Orally Disintegrating Tablets Research Articles

Palatability evaluation of orally disintegrating tablets using a visual analog scale in clinical trials.

Visual analog scale (VAS) can be used to evaluate multiple parameters. There have been no reports on the verification of order effects or reproducibility of the VAS method for overall palatability of oral dosage forms. The purpose of this study was to assess the validity of a method for evaluating the palatability of orally disintegrating tablets (ODTs) using a 100-mm VAS. We conducted clinical trials to evaluate the overall palatability, taste, and scent of 3 ODTs (F1, F2, F3) that contained famotidine (20, 10, and 5mg, respectively). The study protocol was approved by the Research Ethics Committee of the University of Shizuoka, Japan (No. 21-36). To investigate the intergroup reproducibility of the VAS evaluation, 40 participants were divided into three groups, and each group underwent human gustatory sensation test of F1, F2, and F3, performed using a crossover design with 6 different tasting sequences. To evaluate intragroup reproducibility of the VAS evaluation, the participants assessed the same ODTs twice. The VAS scores for overall palatability followed the same order (F3>F2>F1) in all groups. The VAS scores for the overall palatability of F1, F2, and F3 did not significantly differ between the first and second evaluations. The Kruskal-Wallis test indicated a minimal impact of the assessment order on ODT evaluations. We confirm the reliability and reproducibility of the VAS method for evaluating ODT palatability. The VAS method for assessing ODT palatability provides accurate information and can contribute to the design and manufacture of patient-friendly pharmaceutical products.

Review Article A Detailed Study on Disintegrating Agents and an Overview on Oral Disintegration Tablet

Nowadays, the administration of drugs through the oral route is becoming less common, accounting for only about 75% of all drug administrations compared to other routes. A new type of dosage form called oral disintegrating tablets has gained popularity in recent decades due to their rapid disintegration and dissolution. These tablets disintegrate in the mouth within seconds (25-40 seconds) without the need for water, as the oral mucosa alone is sufficient for the tablet to dissolve. The selection of a suitable disintegrating agent is crucial to achieve optimal bioavailability. A preparation may contain one or multiple disintegrating agents to ensure maximum disintegration and bioavailability. These tablets are also known as Oro disintegration tablets. Disintegrating agents are rarely used in solid unit dosage forms, typically comprising only 1-10% of the total dosage unit. The use of super disintegrates in these tablets enhances the drug's efficacy by promoting rapid dissolution. Various disintegrating agents, super disintegrates, and excipients are employed in the formulation of oral disintegrating tablets. This review article provides an overview of different types of disintegrates, including natural, polymer, and synthetic ones, as well as formulation methods, applications, and various parameters of oral disintegrating tablets. These tablets are particularly well-liked by pediatric patients and those who prefer generic medications. Oral disintegrating tablets are highly preferred in the treatment of dysphagia and oral disorders among patients. Keywords: - Oral disintegrating tablets, Oro disintegrating tablets, Disintegrates, Super disintegrates and Fast dissolution tablet.

Rimegepant orally disintegrating tablet 75 mg for acute treatment of migraine in adults from China: a subgroup analysis of a double-blind, randomized, placebo-controlled, phase 3 clinical trial

Background Rimegepant orally disintegrating tablet (ODT), an oral small-molecule calcitonin gene-related peptide receptor antagonist, is indicated for acute and preventive treatment of migraine in the United States and other countries. Previously, a large clinical trial assessed the efficacy and safety of rimegepant ODT 75 mg for the acute treatment of migraine in adults living in China or South Korea. A post hoc subgroup analysis of this trial was performed to evaluate the efficacy and safety of rimegepant for acute treatment of migraine in adults living in China.Methods Eligible participants were ≥ 18 years of age and had a ≥ 1-year history of migraine, with 2 to 8 attacks of moderate or severe pain intensity per month and < 15 headache days per month during the 3 months before screening. Participants self-administered rimegepant ODT 75 mg or matching placebo to treat a single migraine attack of moderate or severe pain intensity. The co-primary endpoints were pain freedom and freedom from the most bothersome symptom (MBS) at 2 h post-dose. Key secondary endpoints included pain relief at 2 h post-dose, ability to function normally at 2 h post-dose, use of rescue medication within 24 h post-dose, and sustained pain freedom from 2 to 24 h and 2 to 48 h post-dose. All p values were nominal. Safety was assessed via treatment-emergent adverse events (TEAEs), electrocardiograms, vital signs, and routine laboratory tests.ResultsOverall, 1075 participants (rimegepant, n = 538; placebo, n = 537) were included in the subgroup analysis. Rimegepant was more effective than placebo for the co-primary endpoints of pain freedom (18.2% vs. 10.6%, p = 0.0004) and freedom from the MBS (48.0% vs. 31.8%, p <  0.0001), as well as all key secondary endpoints. The incidence of TEAEs was comparable between the rimegepant (15.2%) and placebo (16.4%) groups. No signal of drug-induced liver injury was observed, and no study drug-related serious TEAEs were reported in the rimegepant group.ConclusionsA single dose of rimegepant 75 mg rimegepant was effective for the acute treatment of migraine in adults living in China, with safety and tolerability similar to placebo.Trial registration Clinicaltrials.gov NCT04574362 Date registered: 2020-10-05.Graphical

Development of Losartan Orally Disintegrating Tablets by Direct Compression: a Cost-Effective Approach to Improve Paediatric Patient's Compliance.

The development of suitable dosage forms is essential for an effective pharmacological treatment in children. Orally disintegrating tablets (ODTs) are attractive dosage forms that avoid swallowing problems, ensure dosage accuracy and are easy to administer as they disintegrate in the oral cavity. This study aimed to develop ODTs containing losartan potassium (LP) for the treatment of arterial hypertension in children. The ODTs, produced by the cost-effective manufacturing process of direct compression, consisted of a mixture of diluent, superdisintegrant, glidant and lubricant. Five superdisintegrants (croscarmellose sodium, two grades of crospovidone, sodium starch glycolate and pregelatinized starch) were tested (at two concentrations), and combined with three diluents (mannitol, lactose and sorbitol). Thus, thirty formulations were evaluated based on disintegration time, hardness and friability. Two formulations, exhibiting the best results concerning disintegration time (< 30s), hardness and friability (≤ 1.0%), were selected as the most promising ones for further evaluation. These ODTs presented favourable drug-excipient compatibility, tabletability and flow properties. The in vitro dissolution studies demonstrated 'very rapid' drug release. Preliminary stability studies highlighted the requirement of a protective packaging. All quality properties retained appropriate results after 12months of storage in airtight containers. In conclusion, the ODTs were successfully developed and characterised, suggesting a potential means to accomplish a final prototype that enables an improvement in childhood arterial hypertension treatment.

A prediction model based on artificial intelligence techniques for disintegration time and hardness of fast disintegrating tablets in pre-formulation tests

BackgroundThe pharmaceutical industry is continually striving to innovate drug development and formulation processes. Orally disintegrating tablets (ODTs) have gained popularity due to their quick release and patient-friendly characteristics. The choice of excipients in tablet formulations plays a critical role in ensuring product quality, highlighting its importance in tablet creation. The traditional trial-and-error approach to this process is both expensive and time-intensive. To tackle these obstacles, we introduce a fresh approach leveraging machine learning and deep learning methods to automate and enhance pre-formulation drug design.MethodsWe collected a comprehensive dataset of 1983 formulations, including excipient names, quantities, active ingredient details, and various physicochemical attributes. Our study focused on predicting two critical control test parameters: tablet disintegration time and hardness. We compared a range of models like deep learning, artificial neural networks, support vector machines, decision trees, multiple linear regression, and random forests.ResultsA 12-layer deep neural network, as a form of deep learning, surpassed alternative techniques by achieving 73% accuracy for disintegration time and 99% for tablet hardness. This success underscores its efficacy in predicting complex pharmaceutical factors. Such an approach streamlines the drug formulation process, reducing iterations and material consumption.ConclusionsOur findings highlight the deep learning potential in pharmaceutical formulations, particularly for tablet hardness prediction. Future work should focus on enlarging the dataset to improve model effectiveness and extend its application in pharmaceutical product development and assessment.

Recent Advances in Orally Disintegrating Tablet: Properties, Formulation and Production

Abstract:: Healthcare practitioners, patients, and consumers widely recognize the convenience as-sociated with administering oral tablets. The emergence of orally disintegrating tablets (ODTs) represents a significant advancement in solid dosage forms, facilitating more convenient oral de-livery while maintaining medication safety, effectiveness, and quality. The ODTs market is ex-pected to experience continuous growth in the coming years despite the internal challenges faced by commercial manufacturers. This paper initiates a comprehensive discussion of the properties of ODTs, including palatability and taste, drug content, disintegration, mechanical strength, mois-ture content, safety, and efficacy. The formulation factors that affect each of these qualities are also discussed. Additionally, this review delves into the processes of the production of ODTs, en-compassing the approaches and technologies from the mixing of active ingredients and recipients to the formation and packaging of ODTs. This review provides valuable insights into the ad-vancement in ODTs technology, aiming to equip researchers with the knowledge necessary to improve quality and optimize efficiency, ultimately receiving high acceptance from patients or consumers.

FARKLI SÜPER DAĞITICILARIN KETOPROFEN İÇEREN AĞIZDA DAĞILAN TABLETLERİN İN VİTRO KARAKTERİZASYON PARAMETRELERİ ÜZERİNDEKİ ETKİSİNİN DEĞERLENDİRİLMESİ

Objective: Orally Disintegrating Tablets (ODTs) have revolutionized pharmaceutical drug delivery, offering a patient-friendly alternative for those struggling with conventional tablet swallowing. This study delves into the impact of superdisintegrants (crospovidone, sodium starch glycolate, and croscarmellose sodium) on the in vitro characterization of Ketoprofen-containing ODTs. ODTs are designed to rapidly disintegrate in the oral cavity without water, enhancing patient compliance, ensuring faster therapeutic onset, and providing convenience. Material and Method: The micromeritic properties of pre-compression Ketoprofen ODT blends were assessed for bulk density, tapped density, Hausner ratio, and compressibility index. ODTs were formulated using a direct compression method to maintain component uniformity. Comprehensive characterization included weight variation, tablet hardness, friability, wetting time, and in vitro disintegration time assessments. The drug content was determined through UV spectrophotometry of dissolved ODTs, and dissolution studies were conducted in pH 6.8 phosphate buffer using USP apparatus XXIV. Result and Discussion: Results showed uniform tablet mass and favorable powder mixture flowability, ensuring ODT physical properties. Tablets exhibited excellent mechanical resistance with consistent hardness and low friability loss. All formulations demonstrated high and uniform drug content. Different superdisintegrants influenced wetting, disintegration, and dissolution times. Crospovidone exhibited the fastest wetting time but longer disintegration times, attributed to increased tablet hardness. Dissolution studies revealed that crospovidone-containing ODTs had faster drug release compared to croscarmellose sodium and sodium starch glycolate, aligning with literature findings. The study emphasized the importance of considering both wetting and disintegration times for a comprehensive evaluation of ODT performance. Croscarmellose sodium and sodium starch glycolate hindered drug release, forming gel-like masses impeding dissolution, while crospovidone enhanced drug release in formulated ODTs. In conclusion, the study provides valuable insights for pharmaceutical development and patient-centric drug delivery solutions, showcasing the influence of superdisintegrants on ODT performance and emphasizing the importance of considering various parameters for comprehensive evaluation.

Computer-aided optimization of carbidopa/levodopa orally disintegrating tablets

Objective This study aimed to optimize the formulation of carbidopa/levodopa orally disintegrating tablets (ODTs) in order to improve their disintegration performance, and facilitate easier medication intake for Parkinson’s patients. Method The response surface methodology (RSM) was used to optimize the formulation, with the content of cross-linked polyvinylpyrrolidone (PVPP), microcrystalline cellulose (MCC), and mannitol (MNT) as independent variables, and disintegration time as the response parameter. Python was utilized to model Carr Indices and mixing time to determine the suitable mixing time. Direct compression (DC) was used for the preparation of ODTs. Result The optimization process resulted in the following values for the independent variables: 7.04% PVPP, 22.02% MCC, and 16.21% MNT. By optimizing the mixing time using Python, it was reduced to 14.19 min. The ODTs prepared using the optimized formulation and a mixing time of 14.19 min exhibited disintegration times of 16.74 s in vitro and 17.63 s in vivo. The content uniformity of levodopa and carbidopa was found to be 100.83% and 99.48%, respectively. Conclusion The ODTs optimized using RSM and Python demonstrated excellent disintegration performance, leading to a decrease in the time the drug exists in solid form in the oral cavity. This improvement in disintegration time reduced the difficulty of swallowing for patients and enhanced medication compliance, while still ensuring that ODTs prepared by DC had sufficient mechanical strength to meet storage and transportation requirements.

Dissolution Profiles of Oral Disintegrating Tablet with Taste Masking Granule Polymer Coating in Biorelevant Bicarbonate Buffer.

The current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used to mask the bitter taste of drugs. Both generic A and generic B have been known to be bioequivalent to Allegra®. The dissolution tests were conducted using a compendial paddle, with either bicarbonate (10 mM, pH 6.8) or phosphate buffer (25 mM, pH 6.8) as the dissolution media. A floating lid was employed to cover the surface of the bicarbonate buffer to prevent volatilization. Results indicated that in phosphate buffer, the dissolution profiles of Allegra and generic B significantly varied from that of generic A, whereas in the bicarbonate buffer, the dissolution profiles of Allegra, generic A, and generic B were comparable. These findings suggest that the use of bicarbonate buffer may offer a more precise prediction of human bioequivalence compared to phosphate buffer.

Combined eutexia and amorphization for simultaneous enhancement of dissolution rate of triamterene and hydrochlorothiazide: Preparation of orodispersible tablets

ABSTRACT Background: Triamterene is an oral antihypertensive drug with dissolution-limited poor bioavailability. It can be used as monotherapy or in fixed dose combination with hydrochlorothiazide which also suffers from poor dissolution. Moreover, co-processing of drugs in fixed dose combination can alter their properties. Accordingly, pre-formulation studies should investigate the effect of co-processing and optimize the dissolution of drugs before and after fixed dose combination. This is expected to avoid deleterious interaction (if any) and to hasten the biopharmaceutical properties. Objective: Accordingly, the aim of this work was to optimize the dissolution rate of triamterene alone and after fixed dose combination with hydrochlorothiazide. Methodology: Triamterene was subjected to dry co-grinding with xylitol, HPMC-E5 or their combination. The effect of co-grinding with hydrochlorothiazide was also tested in absence and presence of xylitol and HPMC-E5. The products were assessed using Fourier-transform infrared (FTIR), differential scanning calorimetry, X-ray powder diffraction (XRPD), in addition to dissolution studies. Optimum formulations were fabricated as oral disintegrating tablets (ODT). Results: Co-processing of triamterene with xylitol formed eutectic system which hastened dissolution rate. HPMC-E5 resulted in partial amorphization and improved triamterene dissolution. Co-grinding with both materials combined their effects. Co-processing of triamterene with hydrochlorothiazide resulted in eutexia but the product was slowly dissolving due to aggregation. This problem was vanished in presence of HPMC-E5 and xylitol. Compression of the optimum formulation into ODT underwent fast disintegration and liberated acceptable amounts of both drugs. Conclusion: The study introduced simple co-processing with traditional excipients for development of ODT of triamterene and hydrochlorothiazide.

Fast dissolving tablets: Opportunity in herbal drug delivery system

The polyherbal preparation's pharmacological and phytochemical properties have been used all over the world. Single or multiple herbs (polyherbal) are utilized for treatment in Ayurveda. The Sarangdhar Samhita, a work of Ayurvedic literature, emphasized the idea of polyherbalism as a means of enhancing therapeutic efficacy. Individual plants' active phytochemical components are insufficient to produce the desired therapeutic effects. The medicinal effects and toxicity are improved when different herbs are combined in a specific ratio. Comforts of drug administration and patient compliance are given significant weight when designing dose forms. New and developing technology can be used to produce durable, adaptable tablets with exceptional flavor masking and controlled release. Orally disintegrating tablets (ODTs) are solid dosage forms that disintegrate in the mouth in less than 60 s, and are thus swallowed without the need for water. Rapid disintegration of tablet cause quick dissolution thus rapid onset of action. Polyherbal Fast dissolving Tablets disintegrates in mouth quickly and produces fast onset of action without use of water makes it suitable for special population like pediatrics, geriatrics, psychotic, dysphasic, bedridden patient and frequent traveller patient. The current review article explains the features of active ingredients and excipient used in the formulation of ODTs, discusses multiple ODT formulation and preparation techniques with their merits and demerits, and also, offers remedies for problems associated with ODTs. Moreover, quality control steps and required considerations are presented.

Effect of Crospovidone, Croscaramellose Sodium in Combination on the Drug Release of Anti diabetic Medication in Tablet Form

Objective: The current study’s objective is to check the impact of superdisintegrants on the drug release of Vildagliptin by developing oral disintegrating tablets (ODT). Vildagliptin, new class of oral hypoglycemic agent. It acts by inhibiting dipeptidyl peptidase-4. Conventional Vildagliptin tablets are (due to its first pass effect) unsuitable where quicker onset of action is required Hence, it is necessary to develop oral disintegrating tablet, in order to obtain improved patient compliance. Methods: Using Oral disintegrating tablets of Vildagliptin were prepared using various quantities of Crospovidone &amp; Croscaramellose sodium as Superdisintegrants by direct compression method. Nine trials were developed by varying the quantities of Crospovidone, Croscaramellose sodium such as 6 ± 1.5 mg i.e. 4.5, 6, 7.5 mg respectively. Prepared formulations were assessed for Pharmaceutical Product Performance as per official methods such as hardness, friability, weight variation, drug content, wetting time, disintegration time, and drug release studies. Results: Findings indicate that all formulations meet the acceptance criteria such as good mechanical strength (&gt;4.3 kg/cm2), less friable (&lt;0.65%), uniform drug content (&gt;98%) and kinetic modeling was applied to the in-vitro dissolution profiles. Conclusion: The best formulation (F1), which is likewise identical to the marketed product (Galvus-50) (f2= 89.01, f1= 1.85), contained 7.5 mg of Crospovidone and 7.5 mg of Croscaramellose sodium. Formulation (F1) follow first order, whereas release mechanism found to be Fickian type (n= 0.323).

Disintegration testing for orally disintegrating tablets (ODTs): An overview

Prescribing orally disintegrating tablet (ODT) dosage form is a common practice. For several populations, including geriatrics and pediatrics, ODTs are one of the most desired dosage forms. They are solid dosage forms designed to disintegrate or dissolve very quickly in contact with saliva as soon as they are placed in oral cavity of a patient. According to United States Pharmacopeia (USP), every dosage form has to pass some quality control tests to ensure uniformity and performance of this dosage form. For ODTs, disintegration test is fundamental to ascertain time required for tablets to break down and release their contents for dissolution and absorption. Additionally, it is a crucial predictive test for determining in vitro/in vivo association. There are no mandatory universal disintegration testing standards for ODTs, however, as stated in the USP. Instead, recent USP refers to individual manufacturer monograph specifications which may vary from one monograph to another. This article discusses several developed disintegration tests and methods for ODTs such as OD-mate testing, basket rack assembly, CCD camera, texture analyzer (TA), special disintegration equipment, prototype disintegration tester (PDT), simple approach, and modified wetting test and elaborates on their advantages and disadvantages.

Curcumin- β-Cyclodextrin Molecular Inclusion Complex: A Water- Soluble Complex in Fast-dissolving Tablets for the Treatment of Neurodegenerative Disorders.

Orally disintegrating tablets (ODTs) have become an excellent choice for delivering drugs as their palatability is greatly improved. In this work, β-cyclodextrin has been used to improve the solubility of curcumin by encapsulating it into the hydrophobic cavity for the treatment of neurodegenerative disorders. The current study aimed to present the design, formulation, and optimisation of fastdissolving oral tablets of curcumin- β-cyclodextrin molecular inclusion complex using a 32-factorial design with sodium starch glycolate (SSG) and Neusilin® ULF2 as independent factors. The drug-excipient compatibility was studied by FTIR spectroscopy. The inclusion complex of curcumin-β-cyclodextrin was prepared using solvent casting and confirmed using XRD studies. Powder blends were evaluated for flow properties. Tablets prepared by direct compression were evaluated for post-compression parameters. Further, the effect of formulation variables, such as sodium starch glycolate (X1) and Neusilin® ULF2 (X2), on various responses, including disintegration time and dissolution at 2 hours, was studied using statistical models. Post-compression parameters, i.e., hardness (4.4-5 kg/cm2), thickness (3.82-3.93 mm), weight variation (±7.5%), friability (<1%), wetting time (51-85 seconds) and drug content (96.28- 99.32%) were all found to be within the permissible limits and the disintegration time of tablets with super-disintegrants ranged between 45-58 seconds. The in-vitro dissolution profile of tablets showed that higher SSG and Neuslin® ULF2 levels promoted drug release. For statistical analysis, the 2FI model was chosen. Optimised variables for formulation have been determined and validated with the experimental findings based on the significant desirability factor. The current study reveals the validated curcumin-β-cyclodextrin inclusion Complex fast-dissolving tablets with SSG and Neusilin® ULF2 to be an ideal choice for effectively treating neurodegenerative disorders.

Development of α-Cyclodextrin-Based Orally Disintegrating Tablets for 4-Phenylbutyrate.

Despite major improvements brought about by the introduction of taste-masked formulations of 4-phenylbutyrate (PB), poor compliance remains a significant drawback to treatment for some pediatric and dysphagic patients with urea cycle disorders (UCDs). This study reports on the development of a cyclodextrin (CD)-based orally disintegrating tablet (ODT) formulation for PB as an alternative to existing formulations. This is based on previous reports of the PB taste-masking potential of CDs and the suitability of ODTs for improving compliance in pediatric and dysphagic populations. In preliminary studies, the interactions of PB with α and βCD in the solid state were characterized using X-ray diffraction, scanning electron microscopy, dissolution, and accelerated stability studies. Based on these studies, lyophilized PB-CD solid systems were formulated into ODTs after wet granulation. Evaluation of the ODTs showed that they had adequate physical characteristics, including hardness and friability and good storage stability. Notably, the developed αCD-based ODT for PB had a disintegration time of 28 s and achieved a slightly acidic and agreeable pH (≈5.5) in solution, which is suitable for effective PB-CD complexation and taste masking. The developed formulation could be helpful as an alternative to existing PB formulations, especially for pediatric and dysphagic UCD patients.

Novel bioequivalent oral disintegrating tablet of aripiprazole prepared by direct compression technique with shortened disintegration time

Herein, we aimed to formulate a novel oral disintegrating tablet (ODT) of aripiprazole (ARP) capable of rapid disintegration using a direct compression technique. Different ODTs were fabricated with directly compressible excipients, and their disintegration time, wettability (water absorption ratio and wetting time), and mechanical properties (hardness and friability) were evaluated. The optimized ODT comprised F-Melt® type C, Prosolv® SMCC HD90, and Na croscarmellose (10 mg of ARP in a 130 mg tablet). The ODT with 3.1–5.2 kp hardness exhibited rapid disintegration (14.1–17.2 sec), along with appropriate mechanical strength (friability < 0.24%). In a bioequivalent study in Korean healthy subjects (randomized, single-dose, two-period crossover design, n = 37), the novel ODT offered the equivalent pharmacokinetic profile to that of a conventional immediate release tablet (Otsuka, Abilify®, Japan), despite different disintegration and dissolution profiles. The 90% confidence intervals of the geometric mean test to reference ratios considering the area-under-the-curve and maximum plasma drug concentrations were 1.0306–11051 and 0.9448–1.1063, respectively, satisfying FDA regulatory criteria for bioequivalence. The novel ART ODT was physicochemically stable under the accelerated storage condition (40 °C, RH75%) for 24 weeks. Therefore, the novel ARP-loaded ODT is expected to be an alternative to oral ARP therapy, providing improved patient adherence.

Formulation and Drug Release Study of Rivaroxaban Oral Disintegrating Tablets Using Various Super-Disintegrants

This study aims to improve Rivaroxaban's solubility, dissolution, and bioavailability. Orally disintegrating tablets (ODTs) made with super-disintegrants like crospovidone, sodium starch glycolate, and cross-carmellose sodium will do this. Tablet preparation used direct compression and formulation optimization with design expert software. After a thorough factorial design and evaluation of pre- and post-compression parameters, the F3 batch, which contained Rivaroxaban (7.97%), Crospovidone (3.59%), Croscarmellose sodium (5.18%), Sodium Starch Glycolate (5.18%), Lactose Anhydrous (31.08%), Mannitol (15.94%), MCC (27.89%), SSF (1.59%), and Talc (1.59%), was the best. The enhanced tablet formulation (F3) showed positive qualities, including 3.3 kg/cm² hardness, 23 seconds disintegration time, and 99% drug release after 30 minutes. The innovative Rivaroxaban orally disintegrating tablet (ODT) method disintegrated and dissolved faster than market forms. Rivaroxaban's physical and chemical properties were assessed before formulation. The medication was colorless, scentless, crystalline, and melted at 227°C-229°C, as described in published research. The pharmaceutical was found to be a BCS Class II drug with low water solubility and high solubility in acetate buffer pH 4.5 and 0.1 N Hydrochloric acid. Fourier-transform infrared spectroscopy (FTIR) confirmed no drug-polymer-excipient interactions. Every batch of tablets exhibited uniform thickness (3.5 mm to 3.8 mm) and diameter (10.31 mm to 10.36 mm), indicating good compression without adhering to shaping tools. All samples had a 3-5 kg cm-² hardness, indicating strong mechanical properties. The Roche friability method showed that all batches had good abrasion resistance, ranging from 0.1% to 0.5%. Variations in croscarmellose sodium and crospovidone on tablet disintegration time and hardness were examined using design expert software. The ANOVA showed important factors affecting these attributes. Data-driven polynomial equations predict tablet disintegration time and hardness. These models reveal formulation parameters that affect tablet performance. Thus, the improved F3 batch of rivaroxaban orally disintegrating tablets (ODTs) improves solubility, dissolving, and bioavailability. This may improve treatment outcomes.

Application of Design of Experiment for development of orally disintegrating tablets

The current work presents the formulation development methodology for Orally Disintegrating Tablets (ODTs) using Design of Experiment (DoE). The statistical software JMP was used to design the experiments and analyse the data for producing sodium Ibuprofen freeze-dried ODTs. In the first stage, several pure excipients (polymers, amino acids, and polyols) were freeze-dried and the quality attributes of the cakes were evaluated. Four critical quality attributes (CQAs) were determined based on the target profile: disintegration time, mechanical strength, moisture uptake, appearance. In the second stage, the placebo tablets comprising sodium alginate, alanine, and mannitol (working as a matrix shape-former and lyo-/cryo-protectors), were designed using Mixture DoE, freeze-dried and characterized to identify the optimal combination of the excipients. In the third stage, the ODTs containing sodium Ibuprofen were designed within a reduced design space to optimize the formulation. The wettability and dissolution of the ODTs were studied. The proposed methodology enabled the estimation of working design space and facilitated the production of freeze-dried ODTs with the required quality attributes. Sodium alginate was identified as the key excipient in the formulation, affecting all CQAs. The optimal combination of sodium alginate, alanine and mannitol corresponding to the desirable target profile was found (30%:40%:30%).

Development of a novel direct compressible co-processed excipient and its application for formulation of Mirtazapine orally disintegrating tablets

Introduction Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited. Objective This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs. Methods A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation. Results The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min. Conclusion Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

Orally disintegrating tablets: mechanisms, preparation methods, problems and achievements

The oral route of drug administration is considered one of the preferred delivery methods. In recent years, orally disintegrating tablets (ODTs) have become convenient pharmaceutical dosage forms, especially for specific patient populations such as pediatric, geriatric, and psychiatric patients with dysphagia. Rapid disintegration and increased bioavailability are some of the essential characteristics of ODTs that make them superior to other traditional pharmaceutical dosage forms. Orally disintegrating tablets are pills that disintegrate within a few seconds after being placed in the oral cavity. This review describes the mechanisms of drug release from ODTs, manufacturing challenges, and advancements in orally disintegrating tablet technologies.