74.

Kothiya OM, Patel BA, Patel KN, Patel MM. Formulation and characterization of sustained release matrix tablets of ivabradine using 32 full factorial designs. Int J Appl Pharm 2018;10:59-66.

Adedokun M, Onah BE, Attama AN. Physico-mechanical and release properties of sustained-release artesunate tablets in hydroxypropyl methylcellulose matrix. Int J Appl Pharm 2018;10:103-8.

Agarwal G, Agarwal S, Karar PK, Goyal S. Oral sustained-release tablets: an overview with a special emphasis on matrix tablet. Am J Adv Drug Delivery 2017;5:64-76.

Arora P, Arora V. Orodispersible tablets: a comprehensive review. Int J Pharm Sci Res 2013;2:270-84.

Nawale RB, Mohite KP. Formulation and evaluation of domperidone orodispersible tablet. Int J Pharm Sci Res 2013;4:3670-7.

Dash TR, Verma P. Matrix tablets: an approach towards oral extended-release drug delivery. Int J Pharm Sci Rev Res 2013;2:12-24.

Furtado S, Deveswaran R, Bharath S, Basavaraj BV, Abraham S, Madhavan V. Development and characterization of orodispersible tablets of famotidine containing a subliming agent. Trop J Pharm Res 2009;8:153-9.

Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol 1975;27:48-9.

Radke RS, Jadhav JK, Chajeed MR. Formulation and evaluation of orodispersible tablets of baclofen. Int J Chem Eng 2009;1:517-21.

Hardy JG, Healey JN, Reynolds JR. Evaluation of an enteric-coated delayed-release 5-aminosalicylic acid tablet in a patient with inflammatory bowel disease. Aliment Pharmacol Ther 1987;1:273-80.

Paterakis PG, Korakianiti ES, Dallas PP, Rekkas DM. Evaluation and simultaneous optimization of some pellets characteristics using a 33 factorial design and the desirability function. Int J Pharm 2002;248:51-60.

Ferreira SL, Bruns RE, da Silva EG. Statistical designs and response surface techniques for the optimization of chromatographic systems. J Chromatogr A 2007;1158:2-14.

Swain S, Behera A, Dinda SC, Patra CN, Sruti J, Beg SA, et al. Formulation design, optimization, and pharmacodynamic evaluation of sustained-release mucoadhesive microcapsules of venlafaxine hydrochloride. Indian J Pharm Sci 2014;76:354-63.

Ghosh MN. Fundamentals of experimental pharmacology. 3rd edn. Sk Ghosh Publications, Kolkata; 2005. p. 192-4.

Kauss T, Gaudin K, Gaubert A. Screening pediatric rectal forms of Azithromycin as an alternative to oral or injectable treatment. Int J Pharm 2012;436:624-30.

Zeng F, Wang L, Zhang W, Shi K, Zong L. Formulation and in vivo evaluation of orally disintegrating tablets of Clozapine/Hydroxypropyl-β-cyclodextrin inclusion complexes. AAPS Pharm SciTech 2013;14:854-60.

Xu H, He L, Nie S, Guan J, Zhang X, Yang X, Pan W. Optimized preparation of Vinpocetine proliposomes by a novel method and in vivo evaluation of its pharmacokinetics in New Zealand rabbits. J Controlled Release 2009;140:61-8.

Haoping X, Min S, Ying liu Y, Jiang J, Tao Ma. A novel in situ gel formulation of ranitidine for oral sustained delivery. Biomol Ther 2014;22:161-5.

Matter KM. Impact of pregnancy on Zonisamide pharmacokinetics in rabbits. Biomed Res Int 2013;14:327-30.

European Council. European Pharmacopoeia. 4th ed. Strasbourg; 2002.

Bolton S, Bon C. Rev and expanded. 4th ed. Marcel Dekker Inc. New York: Pharmaceutical statistics and practical and clinical application; 2004. p. 96–146.

Singh B, Kumar R, Ahuja N. Optimizing drug delivery systems using systematic Design of experiments. Part-I: fundamental aspects. Crit Rev Ther Drug 2005;22:27–105.

Borawake Payal D, Kauslya A, Jitendra V. Formulation of solid dispersions for enhancement of solubility and dissolution rate of simvastatin. Int J Pharm Pharm Sci 2012;13:94-100.

Nirmala D, Vidyavathi M. Preparation and evaluation of fast dissolving tablets of pitavastatin by 32 full factorial design. Int J Appl Pharm 2020;12:108-14.

Chen H, Aburub A, Sun CC. Direct compression tablet containing 99% active ingredient-a tale of spherical crystallization. J Pharm Sci 2019;108:1396-400.

Cantor SL, Augsburger LL, Hoag SW, Gerhardt A. Pharmaceutical granulation processes, mechanism and the use of binders. In: Augsburger LL, Hoag SW. editors. Pharmaceutical dosage forms: tablets. 3rd ed. London: CRC Press; 2008. p. 261-302.

Gugulothu D, Suraj Kumar C. Design and in vitro evaluation of floating drug delivery system of glipizide using a combination of natural mucilages and synthetic polymers. Int J Pharm Pharm Sci 2021;13:40-8.