Abstract
Minitablets in orodispersible form constitute a flexible drug delivery tool for paediatric and geriatric population as they eliminate the risk of chocking and do not require drinking water in the application. Due to their direct contact with taste buds, taste sensation is an important factor. Preparing microparticles with taste masking polymers utilizing spray drying is an efficient technique for reducing the bitterness of drugs. Ethylcellulose is a hydrophobic polymer widely used as a taste masking material. Rupatadine fumarate, one of the newest antihistamines, features an intensive bitter taste, hence in designing orodispersible formulations, achieving an acceptable taste is a crucial issue. The main objective of this work was to formulate orodispersible minitablets containing taste masked ethylcellulose-based microparticles with rupatadine fumarate and evaluation of their quality, especially in terms of taste masking efficacy. The accessed data indicated that all obtained minitablets were characterized by beneficial pharmaceutical properties. Three independent methods: in vivo with healthy volunteers, in vitro drug dissolution, and “electronic tongue” confirmed that all designed formulations provided satisfactory taste masking rate and that formulation F15 (prepared with Pearlitol® Flash and Surelease® microparticles with rupatadine fumarate) was characterized by the lowest bitterness score.
Highlights
The challenge of modern pharmaceutical technology is designing easy-to-administer drug dosage forms where the dose is sufficiently flexible to enable proper application and dose titration both to paediatric and adult patients
orodispersible minitablets (ODMT) are recommended for patients with swallowing problems, by eliminating the risk of choking to a minimal [5,6,7,8,9,10,11]
Efficient barrier for masking the bitterness of drug enclosed in microparticles was obtained utilizing rupatadine fumarate (RUP):polymer ratio (0.5:1) with 6% EC concentration and this formulation was used for designing ODMT
Summary
The challenge of modern pharmaceutical technology is designing easy-to-administer drug dosage forms where the dose is sufficiently flexible to enable proper application and dose titration both to paediatric and adult patients. The solid drug dosage form, which connects the advantages of liquids (flexibility of dosing, ease of swallowing) with the qualities of solids (taste masking, stability), as well as enables individual dose adjustments for patients of all ages are minitablets (MT). The microparticles prepared with an aqueous dispersion of EC were found to have better properties in terms of taste masking effectiveness and morphology [17], they were used to formulate ODMT. The crucial test—assessment of taste masking effect was carried out according to three alternative approaches: in vivo, by the drug dissolution and with electronic tongue utilization
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
