Academic literature on the topic 'Taste-masking agents'

Bitter taste is aversive to humans, and many oral medications exhibit a bitter taste. Bitter taste can be suppressed by the use of inhibitors or by masking agents such as sucralose. Another approach is to encapsulate bitter tasting compounds in order to delay their release. This delayed release can permit the prior release of bitter masking agents. Suppression of bitter taste was accomplished by encapsulating a bitter taste stimulus in erodible stearic acid microspheres, and embedding these 5 µmeter diameter microspheres in pullulan films that contain sucralose and peppermint oil as masking agents, along with an encapsulated masking agent (sucralose). Psychophysical tests demonstrated that films which encapsulated both quinine and sucralose produced a significant and continuous sweet percept when compared to films without sucralose microspheres. Films with both quinine and sucralose microspheres also produced positive hedonic scores that did not differ from control films that contained only sucralose microspheres or only empty (blank) microspheres. The encapsulation of bitter taste stimuli in lipid microspheres, and embedding these microspheres in rapidly dissolving edible taste films that contain masking agents in both the film base and in microspheres, is a promising approach for diminishing the bitter taste of drugs and related compounds.

Taste masking is of critical importance for active ingredients with an undesirable taste, due to the need for increased patient compliance, especially in pediatric and geriatric population. Various techniques for taste masking involve addition of flavours, sweeteners and amino acids, use of effervescent agents, prodrug formation, salt preparation, adsorption, formation of complex with ion- exchange resins, inclusion complexes and molecular complexes, microencapsulation, granulation, viscosity modifiers, multiple emulsion, liposomes and solid dispersion systems. In pharmaceutical industry, taste masking involves the development of a system that prevents the active substance from interacting with taste buds, thereby reducing the negative sensory response. This article reviews the different technologies which are used for masking the bitter taste and methods for evaluation of taste masking efficacy.

Chewing gum, being a pleasant formulation, requires effective taste-masking techniques, such as encapsulation methods along with an amalgamation of flavors and sweeteners. Taste-masked medicated chewing gum offers a palatable way of administering drugs and dietary supplements to children and old-aged people. The concept of chewing gum development provides a sustained and modified release of actives through various techniques, such as microencapsulation, cyclodextrin-complexation, buffering agents, ion exchange resin, solid dispersions, effervescent agents, etc. The taste, solubility, and stability of the active ingredient are the key parameters to be kept in mind, while formulating a medicated chewing gum. Flavor microencapsulation has been used as a crucial technology in the research and food industry to control sensory performance as demonstrated by the hefty number of chewing gum patents over the years. This manuscript provides an insight into conventional and novel taste-masking techniques employed in developing palatable chewing gums. Additionally, concepts of flavor microencapsulation, its applications, polymers, and patents have been discussed.

Taste-masking techniques are applied to mask or overcome the bitter or unpleasant taste of active pharmaceutical ingredients/drugs to achieve patient acceptability and compliance. Oral administration of bitter or unpleasant tasting drugs is often the biggest barrier for patient groups, such as pediatrics and geriatrics [1, 2]. Unless the active ingredient is tasteless or does not have any unpleasant taste, taste-masking plays a key role in the success of a final solid oral dosage form. The efficiency of taste-masking is often a key determinant for the success of specialized dosage forms like orally disintegrating tablets and films, and chewable tablets [2]. The mechanisms of taste-masking techniques often rely on two major approaches: the first is to add sweeteners, flavors, and effervescent agents to mask the unpleasant taste, and the second is to avoid the contact of bitter/unpleasant drugs with taste buds. In the past few years, significant progress has been made in the area of taste-masking by applying novel strategies and techniques, such as hot-melt extrusion and microencapsulation.[1,3] The following presents an overview and current status of the industrial approaches and platforms used for taste-masking in oral dosage forms. [1, 2, 4] Many pharmaceutical companies are switching their products from tablets to fast dissolving oral thin films (OTFs).[6,7] Films have all the advantages of tablets (precise dosage, easy administration) and those of liquid dosage forms (easy swallowing, rapid bioavailability). Statistics have shown that four out of five patients prefer orally disintegrating dosage forms over conventional solid oral dosages forms. Pediatric, geriatric, bedridden, emetic patients and those with Central Nervous System disorders, have difficulty in swallowing or chewing solid dosage forms.[7,8] Many of these patients are non-compliant in administering solid dosage forms due to fear of choking.[9] OTFs when placed on the tip or the floor of the tongue are instantly wet by saliva. This technology provides a good platform for patent non- infringing product development and for increasing the patent life-cycle of the existing products. [10, 11]

Objective: To formulate orally disintegrating taste masked tablets of drotaverine hydrochloride (HCl) by sublimation technique.Methods: Initially superdisintegrant was selected and its concentration was optimized by pre-compression and post-compression parametric evaluation. Camphor and menthol were used as sublimating agents alone and in combination to mask the taste of drotaverine hydrochloride. Prepared tablets were evaluated for physicochemical evaluation, in vitro dissolution studies and fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies.Results: The optimised formulation DCM2 prepared with a mixture of camphor and menthol was characterised by fourier transformation-infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry studies and found no incompatibility and no major shifts were noticed.Conclusion: The results demonstrated that the prepared drotaverine HCl orally disintegrating tablets showed better taste masking. The present sublimation technique can be effectively used for taste masking and also for orally disintegrating tablets.

Oilseed rape meal is high in protein and available in the UK relatively cheaply. Toxic constituents limit its inclusion in feeds for pigs and poultry but this is not a problem with ruminant animals where microbial action in the rumen removes them. However, the bitter taste of rape meal has been thought to reduce its palatability for ruminant animals (Stedman and Hill, 1987) and it is recommended that its inclusion in compound feeds for cows should not exceed about 150kg/tonne; masking agents are incorporated to reduce this limitation.The question to be addressed can be summarized as “can higher rates of inclusion of rape meal in dairy compound feeds be concealed by more mask?”. Twelve dry cows in late pregnancy were offered feeds with various levels of rape meal in combination with several levels of mask and rate of consumption was monitored.

ABSTRACT Many functional food ingredients activate human bitter taste receptors (hTAS2Rs). In this study, A novel inhibitor, Trp-Trp, for hTAS2R14 was identified by searching for the agonist peptide's analogs. Trp-Trp also inhibited hTAS2R16, hTAS2R43, and hTAS2R46, which share the same agonists with hTAS2R14. The multifunctional characteristic of Trp-Trp is advantageous for use as bitterness-masking agents in functional foods.

The anti-protozoal drug, metronidazole, is developed as an oral disintegrating tablet (ODT) to treat amoebiasis and to bypass hepatic metabolism. The work aimed to prepare, taste-masking oral disintegrating tablets of metronidazole using different proportions of the drug and disintegrants in various ratios by an effervescent method. The ODT was developed by direct compression with various concentrations of super disintegrating agents (1-7%). In this technique, sodium bicarbonate and tartaric acid were used to generate effervescence. The formulated tablets were assessed for physicochemical characteristics. The results of FTIR spectroscopy indicated the stable character of metronidazole. In vitro studies revealed that batch F6 was having a 97.65% cumulative amount of drug release at 20th minute compared to other formulations. Due to the effervescent method, there was a significant increase in drug release, seen at the 1:1.5 ratio. Taste evaluation studies were conducted on healthy human volunteers.

The present review describes the various roles of cyclodextrins (CDs) in vaccines against viruses and in antiviral therapeutics. The first section describes the most commonly studied application of cyclodextrins—solubilisation and stabilisation of antiviral drugs; some examples also refer to their beneficial taste-masking activity. The second part of the review describes the role of cyclodextrins in antiviral vaccine development and stabilisation, where they are employed as adjuvants and cryopreserving agents. In addition, cyclodextrin-based polymers as delivery systems for mRNA are currently under development. Lastly, the use of cyclodextrins as pharmaceutical active ingredients for the treatment of viral infections is explored. This new field of application is still taking its first steps. Nevertheless, promising results from the use of cyclodextrins as agents to treat other pathologies are encouraging. We present potential applications of the results reported in the literature and highlight the products that are already available on the market.

Sumatriptan succinate (SS) is a drug used in the treatment of migraine headaches, but suffers from low patient compliance due to its unpalatable bitter taste. The purpose of the present work was to prepare taste-masked oro dispersible tablets (ODTs) of SS by incorporating drug loaded microspheres into tablets for use in patients experiencing difficulty in swallowing. Microspheres loaded with SS were prepared by solvent evaporation technique. Eudragit EPO, a pH-sensitive aminoalkylmethacrylate copolymer, was used for coating the drug particles, acetone as solvent for the polymer and light liquid paraffin as an encapsulating medium. Drug : polymer ratio of 1:1 was considered to be optimized formulation with a yield of 99.96%, entrapment efficiency of 61.55%, particle size ranging from 30.32 – 90.96μm and in vitro drug release of 85.06% within an hour. FTIR studies suggested absence of drug-excipient interaction. Tablets prepared by direct compression containing microspheres and effervescent agents were evaluated for pre-compression and post-compression parameters. The wetting time, in vitro dispersion time and in vitro disintegration time of the tablets were found to be 39 sec, 35 sec and 32 sec, respectively. The drug release from the tablet was about 85.44% within an hour. The SEM of final ODTs revealed that the microspheres remained intact even after compression. Stability studies indicated that the selected formulation was stable. The results obtained suggested that effective taste-masking was achieved for SS using the technique of microencapsulation and ODTs of acceptable characteristics were obtained by adding effervescent agents followed by direct compression.

L'avvento di numerose tecnologie per produzione di film orodispersibili (ODF) ha suscitato un crescente interesse verso l'impiego di questa forma di dosaggio nell’ambito della personalizzazione della terapia. Difatti, la possibilità di ottenere ODF di diverse forme, colori e dimensioni permette a pazienti di identificare facilmente il medicinale, aumentando così la sicurezza e dell’aderenza al trattamento farmacologico (Capitolo 1). Tale avanzamento tecnologico deve tuttavia procedere parallelamente allo sviluppo di saggi non distruttivi e di facile esecuzione in farmacia per la determinazione e il controllo della qualità chimica e fisica degli ODF, come requisito imprescindibile alla sicurezza e all’efficacia (Capitolo 2). Scopo della presente tesi di dottorato è quello di dimostrate la possibilità di produrre film orodispersibili su piccola scala mediante l’uso di una una nuova tecnologia di stampa costituita da una siringa termostatata in grado di estrudere a velocità costante la massa fusa di principio attivo ed eccipienti su un piatto mobile. La composizione della miscela comprende una maltodestrina plasticizzata con glicerica in quanto questi eccipienti sono idenei per la produzione di ODF sia per i pazienti pediatrici, sia per gli anziani. Il metodo di preparazione prevede dei semplici passaggi: la miscelazione del principio attivo con il polimero, plasticizzzante ed eventuali altri eccipienti; il caricamento dell’impasto nella siringa e il preriscaldamento dell’impasto fino a completo rammollimento; la conseguente forzatura attraverso l’ago per depositare il film orodispersibile con una forma definita su un foglio di alluminio che costituisce il confezionamento primario. La versatilità di questo approccio è stata verificata preparando ODF contenenti principi attivi con diverse caratteristiche chimico-fisiche. Tra le varie molecule modello, il paracetamolo è stato scelto per dimostrare la fattibilità di caricare una quantità di attivo (74 mg/ 6 cm2) più elevate rispetto mercato dosaggi di ODF presenti sul mercato (100 mg/9cm2) (Capitolo 3). Nel caso dei film caricati con diclofenac sodico, utilizzato come esempio di sostanza termosensibile, non si è evidenziata la formazione di prodotti di degradazione dovute alle temperature utilizzate per rammollire la miscela (Capitolo 4). Per migliorare la managgevolezza e le proprietà organolettiche dei film, spesso sono aggiunti altri eccipienti quali edulcoranti, aromi e agenti che ne limitano l’appicicosità. In questo ambito, il diossido di titanio, selezionato come opacizzante, non solo ha permesso di migliorare le caratteristiche estetiche dei film, ma ha anche la rimozione del film dal materiale del confezionamento primario, aspetto che risulta particolarmente importante per evitarne la rottura durante la manipolazione da parte del paziente (Capitolo 4). Infine, è stata caricata nei film una quantità pari a 10 mg olanzapine, come modello di sostanza soggetta a polimorfismo. In questo caso il confronto con processi di produzione che richiedono l’utilizzo di una sospensione su base acquosa, ha permesso di evidenziare che la tecnologia proposta elimina la possibilità di conversione dalla forma I alla forma pseudopolimorfica che è caratterizzata da una minore solubilità che potrebbe influire negarivamente sulla biodisponibilità di questa molecola (Capitolo 5). In conclusione, la tecnologia basata su una modifica dell’estrusione a caldo potrebbe essere utilizzata per stampare film costituiti da maltodestrine e glicerina, limitando gli inconvenienti legati all’uso di solventi e altre temperature. Questa formulazione può essere sfruttata per ottenere film contenenti principi attivi con caratteristiche chimico-fisiche diverse, e altri eccipienti richiesti per migliorare le caratteristiche organolettiche di questa forma farmaceutica finita.
The advent of printing technologies for the production of orodispersible films (ODF) guides a growing interest in the application of these dosage forms to precision dosing in personalized medicine. Indeed, the tailoring of ODF shape, colour and/or dimension allows end-users to easily identify their own medicinal product, improving both safety and adherence (Chapter 1). At the same time, to open real perspectives towards ODF for personalized dosing, the design of such technologies should advance along with the development of easy and non-destructive assays, based on colorimetry and spectroscopy, which can allow to establish the physical and chemical quality of ODF (Chapter 2). This doctoral thesis aimed to demonstrates the feasibility of a novel printing technology to extemporaneously compound ODF on-demand. The basic idea was to propose a novel apparatus that combines a hot-melt ram extruder with the plate of a 3D-printer. As far as the formulation is concerned, maltodextrins plasticized with glycerol were selected since they are excipients accepted for both children and elderly. The preparation method consists of simple operations, involving the mixing of the drug substance with maltodextrins and other excipients, then the loading of the mixture into the ram extruder, heating, and printing of the single ODF directly on the packaging aluminium foil. The versatility of this technology was tested by loading ODF with drugs having different physicochemical characteristics. First, paracetamol was selected as a model to demonstrate the drug payload which resulted in loading up to 74 mg/ 6 cm2 and, therefore, allowing the preparation of ODF with a drug amount higher than the highest in the market (i.e., 100 mg/ 9cm2) (Chapter 3). Then, diclofenac sodium was loaded as a model of heat-sensitive and bitter drug to prepare ODF intended for the treatment of migraine in paediatric population. The data revealed that, the exposure to relatively low temperature (i.e., approximately 90 °C) during the printing limited the formation of degradation by-products of the drug (< 0.2%). Furthermore, to improve ODF palatability and patients’ handing, a combination of taste-masking agents (TMA), opacifiers, and, when required, an anti-sticking agent are often loaded into ODF. Thus, the effect of these excipients on the physical properties of ODF loaded by diclofenac was also studied. The results revealed that titanium dioxide, selected as an opacifier, improved not only the ODF aesthetic appearance, but also ODF detachment from the primary packaging material, an aspect particularly relevant to prevent breakage during handing (Chapter 4). Olanzapine (OLZ) was finally tested because it can undergo solid-state modifications under different processing conditions. In this case, the comparison on the performance of OLZ ODF prepared by the proposed technology and consolidated solvent casting technique, which requires the use of a large amount of water, revealed that hot-melt ram extrusion prevented the conversion of OLZ from anhydrous Form I to a pseudo-polymorphic form with lower solubility, which could affect the drug bioavailability (Chapter 5). In conclusion, hot-melt ram extrusion printing can be advantageously used to prepare small batches of ODF made of maltodextrins and glycerine, avoiding the use of solvent and harsh temperatures. This basic formula can be exploited to load drugs differing in physicochemical characteristics, and other excipients to provide suitable organoleptic features of the final dosage form.