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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

1
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland
2
Departament of Microbioanalytics, Warsaw University of Technology, Koszykowa 75, 00-662 Warsaw, Poland
3
Department of Analytical Chemistry and Instrumental Analysis, Faculty of Chemistry, Maria Curie-Skłodowska University, M. Curie-Skłodowska Sq. 3, 20-031 Lublin, Poland
4
Institute of Chemistry, University of Białystok, Ciołkowskiego 1K, 15-245 Białystok, Poland
5
Department of Biopharmaceutics and Pharmacodynamics, Medical University of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland
*
Author to whom correspondence should be addressed.
Polymers 2019, 11(3), 522; https://doi.org/10.3390/polym11030522
Received: 4 February 2019 / Revised: 6 March 2019 / Accepted: 17 March 2019 / Published: 20 March 2019
(This article belongs to the Special Issue Pharmaceutical Polymers)
The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, utilizing polymers with different physicochemical properties. Rupatadine fumarate (RUP) is one of the newest antihistamines, with an innovative and multidirectional mechanism of action, and an extremely bitter taste. The aim of this work was to investigate the feasibility of utilizing organic or aqueous forms of ethylcellulose (EC) for the preparation of microparticles with RUP by the spray drying technique. Spray dried samples at different drug:polymer ratios were prepared using organic solution (Ethocel®) or aqueous dispersions of EC (Surelease®, Aquacoat® ECD). Evaluation of the taste masking efficacy was performed in vivo in human taste panel, in vitro based on dissolution test, and by self-constructed electronic tongue. It was shown that microparticles obtained from aqueous dispersions of EC have superior pharmaceutical properties in terms of both morphology and taste masking efficacy in comparison to those obtained from organic solution. View Full-Text
Keywords: ethylcellulose; taste masking polymer; cellulose derivative; spray drying; microparticles; rupatadine fumarate ethylcellulose; taste masking polymer; cellulose derivative; spray drying; microparticles; rupatadine fumarate
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MDPI and ACS Style

Wasilewska, K.; Szekalska, M.; Ciosek-Skibinska, P.; Lenik, J.; Basa, A.; Jacyna, J.; Markuszewski, M.; Winnicka, K. 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. Polymers 2019, 11, 522.

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