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Purpose: The current study assessed the potential of a pneumatic 3D printer in developing a taste-masked tablet in a single step. Metronidazole (MTZ) was chosen as the model drug, and Eudragit® E PO was used as a taste-masking polymer to produce taste-masked tablets. Methods: The study focused on optimizing processing parameters, such as the nozzle's printing speed, the printhead's heating temperature, and the pressure. Oval-shaped tablets were printed with a rectilinear printing pattern of 30% and 100% infill and evaluated for in vitro drug release and taste masking. The 3D-printed tablets are also characterized using Differential Scanning Calorimetry (DSC), Fourier-transform Infrared Spectroscopy (FTIR), and Scanning Electron Microscopy (SEM). Results: The infill density impacts the drug release profile of the tablets. F9, F10, and F11 displayed desired printability among the formulations, with F9 and F10 exhibiting over 85% drug release within 60 min in the in vitro dissolution study. The F9 formulation, with 30% infill, effectively masked the bitter taste of MTZ in the in vitro dissolution study carried out in a pH 6.8 artificial salivary medium. The observed release was below the tasting threshold concentration of the model drug. Conclusion: In summary, 3-dimensional extrusion-based printing combines the effects of hot-melt extrusion and fused deposition modeling techniques in a single-step process, demonstrating potential as an alternative to the fused-deposition model 3D printing technique and warranting further exploration. [ABSTRACT FROM AUTHOR]

Background: Propranolol, largely prescribed as an antihypertensive and antiarrhythmic drug in pediatrics, is characterized by a bitter taste and an astringent aftertaste. Currently, the therapy requires crushing of tablets for adults and their dispersion in water many times a day, leading to loss of dosing accuracy, low palatability, and poor compliance for both patients and caregivers. Objectives: This work aimed to exploit cyclodextrin complexation by cogrinding to develop orally disintegrating tablets (ODTs) endowed with reliable dosing accuracy, good palatability and safety, ease of swallowability, and ultimately better compliance for both pediatric patients and caregivers. Results: Different formulation variables and process parameters were evaluated in preparing ODTs. The technological and morphological characterization and disintegration tests were performed according to official and alternative tests to select the ODT formulation based on the drug Hydroxypropyl-β-cyclodextrin (HPβCD) coground complex form containing Pearlitol® Flash as the diluent and 8% Explotab® as the superdisintegrant, which demonstrated the highest % drug dissolution in simulated saliva and acceptable in vitro palatability assessed by the electronic tongue, confirming the good taste-masking power of HPβCD towards propranolol. Conclusions: Such a new dosage form of propranolol could represent a valid alternative to the common extemporaneous preparations, overcoming the lack of solid formulations of propranolol intended for pediatric use. [ABSTRACT FROM AUTHOR]

AbstractTaste masking of any pediatric oral formulation has always been a hurdle. Cubosomses, a type of lyotropic liquid crystal, have been used in this research to develop an oral formulation of ibuprofen. Ibuprofen cubosomes were prepared with glyceryl monooleate (GMO) and poloxamer 407 by high-pressure homogenization (HPH) technique. The formulation experiments were performed using a 2-level, 3-factor central composite design with drug loading, GMO concentration and HPH pressure as independent variables and vesicle size, entrapment efficiency and %drug content as the dependent variables. The most suitable ibuprofen cubosomes showed 94 nm vesicle size, −17.5 mV zeta potential, >75% drug content and >96% entrapment efficiency. The cubosomes released more than 80% of the drug within 2 hours. In vitro taste masking study showed significantly lower drug release than its bitterness threshold. An in vivo taste masking study in healthy adult volunteers showed significant taste masking compared to the marketed formulation and ibuprofen pure suspension. % of the volunteers observed cubosomes as not bitter. In contrast, 67% of the volunteers reported marketed suspension as very bitter. The developed cubosomes resulted in physical stability for three months of proper storage. The study has successfully achieved considerable taste-masking using cubosomes with GMO and Poloxmaer 407 formulation. This proof of concept can initiate a new field of research in taste-masked oral liquid formulation. [ABSTRACT FROM AUTHOR]

Oral liquid prednisolone medications have poor acceptance among paediatric patients due to ineffective masking of the bitterness taste of prednisolone. This study aimed to develop a child-friendly prednisolone tablet using a patented chewable chocolate-based delivery system (CDS) previously applied successfully to mask the bitterness tastes of midazolam and tramadol. Prednisolone sodium phosphate (PSP) and prednisolone base (PB) CDS tablets were prepared, and the manufacturing process was optimised using a design of experiments (DoE) approach. Stability was assessed by quantifying residual drug content via a validated HPLC assay. A pilot randomised crossover taste study involving 25 young adult volunteers evaluated taste-masking effectiveness against Redipred™, a commercial oral PSP liquid medicine. The results showed that the PSP CDS tablet was chemically stable following storage for three months at ambient temperature, while the PB CDS tablet was unstable. The optimised PSP CDS tablet, manufactured at 50 °C with a stirring time of 26 h, was found to release over 80% of its drug load within 20 min in 0.1 M HCl and had a significantly better mean taste score compared to Redipred™ (7.08 ± 2.40 vs. 5.60 ± 2.33, p = 0.03). Fifty six percent of the participants preferred the PSP CDS tablet. In conclusion, compared to Redipred™, the CDS technology provided a more effective taste masking of PSP, potentially offering a child-friendly prednisolone formulation with improved compliance, dosing accuracy, and storage stability. [ABSTRACT FROM AUTHOR]

The objective of the conducted research was to design 2 mm orodispersible minitablets of pediatric doses of hydrocortisone (0.5 mg; 1.0 mg) with desirable pharmaceutical properties and eliminate the sensation of a bitter taste using preparation of solid dispersion by ball mill. Hydrocortisone was selected as the model substance, as it is widely utilized in the pediatric population. ODMTs were prepared by compression (preceded by granulation) in a traditional single-punch tablet machine and evaluated using pharmacopoeial tests, DSC, and FTIR analysis. The methods used to evaluate the effectiveness of the taste-masking effect included in vivo participation of healthy volunteers, in vitro drug dissolution and utilization of an analytical device—"electronic tongue". The research employed a preclinical animal model to preliminary investigate the bioequivalence of the designed drug dosage form in comparison to reference products. The study confirmed the possibility of manufacturing good-quality hydrocortisone ODMTs with a taste-masking effect owing to the incorporation of a solid dispersion in the tablet mass. [ABSTRACT FROM AUTHOR]

A pediatric dosage form for crizotinib (Xalkori) was commercialized using quality-by-design principles in a material-sparing fashion. The dosage form consists of spherical multiparticulates (microspheres or pellets) that are coated and encapsulated in capsules for opening. The crizotinib (Xalkori)-coated pellet product is approved in the US for pediatric patients 1 year of age and older and young adults with relapsed or refractory, systemic anaplastic large cell lymphoma (ALCL) and unresectable, recurrent, or refractory inflammatory myofibroblastic tumor (IMT) that is ALK-positive. The product is also approved in the US for adult patients with non-small cell lung cancer (NSCLC) who are unable to swallow intact capsules. The lipid multiparticulate is composed of a lipid matrix, a dissolution enhancer, and an active pharmaceutical ingredient (API). The API, which remains crystalline, is embedded within the microsphere at a 60% drug loading in the uncoated lipid multiparticulate to enable dose flexibility. The melt spray congealing technique using a rotary atomizer is used to manufacture the lipid multiparticulate. Following melt spray congealing, a barrier coating is applied via fluid bed coating. Due to their particle size and content uniformity, this dosage form provides the dosing flexibility and swallowability needed for the pediatric population. The required pediatric dose is achieved by opening the capsules and combining doses of different encapsulated dose strengths, followed by administration of the multiparticulates directly to the mouth. The encapsulation process was optimized through equipment modifications and by using a design of experiments approach to understand the operating space. A limited number of development batches produced using commercial-scale equipment were leveraged to design, understand, and verify the manufacturing process space. The quality by design and material-sparing approach taken to design the melt spray congeal and encapsulation manufacturing processes resulted in a pediatric product with exceptional content uniformity (a 95% confidence and 99% probability of passing USP <905> content uniformity testing for future batches). [ABSTRACT FROM AUTHOR]

Rhinacanthins, derived from Rhinacanthus nasutus, widely used in traditional medicine, exhibit antifungal, anticancer, antiviral, antibacterial, and antiplatelet aggregation effects. Recently, their anti-diabetic activity was confirmed, which makes them an interesting natural alternative in the therapy of the early stage of diabetes mellitus. The aim of this study was to demonstrate the possibility of formulating orodispersible tablets (ODTs) and orodispersible films (ODFs) containing rhinacanthin-rich extract (RRE). Tablets with 50 mg or 100 mg of RRE were produced by direct compression. ODFs were manufactured by casting of Lycoat RS 720 or polyvinyl alcohol solution with RRE and additional excipients. The mechanical properties and disintegration times of the prepared formulations were studied. The effectiveness of taste masking was analyzed with an electronic tongue system. Six months simplified stability studies were performed in conditions complying to ICH guidelines. Appropriate friability of ODTs was achieved, despite low tensile strength (0.45–0.62 MPa). All prepared ODFs successfully met the acceptance criteria regarding Young's modulus, tensile strength, and elongation at break. The observed variations in their mechanical properties were dependent on the type and quantity of polymers and plasticizers used. Disintegration time of ODTs ranged from 38.7 s to 54.2 s, while for ODFs from 24.2 to 40 s in the pharmacopoeial apparatus. Analyses made with the electronic tongue showed the significant taste-masking effect in both formulations. The addition of sucralose as a sweetener and menthol with mint flavor as a taste-masking agent was sufficient to mask an RRE's taste in the case of ODTs and ODFs. Stability studies of ODTs packed in the PVC/Alu blisters showed a decrease in the RRE content below 90% after 6 months. However, ODFs with PVA were physicochemically stable for 6 months while being stored in Alu/Alu sachets. Our study proved for the first time the possibility of the formulation of orodispersible dosage forms with RRE, characterized by good mechanical properties, disintegration time, and appropriate taste masking. [ABSTRACT FROM AUTHOR]

Copyright of Modern Food Science & Technology is the property of Editorial Office of Modern Food Science & Technology and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Motion sickness also known as kinetosis is a condition in which there exists a disagreement between visually perceived movement and the vestibular system's sense of movement. Nausea, vomiting, dizziness, fatigue, and headache are the most common symptoms of motion sickness. This study mainly focuses on the taste masking of Promethazine Hydrochloride (PMZ) by inclusion complexation method, its formulation development in the chewing gum form by using directly compressible gum base HIG® and its quality and performance testing. Different molar ratios (1:1, 1:2, 1:3 and 1:4) of PMZ-cyclodextrin complexes were prepared by using β-Cyclodextrin (β-CD) as a taste masking agent. These complexes were evaluated for FTIR, DSC, % Entrapment Efficiency, % drug yield, and taste evaluation by E-Tongue. The optimized ratio was further evaluated by sophisticated analytical techniques such as Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD). A central composite design (CCD) (3 ^2) was utilized to examine the effects of independent variables (amount of gum-X1 and amount of plasticizer-X2) on dependent variables (%CDRY1 and hardness Y2). The prepared gums were evaluated for drug content, organoleptic properties, in-vitro dissolution testing by fabricated disintegration apparatus, texture analysis, etc. The optimization statistics showed that on decreasing the amount of gum, in- vitro drug release increases and hardness decreases. The optimized batch MCG-2 of Promethazine MCG showed 92.34 ± 0.92% of drug release, whereas for marketed formulation (Phenergan®-25 mg) drug release value was 86.19 ± 1.88%. Results provided evidence that PMZ MCGs could be a better alternative to conventional tablet formulations with improved drug release, palatability and texture. [ABSTRACT FROM AUTHOR]

Mefloquine (MQ) is an antimalarial medication prescribed to treat or malaria prevention.. When taken by children, vomiting usually occurs, and new doses of medication frequently need to be taken. So, developing pediatric medicines using taste-masked antimalarial drug complexes is mandatory for the success of mefloquine administration. The hypothesis that binding mefloquine to an ion-exchange resin (R) could circumvent the drug's bitter taste problem was proposed, and solid-state 13C cross-polarization magic angle spinning (CPMAS) NMR was able to follow MQ–R mixtures through chemical shift and relaxation measurements. The nature of MQ–R complex formation could then be determined. Impedimetric electronic tongue equipment also verified the resinate taste-masking efficiency in vitro. Variations in chemical shifts and structure dynamics measured by proton relaxation properties (e.g., T1ρH) were used as probes to follow the extension of mixing and specific interactions that would be present in MQ–R. A significant decrease in T1ρH values was observed for MQ carbons in MQ–R complexes, compared to the ones in MQ (from 100–200 ms in MQ to 20–50 ms in an MQ–R complex). The results evidenced that the cationic resin interacts strongly with mefloquine molecules in the formulation of a 1:1 ratio complex. Thus, 13C CPMAS NMR allowed the confirmation of the presence of a binding between mefloquine and polacrilin in the MQ–R formulation studied. [ABSTRACT FROM AUTHOR]

Multiple unit particulate system (MUPS) is a more recent, challenging, effective and attractive option for the pharmaceutical industries that gives an efficient way to deliver the drug in modified pattern. MUPS are the most preferred dosage forms considering their ease of administration and consistency in manufacturing. Topiramate, indicated for schizophrenia, has a very bitter taste. The aim of this study was to develop a MUPS dosage form for taste masking of topiramate. Inert sugar spheres were coated with topiramate by fluid bed technique using povidone as binder. The drug loaded pellets were taste masked with cellulose acetate as taste masking agent. In the taste masking coating also, povidone was used as a binder and pore former. Developed taste masked MUPS were evaluated for polymorphic changes, drug content and dissolution in various media. Drug content of all batches of MUPS were within the range of 95-105%. Dissolution profile of the taste masked topiramate MUPS in 0.1N HCl, acetate buffer (pH 4.5) and phosphate buffer (pH 6.8) was found to be satisfactory. [ABSTRACT FROM AUTHOR]

In the past, the administration of medicines for children mainly involved changes to adult dosage forms, such as crushing tablets or opening capsules. However, these methods often led to inconsistent dosing, resulting in under- or overdosing. To address this problem and promote adherence, numerous initiatives, and regulatory frameworks have been developed to develop more child-friendly dosage forms. In recent years, multiparticulate dosage forms such as mini-tablets, pellets, and granules have gained popularity. However, a major challenge that persists is effectively masking the bitter taste of drugs in such formulations. This review therefore provides a brief overview of the current state of the art in taste masking techniques, with a particular focus on taste masking by film coating. Methods for evaluating the effectiveness of taste masking are also discussed and commented on. Another important issue that arises frequently in this area is achieving sufficient dissolution of poorly water-soluble drugs. Since the simultaneous combination of sufficient dissolution and taste masking is particularly challenging, the second objective of this review is to provide a critical summary of studies dealing with multiparticulate formulations that are tackling both of these issues.

الملخص: أهداف البحث: المضادات الحيوية هي الأدوية الأكثر شيوعا بين المرضى الأطفال. ومع ذلك، في معظم الأحيان، يصبح إعطاء الجرعة الدقيقة للأطفال مشكلة بسبب مذاقه المر للغاية. يعد سيفبودوكسيم بروكسيتيل وروكسيثروميسين أحد المضادات الحيوية التي توصف غالبا للأطفال ولها طعم مرير. التركيبات المسوقة لهذه الأدوية هي معلق جاف و/أو أقراص. من المعروف أن طريقة التجفيد تتضمن خطوات مختلفة وبالتالي فهي تستغرق وقتا طويلا ومكلفة. كان الهدف من هذه الدراسة هو إخفاء الطعم المر لسيفبودوكسيم بروكسيتيل وروكسيثروميسين دون المساس بالذوبان وشكل إطلاق الدواء عند مقارنته بالتركيبات المسوقة. بالإضافة إلى التغلب على العيوب المرتبطة بتقنية التجفيد المستخدمة حاليا. طريقة البحث: تم استخدام تقنية البثق بالذوبان الساخن لمعالجة سيفبودوكسيم بروكسيتيل وروكسيثروميسين بشكل فردي باستخدام بوليمر يودراجيت إيبو. تم تشخيص البثقات التي تم الحصول عليها بواسطة التحليل الطيفي للأشعة تحت الحمراء لتحويل فورييه، وقياس نمط الحيود للمواد البلورية وقياس السعرات الحرارية بالمسح التفاضلي. تمت صياغة البثقات المسحوقة كأقراص قابلة للتشتت وتم تقييمها من حيث كفاءة إخفاء الطعم داخل المختبر وفي الجسم الحي. النتائج: أظهرت الأقراص المحضرة في هذه الدراسة ملامح ذوبان قابلة للمقارنة ولكن تم تعزيز كفاءة إخفاء الطعم بشكل كبير عند مقارنتها بالأقراص المسوقة من سيفبودوكسيم بروكسيل وروكسيثروميسين. وكانت نتائج تقييم إخفاء الطعم البشري داخل الجسم متفقة أيضا مع دراسات إخفاء التذوق داخل المختبر. الاستنتاجات: وبالتالي فإن العمل الحالي قد قدم تكنولوجيا البثق بالذوبان الساخن الخالية من المذيبات والقابلة للتطوير والمستمرة لمعالجة مشكلات الطعم المر في سيفبودوكسيم بروكسيتيل وروكسيثروميسين. علاوة على ذلك، تم التغلب على العيوب المرتبطة بتقنية التجفيد المستخدمة حاليًا من خلال تطوير التركيبات باستخدام تقنية البثق بالذوبان الساخن. Abstract: Objectives: Antibiotics are the most commonly administered medications among pediatric patients. However most of the time, accurate dose administration to children becomes a problem due to the extremely bitter taste. Cefpodoxime proxetil (CP) and roxithromycin (ROX) are antibiotics often prescribed to the pediatric population and have a bitter taste. Marketed formulations of these drugs are dry suspension and/or tablets. The lyophilization method involves various steps and thus is time consuming and expensive. The objective of this study was to mask the bitter taste of CP and ROX without compromising the solubility and drug release profile compared to marketed formulations, as well as to overcome the disadvantages associated with the currently used lyophilization technique. Methods: Hot melt extrusion (HME) technology was used to process CP and ROX individually with Eudragit E PO polymer. The extrudates obtained were characterized by Fourier transform infrared spectroscopy, powder X-ray diffraction, and differential scanning calorimetry. The powdered extrudates were formulated as dispersible tablets and evaluated for in vitro and in vivo taste-masking efficiency. Results: The tablets prepared in this study showed comparable dissolution profiles but the taste-masking efficiency was significantly enhanced compared to the marketed tablets of CP and ROX. The results of in vivo human taste-masking evaluation were also in agreement with the in vitro taste-masking studies. Conclusion: The current work presents solvent-free, scalable, and continuous HME technology for addressing the bitter taste issues of CP and ROX. The disadvantages associated with the currently used lyophilization technique were overcome by developing the formulations using HME technology.

In this review, we aim to highlight the advantages, challenges, and limitations of electronic tongues (e-tongues) in pharmaceutical drug development. The authors, therefore, critically evaluated the performance of e-tongues regarding their qualification to assess peroral formulations containing bitter active pharmaceutical ingredients. A literature search using the keywords 'electronic', 'tongue', 'bitter', and 'drug' in a Web of Science search was therefore initially conducted. Reviewing the publications of the past decade, and further literature where necessary, allowed the authors to discuss whether and how e-tongues perform as expected and whether they have the potential to become a standard tool in drug development. Specifically highlighted are the expectations an e-tongue should meet. Further, a brief insight into the technologies of the utilized e-tongues is given. Reliable protocols were found that enable (i) the qualified performance of e-tongue instruments from an analytical perspective, (ii) proper taste-masking assessments, and (iii) under certain circumstances, the evaluation of bitterness. [ABSTRACT FROM AUTHOR]

The bitter drug, warfarin, has a narrow therapeutic index (NTI) and is used in paediatrics and geriatrics. The aim of this feasibility study was to formulate the taste-masked warfarin-containing pellets to be applicable for dose personalisation and to improve patient compliance, as well as to investigate the effect of the core type (PharSQ® Spheres M, CELPHERE™ CP-507, and NaCl) on the warfarin release from the Kollicoat® Smartseal taste-masking-coated pellets. The cores were successfully drug-loaded and coated in a fluid-bed coater with a Wurster insert. An increase in particle size and particle size distribution was observed by optical microscopy. In saliva-simulated pH, at the Kollicoat® Smartseal level of 2 mg/cm2, none of the pellets demonstrated drug release, confirming their efficient taste-masking. However, in a stomach-simulated pH, a faster drug release was observed from PharSQ® Spheres M- and CELPHERE™ CP-507-coated pellets in comparison with NaCl cores. Additional experiments allowed us to explain the slower drug release from NaCl-containing pellets because of the salting-out effect. Despite the successful taste masking, the drug release from pellets was relatively slow (not more than 91% per 60 min), allowing for further formulation improvements. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Taibah University Medical Sciences is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Age-appropriateness of a formulation is the ability to deliver variable but accurate doses to the paediatric population in a safe and acceptable manner to improve medical adherence and reduce medication errors. Paediatric drug delivery is a challenging area of formulation research due to the existing gap in knowledge. This includes the unknown safety of excipients in the paediatric population, the need for an age-appropriate formulation, the lack of an effective taste-masking method and the lack of paediatric pharmacokinetic data and patient acceptability. It is equally important to establish methods for predicting the biopharmaceutical performance of a paediatric formulation as a function of age. Overcoming the challenges of existing technologies and providing custom-made solutions for the development of age-appropriate formulation is, therefore, a daunting task. Orodispersible films (ODF) are promising as age-appropriate formulations, an unmet need in paediatric drug delivery. New technological improvements in taste masking, improving solubility and rate of dissolution of insoluble drugs, the flexibility of dosing and extemporaneous preparation of these films in a hospital good manufacturing practises (GMP) setup using 3D printing can increase its acceptance among clinicians, patients and caregivers. The current review discusses the problems and possibilities in ODF technology to address the outstanding issues of age-appropriateness, which is the hallmark of patient acceptance and medical adherence in paediatrics. [ABSTRACT FROM AUTHOR]

Background: Propranolol, largely prescribed as an antihypertensive and antiarrhythmic drug in pediatrics, is characterized by a bitter taste and an astringent aftertaste. Currently, the therapy requires crushing of tablets for adults and their dispersion in water many times a day, leading to loss of dosing accuracy, low palatability, and poor compliance for both patients and caregivers. Objectives: This work aimed to exploit cyclodextrin complexation by cogrinding to develop orally disintegrating tablets (ODTs) endowed with reliable dosing accuracy, good palatability and safety, ease of swallowability, and ultimately better compliance for both pediatric patients and caregivers. Results: Different formulation variables and process parameters were evaluated in preparing ODTs. The technological and morphological characterization and disintegration tests were performed according to official and alternative tests to select the ODT formulation based on the drug Hydroxypropyl-β-cyclodextrin (HPβCD) coground complex form containing Pearlitol® Flash as the diluent and 8% Explotab® as the superdisintegrant, which demonstrated the highest % drug dissolution in simulated saliva and acceptable in vitro palatability assessed by the electronic tongue, confirming the good taste-masking power of HPβCD towards propranolol. Conclusions: Such a new dosage form of propranolol could represent a valid alternative to the common extemporaneous preparations, overcoming the lack of solid formulations of propranolol intended for pediatric use.

The advancement in the formulation and characterization techniques have paved the path for development of new as well as modification of existing dosage forms. The present work explores the role of micro-computed tomography (micro-CT) as advanced characterization technique for multi-layered-coated pellets to ascertain the quality of coated pellets. The work further explored in-house e-tongue technique for understanding palatability of formulation in early stages of development thus by reducing clinical taste evaluation time. The developed multi-layered-coated pellets were characterized using microscopy (optical and electron microscopy). The obtained results demonstrated formation of spherical-shaped pellets with uniform coating. The uniform coating was further confirmed by results obtained from scanning electron microscopy (SEM) and cross-sectional SEM analysis, which showed visible difference in pellet surface before and after multi-layered coating. The micro-CT results confirmed the visible demarcation of layers (drug and polymer, i.e., hydroxypropyl methylcellulose (HPMC) and eudragit (EPO)) along with uniform thickness of various layering. The dissolution study of developed pellets suggested the role of layering EPO on drug release from pellets. The e-tongue analysis proved to be an excellent tool for early prediction of taste masking of drug via multi-layered pellets and can serve as potential platform for taste masking with high specificity. The overall results suggest the suitability of developed multi-layered platform as efficient dosage form (sprinkle) in pediatric/geriatric product development. [ABSTRACT FROM AUTHOR]

Orally disintegrating granules (ODGs) are a pharmaceutical form commonly used for the administration of NSAIDs because of their easy assumption and fast dispersion. The development of ODGs is not easy for drugs like dexketoprofen trometamol (DXKT), which have a bitter and burning taste. In this work, high-shear coating (HSC) was used as an innovative technique for DKXT taste masking. This study focused on coating DXKT granules using the HSC technique with a low-melting lipid excipient, glyceryl distearate (GDS). The HSC technique allowed for the coating to be developed through the thermal rise resulting from the friction generated by the granules movement inside the equipment, causing the coating excipient to soften. The design of the experiment was used to find the best experimental coating conditions in order to gain effective taste masking by suitably reducing the amount of drug released in the oral cavity. The influence of the granule dimensions was also investigated. Coating effectiveness was evaluated using a simulated saliva dissolution test. It was found that low impeller speed (300 rpm) and a 20% coating excipient were effective in suitably reducing the drug dissolution rate and then in taste masking. The coated granules were characterized for their morphology and solid-state properties by SEM, BET, XRPD, DSC, and NIR analyses. A human taste panel test confirmed the masking of DXKT taste in the selected batch granules. [ABSTRACT FROM AUTHOR]

The unpleasant extremely bitter taste of the orally administered broad-spectrum antibiotic azithromycin decreases patient compliance, especially in pediatrics. This issue can be overcome by decreasing drug interaction with the tasting buds using insoluble polymers at salivary pH (6.8 − 7.4), like the cationic polymer Eudragit EPO. Supercritical fluid technology is a green synthesis method for preparing pharmaceutical preparations that replace organic solvents with safe supercritical CO2. This study aimed to mask the bitter taste of azithromycin using the supercritical fluid method and a pH-sensitive Eudragit EPO polymer. A foaming process was investigated for preparing a formulation (TEST), which comprises treating the polymer with supercritical carbon dioxide (CO2) fluid to prepare a taste-masked dosage form without employing organic solvents or flavors. The use of the supercritical technique at 40 °C and 10 MPa for 2 h allowed the manufacturing of solvent-free polymeric foam with azithromycin dispersions; the average calculated percentage of apparent volume change was 62.5 ± 5.9% with an average pore diameter of 34.879 Å. The formulated sample showed low drug release in simulated salivary fluid while keeping its crystalline nature. Moreover, clinical studies on healthy subjects showed that the formula successfully masked azithromycin's bitter taste. Overall, it has been shown herein that the supercritical fluid technology foaming method is promising in masking the bitter taste of bitter ingredients. [ABSTRACT FROM AUTHOR]

The objective of the conducted research was to design 2 mm orodispersible minitablets of pediatric doses of hydrocortisone (0.5 mg; 1.0 mg) with desirable pharmaceutical properties and eliminate the sensation of a bitter taste using preparation of solid dispersion by ball mill. Hydrocortisone was selected as the model substance, as it is widely utilized in the pediatric population. ODMTs were prepared by compression (preceded by granulation) in a traditional single-punch tablet machine and evaluated using pharmacopoeial tests, DSC, and FTIR analysis. The methods used to evaluate the effectiveness of the taste-masking effect included in vivo participation of healthy volunteers, in vitro drug dissolution and utilization of an analytical device—“electronic tongue”. The research employed a preclinical animal model to preliminary investigate the bioequivalence of the designed drug dosage form in comparison to reference products. The study confirmed the possibility of manufacturing good-quality hydrocortisone ODMTs with a taste-masking effect owing to the incorporation of a solid dispersion in the tablet mass.

Oral liquid prednisolone medications have poor acceptance among paediatric patients due to ineffective masking of the bitterness taste of prednisolone. This study aimed to develop a child-friendly prednisolone tablet using a patented chewable chocolate-based delivery system (CDS) previously applied successfully to mask the bitterness tastes of midazolam and tramadol. Prednisolone sodium phosphate (PSP) and prednisolone base (PB) CDS tablets were prepared, and the manufacturing process was optimised using a design of experiments (DoE) approach. Stability was assessed by quantifying residual drug content via a validated HPLC assay. A pilot randomised crossover taste study involving 25 young adult volunteers evaluated taste-masking effectiveness against Redipred™, a commercial oral PSP liquid medicine. The results showed that the PSP CDS tablet was chemically stable following storage for three months at ambient temperature, while the PB CDS tablet was unstable. The optimised PSP CDS tablet, manufactured at 50 °C with a stirring time of 26 h, was found to release over 80% of its drug load within 20 min in 0.1 M HCl and had a significantly better mean taste score compared to Redipred™ (7.08 ± 2.40 vs. 5.60 ± 2.33, p = 0.03). Fifty six percent of the participants preferred the PSP CDS tablet. In conclusion, compared to Redipred™, the CDS technology provided a more effective taste masking of PSP, potentially offering a child-friendly prednisolone formulation with improved compliance, dosing accuracy, and storage stability.

Rhinacanthins, derived from Rhinacanthus nasutus, widely used in traditional medicine, exhibit antifungal, anticancer, antiviral, antibacterial, and antiplatelet aggregation effects. Recently, their anti-diabetic activity was confirmed, which makes them an interesting natural alternative in the therapy of the early stage of diabetes mellitus. The aim of this study was to demonstrate the possibility of formulating orodispersible tablets (ODTs) and orodispersible films (ODFs) containing rhinacanthin-rich extract (RRE). Tablets with 50 mg or 100 mg of RRE were produced by direct compression. ODFs were manufactured by casting of Lycoat RS 720 or polyvinyl alcohol solution with RRE and additional excipients. The mechanical properties and disintegration times of the prepared formulations were studied. The effectiveness of taste masking was analyzed with an electronic tongue system. Six months simplified stability studies were performed in conditions complying to ICH guidelines. Appropriate friability of ODTs was achieved, despite low tensile strength (0.45–0.62 MPa). All prepared ODFs successfully met the acceptance criteria regarding Young’s modulus, tensile strength, and elongation at break. The observed variations in their mechanical properties were dependent on the type and quantity of polymers and plasticizers used. Disintegration time of ODTs ranged from 38.7 s to 54.2 s, while for ODFs from 24.2 to 40 s in the pharmacopoeial apparatus. Analyses made with the electronic tongue showed the significant taste-masking effect in both formulations. The addition of sucralose as a sweetener and menthol with mint flavor as a taste-masking agent was sufficient to mask an RRE’s taste in the case of ODTs and ODFs. Stability studies of ODTs packed in the PVC/Alu blisters showed a decrease in the RRE content below 90% after 6 months. However, ODFs with PVA were physicochemically stable for 6 months while being stored in Alu/Alu sachets. Our study proved for the first time the possibility of the formulation of orodispersible dosage forms with RRE, characterized by good mechanical properties, disintegration time, and appropriate taste masking.

Mefloquine (MQ) is an antimalarial medication prescribed to treat or malaria prevention.. When taken by children, vomiting usually occurs, and new doses of medication frequently need to be taken. So, developing pediatric medicines using taste-masked antimalarial drug complexes is mandatory for the success of mefloquine administration. The hypothesis that binding mefloquine to an ion-exchange resin (R) could circumvent the drug’s bitter taste problem was proposed, and solid-state 13C cross-polarization magic angle spinning (CPMAS) NMR was able to follow MQ–R mixtures through chemical shift and relaxation measurements. The nature of MQ–R complex formation could then be determined. Impedimetric electronic tongue equipment also verified the resinate taste-masking efficiency in vitro. Variations in chemical shifts and structure dynamics measured by proton relaxation properties (e.g., T1ρH) were used as probes to follow the extension of mixing and specific interactions that would be present in MQ–R. A significant decrease in T1ρH values was observed for MQ carbons in MQ–R complexes, compared to the ones in MQ (from 100–200 ms in MQ to 20–50 ms in an MQ–R complex). The results evidenced that the cationic resin interacts strongly with mefloquine molecules in the formulation of a 1:1 ratio complex. Thus, 13C CPMAS NMR allowed the confirmation of the presence of a binding between mefloquine and polacrilin in the MQ–R formulation studied.

Objectives: Oral steroids are commonly prescribed to children. Steroids have a strong bitter taste that limits their oral acceptance in children. The objective of this study was to formulate a pediatric-friendly and palatable oral dosage form of steroids. Materials and Methods: Solid dispersions of dexamethasone were prepared using polyethylene glycol, pectin, and Eudragit as carrier polymers, and chocolate as a flavoring agent. Taste masking efficiency was evaluated by healthy volunteers to select the best formula. The selected formula was pressed into chewable tablets with varying amounts of sweeteners. Chewable tablets were evaluated for palatability, hardness, and chewing index. The typical application of the taste masking approach was confirmed using prednisolone. Results: Eudragit-based solid dispersions were effective in dexamethasone taste masking. Using 40% mannitol resulted in palatable tablets with acceptable hardness and chewing difficulty. The effectiveness of the taste masking approach was successfully used to prepare prednisolone chewable tablets. However, an increase in the carrier: drug ratio and a change in the flavor to pineapple were necessary to achieve maximum palatability of prednisolone chewable tablets. Conclusion: Eudragit solid dispersion is an effective method for the taste masking highly bitter steroids. The solid dispersion was successfully pressed into a palatable, easy-to-chew, and pediatric-friendly chewable tablet dosage form. The carrier: drug ratio and the choice of flavoring agent are crucial factors in improving tablet palatability. [ABSTRACT FROM AUTHOR]

One of the main problems in medical practice is the lack of patient adherence to treatment, which is often attributed to the bitterness or sourness of medicines causing discomfort and an aversion during administration, especially in children. Therefore, masking an unpleasant taste is one of the goals of pharmaceutical development. Currently, there are various approaches to improving the taste of oral dosage forms containing bitter or excessively sour pharmaceutical substances. This review covers some of these approaches and their advantages and disadvantages and provides relevant examples of the possible use of each of them. [ABSTRACT FROM AUTHOR]

To address the medication requirements of different populations, efforts have been made to develop sustained-release formulations of andrographolide. In this study, andrographolide tablets (3D-AGT) and encapsulating agents (3D-AGE) were created using a semi-solid extrusion (SSE) 3D printer with varying release rates. Sodium alginate and chitosan were utilized as excipients to produce a hexagonal 3D-AGT with a diameter of 10.00 mm and a height of 3.00 mm. The 3D-AGE was then assembled by combining the upper layer and the ground floor loaded with andrographolide. Both formulations exhibited smooth surfaces and uniform internal composition. FT-IR analysis confirmed that the chemical structures of andrographolide and the excipients remained intact throughout the printing process. The drug loading capacity of 3D-AGT preparations, formulated with four different excipient ratios, exceeded 85%. Additionally, two 3D-AGE preparations (10 and 20 mg) were successfully loaded with the drug. In vitro drug release tests demonstrated that both 3D-AGT and 3D-AGE preparations exhibited satisfactory drug release performance. However, the proportions of excipients and drug loading had minimal impact on the cumulative drug dissolution effect. In terms of antibacterial activity against Escherichia coli, both preparations displayed antibacterial rates of nearly 85% or higher in vitro. Furthermore, the average results from nine volunteers indicated that 3D-AGE effectively masked the bitter taste of andrographolide. This study suggested that the release rate of andrographolide could be regulated using SSE 3D printing through careful structural design and adjustment of printing parameters, thus providing a novel approach for personalized traditional Chinese medicine preparations. [ABSTRACT FROM AUTHOR]

It is widely recognized that many active pharmaceutical ingredients (APIs) have a disagreeable taste that affects patient acceptability, particularly in children. Consequently, developing dosage forms with a masked taste has attracted a lot of interest. The application of cyclodextrins as pharmaceutical excipients is highly appreciated and well established, including their roles as drug delivery systems, solubilizers and absorption promoters, agents that improve drug stability, or even APIs. The first work describing the application of the taste-masking properties of CDs as pharmaceutical excipients was published in 2001. Since then, numerous studies have shown that these cyclic oligosaccharides can be effectively used for such purposes. Therefore, the aim of this review is to provide insight into studies in this area. To achieve this aim, a systematic evaluation was conducted, which resulted in the selection of 67 works representing both successful and unsuccessful works describing the application of CDs as taste-masking excipients. Particular attention has been given to the methods of evaluation of the taste-masking properties and the factors affecting the outcomes, such as the choice of the proper cyclodextrin or guest–host molar ratio. The conclusions of this review reveal that the application of CDs is not straightforward; nevertheless, this solution can be an effective, safe, and inexpensive method of taste masking for pharmaceutical purposes. [ABSTRACT FROM AUTHOR]

Background and purpose: The present study aimed to obtain a taste-masked oral disintegrating tablet (ODT) containing tolterodine tartrate (TT) intercalated into montmorillonite (MMT) Experimental approach: The TT-MMT hybrid was prepared by ion exchange reaction. The effect of the initial concentration of TT, MMT, temperature, and pH on the encapsulation efficiency (EE) % of the drug in MMT was evaluated. The selected TT-MMT hybrid was characterized by X-ray diffraction (XRD), Fourier transforms infrared (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Then, the optimized TT-MMT hybrid was incorporated in the ODT prepared by direct compression method and taste-masking assessment performed by a human test panel. Findings/Results: The EE% of TT was in the range of 22.67 to 71.06% in different formulations. It was found that increases in MMT concentration significantly increased EE%. DSC and XRD studies indicated that the TT was intercalated in the MMT interlayer space in an amorphous or molecular state. In-vitro release studies at pH 6.8 showed that the amount of the drug released from the TT-MMT hybrid was negligible for the first 3 min. The post-compression of ODT also showed satisfactory results in terms of friability, hardness, disintegration time, and taste. Conclusion and implications: MMT-ODT could be a suitable vehicle for the taste masking of TT, with the potential for use in patients with swallowing problems. [ABSTRACT FROM AUTHOR]

In this review, we aim to highlight the advantages, challenges, and limitations of electronic tongues (e-tongues) in pharmaceutical drug development. The authors, therefore, critically evaluated the performance of e-tongues regarding their qualification to assess peroral formulations containing bitter active pharmaceutical ingredients. A literature search using the keywords ‘electronic’, ‘tongue’, ‘bitter’, and ‘drug’ in a Web of Science search was therefore initially conducted. Reviewing the publications of the past decade, and further literature where necessary, allowed the authors to discuss whether and how e-tongues perform as expected and whether they have the potential to become a standard tool in drug development. Specifically highlighted are the expectations an e-tongue should meet. Further, a brief insight into the technologies of the utilized e-tongues is given. Reliable protocols were found that enable (i) the qualified performance of e-tongue instruments from an analytical perspective, (ii) proper taste-masking assessments, and (iii) under certain circumstances, the evaluation of bitterness.

The bitter drug, warfarin, has a narrow therapeutic index (NTI) and is used in paediatrics and geriatrics. The aim of this feasibility study was to formulate the taste-masked warfarin-containing pellets to be applicable for dose personalisation and to improve patient compliance, as well as to investigate the effect of the core type (PharSQ® Spheres M, CELPHERE™ CP-507, and NaCl) on the warfarin release from the Kollicoat® Smartseal taste-masking-coated pellets. The cores were successfully drug-loaded and coated in a fluid-bed coater with a Wurster insert. An increase in particle size and particle size distribution was observed by optical microscopy. In saliva-simulated pH, at the Kollicoat® Smartseal level of 2 mg/cm2, none of the pellets demonstrated drug release, confirming their efficient taste-masking. However, in a stomach-simulated pH, a faster drug release was observed from PharSQ® Spheres M- and CELPHERE™ CP-507-coated pellets in comparison with NaCl cores. Additional experiments allowed us to explain the slower drug release from NaCl-containing pellets because of the salting-out effect. Despite the successful taste masking, the drug release from pellets was relatively slow (not more than 91% per 60 min), allowing for further formulation improvements.

This review paper explores the role of human taste panels and artificial neural networks (ANNs) in taste-masking paediatric drug formulations. Given the ethical, practical, and regulatory challenges of employing children, young adults (18–40) can serve as suitable substitutes due to the similarity in their taste sensitivity. Taste panellists need not be experts in sensory evaluation so long as a reference product is used during evaluation; however, they should be screened for bitterness taste detection thresholds. For a more robust evaluation during the developmental phase, considerations of a scoring system and the calculation of an acceptance value may be beneficial in determining the likelihood of recommending a formulation for further development. On the technological front, artificial neural networks (ANNs) can be exploited in taste-masking optimisation of medicinal formulations as they can model complex relationships between variables and enable predictions not possible previously to optimise product profiles. Machine learning classifiers may therefore tackle the challenge of predicting the bitterness intensity of paediatric formulations. While advancements have been made, further work is needed to identify effective taste-masking techniques for specific drug molecules. Continuous refinement of machine learning algorithms, using human panellist acceptability scores, can aid in enhancing paediatric formulation development and overcoming taste-masking challenges. [ABSTRACT FROM AUTHOR]

The unpleasant taste, which characterizes a large group of medicinal substances, may be a challenge both for scientists at the stage of designing a drug form, as well as for the patient when taking a given preparation. Taste impressions play an important role nowadays, sometimes being one of the selection criteria that a patient follows during visit in a community pharmacies. They could also have a positive impact on the impression of a given preparation and, as a result, the successful commercialization of a medicinal product. The taste experience plays a key role in the case of oral forms of a drug, and above all, soluble forms and other liquid forms of drugs. The main target group of liquid medicinal preparations are pediatric patients and people with problems swallowing oral solid forms, as well as seniors. Especially children are a group of patients for whom the type of taste is extremely important. Drug substances characterized by an unpleasant taste and / or odor, due to low patient acceptance, may also reduce the effectiveness of the treatment process. Effective masking of the unpleasant taste of a given drug substance is possible because of the development of many techniques enabling this process, which in turn may translate into more regular drug intake by the patient according to appropriate recommendations. The masking of the unpleasant taste of API (Active Pharmaceutical Ingredient) can be achieved by a variety of methods. The aim of the article is to discuss some of the most popular. In this article are present techniques using the addition of flavors and / or sweeteners, microencapsulation, rheological changes, formation of inclusion complexes, granulation, multiple emulsions, ion exchange resins and the use of liposomes. It should be noted that the selection of the appropriate method should be guided by several aspects, including, in particular, the physicochemical properties of a given drug substance, the frequency of dosing, and the form of the drug.

The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values < 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.

Etilefrine hydrochloride (ET) is a water-soluble drug that is used to treat hypotension, but it has a bitter taste and low bioavailability due to undergoing the first-pass effect. Thus, this study aimed to develop and evaluate oral medicated jelly (OMJ) containing ET that could offer an easily taken palatable dosage form with higher bioavailability. OMJ is a novel palatable drug delivery system that can easily be taken by pediatric and geriatric patients, as well as those with dysphagia. Moreover, OMJs offer rapid disintegration in saliva and rapid drug absorption through the buccal mucosa, avoiding the first-pass effect and increasing the drug bioavailability. Natural polymers such as pectin, guar gum, xanthan gum, tragacanth gum, and sodium alginate were used as jellifying agents, with the addition of calcium chloride as a crosslinking agent, to prepare OMJs using the heat and congealing method. The prepared OMJs were investigated by testing their viscosity, in vitro release, and texture analysis of firmness, consistency, stickiness, cohesiveness, springiness, gumminess, and chewiness using a texture analyzer. A full factorial design (21 × 51) was utilized to select the optimized OMJ. The optimized OMJ (J2), containing 4 % pectin, had a 7563 ± 55 cps viscosity, 8.32 ± 0.21 N firmness, 5.72 ± 0.18 µJ consistency, 1.30 ± 0.04 mJ stickiness, and 96.02 ± 3.74 % ET dissolved after 10 min. ET release was significantly increased (greater than4-fold) from the optimized OMJ compared with the market tablet. Moreover, the obtained results clarified the stability and the acceptable palatability of the optimized OMJ. The clinical investigation on healthy human volunteers revealed that the optimized OMJ (J2) had significantly higher Cmax (1.7 folds) when compared with the market tablet with a relative bioavailability of 154.55 %. Therefore, OMJs can be considered as promising, palatable, and easily swallowed dosage form that could enhance the bioavailability of drugs undergoing the first-pass effect.

Taste masking is critical to improving the compliance of pediatric oral dosage forms. However, it is challenging for extremely bitter lisdexamfetamine dimesylate (LDX) with a long half-life and given in large dose. The present study aims to develop an immediate-release, taste-masked lisdexamfetamine chewable tablet. Lisdexamfetamine-resin complexes (LRCs) were prepared using the batch method. The molecular mechanism of taste masking was explored by PXRD, PLM, STA, and FT-IR. The results showed that taste masking was attributed to the ionic interaction between drug and the resin. The ion exchange process conformed to first-order kinetics. The rate-limiting step of drug release was the diffusion of ions inside the particles, and the concentration of H+ was the key factor for immediate release. The masking efficiency of the prepared LRCs in saliva exceeded 96%, and the drug could be completely released within 15 min in aqueous HCl (pH 1.2). Furthermore, the SeDeM expert system was used for the first time to comprehensively study the powder properties of LRCs and to quickly visualize their defects (compressibility, lubricity/stability, and lubricity/dosage). The selection of excipients was targeted rather than traditional screening, thus obtaining a robust chewable tablet formulation suitable for direct compression. Finally, the difference between chewable tablets containing LRCs and chewable tablets containing lisdexamfetamine dimesylate was compared by in vitro dissolution test, electronic tongue, and disintegration test. In conclusion, an immediate-released, child-friendly lisdexamfetamine chewable tablets without bitterness was successfully developed by the QbD approach, using the SeDeM system, which may help in further development of chewable tablets. [ABSTRACT FROM AUTHOR]

Bitter gourd extract (BGE) is rich in antioxidants and anti-diabetic components that promote good human health; however, its bitter taste makes it challenging to use in food. In this study, the effect of carboxymethyl cellulose and β-cyclodextrin (β-CD) on the bitterness and properties of BGE were investigated. The bitterness intensity was evaluated by the trained sensory panel, and the physicochemical properties were also determined, including viscosity, total saponin, polyphenol content, antioxidant capacity, and α-amylase inhibition activity. It was found that the bitterness of BGE with 0.75%, w/v β-cyclodextrin decreased significantly by more than 90%. Additionally, FTIR, 1 H-NMR, and thermogravimetric analysis of BGE supplemented with β-CD confirmed the formation of a complex between β-CD and components of BGE. The findings of the current study also reveal that debittering agents did not inhibit the bioactivities of BGE. [ABSTRACT FROM AUTHOR]

Bitterness is one of the basic tastes, and sensing bitterness plays a significant role in mammals recognizing toxic substances. The bitter taste of food and oral medicines may decrease consumer compliance. As a result, many efforts have been made to mask or decrease the bitterness in food and oral pharmaceutical products. The detection of bitterness is critical to evaluate how successful the taste-masking technology is, and many novel taste-sensing systems have been developed on the basis of various interaction mechanisms. In this review, we summarize the progress of bitterness response mechanisms and the development of novel sensors in detecting bitterness ranging from commercial electronic devices based on modified electrodes to micro-type sensors functionalized with taste cells, polymeric membranes, and other materials in the last two decades. The challenges and potential solutions to improve the taste sensor quality are also discussed. [ABSTRACT FROM AUTHOR]

Orally disintegrating granules (ODGs) are a pharmaceutical form commonly used for the administration of NSAIDs because of their easy assumption and fast dispersion. The development of ODGs is not easy for drugs like dexketoprofen trometamol (DXKT), which have a bitter and burning taste. In this work, high-shear coating (HSC) was used as an innovative technique for DKXT taste masking. This study focused on coating DXKT granules using the HSC technique with a low-melting lipid excipient, glyceryl distearate (GDS). The HSC technique allowed for the coating to be developed through the thermal rise resulting from the friction generated by the granules movement inside the equipment, causing the coating excipient to soften. The design of the experiment was used to find the best experimental coating conditions in order to gain effective taste masking by suitably reducing the amount of drug released in the oral cavity. The influence of the granule dimensions was also investigated. Coating effectiveness was evaluated using a simulated saliva dissolution test. It was found that low impeller speed (300 rpm) and a 20% coating excipient were effective in suitably reducing the drug dissolution rate and then in taste masking. The coated granules were characterized for their morphology and solid-state properties by SEM, BET, XRPD, DSC, and NIR analyses. A human taste panel test confirmed the masking of DXKT taste in the selected batch granules.

Promethazine hydrochloride (PMZ), a potent H1-histamine blocker widely used to prevent motion sickness, dizziness, nausea, and vomiting, has a bitter taste. In the present study, taste masked PMZ nanocapsules (NCs) were prepared using an interfacial polycondensation technique. A one-step approach was used to expedite the synthesis of NCs made from a biocompatible and biodegradable polyamide based on l-arginine. The produced NCs had an average particle size of 193.63 ± 39.1 nm and a zeta potential of −31.7 ± 1.25 mV, indicating their stability. The NCs were characterized using differential scanning calorimetric analysis and X-ray diffraction, as well as transmission electron microscopy that demonstrated the formation of the NCs and the incorporation of PMZ within the polymer. The in vitro release study of the PMZ-loaded NCs displayed a 0.91 ± 0.02% release of PMZ after 10 min using artificial saliva as the dissolution media, indicating excellent taste masked particles. The in vivo study using mice revealed that the amount of fluid consumed by the PMZ-NCs group was significantly higher than that consumed by the free PMZ group (p < 0.05). This study confirmed that NCs using polyamides based on l-arginine and interfacial polycondensation can serve as a good platform for the effective taste masking of bitter actives. [ABSTRACT FROM AUTHOR]

Background: prednisolone (PRD) is a very bitter, corticosteroid drug, acts as immunosuppressant and anti-inflammatory used for treatment of many diseases like asthma and arthritis. Objective: This study aimed to formulate and evaluate taste masked PRD-alginate beads to increase patient compliance. Method: PRD taste masked beads were prepared by external ionic gelation technique using sodium alginate (S. Alg) as polymer and 1% calcium chloride as cross linker. The beads were evaluated for their physical properties including general appearance, percentage yield, drug loading, drug content and in vitro taste masking. The effect of S. Alg concentration, addition of tween, addition of hydrophilic polymers (Carbopol 940, PEG 4000, HPMC E5 and PVA) on the physical properties of beads was studied Result: This method was successful in decreasing the release of PRD from beads in phosphate buffer pH 6.8 within 60 seconds. The optimum formula (F6) was obtained by using S. Alg (0.5% W/W) in combination with carbopol 940 in a ratio of 1:1:1 ratio (PRD: S. Alg: Carbopol 940) with percentage yield 88%, drug loading 77%, drug content 98.3 ± 2.1 and 0.77 % ± 0.19 release of PRD in phosphate buffer pH 6.8 within 60 seconds, supposing good taste masking. Conclusion: It can be concluded that oral preparation of PRD with an acceptable taste is possible by using external ionic gelation technique. [ABSTRACT FROM AUTHOR]

Despite the proven health benefits of fish oil to the human body, the unpleasant aftertaste and short shelf-life limit the public acceptability as supplementation. Microencapsulation of the fish oil into microspheres is an approach to overcome these limitations. This study aims to prepare controllable-size fish oil microspheres using pulsed electrospray technique for enhancing fish oil stability and palatability. Fish oil alginate microspheres were prepared and optimized by bipolar wave-based drop on demand (DOD) jetting electrospray. The microspheres were characterized in terms of particle size, aspect ratio (AR), encapsulation efficiency (EE), loading capacity (LC), Fourier Transform Infrared Spectroscopy (FTIR) and drug release. The stability of the fish oil microspheres was assessed based on specific characteristics and antioxidant activity over a period of 6 months. The anticancer effectiveness of encapsulated and unencapsulated fish oil was evaluated using HCT116 and 3T3 cell lines. Additionally, a human panel palatability test was conducted to evaluate the taste masking ability of fish oil microspheres. The optimal formulation exhibited an average particle size of 344.75 ± 10.84 μm, AR of 1.03 ± 0.02, EE of 98.98 ± 0.72%, and LC of 22.60 ± 0.62%. The microencapsulation resulted in minimal fish oil loss in the stomach, leading to enhanced masking of the fishy taste. The FTIR analysis and DPPH assay revealed that the chemical properties of the fish oil and its antioxidant efficacy were preserved after microencapsulation and remained stable after 6 months of storage. The fish oil microspheres showed a superior anticancer effect compared to the free ones. In addition, the panellists of the palatability test of the fish oil microspheres showed an excellent taste masking ability. Hence, this study developed controllable-size fish oil microspheres via pulsed electrospray technique with enhanced fish oil stability, efficacy, and palatability, suggesting their potential utility as dietary supplements to fulfil the daily recommended intake of fish oil. [Display omitted] [ABSTRACT FROM AUTHOR]

It is widely recognized that many active pharmaceutical ingredients (APIs) have a disagreeable taste that affects patient acceptability, particularly in children. Consequently, developing dosage forms with a masked taste has attracted a lot of interest. The application of cyclodextrins as pharmaceutical excipients is highly appreciated and well established, including their roles as drug delivery systems, solubilizers and absorption promoters, agents that improve drug stability, or even APIs. The first work describing the application of the taste-masking properties of CDs as pharmaceutical excipients was published in 2001. Since then, numerous studies have shown that these cyclic oligosaccharides can be effectively used for such purposes. Therefore, the aim of this review is to provide insight into studies in this area. To achieve this aim, a systematic evaluation was conducted, which resulted in the selection of 67 works representing both successful and unsuccessful works describing the application of CDs as taste-masking excipients. Particular attention has been given to the methods of evaluation of the taste-masking properties and the factors affecting the outcomes, such as the choice of the proper cyclodextrin or guest–host molar ratio. The conclusions of this review reveal that the application of CDs is not straightforward; nevertheless, this solution can be an effective, safe, and inexpensive method of taste masking for pharmaceutical purposes.

Taste masking of traditional Chinese medicines (TCMs) containing multiple bitter components remains an important challenge. In this study, berberine (BER) in alkaloids and phillyrin (PHI) in flavonoid glycosides, which are common bitter components in traditional Chinese medicines, were selected as model drugs. Chitosan (CS) was used to mask their unfriendly taste. Firstly, from the molecular level, we explained the taste-masking mechanism of CS on those two bitter components in detail. Based on those taste-masking mechanisms, the bitter taste of a mixture of BER and PHI was easily masked by CS in this work. The physicochemical characterization results showed the taste-masking compounds formed by CS with BER (named as BER/CS) and PHI (named as PHI/CS) were uneven in appearance. The drug binding efficiency of BER/CS and PHI/CS was 50.15 ± 2.63% and 67.10 ± 2.52%, respectively. The results of DSC, XRD, FTIR and molecular simulation further indicated that CS mainly masks the bitter taste by disturbing the binding site of bitter drugs and bitter receptors in the oral cavity via forming hydrogen bonds between its hydroxyl or amine groups and the nucleophilic groups of BER and PHI. The taste-masking evaluation results by the electronic tongue test confirmed the excellent taste-masking effects on alkaloids, flavonoid glycosides or a mixture of the two kinds of bitter components. The in vitro release as well as in vivo pharmacokinetic results suggested that the taste-masked compounds in this work could achieve rapid drug release in the gastric acid environment and did not influence the in vivo pharmacokinetic results of the drug. The taste-masking method in this work may have potential for the taste masking of traditional Chinese medicine compounds containing multiple bitter components. [ABSTRACT FROM AUTHOR]

Orally disintegrating tablets, over the years, have become the preferred alternative to conventional tablets and capsule dosage forms because of better compliance. These are suitable for special populations like pediatrics, geriatrics, patient with dysphagia, patients with hand tremors, patients with frequent traveling, etc. The focus of this research was to mask the unpleasant taste of type 2 antidiabetic drug "Pioglitazone Hydrochloride" followed by designing an orally disintegrating tablet of the same. Taste masking was accomplished using a pH-independent polymeric dispersion of ethylcellulose i.e. "Surelease E-7-19040" in combination with a Hypromellose-based ready-tocoat film coating system i.e. "Opadry YS-1-19025-A" in a different ratio. Uncoated powder, coated granules, and prepared tablets of Pioglitazone Hydrochloride were investigated for in-vivo taste evaluation and flow as well as compression behavior, Fourier Transform Infrared spectra, scanning electron microscopy, powder X-ray diffraction, and in-vitro dissolution, disintegration properties. The study demonstrated the use of 32 full factorial design study to identify optimal ratio of pore former in Surelease and Opadry polymeric coating combination to achieve desired taste masking of unpleasant Pioglitazone Hydrochloride without any impact on immediate release characterstic of the orally disintegtrating tablet formulation. It further demonstrated that, an increase in pore former concentration resulted in a lower rating by human volunteers indicating relatively more bitterness, however, an increase in percent weight gain resulted in a higher rating by human volunteers indicating efficient taste masking. [ABSTRACT FROM AUTHOR]