Taste Masking Research Articles

Enhancing Bioavailability with Oromucosal Products: Opportunities and Challenges

The oral mucosa offers an attractive route for the systemic delivery of drugs. The bioavailability and effectiveness of many drugs can be increased by administering them through the oral mucosa which bypasses the first-pass metabolism effect. This article will discuss principles, application areas, benefits & drawbacks as well as possible future perspectives for the study and development of oromucosal drug delivery systems. Among the critical benefits of administering drugs via the mouth is that it starts acting fast, is easily absorbed into the bloodstream, makes it easier for patients to follow their prescriptions as well and offers more freedom in terms of dosage control. The article emphasizes innovative technologies such as nanoparticulate formulations as well as microfabricated devices which are slated to improve drug targeting and delivery. It also touches on such related issues as taste masking, variability in bioavailability, and regulatory concerns.

Solubility and Taste Masked Behaviour of Cyclodextrin Molecular Inclusion Complex of Artemether

Artemether by forming a complex with β-cyclodextrine (βCD) is used to improve solubility and taste masked by the kneading method. Artemether with β-cyclodextrine complex prepared with βCD in a drug-polymer ratio 1:1 gave complete taste masking with the satisfactory result obtained in term of in-vivo and in-vitro evaluation. The standard calibration curve of Artemether shows a slope of 0.0154 and a correlation coefficient of 0.9992. Compatibility studies show that drugs are compatible with polymers. Solubility studies show that the solubility of drug are increased in Phosphate buffer 6.8 by successfully forming a complex with βCD. In-vitro dissolution results showed that a maximum of 97.05% of Artemether, drug release less than 15 minutes in formulation. The solubility of Artemether in saliva (PH 6.8) is 0.00735 mg/mL, After complex forming with β-cyclodextrin the solubility of (Artemether complex) is 0.124 mg/mL. In-vitro drug release investigation, taste masking occurs when the amount of drug substance in the dissolve medium is either not identified or is below the threshold for recognizing its flavor in the early time points (between 0 and 5 minutes). Taste masking ( Taste perception test) 11 volunteers were selected for this test, results show that complex is taste masked. Artemether with βCD complex is a hopeful method to augment the solubility, dissolution and taste masking of the drug.

Solubility and Taste Masked Behaviour of Cyclodextrin Molecular Inclusion Complex of Lumefantrin

Lumefantrine is an antimalarial drugs used especially for pediatric persons. β-Cyclodextrine is used to improve the taste of lumefantrine by forming complexes with them by the solvent evaporation method, respectively. β-Cyclodextrine prevent the release of drug in the saliva. Lumefantrine is a bitter drug. So masking of bitter taste in the formulation is a prerequisite as it improves the compliance of the patient and product value. Lumefantrine with β-cyclodextrin in a drug-polymer ratio 1:1 gave complete taste masking with a satisfactory result obtained in term of in-vivo and in-vitro evaluation visual inspection revealed that lumefantrine was yellow-crystalline. The melting point of lumefantrine was found to be 127℃, respectively. The standard calibration curve of Lumefantrine shows a slope 0.0108 and a correlation coefficient of 0.9997. Compatibility studies show that drugs are compatible with polymers. Solubility study show that the solubility of both drugs are increased in phosphate buffer 6.8 by successfully forming a complex with β-cyclodextrin. The solubility of lumefantrine in saliva (pH 6.8) is 0.408 mg/mL, after complex forming with β-cyclodextrine the solubility of (Lumefantrine complex) is 0.526 mg/mL. In an in-vitro drug release investigation, taste masking occurs when the amount of drug substance in dissolved media is either below the detection threshold for recognizing its taste or is undetectable in the early time points (between 0 and 5 minutes). Taste masking (Taste perception test) 11 volunteers are selected for this test, results show that complex is taste masked successfully. Lumefantrine with β-Cyclodextrine complex is a hopeful approach to enhance solubility, dissolution and drug taste.

Potential of Nitrofurantoin Cyclodextrin Nanosponge Complex to Enhance Solubility and Masking Bitter Taste

This study aimed to produce b-cyclodextrin (β-CD) based nanosponges (NS) loaded with nitrofurantoin (NFN) to improve oral bioavailability, solubility, and dissolution rate while concealing bitter tastes. The cross-linker diphenyl carbonate and β-CD were reacted in various ratios (1:1, 1:2, 1:4, 1:6, and 1:8) to produce NFN-loaded NS. The developed NS were evaluated for phase solubility study, particle size, drug loading, polydispersity index, scanning electron microscope (SEM), zeta potential, fourier transform infrared (FTIR), differential scanning calorimetry (DSC), a study of phosphate buffer at pH 7.2 for in-vitro release and taste masking ability in human volunteers. Pure NFN showed nearly 100 mcg/mL solubility in ditilled water while at 1:8 (β-CD: DPC) ratio the solubility was found to be 250 mcg/mL, i.e., nearly 2.5 fold enhancement in solubility was observed. The SEM of the NFN-loaded NS (1:8 β-CD: DPC ratio) showed highly spherical surface morphology. For formulation containing a 1:8 proportion of β-CD to DPC, the average particle size was measured at 324.78 ± 10.45 nm, possessing a low polydispersity index of 0.196 ± 0.054. It was found that the zeta potential’s value was -20.59 ± 0.4 mV, indicating sufficient electrostatic repulsion to maintain particle dispersion. FTIR, DSC study reveled excellent drug and excipient compatability. As compared to pure NFN, NFN-loaded NS showed faster release in pH 7.2 phosphate buffer. Research conducted in-vitro showed a gradual release of NFN from pure NFN throughout a two-hour period. The plain NFN suspension was found to have a pronounced bitterness. With 3.95 ± 0.57 as the average score, while the NFN nanosponges (1:8 ratio) had a mean bitterness score of only 0.10 ± 0.00. These findings suggest that the NFN (1:8 ratio) has the capacity to thoroughly cover up the bitter taste of NF.

Orodispersible Films: Current Innovations and Emerging Trends.

Orodispersible films (ODFs) are thin, mechanically strong, and flexible polymeric films that are designed to dissolve or disintegrate rapidly in the oral cavity for local and/or systemic drug delivery. This review examines various aspects of ODFs and their potential as a drug delivery system. Recent advancements, including the detailed exploration of formulation components, such as polymers and plasticizers, are briefed. The review highlights the versatility of preparation methods, particularly the solvent-casting production process, and novel 3D printing techniques that bring inherent flexibility. Three-dimensional printing technology not only diversifies active compounds but also enables a multilayer approach, effectively segregating incompatible drugs. The integration of nanoparticles into ODF formulations marks a significant breakthrough, thus enhancing the efficiency of oral drug delivery and broadening the scope of the drugs amenable to this route. This review also sheds light on the diverse in vitro evaluation methods utilized to characterize ODFs, ongoing clinical trials, approved marketed products, and recent patents, providing a comprehensive outlook of the evolving landscape of orodispersible drug delivery. Current patient-centric approaches involve developing ODFs with patient-friendly attributes, such as improved taste masking, ease of administration, and enhanced patient compliance, along with the personalization of ODF formulations to meet individual patient needs. Investigating novel functional excipients with the potential to enhance the permeation of high-molecular-weight polar drugs, fragile proteins, and oligonucleotides is crucial for rapid progress in the advancing domain of orodispersible drug delivery.

Advanced Tablet Coating Technique: Dip Coating Technique

The dip coating technique is a widely used method in thin film deposition, particularly in industries like electronics, optics, and materials science. This process involves immersing a substrate material into a liquid solution or suspension (the coating material) and then slowly withdrawing it at a controlled speed. As the substrate is pulled out, a thin film of the coating material adheres to its surface due to capillary action, forming a uniform layer upon subsequent drying or curing. Factors like viscosity, surface tension, and concentration of the coating solution, as well as withdrawal rate and drying techniques, are carefully controlled to achieve the desired film characteristics. This technique offers advantages such as simplicity, cost- effectiveness, and scalability for large-scale production. However, challenges related to controlling film thickness, achieving uniformity, and handling high-viscosity coatings exist and require precise process optimization(1). In this process, the cores are held in a suitable device (e.g. baskets) and dipped into the coating solution and then dried carefully to avoid sticking to each other. For better or heavier coats, the dipping and drying process may need to be repeated multiple times one after the other. There are several dipping arrangements available, some of which include small suction tubes that hold the tablets apart until the drying process is complete, after which you can add more tablets or start the recoating cycle(2). The coating techniques used in tablet production greatly influence the aesthetic qualities such as colour, texture, mouthfeel, and taste masking. However, these techniques have certain limitations and drawbacks. To overcome these limitations, Tablet in Tablet is considered one of the best alternatives. The objective of this study is to comprehensively review the formulation, characterization, and challenges associated with the development of Tablet in Tablet dosage form. Currently, there are only a few patents filed or granted on this topic, including the Tablet in Tablet of cyclophosphamide and capecitabine. Our focus is to provide the rationale behind the development of such dosage forms (3).

Taste Masking of Bitter Drugs in Pharmaceutical Suspension: A Review

One of the most vital factors in the formulation of medications for children, the elderly, immobile patients, and uncooperative patients is taste, which is mainly controlled by taste buds in the tongue. The biggest challenge for the compounding scientists is to mask the unpleasant and bitter tastes of the pharmaceuticals, which prevent patients from obtaining the full therapeutic benefit of their prescription. In order to increase patient compliance, which ultimately determines the product's economic success, it may be possible to mask the bitter taste of medications. Inclusion complexation, the use of ion exchange resin, mass extrusion, solid dispersions, coating granulation, spray drying, microencapsulation, liposomes, emulsions, and gel formation effervescence are current methods of flavour masking. Active pharmaceutical ingredient (API) taste masking is an area that is constantly developing because of unusual excipients and a variety of techniques.

Unmet technological demands in orodispersible films for age-appropriate paediatric drug delivery.

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.

Investigation of bitter taste masking in the development of functional beverages based on sedative collection

The article considers the possibility of masking bitter taste in the development of a functional drink based on sedative collection and juices: grape and cherry, used as masking agents. Sensory studies were conducted on the formulation of the proposed beverages. In the study, respondents were asked to analyze samples with cherry and grape juices without added sugar with successively decreasing concentrations of sedative levy from 25 to 5%, then samples with added sugar and answer the question whether an unpleasant bitter taste and herbal aroma were present and at which sample the bitter taste ceased to be felt. The findings showed that the addition of sugar to the beverages altered the taste perception thresholds in the direction of increasing the concentration of the sedative collection decoction. Without the addition of sugar, the bitter taste ceases to be perceived at 15% of the functional additive using grape juice and at 20% using cherry juice. With the addition of sugar, the bitter taste was no longer felt at 20% of the functional additive with grape juice and 25% with cherry juice. Studies were conducted to identify the associative series: regarding with which fruit/berry the flavor of the beverage in general is associated. When analyzing the obtained results it was revealed that respondents accurately associated the samples of the row with cherry juice with cherry aroma (88%), when using grape juice 31% of respondents associated with strawberry aroma and 25% with cranberry aroma. As a result of the behavioral study it can be concluded that when developing a functional drink enriched with sedative collection it is possible to use cherry and grape juices with the concentration of functional ingredient 5 - 20% with the discretion of adding 5% in each flavor range

Review of Applications of Cyclodextrins as Taste-Masking Excipients for Pharmaceutical Purposes.

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 Cetirizine Hydrochloride using Ion-exchange Resins

Aim: The scope of the study is to determine the exact drug content present in the dry resinate and the utilization of ion-exchange resin in taste masking highly bitter cetirizine hydrochloride (CTZ). The Amberlite® IRP-69 cross-linked polystyrene was used. Objective: The objectives of this study are drug loading, drug–resin ratios, effect of particle size determination, and qualitative evaluation of taste masking ion-exchange resins. Background: The resinate (drug–resin complex) preparation process was completed by batch method in the ratio of 1:1, 1:2, and 1:3. The loaded drug amount in the resin was evaluated spectrophotometrically by measuring the remaining drug to be loaded in the solution at 278nm. Different sieve sizes of Amberlite® IRP-69 resins were employed to determine the effect of the particle size in drug loading and drug releasing profiles in simulated gastric fluid without enzymes. The X-ray diffractograms of cetirizine hydrochloride, Amberlite® IRP-69, and a mixture of cetirizine hydrochloride with resins (resinate) were obtained by using an X-ray diffractometer. Results: Resinates were developed by using single-batch and double-batch methods. Both of them are giving almost the same results of drug loading into ion-exchange resins. We selected 1:1 drug–resin ratio to see the effect of the particle size on the rate and extent of drug loading and drug releasing from the complex. In the 1:1 drug-to-resin ratio, almost 78% of the drug was involved in the complex after 24 hours; in the case of 2:1 and 3:1 ratios, only 49% and 25% of the drug were involved in the complex, respectively. Conclusion: Among many taste masking methods, the formation of resinates with an ion-exchange resin is simple and inexpensive. The present work reveals that the degree of bitterness of cetirizine hydrochloride is reduced to zero by strong cation-exchange resin. The present study deals on the scope of utilizing ion-exchange resins in taste masking cetirizine hydrochloride (CTZ), a highly bitter drug.

Formulation and In Vitro Evaluation of Taste- Masked Prednisolone Orodispersible Tablets

Background: prednisolone is a corticosteroid with a very bitter taste acts as anti- anti-inflammatory and immune suppressant drug and it is used at any age. Objective: To improve patient compliance by masking the bitter taste of the drug to be delivered as an orodispersible tablet. Methods: External ionic gelation using sodium alginate (0.5%w/v) and calcium chloride (1% w/v) in presence of 0.5% w/v carbopol 940 was used to prepare taste masked beads loaded with prednisolone to be compressed as orodispersible tablets. Results: The bitter taste of was masked by preparing beads composed of 1:1:1 (sodium alginate: Carbopol 940: prednisolone) which released only 0.77 % of the drug in pH 6.8 (pH of oral cavity). The ODT prepared by direct compression using taste masked beads equivalent to 5 mg PRD, 3% crospovidone, 2% PVP, 1% talc, 1% magnesium stearate and combination of Avcil® PH 102 and mannitol at (1:1) ratio was the optimum formula (T6) with hardness of 3.9± 0.32 kg, , friability 0.45%, thickness 2.5 ± 0.05 mm, % drug content 98.2% ± 1.8, wetting time 18.7 ± 1.3 sec, water absorption 41 ± 2.1%, disintegration time 15.3 ± 0.5 sec. and released only 0.75% ± 0.01 of PRD in an oral pH of 6.8 within one minute (indicating good taste masking). Its release in the stomach (pH 0.1N HCl) and intestine (pH 6.8) was continued for up to two hours. Conclusion: it can be concluded that the external ionic gelation method successfully masked the bitter taste of prednisolone and can also be formulated as taste-masked orodispersible tablets by the direct compression method. Received: Jan. 2023 Accepted: May 2023 Published: Oct.2023

Formulation development, in vivo bioequivalence and pediatric PBPK modeling studies of taste-masked ciprofloxacin chewable tablets

A taste-masked chewable tablet of ciprofloxacin using ion exchange resin Kyron T-134 for enhancing compliance for the paediatric population was developed. The drug-to-resin ratio was optimized for maximum taste masking by studying the effects of soaking time (X1) and mixing time (X2) on complexation (%) using Central Composite Rotatable Design (CCRD). The resin complexes were characterized by bitterness score, DSC, FTIR, and PXRD. The complex was further formulated and optimized into chewable tablets through full factorial design, The optimized formulation was subjected to a bioequivalence study, and a virtual approach of PBPK modelling was adapted to predict the pharmacokinetics of the drug in the paediatric group. The drug resin ratio of 1:1.5 yielded an optimum drug loading of 99.05%. The optimized formulation shows minimum disintegration time with more than 99% drug release within 30 min. The formulation F-9 was found to be bioequivalent with a geometric mean ratio of Cmax, Tmax, AUC0–t, and AUC0–∞ within 90% CI. It was concluded that quality by design approach can successfully be applied to optimize the drug resin ratio and PBPK modeling is a successful predictive tool for estimating the pharmacokinetics of ciprofloxacin HCl in the paediatric population.

A Bird Eye View on Effervescent Drug Delivery System

Effervescent drug delivery systems (EDDS) have gained significant attention in the pharmaceutical industry due to their unique characteristics and potential advantages over conventional dosage forms. This comprehensive review aims to provide an in-depth understanding of EDDS, including their formulation strategies, underlying mechanisms, and diverse applications in drug delivery. EDDS are effervescent dosage forms that release drugs upon water dissolution, leading toward carbon dioxide gas generation. The effervescence, resulting from the reaction between an acid and a base, facilitates rapid drug dissolution and enhances drug bioavailability. The primary components of an EDDS include an active pharmaceutical ingredient (API), effervescent agents (e.g., organic acids and bases), binders, disintegrants, and other excipients. Effervescent tablets, granules, powders, and effervescent-coated dosage forms are commonly employed formulations. Several factors, such as pH, temperature, solubility, and particle size, influence the drug’s effervescence process and subsequent release kinetics. The drug release mechanisms from EDDS can be attributed to various phenomena, including effervescence-driven disintegration, gas evolution, and solubilization. The effervescence-induced carbon dioxide bubbles mechanically disrupt the dosage form, leading to enhanced drug dissolution and subsequent release. Additionally, the carbon dioxide gas acts as a propellant, providing rapid drug delivery and potentially improving patient compliance. EDDS find applications in diverse therapeutic areas, including analgesics, antacids, dietary supplements, and antiviral agents. They offer several advantages, such as improved drug stability, enhanced bioavailability, increased patient convenience, and ease of administration, particularly for populations with swallowing difficulties. Furthermore, EDDS can be tailored to achieve controlled release, targeted drug delivery, and taste masking through appropriate formulation modifications. However, challenges associated with EDDS include their sensitivity to environmental conditions, potential drug degradation during effervescence, and the need for specialized packaging to maintain stability. The selection of suitable effervescent agents, excipients, and manufacturing processes is crucial to overcome these limitations and ensure consistent product performance. In conclusion, effervescent drug delivery

Bioelectronic Tongue for Identifying and Masking Bitterness Based on Bitter Taste Receptor Agonism and Antagonism

AbstractBitterness elicits unpleasant sensations in humans, which can hinder the acceptance of foods and medication adherence. Therefore, identifying and masking bitter tastes is crucial for developing palatable foods and promoting medication compliance in the food and pharmaceutical industries. To achieve this, employing agonism and antagonism of bitter taste receptors as effective strategies at the molecular level is essential. In this study, a bioelectronic tongue is developed to characterize the agonism and antagonism of bitter taste receptors. The human bitter taste receptors hTAS2R16 and hTAS2R31 are produced using an Escherichia coli expression system and reconstituted into nanodiscs (NDs). Subsequently, hTAS2R16‐ and hTAS2R31‐NDs are immobilized on the surface of graphene field‐effect transistors (FETs) to construct bioelectronic tongues. The developed system sensitively detected the bitter agonists, salicin and saccharin, at concentrations as low as 100 fM, with high selectivity in real‐time. The dose‐dependent curves shifted and K values decreased by the antagonists of hTAS2R16 and hTAS2R31, indicating antagonism‐based masking of bitter taste. Therefore, the developed bioelectronic tongue holds promise for identifying bitter tastes and evaluating the masking of bitterness based on the agonism and antagonism of hTAS2Rs.

Mucoadhesive Drug Delivery Systems for Pediatric and Geriatric Patients

A mucoadhesive drug delivery system (MDDS) has been a smart approach to the delivery of drugs at the target site. In MDDS mucus membrane and type of polymer plays an important role in the mucoadhesion phenomenon. To explain the mechanism behind mucoadhesion, various theories have been proposed such as electronic, adsorption, wetting, diffusion, and fracture theory. MDDS has been beneficial to some special patients, preferably pediatric and geriatric. Several challenges such as taste masking, dose determination, dosage form spitting, target delivery, the bioavailability of the drug, adverse drug reaction, toxicity, etc. are faced while developing any delivery system for these special patient populations. Keeping these challenges in mind several researchers have attempted to design and formulate MDDS according to their convenience. The current review focuses on a basic overview of mucoadhesion, various theories of mucoadhesion, and mucoadhesive polymers. The later part of the review focuses on the MDDS for pediatric and geriatric patients with their significance. Various patented formulations and clinical trials going on for these populations have also been discussed.

DEVELOPMENT AND EVALUATION OF RAMOSETRON HYDROCHLORIDE MOUTH DISSOLVING THIN FILM FOR ENHANCED THERAPEUTIC EFFICACY AND PALATABILITY

Objective: Many people have difficulties in swallowing traditional dosage forms such as tablets and capsules. The goal of this study was to develop the mouth-dissolving thin film of Ramosetron HCl (RH) for quick onset of action in the treatment of vomiting and irritable bowel syndrome, with the added benefit of disguising the bitter taste of RH. Methods: The solvent-casting approach was employed to formulate mouth dissolving thin film. The effect of variable concentrations and different grades of hydrophilic polymer HPMC (E5, E15 and E50), and plasticizers like glycerol and PEG 400 on disintegration time, drug release, thickness, tensile strength, percent elongation, folding endurance, and on appearance were studied. The optimized batch was kept for stability study at40±2 °C/75±5% RH for 30 d. Results: The formed films were transparent with a smooth surface texture. The thickness, weight variation, drug content and pH of the surface were within acceptable limits. Tensile strength and folding endurance values demonstrated adequate mechanical strength. In 45 seconds, the formulation F6 comprising HPMC E5 (150 mg) and HPMC E15 (150 mg) with PEG 400 (0.4 ml) disintegrated. The F6 formulation released 98.78±0.96 %drug in 8 min and considered as optimal formulation. The taste masking of drug was evaluated by a taste perception study using volunteers. The optimized batch was found to be stable at 40±2 °C/75±5% RH for 30 d. Conclusion: The concentration of hydrophilic polymers and plasticizers had a significant effect on the formulation and assessment characteristics of thin film. Mannitol assisted in masking the bitter taste of RH.

Investigation of the effects of some process variables on the Azithromycin Microencapsulation by the Quasi-Emulsion Solvent Evaporation Method

The aim of the present work was to identify the optimum formulation parameters required to achieve a maximum production yield and entrapment efficacy for Azithromycin-loaded Ethylcellulose microparticles for taste masking of Azithromycin (AZI). Quasi-emulsion solvent evaporation method was employed using Ethylcellulose. Several factors that influence the microparticles such as polymer-to-drug ratio, the inner phase volume (DCM), and the emulsifying agent concentration (PVA) were studied to determine their effects on the production yield, entrapment efficiency, and particle size of microparticle formulations. The formula F3 that provided the highest yield and entrapment efficiency (66.6±0.3%, 86.42±0.05% respectively) was evaluated using Scanning electron microscopy (SEM), Fourier transform infrared (FT‑IR), and Differential scanning calorimetry (DSC). Taste masking assessment performed in vitro. FT‑IR study showed that there was no interaction occurring between azithromycin and ethylcellulose. DSC confirmed the conversion of azithromycin from crystalline phase to amorphous phase and entrapped inside the microparticles. SEM micrographs revealed that microparticles were spherical in shape with a porous nature, where no drug crystals on the surface could be observed, indicating an encapsulation of AZI inside the polymeric matrix. In vitro, the taste assessment revealed no azithromycin release in salvia pH which could effectively mask the bitter taste of AZI.

Formulation Optimization and Evaluation of Novel Oro-dispersible Tablet of Bilastine

The current study focuses on the development, optimization, and assessment of bilastine orodispersible tablets (ODTs) for the treatment of allergic disorders such as rhino-conjunctivitis and urticaria flavour concealed by an organoleptic technique. The formulation was optimized based on the direct compression method by the use of various super disintegrants such as cross povidone, sodium starch glycolate and croscarmellose sodium. The excellent product performance of ODTs in terms of disintegration time and in-vitro drug release may be achieved by varying the amount of super disintegrants. The direct compression approach was used to create novel anti-histamine Orodispersible tablets of bilastine. Design expert software was used to create nine formulations (BLS1-BLS9) by altering super disintegrant concentrations in order to optimise the optimal formulation using 32 factorial design and central composite design in the quadratic model (version 13.0.5.0). Pre-Compression studies like bulk density, tapped density, angle of repose, carr's index, Hausner’s ratio to note flow properties of powder and compatibility such as Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were performed to check any interaction between drug and various super disintegrant. The hardness, thickness, diameter, weight variation, friability, disintegration time, dissolution studies, wetting time, and uniformity of content of formulated ODTs were all evaluated. All the results were within the acceptable pharmacopeial limits and were evaluated statistically by using one-way ANOVA test. From the result, BLS8 was observed optimized formulation prepared by taste masking by an organoleptic method as a novel technique using direct compression as conventional technology containing a combination of various sweetening and flavoring agents such as orange and peppermint flavor.

Formulation and evaluation of taste-masked oral disintegrating tablet containing tolterodine-loaded montmorillonite.

The present study aimed to obtain a taste-masked oral disintegrating tablet (ODT) containing tolterodine tartrate (TT) intercalated into montmorillonite (MMT). 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. 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. MMT-ODT could be a suitable vehicle for the taste masking of TT, with the potential for use in patients with swallowing problems.