Fast Disintegrating Tablets Research Articles

Effect of Disintegrating Agents on Red Ginger (Zingiber officinale Roxb) Dry Extract Fast Disintegrating Tablets Using Direct Compression Method

Red ginger (Zingiber officinale Roxb) is one of the medicinal plants that is effective as a medicine for nausea and vomiting. One of the techniques for developing traditional medicinal products is to make fast disintegrating tablets (FDT). This research aims to compare the effect of these various disintegrating materials on the physical properties of FDT. FDT red ginger extract is made using the direct compression method. The tablets obtained were physically evaluated including weight uniformity, hardness, friability, and disintegration time. The statistical results using the one-way ANOVA test show that between tablet formulas there are significant differences in tablet disintegration time with differences in the type of disintegrating agent. The data obtained shows that all formulas meet the physical properties test requirements for tablets. The tablet formula using crospovidone produces tablets with high hardness, low friability, and fast disintegration time

Enhanced Anti-Inflammatory Activity of Kaempferia galanga Extract by Solid Self-Nanoemulsifying Drug Delivery System and Its Development in Fast Disintegrating Tablet

The increasing global incidence of osteoarthritis (OA) emphasizes the need for effective treatments, particularly for the elderly. Conventional OA treatments pose administration challenges, leading to patient discomfort due to difficulties in administration. Herbal formulations offer an alternative to mitigate these issues. Kaempferia galanga (KG) contains ethyl p-methoxycinnamate, a compound displaying anti-inflammatory properties that hold promise for OA treatment. This study explores the formulation of a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of Kaempferia galanga extract (KGE) and evaluates its anti inflammatory efficacy, subsequently developing it into a fast disintegrating tablet (FDT) dosage form. Initially, a liquid SNEDDS (L-SNEDDS) was prepared with varying surfactant and co surfactant concentrations. The optimal formula of L-SNEDDS (FL2) using tween 80: cremophor RH 40: PEG 400 in a ratio of 1:1:2 demonstrated favorable characteristics, including transmittance of 86.93 ± 1.16%, emulsification time of 28 ± 2.65 s, particle size of 27.79 ± 2.00 nm, PDI of 0.21 ± 0.014, and zeta potential of -12.57 mV. FL2 was solidified using aerosil 200 to produce S-SNEDDS and tested for anti-inflammatory efficacy in vivo using a carrageenan induced rat model. Results showed enhanced anti-inflammatory efficacy of KGE via S-SNEDDS, marked by reduced edema volume. Afterward, FDT S-SNEDDS were prepared using the direct compression method by comparing different types of superdisintegrants. The formulation using the combination of crospovidone and croscarmellose sodium (FT2) demonstrated excellent flow properties, tablet disintegration time of 63 s, wetting time of 34.01 ± 7.87 s, friability of 0.19%, and hardness of 3.53 ± 6.16 kg/cm2. The dissolution test indicated a better dissolution profile for FT2 compared to other formulations. In conclusion, this research presents the potential of FDT S-SNEDDS as a promising drug delivery system for enhancing the therapeutic effects of Kaempferia galanga extract in treating inflammatory conditions such as osteoarthritis.

Revolutionizing fast disintegrating tablets: Harnessing a dual approach with porous starch and sublimation technique

This study investigates the transformation of neat starch (NS) from mung beans into porous starch (PS) for the formulation of fast-disintegrating tablets (FDTs) using the sublimation technique, contrasting their performance with superdisintegrants such as sodium starch glycolate (SSG) and croscarmellose sodium (CS). Camphor was used as a sublimating agent. The interaction between drug and excipients was analyzed using Fourier-transform infrared spectroscopy (FTIR), while preformulation assessments were conducted on powder blends. Model drug Diclofenac sodium (DL)-loaded FDTs were prepared via direct compression technique. Thermal behavior and crystalline properties were evaluated using differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), respectively. Compressibility of tablets was assessed through Heckel and Kawakita analyses. Post-compression evaluations encompassed hardness, thickness, in vitro disintegration, and dissolution studies. FTIR analysis indicated the absence of chemical interactions among constituents, while precompression analyses confirmed favorable flow properties of the blends. Heckel analysis supported the material's notable compressibility. Microscopic examination revealed the formation of pores on the tablet surface due to the sublimation process. Integration of PS significantly accelerated the disintegration time of FDTs, with durations ranging from 50 to 82 s, compared to 76–104 s for NS-FDTs. While PS-FDTs exhibited a longer disintegration time compared to SSG, they demonstrated faster disintegration compared to croscarmellose sodium. A significant disparity (p<0.01) in drug release at 60 min was observed between SSG and PS-FDTs, with DP3 achieving 97.65 % drug release. Most batches followed the Korsmeyer-Peppas model, except for DN2 and DN3, which adhered to Higuchi-matrix drug release kinetics. Stability assessments after 90 days revealed no significant differences (p>0.05). Conclusively, this study highlights the effectiveness of PS and the sublimation method in creating FDTs with enhanced drug release properties.

REVIEW : OF SUPERDISINTEGRANT INGREDIENTS IN FAST DISINTEGRANT TABLET TABLET PREPARATIONS

This study aimed to evaluate the potential of synthetic and natural disintegrating agents in fast-disintegrating tablet (FDT) formulations. The methodology used includes a comprehensive literature review on the definition, characteristics, working mechanisms, and applications of super disintegrants in the manufacture of FDTs. The results of the study showed that super disintegrants play an important role in facilitating rapid disintegration of tablets. Synthetic super disintegrants such as crospovidone, croscarmellose sodium, and sodium starch glycolate have the advantage of lower concentrations and better intragranular effectiveness. On the other hand, natural superdisintegrants such as mucilages, gums, and polysaccharides from plants have easy availability, affordable prices, non-toxic properties, and biologically acceptable characteristics. In conclusion, the selection of an appropriate super disintegrant, whether synthetic or natural, is a key factor in effective FDT formulation and providing rapid disintegration. The combination of using super disintegrants at the granulation stage (intragranular) and before compression (extragranular) can produce better performance compared to a single method. Keywords: FDT, Super disintegrant, Synthetic, Natural

Development and Assessment of Loratadine Fast-Disintegrating Tablets via β-Cyclodextrin Complexation with Superdisintegrants

ABSTRACT: This study aimed to enhance the solubility and consequent bioavailability of Loratadine, a widely used medication for seasonal allergic rhinitis and chronic idiopathic urticaria. The approach involved complexation with β-cyclodextrin to improve solubility and the formulation of fast-disintegrating tablets via the sublimation method. Crosspovidone acted as a superdisintegrant, while camphor served as a sublimating agent. Methodology: Pre-compression parameters were assessed to ensure adequate flow properties, while post-compression parameters were evaluated against IP acceptable limits for variations in hardness, weight, wetting time, friability, drug release, and disintegration time, drug content, FTIR, and DSC. Dissolution studies were conducted in 0.1N HCL, and statistical analysis employed a central composite design for optimization. Results: Formulation B14 emerged as the optimized batch, demonstrating favourable characteristics including wetting time, in vitro drug release, drug content, and disintegration time. Analysis of stability conducted in accordance with ICH guidelines affirmed the formulations' stability. Conclusion: The developed fast-disintegrating tablet formulation of Loratadine exhibited enhanced solubility, potentially translating to improved bioavailability. These advancements suggest increase efficacy and improved patient compliance in the management of allergic rhinitis and urticaria.

Design and Development of Propranolol HCl Fast Dissolving Tablets by Using Isolated Mucilage of Salvia Hispanica for the Treatment of Hypertension by Using DoE tools.

The main issue with Hypertension therapy is quick commencement of effect. The creation of suitable dose forms may help address the issue of medications having a delayed beginning of effect. Oral Antihypertensive medication treatment is best suited for and has seen a rise in popularity with fast-disintegrating tablets. In terms of patient compliance, quick start of action, precise dosage, strong chemical stability, ease of self-administration, and compactness, they are superior to other traditional methods. As a popular hypertension medication, Propranolol HCl is a strong candidate for development into Fast Dissolving Tablets (FDTs). Because to first pass metabolism, it has a limited bioavailability. Therefore, the primary goal of the research was to create Propranolol HCl fast-dissolving tablets in order to increase the drug's bioavailability and dissolution rate. Microcrystalline cellulose used to make fast-dissolving Propranolol HCl tablets, together with varying concentrations of super disintegrates such as Chia Seed mucilage and sodium starch glycolate. Each batch was made by compressing it directly. Three formulation variables were combined, and the combined impact was examined using a 23 Full Factorial design. Here, the disintegration time is examined as a dependent parameter and the concentrations of chia seed mucilage, Sodium Starch Glycolate, and Microcrystalline Cellulose were considered as independent variables, X1, X2, and X3, respectively. The program Design Expert is used to depict the data.

A data-driven approach utilizing a raw material database and machine learning tools to predict the disintegration time of orally fast-disintegrating tablet formulations

Orally fast-disintegrating tablets (OFDTs) have seen a significant increase in popularity over the past decade, becoming a rapidly expanding sector in the pharmaceutical market. The aim of the current study is to use machine learning (ML) methods to predict the disintegration time (DT) of OFDTs. In this study, we have developed seven ML models using the TPOT AutoML platform to predict the DT of OFDTs. These models include the decision tree regressor (DTR), gradient boost regressor (GBR), random forest regressor (RFR), extra tree regressor (ETR), least absolute shrinkage and selection operator (LASSO), support vector machine (SVM), and deep learning (DL). The results indicate that ML methods are effective in predicting the DT, especially with ETR. However, after fine-tuning the deep neural network with a 10-point cross-validation scheme, the DL model showed superior performance with an NRMSE of 6.2% and an R2 of 0.79. The key factors influencing the DT of OFDTs were identified using the SHAP method.

Fast-disintegrating tablets : a novel approach in pharmaceutical preparation

Fast-disintegrating tablets : a novel approach in pharmaceutical preparation

Posaconazole-glutaric acid cocrystal tablet with improved Dissolution rate

Posaconazole is used to prevent fungal infections in patients having severely weakened immune system and has poor aqueous solubility which impairs its dissolution in upper gastric fluid producing problems in different formulations. These characteristics hinder its therapeutic application by delaying absorption rate and thereby onset of action. In the present study, an attempt was made to prepare posaconazole cocrystals with improved physicochemical properties for better therapeutic activity. Cocrystals were prepared with glutaric acid in 1:1 molar using ethanol by solvent drop grinding technique. The co-crystals formed were characterized by melting point determination, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and dissolution studies. Posaconazole-glutaric acid co-crystals were further formulated as fast disintegrating tablets. The IR study revealed the shifting of characteristic bands of posaconazole. The PXRD pattern indicated cocrystal crystallinity and a considerable difference in 2θ value of intense peaks. The variation in fusion endotherm, which is in agreement with melting point, was designated by DSC spectra of posaconazole cocrystal. A significant improvement in the dissolution rate was observed in the case of cocrystals based tablets than pure posaconazole tablets.

A Review on Mouth Dissolving Tablets

Traditional dosage forms, such as pills and capsules, are now used to treat conditions like dysphagia, which increases the risk of non-compliance and makes therapy ineffective. Mouth dissolving tablets were created to solve the problems associated with traditional dosage forms. They offer good hardness, dose uniformity, and convenience of administration. For pediatric, geriatric, and travel patients, they are the preferred dose form. Providing the MDTs with enough hardness, integrity, and disintegration speed without the requirement for water was the aim of their development. For fast-dissolving tablets to dissolve in saliva quickly, water is not needed. Some tablets are designed to dissolve in saliva very quickly in just a few seconds and are therefore referred to as "fast-dissolving" tablets. Because they contain substances that accelerate the pace at which the tablet dissolves in the mouth otherwise, it might take up to a minute some tablets are best referred to as fast-disintegrating tablets. This tablet type is designed to make it possible to administer an oral solid dose form in situations when no water or fluids are taken. These tablets typically dissolve in less than 60 seconds when dissolved in saliva.

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.

Formulation and evaluation of aceclofenac fast disintegrating tablets using sida acuta powder

Aceclofenac is a NSAID with anti-inflammatory, analgesic activity. The aim is to develop the Aceclofenac tablets with sida acuta powder that exhibit rapid disintegration, dissolution and showing maximum pharmacological activity in less time. This is desirable for improving patient compliance. The present study was to formulate and evaluate the fast-disintegrating tablets of Aceclofenac using Sida acuta powder by direct compression technique with varying concentrations. Each formulation was evaluated for pre and post evaluation tests such as Flow property, Bulk density, tapped density, Weight variation, Hardness, Friability, Wetting time, Disintegration time, Assay, in-vitro dissolution. Among the 06 formulations, F6 formulation Aceclofenac with 6%w/w of Sida acuta showed the in-vitro dissolution (99.75%) release of drug within 20 minutes and release of drug mechanism as first order kinetics. It was concluded that the fast-disintegrating tablets are prepared by Natural polymer Sida acuta acts as a disintegrant and showed excellent disintegration time,enhance the dissolution rate.

Development of Fast Disintegrating Tablets Containing Loxoprofen Sodium by HYDROFLASH Manufacturing Method.

In order to create and offer superior pharmaceuticals for consumers who wish to be relieved of headache and fever as soon as possible, we established HYDROFLASH manufacturing method that enables us to offer fast disintegration tablets containing loxoprofen sodium (LX), which are difficult to disintegrate. As a result of screening excipients, tablets using mannitol showed the fastest disintegration time, about 2 min. From the result of viscosity measurement, we found that LX produced higher viscosity when dissolved in water. This suggests that tablets containing LX disintegrate slower by inhibiting the penetration of water into the tablet due to the viscosity caused of LX. Therefore, we created a manufacturing method to make it easy for water to penetrate the tablet. It is possible to achieve fastest disintegration in about 30 s for tablets containing LX by granulating in a fluidized-bed with spraying of the dispersion of light anhydrous silicic acid (LASA). LX-containing tablets manufactured by the HYDROFLASH method disintegrated immediately after contact with water. Furthermore, it was observed that LASA was uniformly dotted on the surface of tablets by HYDROFLASH method, compared with other manufacturing methods. We considered that by fluidized-bed granulation with LASA dispersion (HYDROFLASH manufacturing method), water permeates through LASA on the tablet surface regardless of viscosity of LX. Futhermore, LX-containing tablets by the HYDROFLASH method showed that the dissolution rate of LX was nearly 100% at 5 min after starting the test. We considered that the initial dissolution became faster because of the fast disintegration.

Development and Assessment of a New Oral Selenium Fast-disintegrating Tablets

Selenium is an essential trace element and its deficiency causes myositis, myocardial damage, and other symptoms. Patients receiving long-term intravenous nutrition or tube-feeding in particular are deficient in essential trace elements, including selenium, and require regular supplementation. In Japan, injectable selenium-containing products are listed on the National Health Insurance drug price list, and oral solutions are prepared and used in hospitals. However, these formulations have problems related to preservation and require complicated administration procedures. In this study, we developed a new fast-disintegrating tablet formulation of selenium, using SmartEx® (D-mannitol·low substituted hydroxypropylcellulose (L-HPC)·fully hydrolyzed polyvinyl alcohol (PVA) mixture) as a coprocessing additive, that can be administered orally or by feeding tube. The tablet formulation had excellent disintegrable capability, sufficient hardness, and did not cause tube blockage when administered in the simple suspension method. In addition, the tablet formulation showed no changes in properties in an accelerated test without packaging for 42 d, indicating that it could be stored for a long period. Fast-disintegrating tablets prepared with SmartEx® are expected to improve the adherence and quality of life of patients who require selenium supplementation.

Comparing deep freezing, flash freezing and annealing induced materialistic changes during the formulation of alanine and serine monomers mediated fast disintegrating tablets

Despite significant advancements in the formulation of lyophilized fast disintegrating tablets (FDTs), saccharides and polyols remain ubiquitous matrix support agents and disintegration enhancers. This also impeded the use of FDTs in the treatment of chronic disorders wherein sugar intake is restricted to the patients. The present work utilizes the combination of alanine and serine as amino acid material to prepare zero saccharide/polyols FDTs. For the formulation of FDTs, we uniquely employed three different techniques namely, deep freezing, flash freezing and annealing and evaluated the impact of these processes on sublimation rate (thermal modelling), crystallization tendencies and different FDTs properties such as hardness, fracturability, disintegration time (DT), porosity, % weight variation, friability, lyophilization index etc. The findings demonstrated that, in comparison to their individual counterparts, the addition of alanine and serine at optimized ratio could improve the powder characteristics and thereby FDTs characteristics. Annealing also sped up the sublimation process and decreased the amount of time it took for the FDTs to disintegrate. Moreover, it has been found that the tableting properties, including DT, friability, and % weight variation, were under compliance with the United States pharmacopeial (USP) standards, indicating the acceptability of the developed FDTs to the pharmaceutical industries.

Optimization of Fast Disintegrating Tablets Diphenhydramine HCl using Co-process of Cross-link Yellow Kepok Banana Starch, Crospovidone, and Microcrystalline Cellulose

Diphenhydramine HCl is an antihistamine drug that is available in conventional tablet form. This study aimed to produce the optimum formula for a diphenhydramine fast disintegrating tablet (FDT) using a modification of starch, crospovidone, and microcrystalline cellulose (MCC) to produce quality tablets that meet the tablet's physical requirements and tablet dissolution. Starch modification was made using a two-step method of starch cross-link, then continued with silica coprecipitation. FDT was prepared by the direct compression method. Optimisation with the simplex lattice design (SLD) model uses three components: co-process starch crosslink-silica, crospovidone, and MCC, which obtained 14 formula designs. The hardness, wetting time, disintegration time, and percent dissolution are optimisation parameters. Equations, contour plots, and desirability values were determined as the optimum formula. Based on the research results, an optimum formula was obtained with the proportion of co-process cross-link starch-silica was 56.185 mg, crospovidone at 6 mg, and MCC at 45.815 mg. The result of hardness was 5 kg, wetting time 51.061 seconds, disintegration time 63.129 seconds, and dissolution was 100.972%. The interaction of the three components reduces hardness and increases disintegration time, wetting time, and percent dissolution.

Fast disintegrating dosage forms of mucoadhesive-based nanoparticles for oral insulin delivery: Optimization to in vivo evaluation

The aim of this work was to develop fast disintegrating dosage forms, including fast disintegrating tablets (FDTs) and films (FDFs), for oral insulin delivery incorporating mucoadhesive thiolated chitosan (TCS)-based nanoparticles (NPs). Cyclodextrin (CD)-insulin complexes were formed to prevent insulin from degradation and further optimally prepared NPs in order to improve the mucoadhesive properties. After that, these NPs were incorporated into the dosage forms and then evaluated for their morphology as well as physical and mechanical properties. The disintegration time, insulin content, mucoadhesive properties, insulin release, cytotoxicity, in vivo hypoglycemic effect, and stability of dosage forms were studied. Results showed that the CD-insulin complexes were successfully encapsulated into the mucoadhesive NPs. The 15 %w/w CD-insulin complex-loaded NPs, which were probably dispersed and/or fused into the dosage forms, showed promising characteristics, including rapid disintegration as well as good physical and mechanical properties to withstand erosion during handling and storage. The porous structure of the FDTs promoted liquid flow and induced rapid disintegration. The dosage forms provided buccal mucoadhesion before, during, and/or after the disintegration. The FDFs containing hydroxypropyl β-cyclodextrin (HPβCD)-insulin complex-loaded NPs increased mucoadhesion, increasing insulin release. Furthermore, these dosage forms provided excellent in vivo hypoglycemic response with a prolonged effect in diabetic mice and had no cytotoxicity toward the gingival fibroblast cells. In addition, they were stable at temperatures between 2 and 8 °C for three months. The results indicate that these formulations could be applied as promising dosage forms for use in oral insulin delivery.

Formulation and Stability of Orally Fast Disintegrating Tablets of Amlodipine besylate

The demand for fast disintegrating tablets has been growing during the last decade especially for geriatric and pediatric patients because of swallowing difficulties. Amlodipine besylate is commonly used for the treatment of chest pain, commonly known as angina, due to ischemia of the heart muscle and a result of obstruction or spasm of the coronary arteries. The study would involve the use of various disintegrants along with other excipients for the formulation of orally fast disintegrating tablets to achieve rapid disintegration and release. The stability studies of the prepared dosage form would be carried out according to the guideline of the ASEAN guideline. In this study, we researched on formulating orally fast disintegrating tablets containing 5 mg of amlodipine at pilot scale. Fast-dissolving amlodipine tablets were prepared by direct compression method. Formulations were designed by Design Expert v11 using D-optimal model and optimized by BC-PharSoft OPT software. Studied ingredients are disintegrants and fillers for directly compressed tablets. After successfully developing the optimal formulation, the batch size was scaled up to 10.000 tablets. Then the tablet stability study was proceeded and shelf life of the product under accelerated conditions was determined within 6 months according to Van’t Hoff principle. It was revealed that tablets had good stability and shelf life of 766.3 days (at 30oC). This satisfactory result may show a great promise for large-scale production.

Formulation and Evaluation of Fast Disintegrating Tablets of Ondansetron Using Natural Superdisintegrants

Background: Fast disintegrating tablet (FDT) of ondansetron has better patient compliance as it is easy to swallow for the treatment of nausea and vomiting. Moreover, fast absorption, rapid onset, reduced loss of drugs, and enhanced bioavailability are making oral dispersible systems a better drug delivery system. This research was conducted with the objective to formulate and evaluate the oral FDT of ondansetron HCl using natural polymers. Methods: The tablets were formulated employing the direct compression technique using different ratios of natural super disintegrants such as spray-dried banana powder, ispaghula husk powder, and combination of both polymers. The developed powders were subjected to the pre-compression parameters and the powders were punched using a single-head rotatory compression machine. The formulated 200 mg tablets were subjected to post-compression evaluation. Results: The Fourier-transform infrared spectroscopy studies showed no chemical interaction between pure drugs, natural super disintegrants, and other excipients. Formulation F6 containing ispaghula husk powder in a 1:4 ratio demonstrated 98.60±0.003% of drug release within 10 minutes indicating the best formulation. Conclusion: FDT of ondansetron was considered the best formulation in the drug delivery system which followed the Higuchi model with the Fickian release.

A Review on Mouth Dissolving Tablet

Nowadays, dysphagia is an issue with traditional dosage forms like tablets and capsules, which leads to a high prevalence of non-compliance and renders therapy ineffective. Mouth dissolving tablets, which have good hardness, dose homogeneity, and ease of administration and serve as the preferred option of dosage form for paediatrics, geriatrics, and travelling patients, have been designed to eliminate the issues associated with conventional dosage forms. In order to have enough hardness, integrity, and speed up disintegration without water, the MDTs were invented. rapid dissolution Without the use of water, tablets easily dissolve or disintegrate in saliva. Some tablets are truly fast-dissolving tablets because they are made to dissolve in saliva amazingly quickly—within a few seconds. Others have additives that speed up the process of Tablet disintegration in the oral cavity is more properly referred to as fast-disintegrating tablets because it can take them up to a minute to do so. This tablet shape was created to make it possible to administer an oral solid dose form without drinking any liquids. These tablets easily dissolve or break down in the saliva, usually in under 60 seconds.