Dispersible Tablets Research Articles

Evaluation of two different orally disintegrating tablet formulations containing flurbiprofen inclusion complex and its solid dispersion

Purpose: To prepare orally dispersible tablet formulations (ODTs) by increasing the solubility of flurbiprofen (FB), which has low water solubility. 
 Methods: The ODTs were prepared using direct compression method the inclusion complexes and solid dispersions with the highest solubility were further evaluated. Flurbiprofen, polyvinylpyrrolidone (PVP) solid dispersions were blended together by solvent evaporation method, while the inclusion complexes were co-formulated with beta cyclodextrin (β-CD) by kneading at three different ratios. The ODTs were characterized by differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR) and for their micromeritic properties. In addition, the solubility properties of the inclusion complexes and solid dispersions in distilled water were compared with the solubility of flurbiprofen. 
 Results: The highest solubility value of PVP-FB solid dispersions was found at 1:6 (0.501 mg/mL) and for FB β-CD inclusion complex at 1:2 (0.701 mg/mL). Angle of repose ranged from 28.09 – 32.15 (o); Carr’s index from 7.59 to 10.01; and Hausner’s ration from 1.05 – 1.15. DSC and spectral studies indicate that FB did not chemically interact with either PVP or β-CD. 
 Conclusion: Orally dispersible tablets containing flurbiprofen β-CD complex exhibit significantly higher bioavailability than the drug alone due to its increased solubility. 

Optimization of migraine attacks relief

On December 24, 2022, in Moscow an interdisciplinary Council of Headache Experts, held under the auspice of the interregional public organization “Russian Society for the Study of Headache”, discussed the key problems of effective treatment of a migraine attack and the possibilities of a specific drug Kaporiza® (rizatriptan). Despite the development of strategies for the relief of migraine attacks and the effectiveness of triptans as first-line therapy, the choice of a specific drug in accordance with the individual clinical profile of the patient is difficult due to the existence of drugs in various forms (standard tablets, oral dispersible forms, injections, nasal sprays, rectal suppositories). Rizatriptan in the form of an orally dispersible tablet (ODT) has a number of advantages: high bioavailability, fast onset of action, and ease of use. Therefore, Kaporiza® (rizatriptan ODT) may be recommended as a priority therapy for all migraine patients who prefer the dispersible tablet form and who experience symptoms of nausea and vomiting, as well as for patients who have experience of poor efficacy and/or poor tolerability of other triptans. The Expert Council recommends to include rizatriptan ODT in the next edition of the clinical guidelines for the diagnosis and treatment of migraine as a first-line agent with Level A evidence.

A review on co-processed excipients used in direct compression of tablet dosage form

Co-processed excipients may enhance functionality and reduce drawbacks of traditional excipients for the manufacture of tablets on a commercial scale. The following study aimed to characterize a range of co-processed excipients that may prove suitable for dispersible tablet formulations prepared by direct compression. The dosage form that is used the most is tablets. Their accessibility, simplicity of administration, consistency, and affordability are advantages. Direct compression is the most straightforward method for making tablets, despite the fact that it comes with several challenges, including those connected to the homogeneity and mass variation of the content, disintegration, dissolution, and the radial hardness of the tablets. In today's world, "co-processed excipients," which include frequently processed mixtures of fillers, binders, disintegrants, lubricants, and other excipients, are becoming more popular. Spray drying, fluid bed granulation, wet granulation, melt granulation, dry granulation, and co-crystallization are used to create these mixes. This review article lists technologies, co-processed excipients that are commercially available, and excipients that are typically utilized to make them.

Preparation and evaluation of ciprofloxacin solid dispersion tablets developed from stearic acid, Polyethylene Glycol 4000 and Soluplus

Ciprofloxacin is a fluoroquinolone antibiotic with a broad spectrum of activity used for the treatment of various bacterial infections and is characterized by poor aqueous solubility and low permeability. The aim of this study is to formulate and characterize ciprofloxacin solid dispersions using hydrophilic and lipophilic matrices for improved product qualities and drug delivery. Ciprofloxacin hydrochloride tablets were formulated as solid dispersions by melting and solvent evaporation in tablet moulds using varying concentrations of stearic acid (10-40 %w/w), Polyethylene glycol 4000 (PEG 4000) (10-40 %w/w) and Soluplus® (10-20 %w/w as ethanolic solution) as components. The prepared tablets were evaluated for weight uniformity, friability, hardness, Fourier transform-infrared spectroscopy (FT-IR), moisture uptake, swelling index, disintegration time and dissolution rate, using standard methods and optimization techniques. The results showed uniform solid dispersion weights with friability, hardness, moisture uptake and swelling index of 0.4-0.5%, 3.0-7.5 kgf, mostly <20% and 1-71%, respectively. The formulations were chemically stable with no transformational interactions between components. Formulations without stearic acid disintegrated within 30 min whereas those containing the lipid broke up after more than 1 h. Drug release studies showed high immediate release in tablets without stearic acid but with cumulative steady state release higher in formulations with 10 %w/w Soluplus and different concentrations of stearic acid and PEG 4000. In conclusion, ciprofloxacin was presented as solid dispersion tablets with modified physicochemical attributes for improved drug delivery.
 Keywords: Ciprofloxacin; solid dispersion; drug delivery

A Brief Introduction on Oro Dispersible Tablets

Oro dispersible tablets (ODTs), which have improved solubility and stability over the past three decades, have drawn a lot of interest as a superior alternative to traditional tablets and capsules. ODTs—solid dosage forms with medications that dissolve on the tongue fast, usually in a few seconds. New ODT technologies answer a wide range of pharmaceutical preparations and patient needs, to enhance the lifecycle management to straightforward dosage regimen for dysphagic, children, old, and mentally imbalanced patients. Methods for administering orally dispersible drugs are frequently used to improve patient compliance and bioavailability. Researchers in academia and business have been motivated by this to create novel technologies and orally disintegrating formulations in this field. This article's main objective was to cover the development of ODTs, formulation concerns, novel oral dispersible technology, different types of methodology to evaluate, the selection of drug candidates, and novel possibilities in future.

Retrospective analysis of cefpodoxime proxetil dispersible tablets in the treatment of respiratory tract infection in children and study of the antibacterial effect of cefpodoxime proxetil nanoemulsion

A study was conducted to determine the efficacy and safety of cefpodoxime proxetil (CFP) dispersible tablets in the treatment of respiratory tract infection in children and to analyze the antibacterial effect of cefpodoxime proxetil nanoemulsion (CFP-NE). A retrospective analysis was conducted on 118 children with upper respiratory tract infection who received antibiotic treatment between March 2018 and March 2021. The control group was treated with cefradine and the CFP group was treated with CFP dispersible tablets. The serum indexes and bacteriological test results of the two groups were collected before and after treatment, and the bacterial clearance rate, infection control, and occurrence of adverse reactions were observed and compared between the two groups. Cefpodoxime proxetil nanoemulsion (CFP-NE) was prepared and its surface characteristics were observed. CFP-NE and CFP were used to treat infections by multiple strains of bacteria and the antibacterial effect and minimum inhibitory concentration (MIC) of CFP-NE were observed. The bacterial strain clearance rate of the CFP group was 96.2% and the total infection control rate was 94.92%. The bacterial strain clearance rate of the control group was 88.9% and the total infection control rate was 81.36%. Serum index detection showed that antibiotic treatment could reduce serum indexes of amyloid A, C-reactive protein, procalcitonin, and other indexes and CFP had better efficacy. There were only four cases of adverse reactions after treatment with CFP, a result similar to that of other antibiotics. The prepared CFP-NE system was stable, the particles were uniform, and the diameter of the inhibitory zone against pathogenic Escherichia coli and Salmonella was larger than that of the CFP group. The MIC of CFP-NE was significantly lower than the MIC of the CFP group (P < 0.05). CFP dispersible tablets are safe and effective for the treatment of respiratory tract infection in children and the antibacterial effect of CFP-NE is greater than that of CFP.

Formulation Development and Evaluation of Taste-masked Moxifloxacin Dispersible Tablets for the Treatment of Pediatric Tuberculosis

Moxifloxacin (MOX) is a fluoroquinolone antibiotic, a second-line anti-TB drug widely used in the treatment of multidrug-resistant tuberculosis (MDR TB) and drug-susceptible TB. MOX have taste and smell issues with low patient compliance, especially in the pediatric population. MOX taste-masked dispersible tablets were developed by direct compression method using mannitol, aspartame as a sweetening agent and lemon flavor as a flavoring agent. The prepared granules were evaluated for flow properties and compressed tablets for hardness, friability, content uniformity, weight variation, DT and in-vitro drug release. Instrumental analysis like FTIR, DSC and XRD was also performed. The flow properties of the granules of batch F6 were found to be excellent based on the results obtained. The weight variation and content uniformity of the tablets was found to be excellent F6 due to the excellent flow properties of the granules. All of the tablets in the study disintegrated between 22 (F6) to 135 seconds (F1), meeting the official requirement (3 minute) for dispersible tablets. The optimized batch showed complete drug release within 10 minutes time period. The FTIR and DSC study found no incompatibility between the drug excipients. The MOX in the final formulation was present in crystalline form, as shown by XRD. The dispersible MOX tablets could be a better option for treating pediatric TB.

Meeting Challenges of Pediatric Drug Delivery: The Potential of Orally Fast Disintegrating Tablets for Infants and Children.

A majority of therapeutics are not available as suitable dosage forms for administration to pediatric patients. The first part of this review provides an overview of clinical and technological challenges and opportunities in the development of child-friendly dosage forms such as taste masking, tablet size, flexibility of dose administration, excipient safety and acceptability. In this context, developmental pharmacology, rapid onset of action in pediatric emergency situations, regulatory and socioeconomic aspects are also reviewed and illustrated with clinical case studies. The second part of this work discusses the example of Orally Dispersible Tablets (ODTs) as a child-friendly drug delivery strategy. Inorganic particulate drug carriers can thereby be used as multifunctional excipients offering a potential solution to address unique medical needs in infants and children while maintaining a favorable excipient safety and acceptability profile in these vulnerable patient populations.

Formulation and in vitro Evaluation of Taste-Masked Orodispersible Tablets of Levocetirizine Dihydrochloride

The main aim was to formulate and evaluate and optimize taste- masked orodispersible tablets of Levocetirizine Dihydrochloride, a drug used in Allergic Rhinitis was prepared by direct compression method. The study involved different excipients which were used for the formulation and tested for their compatibility with Levocetirizine Dihydrochloride by the FT-IR studies. Based on the results of FT-IR studies, most of the excipients were found to be compatible with Levocetirizine which was used for the preparation of Levocetirizine oral disintegrating tablets. Levocetirizine Dihydrochloride is bitter in taste so the Tulsian-339 (ion exchange resin) was used to mask the taste to formulate an orodispersible dosage formulation using drug resin complex. Nine batches (F1-F9) of oro dispersible tablets of Levocetirizine Dihydrochloride were prepared by using super disintegrants like Sodium starch glycolate, Avicel PH102 and Low Hydroxy Propyl Cellulose in variable concentrations along with excipients for the development of optimized formulation. All formulations were subjected to evaluation studies of drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, dispersion time, hardness, friability and thickness uniformity. The tablets were disintegrated in vitro within 28-38 seconds, the complete drug was released from the tablets within 15 min. The results showed that Levocetirizine dihydrochloride was successfully formulated into an orodispersible dosage form.

Interventions for improving adherence to iron chelation therapy in people with sickle cell disease or thalassaemia.

Interventions for improving adherence to iron chelation therapy in people with sickle cell disease or thalassaemia.

Stable, compounded bedaquiline suspensions to support practical implementation of pediatric dosing in the field.

BACKGROUND: Bedaquiline (BDQ) tablets are indicated as part of a combination regimen for the treatment of multidrug-resistant TB in adults, adolescents and children. A dispersible tablet formulation is now approved but is not currently available in all settings. The aim of this study was to develop stable extemporaneous liquid formulations of BDQ that can be stored at room temperature or 30°C for several weeks, to support pragmatic pediatric dosing in the field and reduce wastage.METHODS: BDQ tablets were suspended in simple syrup and a sugar-free vehicle. Each 20 mg/mL formulation was stored at room temperature or 30°C for 30 days in amber dispensing bottles. Appearance, BDQ potency, pH and microbial counts were determined on Days 0, 15 and 30.RESULTS: The BDQ potency in both formulations remained at 98-101% of the theoretical concentration for 30 days. The appearance, pH and microbial count of sugar-free formulation did not change during the 30-day storage. The simple syrup formulation was stable for 15 days as microbial growth was observed on Day 30.CONCLUSIONS: BDQ may be prepared in syrup or sugar-free suspensions: syrup suspensions can be stored for 15 days at room temperature and 30C, whereas sugar-free suspensions can be stored for 30 days at room temperature and 30C. This information will support practical BDQ dosing for children in the field.

Relative bioavailability of delamanid 50 mg tablets dispersed in water in healthy adult volunteers.

Delamanid is a novel drug for the treatment of drug-resistant tuberculosis, manufactured as 50-mg solid and 25-mg dispersible tablets. We evaluated the effects of dispersing the 50-mg tablet, focusing on the relative bioavailability. Delamanid, 50-mg tablets administered dispersed vs swallowed whole, was investigated in a phase I, four-period, crossover study. Two of three dose strengths of delamanid (25, 50 or 100 mg) were given to healthy adult participants, in both whole and dispersed forms, with a 7-day washout period. Blood samples were collected over 168 h after each dose. Delamanid and its metabolite DM-6705 were analysed with a validated liquid chromatography tandem mass spectrometry assay. The pharmacokinetics of both analytes were analysed using nonlinear mixed-effect modelling. Palatability and acceptability were determined using a standardized questionnaire. Twenty-four participants completed the study. The bioavailability of dispersed tablets was estimated to be 107% of whole tablets, with a 90% confidence interval of 99.7-114%, fulfilling bioequivalence criteria. The two formulations were not significantly different regarding either bioavailability or its variability. Bioavailability increased at lower doses, by 34% (26-42%) at 50 mg and by 74% (64-86%) at 25 mg, relative to 100 mg. The majority of participants (93%) found the dispersed formulation acceptable in palatability across all delamanid doses. Dispersed 50-mg delamanid tablets have similar bioavailability to tablets swallowed whole in adult volunteers. This can be an option for children and other patients who cannot swallow whole tablets, improving access to treatment.

Formation of Dispersible Taohong Siwu Tablets.

Here, we optimize the process used to formulate and prepare dispersible Taohong Siwu tablets and provide a foundation for expanding their clinical application. Taking dispersion uniformity and disintegration time as the indices for investigation, we used a single-factor test to match and filter the excipient categories for Taohong Siwu tablets. The formulation was optimized by an orthogonal test design. The content and dissolution rates of the effective substances in dispersible Taohong Siwu tablets when prepared with optimized prescriptions were determined by ultra-high performance liquid chromatography (UPLC), and the optimal preparation process was determined. The optimal composition for dispersible Taohong Siwu tablets was 17% Taohong Siwu extract powder, 1% magnesium stearate, 49% microcrystalline cellulose, 20% cross-linked polyvinylpyrrolidone, and 13% sodium carboxymethyl starch. When dispersible Taohong Siwu tablets were prepared by direct compression and the optimized prescription powder was uniformly dispersed within 3 min, the dissolution rate reached more than 90% within 50 min.When prepared according to the optimized methods,dispersible Taohong Siwu tablets disintegrate rapidly in water with good dispersion uniformity and controllable quality.

A REVIEW ON: FORMULATION, TECHNOLOGICAL AND BENEFICIAL ASPECTS OF ORAL DISPERSIBLE TABLETS

This review is about oral dispersible tablets a novel approach in drug delivery systems that are now a day’s more focused in formulation world, and laid a new path that, helped the patients to build their compliance level with the therapy, also reduced the cost and ease the administration especially in case of pediatrics and geriatrics. Oral dispersible tablets are advantageous for pediatric, geriatric mentally ill, nausea patients who have difficulty in swallowing conventional tablets and capsules. Using various excipients, evaluation tests marketed formulation and drugs used in the research area. The advantages of mouth dissolving dosage form are increasingly being recognized in both, industry and academia. Their growing importance has been underlined recently when European Pharmacopoeia adopted the term “Oral dispersible Tablet” as tablet that is to be place in the mouth where it disperses rapidly before swallowing. When ODTs are put on tongue they disintegrate instantaneously, releasing the drug which dissolve or disperses in the saliva. Some drugs are absorbed from the mouth, pharynx and esophagus as the saliva passes down in to the stomach. In such cases, bioavailability of a drug is significantly greater than those observed from conventional tablet dosage form.

Extemporaneously compounded liquid formulations of clofazimine.

BACKGROUND: Clofazimine (CFZ) is routinely used worldwide for the treatment of leprosy and TB. However, no liquid or dispersible tablet formulations of CFZ are currently available commercially for patients with challenges ingesting soft gelatin capsules or solid formulations. The aim of this research was to develop stable extemporaneous liquid formulations of CFZ that can be stored at room temperature for several weeks to enable practical dosing in the field. METHODS: Two formulations were prepared in syrup and sugar-free vehicles with CFZ tablets using a simple method that can be used in a routine pharmacy. Suspensions were stored at room temperature and at 30°C for 30 days. Formulation aliquots were tested on Days 0, 15 and 30 for appearance, pH, potency and microbial counts. RESULTS: Appearance remained unchanged during storage. The pH of both formulations was between 4.0 and 6.0. Potency was between 90% and 110% for 30 days in the syrup formulation and for 15 days in the sugar-free formulation. Microbial counts met United States Pharmacopeia 1111 limits for oral aqueous liquids and specific organisms were absent. CONCLUSIONS: A simple field-friendly method was successfully developed for the preparation of CFZ liquid formulations using commonly available ingredients. This will permit practical dosing and titration for children and other patients with swallowing challenges.

DISPERSIBLE TABLET AS A FORMULATION FOR ORAL DRUG DELIVERY SYSTEM

Dispersible drug delivery methods are widely utilized nowadays to increase patient compliance and bioavailability. Overthe past years, dispersible tablets have gained a lot of attention as a preferable alternative to conventional tablets andcapsules due to increased patient compliance, improved solubility, and improved stability profiles. Dispersible tabletsmay be a better option, particularly for medications that react negatively to GI fluids, to cover up a medication's bittertaste, and for patients, who fall into the paediatric or geriatric categories, are bedridden, have recently undergonesurgery, or may have trouble swallowing conventional tablets and capsules. These tablets instantly break down in thewater to create the suspension. The key component of a dispersible tablet is the super disintegrants. When a dispersibletablet comes into touch with water, it becomes moist and swells significantly, quickly disintegrating.

TO OBSERVE EFFECTS OF MELATONIN PREMEDICATION ON HAEMODYNAMIC RESPONSES TO LARYNGOSCOPY AND INTUBATION

Laryngoscopy using rigid metal blade produces noxious stimuli that causes stimulation of sensory receptors which in turn causes release of endogenous catecholamines, which in turn provokes hemodynamic changes called stress response. Due to its inhibitory action on CNS which causes sedation and anxiolysis as well as suppression of catecholamine release, we hypothesized that oral melatonin tablet 10 mg, administered orally about 120 minutes before the procedure should provide hemodynamic stability and blunt this response. The primary objective of the study was to observe magnitude and duration of changes in vital parameters before, during and after laryngoscopy and intubation, in a group of patients who were premedicated with 10 mg mouth dispersible tablet melatonin 120 min anesthesia. Continuous numeric data on pulse rate, blood pressure, SPO2 were analyzed as mean and standard deviation. Signicance of observation was derived by applying student's t-test. Non parametric data on complication of study drug was reported as number of patients exhibiting the complication and also as percentage. One group of 35 patients received 10 mg of oral melatonin as mouth dispersible tablet 120 minutes before conduct of anesthesia and other group did not received the study drug and acted as control group for comparison. Pre induction hemodynamic parameters after 120 minutes of oral melatonin administration were recorded and after induction of anesthesia and intubation hemodynamic parameters were recorded. In group of patients who received melatonin the magnitude of rise of heart rate, systolic, diastolic and mean arterial pressure was less returning to pre induction value within 3 minutes. .In control group patients we observed a statistically signicant rise in magnitude of heart rate and blood pressure that remained elevated till 10 minutes after laryngoscopy and intubation. The rate pressure product, an indicator of myocardial oxygen demand and consumption was signicantly higher in control group and lasted for longer time. While in melatonin treated patients insignicant rise of RPP occurred. The clinical observations made in the present study allow us to conclude that oral melatonin administered 120 minutes before induction of anesthesia effectively controlled the stress response to laryngoscopy and endotracheal intubation and shown cardio-protective effect.

Off-time Treatment Options for Parkinson's Disease.

Motor fluctuations (MF) are deemed by patients with Parkinson's disease (PD) as the most troublesome disease feature resulting from the increasing impairment in responsiveness to dopaminergic drug treatments. MF are characterized by the loss of a stable response to levodopa over the nychthemeron with the reappearance of motor (and non-motor) parkinsonian clinical signs at various moments during the day and night. They normally appear after a few years of levodopa treatment and with a variable, though overall increasing severity, over the disease course. The armamentarium of first-line treatment options has widened in the last decade with new once-a-daily compounds, including a catechol O-methyltransferase inhibitor - Opicapone-, two MAO-B inhibitors plus channel blocker - Zonisamide and Safinamide and one amantadine extended-release formulation - ADS5012. In addition to apomorphine injection or oral levodopa dispersible tablets, which have been available for a long time, new on-demand therapies such as apomorphine sublingual or levodopa inhaled formulations have recently shown efficacy as rescue therapies for Off-time treatment. When the management of MF becomes difficult in spite of oral/on-demand options, more complex therapies should be considered, including surgical, i.e. deep brain stimulation, or device-aided therapies with pump systems delivering continuous subcutaneous or intestinal levodopa or subcutaneous apomorphine formulation. Older and less commonly used ablative techniques (radiofrequency pallidotomy) may also be effective while there is still scarce data regarding Off-time reduction using a new lesional approach, i.e. magnetic resonance-guided focused ultrasound. The choice between the different advanced therapies options is a shared decision that should consider physician opinion on contraindication/main target symptom, patients' preference, caregiver's availability together with public health systems and socio-economic environment. The choice of the right/first add-on treatment is still a matter of debate as well as the proper time for an advanced therapy to be considered. In this narrative review, we discuss all the above cited aspects of MF in patients with PD, including their phenomenology, management, by means of pharmacological and advanced therapies, on-going clinical trials and future research and treatment perspectives.

Pharmaceutical development of Lekhaniya Mahakashaya into dispersible tablet–A polyherbal formulation

Pharmaceutical development of Lekhaniya Mahakashaya into dispersible tablet–A polyherbal formulation

Effectiveness, safety and adherence to therapy with Elicea Q-Tab in real clinical practice

To evaluate the effectiveness and safety of escitalopram in the form of oral dispersible tablets (Elicea Q-Tab) in real-life clinical practice in patients with depressive and anxiety disorders. The study included 1.892 outpatient patients, 1.860 of whom completed participation in accordance with the protocol and entered the statistical analysis. Most patients were diagnosed with depressive and anxiety disorders of varying severity, as a rule, these diagnoses were established for the first time. The drug was most often prescribed at a dosage of 10 mg/day. The patients were monitored for 90 days and at each of the 3 visits, scales were used to assess the clinical condition (CGI-S and CGI-I), scales «Interaction with people, maintaining relationships (social functioning)» and «Availability of work, task completion, school attendance (professional functioning)», scales satisfaction with the convenience of admission/appointment and the effectiveness of treatment, various indicators of quality of life (autonomy, social and professional functioning, hobbies and hobbies), as well as the severity of cognitive disorders were measured. Patients treated with escitalopram in the form of oral tablets dispersible in the oral cavity (Elicea Q-Tab) showed an improvement in their clinical condition (a decrease in CGI-S scores from 3.65 at visit 1 to 2.63 by visit 3, by 28%; a decrease in CGI-I scores from 2.39 at visit 1 to 1.57 to visit 3, by 34%), as well as improving the quality of life, social (from 2.74 points on 1 visit to 4.32 on 2 visits, by 58%) and professional functioning (from 2.81 on 1 visit to 4.35 on 2 visits, by 55%), the level of concentration (from 3.28 points on 1 visit up to 4.5 on 3 visits, by 37%). Doctors and patients noted high satisfaction with the effectiveness and convenience of using the drug, the frequency of adverse events was low. The study showed that escitalopram in the form of oral tablets dispersible in the oral cavity (Elicea Q-Tab) is an efficient and safe treatment for depressive and anxiety disorders in real-world clinical settings. Patients and physicians have evaluated the drug positively and it can be considered as an effective agent in psychiatric practice.