Preparation and Evaluation of Mouth Dissolving Tablet of Albendazole Using Different Concentrations of Super-Disintegrant

This study was done to mask the bitter taste of ondansetron HCl using complexing agent, a polacrilex resin: Tulsion 335 and subsequently forming mouth dissolving tablet using superdisintegrants: Croscarmellose sodium and sodium starch glycollate. A preliminary screening was done. Batch process, a most preferential method for drug loading with ion exchange resins was selected. The process was optimized for drug: resin ratio to get maximum drug loading. A ratio of drug: resin at 1:3 was selected. Taste evaluation was carried out by selecting volunteers. Drug resin complex (DRC) was evaluated for drug release. The resultant DRC was formulated by direct compression into mouth dissolving tablet using microcrystalline cellulose PH 102, as diluent and croscarmalose sodium and sodium starch glycolate as superdisintegrants and aspartame was used as sweetening agent to enhance palatability. Thirteen formulations were developed by using superdisintegrants: croscarmellose sodium and sodium starch glycolate. Concentration of superdisintegrants ranged from 0.75-9.24 %. The formulated tablet had satisfactory disintegration time and dissolution profile. Optimization was carried out using central composite design. The disintegration and dissolution times were tallied with marketed ondansetron HCl tablets. From the results, it was deduced that the most effective concentration for desired disintegration was of croscarmellose sodium and sodium starch glycollate respectively at concentration above 5%. Therefore, it can be concluded that the intensely bitter taste of ondansetron HCl can be masked by using tulsion 335 and mouth dissolving ondansetron HCl can be successfully prepared by adding aforementioned superdisintegrants. This sort of mouth dissolving ondansetron HCl can be used in controlling vomiting in paediatric and geriatric patients and also for pregnancy induced vomiting.

In the present investigation solid dispersion of olanzapine has been prepared to improve its solubility. Further, using solid dispersion, mouth dissolving tablet was prepared to overcome the problem of swallowing. A Simplex Lattice design was applied using three factors, i.e. superdisintegrants like croscarmellose sodium(X 1 ) crospovidone(X 2 ), and sodium starch glycolate(X 3 ) in tablet formulation. Disintegration time and T 50 (Time required to 50% drug release) taken as responses. Solid dispersion showed significant enhancement in solubility of olanzapine. For mouth dissolving tablet, batch containing 5% croscarmellose sodium alone had minimum disintegration time (44 sec.) and faster drug release (T 50 : 40 sec) compared to other batches.

Objective: The rationale of the current work is to design, develop and optimize of mouth dissolving tablet of ambrisentan to treat hypertension. Methods: Sodium starch glycolate and crospovidone were used as the super disintegrants in the direct compression method to create nine ambrisentan mouth-dissolving tablet formulations. Wetting time, drug content, in vitro disintegration time, dispersion time, and dissolution time were all assessed for the produced formulations. Results: Based on the results obtained, formulation F6 containing 30 mg of crospovidone exhibited good wetting time, dispersion time, disintegration time and drug release. The hardness of formulations AS1 to AS9 was found to be in the range of 2.5 to 3.11 Kg/cm2. The friability of formulations AS1 to AS9 was found to be less than 1%. A water absorption ratio was performed for ensuring the moisture sorption and water uptake properties of super disintegrants. The in vitro drug release of formulation AS6 containing a concentration of Crospovidone 30 mg, shows 91.30% drug release respectively at the end of 12 min. Conclusion: The mouth-dissolving tablets of ambrisentan were successfully designed, developed, and fabricated. It can be reasonably concluded that the AS6 batch of mouth-dissolving tablets of ambrisentan with 30 mg of crospovidone exhibited maximum cumulative drug release in 12 min.

Introduction: Oro-dispersible tablets are rapidly dissolved in saliva without the need for water and are beneficial for renal impaired, bedridden and psychiatric patients. Objective: The study aimed to formulate oro-dispersible tablets of indomethacin with reduced adverse effects, better patient compliance, faster action, and convenience for patients. Methods: Oro-dispersible tablets of indomethacin were prepared using three different super disintegrants; crospovidone, croscarmellose sodium and sodium starch glycolate with three different concentrations (2.5%, 5.2%, and 7.7%) by direct compression method. The prepared tablets were evaluated for pre and post-compression parameters including bulk density, tapped density, compressibility index, angle of repose, Hausner's ratio, hardness, friability, wetting time, in vitro disintegration time, and in vitro drug release. Results: The percentage of drug released in 5 minutes of all formulations of Oro-dispersible tablets of Indomethacin was found to be 74.36% to 80.16% and the percentage of drug released in 10 minutes was 96.18% to 100%. All formulations showed disintegration time in the range of 19-78 seconds. The tablets prepared with 7.7% crospovidone (F6) shows faster disintegration (19 seconds) as compared to tablets prepared with sodium starch glycolate and croscarmellose sodium. The in-vitro dissolution studies showed that tablets of formulations batch containing 7.7% crospovidone releases 100% of the drug after 10 minutes which was fast released as compared to sodium starch glycolate and croscarmellose sodium. Conclusions: Oro-dispersible tablets of indomethacin prepared with crospovidone showed better disintegration time and dissolution profile as compared to other superdisintegrants.

: Objective: To formulate a mouth dissolving tablets of dexamethasone for the use of paediatrics, geriatric patients and also dysphagic patients. Methodology: Tablets were formulated by using different types of natural Super disintegrants in different concentration such as Guar gum and Xanthan gum. A manual 7 mm single punch tablet compression machine was used to compress the tablet. Powder mixture of 150mg was weighed accurately and added into the die cavity. The prepared dexamethasone MDT tablets were evaluated for its physico-chemical parameters such as thickness, hardness, weight variation, friability, disintegration time, wetting time, in-vitro dispersion time, water absorption ratio and also in-vitro drug release. Results: The FTIR and DSC studies conferred that there is no interaction between dexamethasone and Super disintegrants. The dissolution profile of dexamethasone MDT compared with conventional dexamethasone tablet shows improved in % drug release and faster % drug release. An increase in the concentration of Super disintegrants showed faster % of drug release and similar % of cumulative drug release. Conclusion: Dexamethasone MDT using Guar Gum and Xanthan Gum could be considered as good formulation and delivery system to increase the patient’s compliance as the % drug release and disintegration time are much better than conventional Dexamethasone tablet. Key words: Mouth Dissolving Tablets, dexamethasone, Super disintegrants, Rapid disintegration, Dysphagia.

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.

The aim: This study aimed to develop mouth-dissolving tablets of Acrivastine, an antihistamine medication, in order to increase its oral bioavailability. Materials and methods: Different super disintegrants, such as crospovidone, croscarmellose sodium, and sodium starch glycolate, were used to make Acrivastine oral dispersible tablets (ODTs). These super disintegrants were utilized in various concentrations. The formulation (F3) with 6% w/w crospovidone had a fast disintegration time (less than 30 seconds) and practically total drug release within 10 minutes. All of the formulations were made using the direct compression method and proper diluents, binders, and lubricants. Fourier transform infrared spectroscopy (FTIR) tests were used to investigate the drug-ex¬cipient interaction, and all formulations demonstrated improved drug-excipient compatibility. Results: The average weight of all formulations was between 175 and 180 mg. All formulations' hardness and friability were within acceptable ranges. Direct compression tablets had a hardness of 3.2 to 4 kg/cm2. All formulations were determined to have a friability of less than 1.0%. For oral dissolving tablets, the in vitro disintegration time is critical, and this time preferred to be < 60 seconds. The results also showed that crospovidone disintegrated after 24 seconds and sodium starch glycolate disintegrated in 40 seconds in vitro. Conclusions: When compared to croscarmellose sodium and sodium starch glycolate, crospovidone performs better as a super disintegrant. In comparison to other formula, tablets breakdown in the mouth in 30 seconds and have a maximum in vitro drug release time in 1-3 minutes.

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.

Bosentan, a biopharmaceutical classification system (BCS) Class II drug (low solubility, high permeability), suffers from poor oral bioavailability due to its limited solubility and extensive first-pass metabolism. The objective of this study was to formulate, develop and evaluate mouth-dissolving tablets (MDTs) of Bosentan to enhance its dissolution rate, patient compliance, and potentially improve bioavailability by pre-gastric absorption. MDTs were prepared by direct compression method using various superdisintegrants such as croscarmellose sodium (CCS), sodium starch glycolate (SSG) and crospovidone (CP) in different concentrations (2%, 4%, 6% w/w). Microcrystalline cellulose and mannitol were used as diluents. The formulated tablets were evaluated for pre-compression parameters (angle of repose, bulk density, tapped density, Carr’s index, Hausner’s ratio) and post-compression parameters (weight variation, hardness, friability, drug content, wetting time, water absorption ratio, in-vitro disintegration time and in-vitro dissolution studies). All formulations showed good pre-compression properties. The post-compression evaluation revealed that all tablets complied with pharmacopoeial standards. Formulation F5, containing 6% w/w crospovidone, exhibited the shortest disintegration time (14.2 ± 1.3 seconds) and the highest drug release (99.45% within 15 minutes), which was significantly higher than the conventional tablet. The results of the optimized formulation (F5) were found to be satisfactory. In conclusion, the study successfully demonstrated that mouth-dissolving tablets of Bosentan with enhanced dissolution characteristics can be formulated using superdisintegrants by direct compression. Croscarmellose sodium and crospovidone were particularly effective, with crospovidone at a higher concentration yielding the best results, offering a promising approach to improve the therapeutic efficacy of Bosentan.

In the present study, the effects of a natural superdisintegrant vis-a-vis isolated mucilage of Plantago ovata and synthetic superdisintegrants like sodium starch glycolate (SSG) and croscarmellose sodium (Ac-di-sol) were compared in the formulations of fast dissolving tablets (FDT). FDTs of aceclofenac (model drug) were prepared by direct compression method using microcrystalline cellulose as direct compressible vehicle. Th ose tablets were evaluated for weight variation, hardness, disintegration time, drug content, friability and dissolution. Swelling index was also investigated with an aim to compare the swelling property of mucilage of Plantago ovata with SSG and Ac-di-sol. Among all the super disintegrants, Plantago ovata mucilage showed the highest swelling index. Hence, the present study revealed that this natural superdisintegrant (Plantago ovata mucilage) showed better disintegrating property than the most widely used synthetic super disintegrants like SSG and Ac-di-sol in the formulations of FDTs. Key words: Fast dissolving drug delivery, Plantago ovata mucilage, swelling index, sodium starch glycolate, croscarmellose sodium

Introduction: Gliclazide is a sulfonylurea derivative used for the treatment of type 2 Diabetes, it is an anti-diabetic drug it is marketed under the brand name Diamicron. It is taken orally and used when dietary changes, lack of exercise, and weight loss are not sufficient. &#x0D; Aim: The principal objective of this work was to develop, formulate and evaluate the pellet formulations prepared with the incorporation of different super disintegrants in different ratios and in different combinations. In this research work, the drug gliclazide was chosen as a model drug and it was formulated into fast-dissolving pellets, which can be compressed into pelltabs and can also be filled into capsules. &#x0D; Methods: Pellets were prepared by extrusion and Spheronization containing microcrystalline cellulose (MCC) and using gliclazide as a model drug with different super disintegrants namely croscarmellose sodium, crospovidone and sodium starch glycolate in different ratios, and in different combinations. Thus, in the present study, gliclazide pellets were developed using Extrusion-Spheronization for immediate drug delivery. The pellets were evaluated for percentage drug content, flow properties, friability, size analysis, shape analysis, disintegration test, and dissolution studies. Preformulation studies were then performed using solubility studies, partition co-efficient studies, infrared spectroscopy, and drug-excipients compatibility studies between the drug and selected excipients (croscarmellose sodium, crospovidone, and sodium starch glycolate) investigated.&#x0D; Results: Formulations containing MCC, super disintegrants, and drugs in different ratios of 60/0/40, 55/5/40, and 50/10/40 w/w of croscarmellose sodium, crospovidone, and sodium starch glycolate were found to show faster release of the drug for 9 hours. Croscarmellose sodium releases the drug as it disintegrates the &#x0D; &#x0D; pellets. Sodium starch glycolate releases the drug by inducing swelling in the pellet &#x0D; matrix. Unlike the other two super disintegrants, there was no apparent change in the swelling capability of the pellets of polymer crospovidone (Polyplasdone XL10) in water. The percentage increase in diameter for Ac-Di-Sol (croscarmellose sodium), Primojel (sodium starch glycolate), and Polyplasdone XL10 were 104%, 251%, and 29% in water.&#x0D; Conclusions: Various types of super disintegrants can be investigated for their suitability in formulating pellets. In vivo drug release rate, and bioavailability studies on animals and humans may be carried out to assess the superiority of the pellets over the tablet dosage form.

Fast Dissolving Tablet instead of dissolving or disintegrating in water is expected to dissolve or disintegrate in oral cavity without drinking water. Super disintegrates are added to a drug formulation to facilitate the break-up or disintegration of tablet or capsule content into smaller particles that can dissolve more rapidly than in the absence of disintegrates In the present study, the effects of a natural superdisintegrants Plantago ovata, Hibiscus rosa sinensis and synthetic superdisintegrants like sodium starch glycolate (SSG), Crosspovidone and Croscarmellose sodium (Ac-di-sol) were compared in the formulations of fast dissolving tablets (FDT). FDTs of Cefixime were prepared by direct compression method and were evaluated for weight variation, hardness, thickness, disintegration time, wetting time, water absorption ratio, In vitro dispersion, friability and dissolution. Among all the super disintegrates, Plantago ovata showed the highest swelling index and natural super disintegrates like husk of Plantago ovata showed better disintegrating property than the most widely used synthetic super disintegrates like AC-di-Sol, C.P and SSG in the formulations.

The present study was aimed to formulate and evaluate fast-disintegrating tablets (FDTs) having Flurbiprofen (FP) and Metoclopramide HCl (MHCl) in combination. Direct compression was used to formulate FDTs of FP and MHCl as a combination regimen in six formulations. FDTs are defined as solid oral dosage form that disintegrates rapidly within seconds when placed in the oral cavity. FDT-1, FDT-2, FDT-3, FDT-4, FDT-5, and FDT-6 were formulated using crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants each in two formulations. Several pre-compression tests (angle of repose, bulk density, tapped density, Hausner’s ratio, and compressibility index), post-compression evaluation (weight variation, friability, hardness, disintegration time, wetting time, assay, in vitro dissolution study, release kinetics study, statistical analysis, and stability study), and drug compatibility study were done for all six formulations. Pre-compression evaluation showed good flow properties of powder blend. Drug compatibility study showed no interactions between active drugs and excipients. Disintegration and wetting time of all the formulations were in seconds indicating immediate release of drug. Optimized formulation (FDT-6) containing sodium starch glycolate in 15 mg gave 100% release in 15 min for MHCl and in 20 min for FP. Optimized formulation was found stable after being placed at accelerated stability conditions for 6 months. Release kinetics study showed that all formulations followed Korsmeyer-Peppas model indicating drug release from modified release dosage form. Statistical analysis revealed no significant difference statistically (p > 0.05) between drug release rate of all prepared formulations. FDTs improved the release rate that assured that this tactic may be beneficial to increase the dissolution rate of FP and MHCl in order to increase patient compliance.

Objective: The objective of this study was solubility and dissolution enhancement of domperidone (DOM), and further they were formulated as mouth dissolving tablets (MDT). Method: DOM-solid dispersion (DOM-SD) was prepared using suitable complexing agent (2-hydroxypropy-β-cyclodextrin) by kneading method; the solid dispersion prepared was further formulated into MDT by direct compression using super disintegrants (Kyron-T314, sodium starch glycolate, and Plantago ovata husk) in varying ratios. The prepared SDs were evaluated on Fourier transform infrared (FT-IR), percent yield, percent drug content (DC), saturation solubility, phase solubility, in vitro release, pre- and post-compression test. Results and Discussions: Percent yield and DC of DOM-SD was 81.48 ± 4.35% to 95.31 ± 3.01% and 91.96 ± 0.72% and 99.28 ± 0.23%, respectively, saturation solubility was at higher in DOM-SD as compared to DOM alone, FT-IR studies revealed no drug excipient interaction except DOM-2-hydroxypropyl-β-cyclodextrin (2- HPβCD) which was deliberate, formulation KF5 showed best in vitro dissolution for DOM-SD. Pre-compression parameters like supported formulation of MDT of DOM. Post-compression parameters such as thickness, hardness, weight variation, friability, percent DC, water absorption ratio, wetting time, disintegration time, and in vitro dissolution suggested effective improvement and prompt release in the simulated conditions. The selected formulation KF2 also showed good stability data at accelerated conditions. Conclusion: DOM-SD was prepared using 2HPβCD which effectively enhanced DOM solubility and dissolution; moreover an effective DOM-MD was also prepared for prompt relief from nausea and vomiting.

Objective: Teneligliptin is a newly advanced oral dipeptidyl peptidase 4 inhibitor used for the treatment of type 2 diabetes mellitus in adults alongside exercise and diet. In this study, teneligliptin orodispersible tablets (ODTs) were developed to improve solubility and bioavailability. Methods: In the present work, using various superdisintegrants such as croscarmellose sodium, sodium starch glycolate (SSG), and Crospovidone, a total of nine formulations of teneligliptin ODTs were developed by the direct compression method. All the developed formulations were subjected to in vitro characterization and studied for various physicochemical properties, drug release studies, and release kinetics. The physical stability study was conducted on the optimized formulation for 6 months. Results: All the developed formulations met the pharmacopoeial limits for weight variation, hardness, friability, and drug content. Among nine formulations, the F9 formulation showed the fastest disintegration time of 15 s and 99.12% of drug release within 15 min. Based on the wetting time, disintegration, and drug release studies, the F9 formulation was selected as the optimized formulation. Further, the F9 formulation was stable for 6 months. Conclusion: Teneligliptin ODTs were successfully prepared by the direct compression method using croscarmellose sodium, SSG, and crospovidone as super disintegrants. The optimized formulation F9 showed the highest drug release and was stable for 6 months.