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

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.

Implementing the Design of Experiments (DoE) Concept into the Development Phase of Orodispersible Minitablets (ODMTs) Containing Melatonin

“…Several examples of development and characterization of minitablets with various release types have been described, e.g., (6)(7)(8)(9)(10)(11)(12)(13)(14)(15). However, to the authors' knowledge, reports of comprehensive approach to minitablets' formulation and process optimization in an industrially relevant setting are lacking in the publicly available literature, especially in the topic of ODMTs.…”

Development and Characterization of Oro-Dispersible Tablets of Metformin Hydrochloride Using Cajanus Cajan Starch as a Natural Superdisintegrant

“…For individuals that have swallowing problems, ODTs are very beneficial [2][3][4]. The disintegrate time of ODTs is within a minute and is suitable for patients with dysphasia [5,6]. ODTs have high bioavailability because as the saliva passes down the stomach, the absorption of some drugs from the mouth, pharynx, and esophagus follows.…”

Orodispersible Membranes from a Modified Coaxial Electrospinning for Fast Dissolution of Diclofenac Sodium

“…Shown in Figure 1 is a diagram about the progress and division of orodispersible dosage during the past several decades. From a standpoint of "forms", orodispersible dosage forms have the form of tablets (such as fast disintegrating tablets [15][16][17][18][19] and fast dissolving mini tablets [20][21][22], strips (such as fast dissolving strip [23,24] and mouth melting strip [25]), fast disintegrating pellets [26] and capsules (often with fast disintegrating particles in them) [27], and many new types of films or membranes [28][29][30][31]. Based on the manufacture methods, orodispersible membranes (OMs) can be further divided into several categories, such as the most common one-solvent casting film [32,33], hot melt extrusion film [34,35], solid dispersion extrusion film [36,37], printed membrane [38][39][40][41], and the present hot topic: electrospun nanofiber membrane [42][43][44].…”