Background: Design, formulation and physicochemical evaluation of dimenhydrinate 25 mg oral tablets that disintegrate in oral cavity in a proper time. This product is easy to use for babies, geriatrics and people who have difficulty in swallowing. Materials and Methods: 31 formulations were designed in 3 categories via Design-Expert software version 7. Group 1 consist of super-disintegrating bases, group 2 consist of effervescent bases and group 3 consist of super-disintegrating and effervescent bases together. Proposed by DesignExpert software, the optimum formulations were selected in each category and the tablets were produced by direct compression method. tablets evaluated by friability, thickness, hardness, weight variation, drug content, content uniformity, disintegration time, wetting time, dissolution and moisture uptake tests. Results: The angle of repose and compressibility index of formulations were in the range of 24. 65-29. 08 and 5. 02-9. 01 % respectively. Thickness, hardness, wetting time, friability and content uniformity of formulations were in the range of 3. 36-3. 84 mm, 33. 25-38. 03 N, 19-37 seconds, 0. 31-0. 42 % and 96. 44-99. 02 % respectively. Disintegration time of the groups 1, 2 and 3 were in the range of 16-70, 47-72 and 12-35 seconds respectively. Conclusion: Mixture of powders and orally dispersible tablets passed all tests. The results showed that formulations containing both of super-disintegrants and effervescent bases had better disintegration time compare to other formulations.

Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating Fast dissolving tablets for geriatrics and those of swallowing difficulties. Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted. Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste improving agents. The obtained products were investigated regarding differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction, scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets were prepared and evaluated. Results: Thermal behavior of the developed products reflected reduced crystallinity, it also suggested possible existence of new crystalline species with sucralose. Eutexia was also suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated size reduction with the deposition of the drug as submicron particles over the excipient surface. Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The optimized formulations were successively formulated into Fast disintegrating tablets. Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a platform for the formulation of easy to use tablets with optimum drug release.

The aim of this study was to prepare orally disintegrating tablets (ODTs) containing dexamethasone (DEX) by direct compression method with sufficient hardness and rapid disintegration time. In order to save time, money, and human resources in designing and improvement of formulation, the statistical software Design Expert is used. Box–Behnken response surface methodology was applied to evaluate and optimize the effects of concentrations of three excipients, Kollidon CL-SF (X1), Pearlitol SD200 (X2), and Prosolv SMCC (X3) as independent factors on four responses: percentage of drug released after 5 min, disintegrating time, hardness, and friability. Thirteen formulations offered by the Box–Behnken design were prepared by direct compression method and ultimate weight of 200 mg, while the amount of DEX was 4 mg. All formulations were characterized for parameters such as diameter, hardness, weight, thickness, friability, and disintegration time. Following the statistical results, the effects of independent variables on responses were evaluated and the optimum formulation regarding acceptable responses consisted of 15% Kollidon, 39.66% Pearlitol, and 7.5% Prosolv which showed 95.28% release of the drug after 5 min, disintegrating time of 30 sec, 6.1 kg hardness, and 0.12% of friability with an acceptable taste as the optimized formulation.

Pramipexole is the mostly prescribed drug in patients with Parkinson disease. The incidence of Parkinson disease is related to aging and mostly developed in elderly people with difficulty in swallowing or dysphagia. In the current study we aimed to develop an orally Fast disintegrating tablet (ODT) of pramipexole as a preferable alternative in geriatric patients. Hence, the Fast disintegration is a critical for ODTs, the effects of four different superdisintegrants including, crospovidone, croscarmellose, sodium starch glycolate, and agar were evaluated on physical characteristics of the tablets. All of the formulations were prepared through direct compression method using aspartame and mannitol as taste masking agents. The flow properties of all of the mixtures were in the acceptable limits. Croscarmellose and Avicel® were chosen as the best superdisintegrants which resulted in the lowest disintegration time and the least friability. In subsequent studies, a 32 full factorial design was adopted to assess the impact of different amounts of croscarmellose and Avicel® . The overall results suggest that the tablet containing 2. 5 mg croscarmellose and 70 mg Avicel® as superdisintegrants is the best formulation. Mean hardness, disintegration time, friability, and the drug release percent during 5 min for the optimized formulation were confirmed 42. 05 ± 4. 6 Kg/cm2, 24. 98 ± 6. 8 Sec, 0. 13 %, and 95. 52 ± 2. 23%, respectively.

The aim of this study was to design orally disintegrating tablets of Olanzapine and to complexOlanzapine with 2-hydroxypropyl-b-cyclodextrin with special emphasis on disintegration and dissolution studies. Phase solubility studies demonstrated the formation of 1:1 molar inclusion complex by kneading method. tablets were prepared by using superdisintegrants namely, sodium starch glycolate, croscarmellose sodium, crospovidone, tulsion 339, and indion 414. Complex was characterized using infrared spectroscopy, drug content estimation, saturated solubility study, diffrerential scanning calorimetry and X-ray diffractometry.5% w/w croscarmellose sodium showed the minimum disintegration time 39 ± 1.76 sec and in-vitro drug release 99.19 ± 0.18% within 6 min. In general, solubility of Olanzapine can be improved by complexing with 2-hydroxypropyl-b- cyclodextrin. Croscarmellose sodium can be used for Faster disintegration of tablets.

The main objective of the present research work is to formulate the Clopidogrel Fast Dissolving tablets. Clopidogrel, an antiplatelet drug, belongs to BCS Class-II and used to control Heart attack, Hypertension by inhibiting Platelet activation and aggregation. The Fast Dissolving tablets of Clopidogrel were prepared employing different concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Superdisintegrant by Direct Compression technique using 32 factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1 and X2 respectively whereas, wetting time, Disintegration time, t50%, t90% were selected as dependent variables. Totally nine formulations were designed and evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, and in-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of developed polynomial equations was verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines, the formulation (F5) containing combination of 15% Crospovidone and 15% Croscarmellose, is the most similar formulation (similarity factor f2=91. 3936, dissimilarity factor f1= 1. 203& No significant difference, t=-0. 00062) to marketed product (PLAVIX-75). The selected formulation (F1) follows First order, Higuchi’ s kinetics, mechanism of drug release found to be Fickian Diffusion (n= 0. 226).

The purpose of the current study is to design and optimize Rosuvastatin calcium orally Fast disintegrating tablet (OFDT) with the assistance of an Artificial Neural Network (ANN) based Multi-layer Perceptron (MLP) model. Rosuvastatin calcium is commonly employed as a cholesterol-lowering agent. In our previous work established literature raw material data of OFDTs were collected from 92 research articles, which contain compositional and evaluation parameters and the data trained with Machine learning techniques (ML) to evaluate the optimal ingredients which helps further to develop and optimize Rosuvastatin calcium OFDTs using ANN based MLP. Rosuvastatin calcium OFDTs were formulated according to a 32-factorial design (randomized Box-Behnken method), and formulations were compressed using the direct compression method with varying compositions of superdisintegrant (Crospovidone) 2-4% binder microcrystalline cellulose (MCC) 5-20%, Mannitol as a diluent, magnesium stearate (Mg st) as a lubricant, and talc (1-3%) as a glidant. The developed formulations were assessed to determine their thickness, hardness, friability, disintegration time, and drug content. ANN was used for optimization, and the MLP model was trained using experimental data until a satisfactory R2 of 0.99 and normalized root mean square error (NRMSE) of 0.024 was reached. The compressed tablets (F19) exceeded the desired criteria in terms of thickness (2.6mm), hardness (2.8 kg), friability (0.6%), drug content (99%), and disintegration time (36 sec). The potential use of ANN in pharmaceutical formulation optimization to achieve desired performance characteristics is demonstrated by this work. This study shows the efficacy of ANN with MLP in the development of Rosuvastatin calcium OFDTs.

Background: Orally disintegrating tablets (ODTs) are a modern form of tablets that when placed in the oral cavity, disperses rapidly. These tablets have advantages, particularly good applications for children and old patients who have a complication in chewing or swallowing solid dosage forms.The aim of this study was to design, formulate, and evaluate the physicochemical properties of 5 mg montelukast ODTs for the prevention of asthma and seasonal allergies.Methods: Formulations were prepared with different amounts of super disintegrating agents and effervescent bases as disintegrant agents. Flowability and compressibility of mixed powders were evaluated. The prepared formulations were tested for hardness, thickness, friability, weight variation, drug content, wetting time, disintegration time, dissolution study, and moisture uptake studies.Results: The compressibility index and angle of repose were in the range of 15.87%–23.43% and 32.93–34.65, respectively. Hardness, thickness, friability, wetting time, and content uniformity of formulations were in the range of 33.7–37.1 N, 3.00–3.81 mm, 0.27%–0.43%, 31–50 s and 96.28%–99.90%, respectively. Disintegration time of the tablets prepared with super disintegrating agents, effervescent bases, and combination of two were in the range of 30–50, more than 60 and 20–36 s, respectively.Conclusions: Mixture of powders and tablets passed all the specified tests. The results showed formulations prepared by super disintegrating agents and super disintegrating agents with effervescent bases had shorter disintegration time compared to formulations with effervescent bases alone.