Optimization of Taste Masked Orodispersible Tablet of Cetirizine Dihydrochloride for Enhanced Palatability

Abstract

Orodispersible tablet is a patient-friendly alternative for delivering the drug to patients having problems with swallowing and sensitive to the bitterness of the drug. This study focuses on taste masking of cetirizine dihydrochloride by applying coating technique. Taste masked orodispersible tablet (ODT) was formulated using superdisintegrants and apply hydrophilic/hydrophopic polymer/lipid coating. Formulations were designed by 22 factorial central composite design, in which stearic acid and compritol 888 ATO were taken as independent variables. The taste masking was evaluated using the small-volume shake flask method, as an alternative to testing with a human panel. The concentration of stearic acid and compritol 888 ATO in the optimized formulation obtained from the Minitab software response optimization was nearly as same as that of formulation F3. Thus, formulation F3 was considered to be formulation of choice. The weight variation, disintegration time, friability, and dissolution were found to be satisfactory. The coating of API with compritol 888 ATO exhibited effective taste-masking properties while maintaining rapid disintegration and acceptable mechanical strength while masking the bitterness of the drug molecule. Taste masking of cetirizine dihydrochloride was successfully achieved using a lipid-based coating approach, with Compritol® 888 ATO and stearic acid as coating materials. Thus, the study successfully developed a taste-masked orodispersible tablet of cetirizine dihydrochloride using a lipid-based coating technique.

Introduction

“A system of formulation or process developed to introduce therapeutic agents into the body is called drug delivery system (DDS) [1]. Developing a new drug is costly and time-consuming, and also need to enhance safety, efficacy, and improve patient compliance. The conventional drug delivery system, such as tablets, capsules, etc., has a variety of drawbacks, such as the bitterness of the drug molecule, lack of target specificity, and severe side effects of the drugs [2]. Most of the drugs are undesirable to patients due to their bitterness. This can be seen in all patient groups, such as pediatric and geriatric populations [3]. Orally disintegrating tablets (ODTs), also called orodispersible tablets, are uncoated tablets designed to dissolve in the mouth within three minutes, making them easy to swallow without water. These tablets are good for children, the elderly, and individuals having difficulty swallowing traditional tablets and have the advantages of improved stability, ease of use, and accurate dosing. The popularity is increasing in the pharmaceutical industry due to their high patient acceptance, especially among those who struggle with conventional dosage forms. [4]. These tablets are designed to dissolve or break apart in the oral cavity without water, improving the administration of active pharmaceutical ingredients [5].

Literatures show that croscarmellose (3.00%) and crospovidone (3.92%), show good result giving disintegration time 40 seconds and a wetting time was of 33 seconds [6]. Orally disintegrating tablets are uncoated tablets intended to be used in the mouth, where they disperse within 3 min before swallowing [7]. Elwani et al has conducted an experimental study to compare different taste masking technique, such as granulation, coating, and complexation, followed by assessment of drug release and patient compliance [8]. A study conducted by Nakano, Y.et al. investigated the impact of different flavors on the taste perception and acceptability of orally disintegrating tablets which concluded that specific flavors influence the taste perception of drug [9]. Kurella et al showed the effectiveness of compritol 888 ATO in taste masking using met granulation technique while meeting required parameters for ODT formulation [10]. Cherian et al has demonstrated effective masking of bitterness of drug molecule by encapsulating the drug in erodible stearic acid which delay their release in the mouth [11].

An effective taste-masking techniques are required to enhance palatability and promote patient compliance. Nowadays, the pharmaceutical industries applied various approaches to address this challenge. These include the use of flavors, sweeteners, and amino acids. Advanced techniques, such as polymer coating, conventional granulation, desalination, salting-out systems, and ion-exchange resins are also applied for taste-masking [12]. Masking the bitter taste of the drug is necessary in ODT formulation; however, taste-masking strategies must not interfere with the drug’s intended bio-performance, ensuring proper in vivo release for effective treatment. To ensure the taste masking, the drug should dissolve as little as possible in the mouth but release quickly when it reaches the gastrointestinal tract [13]. The in vitro drug release using phosphate buffer at pH 6.8 as dissolution media can be used as a surrogate for in-vivo taste evaluation [14,15].

Various coating techniques have been developed to coat APIs, forming a physical and chemical barrier that prevents drug dissolution or diffusion. These coated particles serve as key components in the overall pharmaceutical formulation. The coating must remain intact throughout storage to avoid the perception of bitterness while ensuring that it dissolves or becomes permeable at the appropriate time for the drug to take effect [16]. The coated drug-polymer mixture can be processed into granules. Ethylcellulose was used to form a continuous and effective coating on the core element [17].The physical properties of granules could be improved after coating, which results in masking the unpleasant taste and can be formulated into orodispersible tablet [18]. In this paper, we report that hot melt granulation method was used to develop taste masked orodispersible tablet using stearic acid and compritol 888 ATO as coating agents. The formulations were evaluated for taste masking, disintegration behavior, mechanical properties, and in-vitro drug release to ensure minimal release in the oral cavity with rapid release under gastrointestinal conditions. The optimized formulation showed effective bitterness masking and acceptable tablet performance.

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Excipients mentioned in the study: Compritol 888 ATO, Aerosil 200, Mannitol

Das, G. P.; Pant, L. M.; Bajaj, A.; Shakya, S. Optimization of Taste Masked Orodispersible Tablet of Cetirizine Dihydrochloride for Enhanced Palatability. Preprints 2026, 2026020549. https://doi.org/10.20944/preprints202602.0549.v1

Read also our introduction article on Stearic Acid here: