Utilization of Ethylcellulose Microparticles with Rupatadine Fumarate in Designing Orodispersible Minitablets with Taste Masking Effect

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.

Download the full article here  or continue reading here: Wasilewska, K.; Ciosek-Skibińska, P.; Lenik, J.; Srčič, S.; Basa, A.; Winnicka, K. Utilization of Ethylcellulose Microparticles with Rupatadine Fumarate in Designing Orodispersible Minitablets with Taste Masking Effect. Materials 2020, 13, 2715. https://doi.org/10.3390/ma13122715

Materials
Aquacoat® ECD was donated from FMC BioPolymer, Newark, NJ, USA. Surelease® E-7-19040 was given from Colorcon Inc., Harleysville, PA, USA. Parteck® ODT was received from Merck KGaA, Darmstadt, Germany. SmartEx® QD-50 was handed over from Shin-Etsu Chemical Co., Ltd., Tokyo, Japan. F-Melt C was purchased from Fuji Chemical Industry Co., Ltd., Toyama, Japan. Pearlitol® Flash was a gift from Roquette, Lestrem, France. Magnesium stearate and methylene blue were acquired from POCh, Piekary Śląskie, Poland. RUP was procured from Xi’An Kerui Biotechnology Co., Ltd., Xi’An, China.