Implementation and comparison of different taste masking techniques to design and assess dispersible tablet formulations
Keywords:Dispersible tablet, taste masking, Factorial design, super-disintegrant
The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values < 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.
Aulton ME. Pharmaceutics : the science of dosage form design. 2nd ed. ed., Churchill Livingstone, Edinburgh, (2002).
Kottke MJ, Rudnic EM. Tablet Dosage Forms. Modern Pharmaceutics Volume 1. 5th ed. (Florence Alexander T , Siepmann Juergen ed.) Vol. 1, Chap. 13, CRC Press, New York, pp.499–516 (2009).
Kumar N, Pahuja S. Dispersible Tablets: An Overview. Journal of Medical Pharmaceutical and Allied Sciences, 8, 2183–99 (2019).
Schiermeier S, Schmidt PC. Fast dispersible ibuprofen tablets. European Journal of Pharmaceutical Sciences, 15, 295–305 (2002).
Dave BS, Amin AF, Patel MM. Gastroretentive drug delivery system of ranitidine hydrochloride: formulation and in vitro evaluation. AAPS PharmSciTech, 5, e34 (2004).
U.S. FDA. “FDA Requests Removal of All Ranitidine Products (Zantac) from the Market.”: <https://www.fda.gov/news-events/press-announcements/fda-requests-removal-all-ranitidine-products-zantac-market>, cited 1 April, 2020.
Kane S. “Ranitidine. Drug Usage Statistics, United States, 2013 – 2020.”: <https://clincalc.com/DrugStats/Drugs/Ranitidine>, cited 20 September, 2022.
Rajan R, Makenna P, Thangavel S. Formulation and Evaluation of Orodispersible Tablets of Taste Masked Nizatidine. International Research Journal of Pharmacy, 3, 204–209 (2012).
Sasikumar R. “Formulation Development and Evaluation of Taste Masked Chewable Tablet of Sildenafil Citrate.”: < http://repository- tnmgrmu.ac.in/4479/1/261510402Sasikumar%20R.pdf>, cited 19 December, 2017.
National Center for Biotechnology Information. “PubChem Compound Summary for CID 444041, beta-CYCLODEXTRIN.”: <https://pubchem.ncbi.nlm.nih.gov/compound/beta-CYCLODEXTRIN.>, cited 20 September, 2022.
Jagdale SC, Gawali VU, Kuchekar BS, Chabukswar AR. Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride. Brazilian Journal of Pharmaceutical Sciences, 47, 907–16 (2011).
ECA Academy. “Causes for Weight Variations during Tableting.”: <https://www.gmp-compliance.org/gmp-news/causes-for-weight-variations-during-tableting>, cited 20 September, 2022.
JRS Pharma. “Vivapur. The High Quality MCC with Reduced Carbon Footprint.”: <https://www.jrspharma.com/pharma_en/products-services/excipients/binders/vivapur.php>, cited 20 September, 2022.
Mehta S, de Beer T, Remon JP, Vervaet C. Effect of disintegrants on the properties of multiparticulate tablets comprising starch pellets and excipient granules. Int J Pharm, 422, 310–7 (2012).
Reza MMA. Comparative Evaluation of Wet Granulation and Direct Compression Methods for Preparation of Compressed Tablets Using Avicel PH 101. Bangladesh Pharmaceutical Journal, 12, 19–22 (2002).
Patra ChN, Pandit HK, Singh SP, Devi MV. Applicability and Comparative Evaluation of Wet Granulation and Direct Compression Technology to Rauwolfia serpentina Root Powder: A Technical Note. AAPS PharmSciTech, 9, 100–4 (2008).
Zhao N, Augsburger LL. The Influence of Granulation on Super Disintegrant Performance. Pharm Dev Technol, 11, 47–53 (2006).
Rowe RC, Shesky PJ, Quinn ME. Handbook of Pharmaceutical Excipients. 6th ed., Pharmaceutical Press, London, (2009).
Rojas J, Guisao S, Ruge V. Functional Assessment of Four Types of Disintegrants and their Effect on the Spironolactone Release Properties. AAPS PharmSciTech, 13, 1054–62 (2012).
United States Pharmacopeia and National Formulary (USP39-NF34). 39th ed., The United States Pharmacopeial Convention, Rockville, (2016).
Reckitt Benckiser. “Dissolution and solubility”: <https://edu.rsc.org/download?ac=12809>, cited 21 September, 2022.
Priya VAV, Rao GCS, Reddy DS, Reddy VP. The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets. International Journal of Pharmaceutical Sciences and Nanotechnology, 2, (2009)
Setty CM, Prasad DVK, Gupta VRM, Sa B. Development of fast dispersible aceclofenac tablets: effect of functionality of superdisintegrants. Indian J Pharm Sci, 70, 180–5 (2008).
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