OPTIMIZED FAST DISINTEGRATING TABLETS, BOOSTED OSELTAMIVIR PHOSPHATE ORALLY FAST DISINTEGRATING TABLETS

Background Around 33% of the populace (fundamentally pediatric and geriatric) has gulping hardships, bringing about helpless consistence with oral tablet drug treatment which prompts decreased in general treatment viability. For this explanation, tablets that can quickly break down or deteriorate in the oral cavity have drawn in a lot of consideration. Objective research was designed to develop and evaluate boosted orally fast disintegrating tablets (OFDT) for oro-buccal drug delivery of oseltamivir phosphate. Methods In the present study six formulations of mouth dissolving tablet of oseltamivir were prepared by direct compression method using SSG as a super disintegrating agent with lactose, talcum, mannitol, SLS and starch. The prepared tablets were then subjected to various evaluation parameters. Results every one of the outcomes was observed to be inside satisfactory reaches. The formulation F6 manufacturing utilizing SSG 50mg and SLS 10mg showed the higher medication content (98%), while the formulation F2 showed the least medication content (92%). It was seen that with the increment in SSG concentration, the medication content was additionally increased. SEM concentrate on showed request of expanding unpleasantness of tablet surface is F1<F2<F3<F4<F5<F6. The expanding unpleasantness may be answerable for higher % of medication release. Formulation F1 showed the most elevated medication discharge (97.735%), while the formulation F5 showed the least medication discharge (56.24%). Finally, it was inferred that SSG, SLS, D-mannitol, starch, lactose, and talcum powder can be effectively utilized in the formulation of Oseltamivir phosphate mouth dissolving tablets. Conclusion: From the above work it was presumed that the formulation of the Oseltamivir Phosphate was observed to be more achievable than the regular one.

DEVELOPMENT AND CHARACTERIZATION OF TACROLIMUS TABLET FORMULATIONS FOR SUBLINGUAL ADMINISTRATION

Objective: The study aimed to prepare and characterize inclusion complexes of tacrolimus with β-cyclodextrin to improve its solubility and to formulate them into sublingual fast disintegrating tablets with a view to bypass the first-pass metabolism. Methods: Tacrolimus: β-cyclodextrin inclusion complexes (1:1 and 1:2 molar proportions) were prepared using the kneading method. Their characterization was accomplished by determining the drug content, solubility, Attenuated Total Reflection-Infrared Spectroscopy (ATR-IR), Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and powder X-Ray Diffraction analysis (pXRD). These were then formulated to fast disintegrating tablets and evaluated for precompression as well as post compressional characteristics. Results: SEM analysis showed the inclusion complexes as rough, non-porous, irregular surfaced aggregate particles. DSC and pXRD analyses confirm the crystallinity change and partial conversion to the amorphous form of the drug in the inclusion complexes. From the solubility studies, it was observed that both the inclusion complexes of 1:2 molar ratio (14.82±0.889 µg/ml) and 1:1 molar ratio (12.72±0.1004 µg/ml) improved the aqueous solubility to greater extents in comparison to that of the pure drug (3.05±0.121 µg/ml). All the tablet formulations showed good precompression and mechanical properties. The inclusion complex loaded tablets exhibited a superior drug release pattern when compared to tablets prepared with tacrolimus alone. The optimized formulation (TT3) showed an in vitro disintegration time of 34.33 s and a percent drug release of 97.87. Conclusion: The inclusion complex formulation combined with the sublingual route of administration can be expected to result in an improved bioavailability of tacrolimus by increasing its solubility and bypassing first-pass metabolism.

Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Measuring tablet disintegration is essential for quality control purposes; however, no established method adequately accounts for the timeframe or small volumes of the medium associated with the dissipation process for fast disintegrating tablets (FDTs) in the mouth. We hypothesised that digital imaging to measure disintegration in a low volume of the medium might discriminate between different types of FTD formulation. A digital image disintegration analysis (DIDA) was designed to measure tablet disintegration in 0.05–0.7 mL of medium. A temperature-controlled black vessel was 3D-printed to match the dimensions of each tablet under investigation. An overhead camera recorded the mean grey value of the tablet as a measure of the percentage of the formulation which remained intact as a function of time. Imodium Instants, Nurofen Meltlets and a developmental freeze-dried pilocarpine formulation were investigated. The imaging approach proved effective in discriminating the disintegration of different tablets (p < 0.05). For example, 10 s after 0.7 mL of a saliva simulant was applied, 2.0 ± 0.3% of the new pilocarpine tablet remained, whereas at the same time point, 22 ± 9% of the Imodium Instants had not undergone disintegration (temperature within the vessel was 37 ± 0.5°C). Nurofen Meltlets were observed to swell and showed a percentage recovery of 120.7 ± 2.4% and 135.0 ± 6.1% when 0.05 mL and 0.7 mL volumes were used, respectively. Thus, the new digital image disintegration analysis, DIDA, reported here effectively evaluated fast disintegrating tablets and has the potential as a quality control method for such formulations.

FORMULATION AND EVALUATION OF PRAVASTATIN FAST DISINTEGRATING TABLETS USING NATURAL SUPERDISINTEGRANT

The basic concept of FDT is the incorporation of superdisintegrants, which promotes breakdown of tablet quickly when kept or positioned on the tongue, allowing the drug to be released into the saliva. The rate of absorption is regulated by the solubility of the medication. The faster the dosage form of the medication dissolves in solution, the faster the therapeutic action is absorbed and initiated. In FDT, a medicine or dose form should dissolve or disintegrate in the saliva within 60 seconds. The objective of this research work is to formulate a Pravastatin tablet that disintegrated quickly using natural disintegrants. As a diluent, we employed microcrystalline cellulose. Synthetic superdisintegrant such as crospovidone and croscarmellose sodium were used, they were replaced with natural superdisintegrant. In this study, natural superdisintegrant dehydrated banana powder were used synthetic superdisintegrants viz. croscarmellose sodium, crospovidone. A Natural superdisintegrant was used in this formulation at concentrations of 2, 4, 6 and 8% of total weight of tablet i.e. 4, 8, 12 and 15 mg respectively in 200 mg tablet. According to the data, the tablet formulation containing 6% banana powder (i.e., 12 mg per tablet, formulation code FB4) showed a faster and higher drug release of 97.75% during the in-vitro dissolution investigation.

Natural Polymer Chitosan as Super Disintegrant in Fast Orally Disintegrating Meloxicam Tablets: Formulation and Evaluation

The aim of the present investigation was to formulate fast disintegrating tablets of meloxicam by wet granulation technique using medium molecular weight chitosan. The orally disintegrating tablets of meloxicam with chitosan showed good mechanical and disintegration properties and good dissolution rate when prepared in tablet press using 10.8 kN and 11.0 kN compression force. Chitosan is a suitable biopolymer to moderate the disintegration process in orally disintegrating tablets.

Formulation, Optimization and In Vitro Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate using a Combination of Superdisintegrant and Subliming Agent

Aim: The present research work was aimed to formulate fast disintegrating tablets (FDTs) of salbutamol sulphate (SBS) using a combination of superdisintegrant and subliming agent, optimize the formulation and evaluate the in vitro performance of the developed FDTs. Materials and Methods: A formulation of SBS FDT was developed using a combination of superdisintegrant – crospovidone and subliming agent – ammonium bicarbonate (AB) in which formulation variables, namely levels of crospovidone and microcrystalline cellulose (MCC):Mannitol (MNTL) ratio were evaluated for their effects on the response variables - disintegration time, hardness, friability and wetting time of the resulting FDTs. By employing a central composite design (CCD) methodology, the FDTs were optimized to achieve optimum levels of the formulation factors. Results: The desired optimum condition was obtained at 7.82% crospovidone and 70% of 1.56:1 MCC: MNTL ratio while maintaining AB at 5% level for aesthetic reasons. Under the optimized conditions, the disintegration time, hardness, friability and wetting time were 14.57±0.53 sec, 7.17±0.82 kg/cm2, 0.311% and 13.14±0.69 sec, respectively. The experimentally observed responses were found to be in close agreement with the predicted values for the optimized formulation. Moreover, the validity of the obtained optimal point was confirmed by the low magnitude of percent prediction error (<5%). Conclusion: FDTs of SBS were successfully formulated and optimized using CCD employing a combination of superdisintegrant and subliming agents.

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.

Preparation and optimization of fast disintegrating tablets of isosorbide dinitrate using lyophilization method for oral drug delivery

Background: Orally disintegrating tablets rapidly disintegrate in saliva and then swallowed without the need for water. Materials & methods: The orally disintegrating tablets were prepared by freeze-drying of an aqueous dispersion of isosorbide dinitrate containing a matrix former (gelatin), a cryoprotectant (mannitol), a plasticizer (glycerin) and a dissolution enhancer (Tween/polyethylene glycol). Results: Results demonstrated that the selected formulation, Ft9, disintegrated within 1 min and showed faster dissolution rate compared with the commercial tablet. Conclusion: Having a fast disintegration time, the developed lyophilized tablet does not need to be swallowed as a whole. So, it is a convenient solid oral dosage form for the patients who have difficulty with swallowing such as the pediatric and elderly ones.

FORMULATION AND EVALUATION OF MODIFIED DISINTEGRATING SUSTAINED RELEASE TABLETS OF DICLOFENAC SODIUM

Oral drug delivery is the largest and the oldest segment of the total drug delivery market. It is the fastest growing and most preferred route for drug administration. In oral drug delivery, the sustained release (SR) tablets maintains the desired drug concentration for prolong period of time, reduced 'see- saw' fluctuation, reduced total dose, improved efficiency in treatment. But many patients like paediatric, geriatric and also patients may have difficulty in swallowing (Dysphagia) find it difficult to swallow tablets and thus do not comply with prescription. This problem is overcome by formulating and developing modified disintegrating sustained release tablets. In this case, first microspheres of the drug are formulated by using any suitable technique. And then optimized microspheres formulation is further formulated in to the fast disintegrating tablets (FDT) by using superdisintegrants. So that after taking such a tablets, the tablet only disintegrates into the mouth then microspheres are separated and ingestion of such microspheres starts releasing drug for prolonged period of time. This concept fulfills both the advantages of sustained release and fast disintegrating tablets.