Taste-masking assessment of orally disintegrating tablets and lyophilisates with cetirizine dihydrochloride microparticles

Abstract

Orally disintegrating tablets and oral lyophilisates are novel attractive dosage forms that disintegrate or dissolve in the buccal cavity within seconds without necessity of drinking. The major limitation in designing of these dosage forms is unpleasant taste of the drug substance. Cetirizine dihydrochloride is a H-antihistamine substance indicated for the treatment of allergy. It is characterized by extremely bitter taste, therefore in order to deliver cetirizine dihydrochloride using orodispersible formulations, effective taste-masking is required. The aim of this study was to investigate whether microparticles containing cetirizine dihydrochloride could be successfully used to formulate orally disintegrating tablets by direct compression method and oral lyophilisates by freeze-drying process. Taste masking of cetirizine dihydrochloride was achieved by the spray-drying technique using Eudragit E PO as the drug agent carrier. Based on the preliminary studies, optimal compositions of microparticles, tablets and lyophilisates were chosen. Obtained dosage forms were characterized for drug content, disintegration time and mechanical properties. In order to determine whether the microparticles subjected to direct compression and freeze-drying process effectively mask the bitter taste of cetirizine dihydrochloride, the and evaluation was performed. The results showed that designed formulates with microparticles containing cetirizine dihydrochloride were characterized by appropriate mechanical properties, uniformity of weight and thickness, short disintegration time, and the uniform content of the drug substance. Taste-masking assessment performed by three independent methods (e-tongue evaluation, human test panel and the drug release) revealed that microparticles with Eudragit E PO are effective taste - masking carriers of cetirizine dihydrochloride and might be used to formulate orally disintegrating tablets and oral lyophilisates.

Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate

“…The following scale was used to evaluate the taste: 0—not bitter, 1—slightly bitter, 2—moderately bitter, 3—very bitter. Prior to the test, the volunteers were selected by sensory sensitivity test, using basic flavors: sour—tartaric acid, sweet—sucrose, salty—sodium chloride, bitter—quinine hydrochloride [30].…”

Critical Evaluation of Laboratory Potentiometric Electronic Tongues for Pharmaceutical Analysis—An Overview

“…The difficulty of this test lies in the subjectivity of human taste sensation, because it depends on nationality, sex, eating habits, etc. Nevertheless, such a test is still the most reliable method for the assessment of taste-masking efficiency; therefore, some authors correlated the results obtained using electronic tongue systems with in vivo analysis [47,58].…”

“…Recently, a commercial taste sensing system (TS-5000Z) was used to differentiate novel oral dosage forms (i.e., orally disintegrating tablets (ODTs)) containing diclofenac [45] and lyophilisates containing cetirizine hydrochloride [46]. A laboratory prototype of an electronic tongue was able to distinguish microparticles, lyophilisates, and ODTs containing dihydrochloride cetirizine [47]. Taste-masked ODTs and self-emulsifying drug delivery systems (SEDDS) with cyclosporine were evaluated using the αAstree electronic tongue.…”

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

“…Pharmaceutical excipients have a significant influence on tablet properties. Thus, selection of excipients and their amount is a critical need, and depends on the drug properties, target dosage form, and manufacturing process [ 26 ]. Mannitol is a preferred excipient for developing ODT of the moisture-sensitive drugs like metformin owing to its non-hygroscopic nature, compactibility, sweet taste, and cool feeling that it leaves in the mouth [ 27 ].…”