Design and Optimization of Nadolol sublingual tablet

Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.

The aim of present work was to show the effect of various superdisintegrant on the disintegration time and in vitro drug release rate. In this study, an attempt had been made to prepare orally disintegrating t ablets of the Hydrochlorthiazide using co - processed super disintegrant following direct compression method. Sodium starch glycolate, crospovidone and starch were used in different concentrations as the super disin tegrant. The tablets were evaluated for dia meter, thickness, hardness, friability, weight variation, wetting time, disintegration time, dispersion time, drug content an d in vitro dissolution studies. Friability value of none of the formulation exceeds 0.245 %. The dispersion time of all Formulatio n were found to be in between 17.95(±0.06) to 55.61(±0.06) seconds. The we tting time of all the tablets was in the range 25.70 - 52.70 second s . Overall, the formulation A5 containing 4 % w/w of co - processed superdisintegrants (1:1 mixture of crospovidone a nd sodium starch glycolate) was found to be promising and has shown an in vitro dispersion time 17.95 sec. , wetting time 21.14 sec and disintegration time 17.05 sec. Percentage cumulative drug release of formulation A5 was found to be 98.51% that is maximu m % drug release than other formulation. Formulation A5 containing 4%w/w of co - processed superdisintegrant (1:1 mixture of Crospovidone and sodium Starch glycolate) , using direct compression method was found to be the best formulation that has minimum di sintegration time, wetting time hence this formulation was selected for In - vitro dissolution study and more than 95% drug was dissolved within 15 min.

Objective: The main aim is to design, optimize, and evaluate ibuprofen fast-dissolving tablets by employing starch valerate-A novel super disintegrant.
 Methods: The fast-dissolving tablet of ibuprofen was prepared by employing starch valerate as super disintegrant in different proportions in each case by direct compression method using 23 factorial design, sodium starch glycolate, and crospovidone used as super disintegrants. In the 23 factorial design, these super disintegrants were applied to investigate the interaction effects of three variables, that is, (a) starch valerate, (b) sodium starch glycolate, and (c) crospovidone. The drug content, hardness, friability, disintegration time, and other dissolution characteristics were determined.
 Results: The starch valerate prepared was found to be fine, free-flowing, slightly crystalline powder. Starch xanthate exhibited good swelling in water with 125.2%. All the fast-dissolving tablets formulated employing starch valerate were of good quality with regard to drug content (100±5%), hardness (3.6–3.8 kg/sq. cm), and friability (0.11-0.12%). The disintegration time of all the formulated tablets was found to be in the range of 12±0.02 to 30±0.02s. The optimized formulation FL8 has the least disintegration time, that is, 12±0. 02s. The in vitro wetting time of the formulated tablets was found to be in the range of 21±0.09 to 44±0.10s. The in-vitro wetting time was less (i.e., 90s) in optimized formulation FL8. The water absorption ratio of the formulated tablets was found to be in the range of 30±0.12 to 100±0.09%.
 Conclusion: Starch valerate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, crospovidone, with the ibuprofen.

Development and characterization of sublingual tablet of Lisinopril

Objective: The aim of the present study was to prepare and optimize levamisole chewable tablets by using various super disintegrants, namely; sodium starch glycolate, DRC Indion 204, and DRC Indion 234.
 Methods: Drug excipient compatibility study was carried out by FTIR spectroscopy to verify the compatibility of levamisole with the excipients. Nine batches of levamisole chewable tablets were prepared according to 32 factorial designs using a direct compression method by optimizing the super disintegrant concentration. The powder blend was exposed to pre-compression studies of the powder blend followed by post-compression studies of the formulated tablets.
 Results: FTIR study revealed that the excipients used in the formulations were compatible with the drug. The pre-compression and post-compression parameters were found within the IP limits. Form the dissolution studies, it was evident that the formulation prepared with DRC Indion 234 (50 mg) showed maximum percentage drug release in 45 min (97.13%) hence it is considered as optimized formulation. When compared to all other formulation, the batches with DRC Indion 234 (F7-F9) showed a better release of the drug (90 % drug release within 45 min).
 Conclusion: Nine batches of levamisole chewable tablets were successfully formulated by optimizing the concentration of super disintegrants such as sodium starch glycolate, DRC Indion 204, and DRC Indion 234. It was concluded from the dissolution studies that the DRC Indion 234 is the best super disintegrant irrespective of their concentration for the formulation of levamisole chewable tablets when compared to sodium starch Glycolate and DRC Indion 204.

The study was carried to formulate and evaluate dispersible tablet dosage form obtaining Nateglinide.Nateglinideis adrugfor the treatment oftype 2 diabetes. The present study is an attempt to select best possible combination of diluents and disintegrates to formulate dispersible tablet of Nateglinide which disintegrates within few minutes thereby reducing the time of onset of action. Mannitol is selected as diluents, Sodium starch glycol ate, Cross-povidone, cross-carmellose sodium were selected as super disintegrates, citric acid and sodium bi carbonate is effervescent active ingredient in different concentrations. Aspartame as a sweetening agent, Magnesiumstearate as a Lubricant and glidant.Direct Compression method was used to formulate the tablets.All the formulations were showed the acceptable flow properties and the pre-compression parameters like Bulk density, Tapped density and Hausner ratio. The post compression parameters like Hardness, Friability, Disintegration time, Weight variation, wetting time, Dispersion time values were found to be within the IP limits.The percentage Drug content of all tablets was found to be between 99% - 100 % of Nateglinide, which is within the limit.As the concentrations of the Citric acid (preservative) & sodium bicarbonate (active ingredient respectively taking increases in the formulations F7 F9 the disintegration time found to be decreased and the disintegration time for these formulations were 33, 31, 30 seconds respectively and the percentage drug release was also found to be increased for these formulations as 94 ,96, and 99 % respectively. From the above results it was found that as the concentration of citric acid decreased and sodium bi carbonate increases the disintegration and dissolution time was found to be improved, so considering the above results it was found that the F9 batch was found to be optimized batch and it pass all the pre-formulation parameters and evaluation results as per the IP limits.

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.

Ebastine is a long-acting, nonsedating, second-generation antihistaminic drug that prevents histamine action, mainly in immediate hypersensitivity. This project was aimed to formulate and characterize orodispersible tablets of ebastine, utilizing different proportions of three disintegrants, namely crospovidone, sodium starch glycolate, and coprocessed superdisintegrant. Initially, fifteen trial batches of ebastine orodispersible tablets were outlined using the central composite design of Minitab software. The tablets were formulated by the direct compression method. The compressed tablets were then evaluated for precompression and postcompression physicochemical parameters, such as angle of repose, Carr's index, Hausner's ratio, hardness, thickness, weight variation, drug content, friability, wetting time, disintegration time, dispersion time, and water absorption ratio. The in vitro dissolution test was conducted according to Indian Pharmacopeia 2018, with the help of the rotating paddle method using 0.5% w/v sodium lauryl sulfate buffer in 0.1 N HCl. For the optimized batch (8th batch), all the physicochemical parameters like angle of repose (33.77°), Carr's index (19.34%), Hausner's ratio (1.24), weight variation (202.5 mg), hardness (4.3 kg/cm2), friability (0.44%), thickness (3.16 mm), dissolution (95.78%), and drug content (101.67%) were within the acceptable limit as per Indian Pharmacopeia 2018. The wetting time, disintegration time, dispersion time, and water absorption ratio were reported to be 25.1 seconds, 16.0 seconds, 38.6 seconds, and 91.92%, respectively. Hence, the results suggested that orodispersible tablets of ebastine can be formulated. Furthermore, the mixing of crospovidone, sodium starch glycolate, and coprocessed super disintegrants can result in excellent desirable properties in the orodispersible tablet.

The present study deals with the formulation of fast dissolving tablets of poorly soluble carbamazepine by the direct compression technique with β-cyclodextrin complexes using various super disintegrants like Indion-414, croscarmellose sodium, crospovidone and sodium starch glycolate. Carbamazepine is used to control different types of seizures in the treatment of epilepsy. Poor solubility in biological fluids is the major problem with this drug as also its poor bioavailability after oral administration.The rate of absorption and/or the extent of bioavailability for such a poor soluble drug is controlled by rate of dissolution in gastrointestinal fluids. Hence, to enhance the solubility of the drug, a complex of carbamazepine was prepared with β-cyclodextrin and this complex was compressed into tablets. The prepared tablets were evaluated for hardness, friability, drug content, weight variation, disintegrating time, wetting time, in vitro dissolution studies, etc. The prepared tablets were characterized by DSC, Fourier transform infrared spectroscopy (FTIR) and stability studies.The different formulations showed disintegration times between the ranges of 26.86 and 58.54 s. Drug release showed time between the ranges of 4 and 12 min. Among all the formulations, B8 showed 99.89% drug release within 4 min.Thus, B8 was considered as the best among the other formulations. No chemical interaction between the drug and the excipients was confirmed by DSC and FTIR studies. The stability study was conducted as per the ICH guidelines and the formulations were found to be stable, with insignificant changes in hardness, drug content and disintegration time.These results revealed that fast dissolving tablets of the poorly soluble drug, carbamazepine, showing enhanced dissolution and, hence, better patient compliance.

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

Bilastine (BLS) is a second-generation H1-antihistamine that is approved recently for the symptomatic treatment of chronic urticaria. The present investigation was to develop oral disintegrating tablets of BLS to produce a fast onset of action. In this study, an attempt was made to compare the effect of different natural and synthetic super disintegrants on the release profile of the formulation. The formulations (BF1-BF15) of BLS oral disintegrating tablets were prepared by direct compression technique using synthetic and natural super disintegrants (Chitosan, Fenugreek mucilage, Sodium starch glycolate, Ludiflash, Cross povidone) in three different concentrations (2, 4, and 6%). The formulated tablets were analyzed for pre-compression and post-compression parameters and in vitro drug release. The best formulation, F15 containing 6% Ludiflash as a super disintegrant, was found to have a maximum water absorption ratio and disintegration time and in vitro dissolution was found to be less than 5 min, ensuring faster disintegration and dispersion. The F15 formulation shows less disintegration and dispersion time because of its combined effect and formulation, which had a better drug release of 99.79% within 20 min. The dissolution pattern of various disintegrants used in the formulation was found to be in the order of Ludiflash>Cross povidone>chitosan>SSG>Fenugreek mucilage. Overall, the results show that the formulated oral disintegrating tablets of BLS with Ludiflash as a super disintegrant, indicating that this could be a feasible drug delivery for BLS.

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

Prednisolone is a glucocorticoid with the general properties of the corticosteroids. It is used as anti-inflammatory or immunosuppressive agent in asthmatic condition mostly in pediatric and geriatric population. So the present investigation was conducted with an aim of to formulate a taste masked patient friendly dosage form i.e. mouth dissolving tablets of prednisolone. In this study, taste masking of drug was critical parameter for this study. Masking of bitter taste of prednisolone was carried out using techniques like preparation of solid dispersion with PEG 6000, complex formation with Indion-204 resin and β-cyclodextrin. Among them complex prepared from β-cyclodextrin in weight ratio 1:4 was optimized basis on taste panel evaluation and drug release from complex. A successful taste masking of complex was confirmed by time intensity method and also by taking drug release in simulated gastric fluid and in simulated salivary fluid. The values of pre-compression parameters evaluated, were within prescribed limits and indicated good free flowing properties. Tablets optimization was carried out through 32 full factorial designs, concentration of superdisintegrants like croscarmellose sodium and sodium starch glycolate as independent variable. Whereas wetting time, disintegrating time and cumulative percentage of drug release as dependent variable. The data obtained of post-compression parameters such as weight variation, hardness, friability, wetting time, water absorption ratio, content uniformity, disintegration time and dissolution was found within specified limit. Prepared check point batch having disintegrating time 16.12 s and drug release 98.34 after 30 min was selected as optimized formula. This formula was compared with marketed formulation and was found better disintegration and drug release property. Optimized formulation was subjected for accelerated stability study as per ICH guideline.

The current study mainly focused on treating cardiovascular diseases such as angina pectoris and chronic hypertension by modifying the existing commercial tablet available for Nifedipine. The limitation of Nifedipine is poor solubility, which comes under BCS class II drug category, which needs improvement in formulation to achieve better bioavailability. The objective of this research work is to enhance the oral bioavailability (first-pass metabolism in the liver (42–56%)) of Nifedipine by improving dissolution property. Sublingual fast dissolving tablets of Nifedipine formulated by sublimation method, designed to increase its disintegration time in the presence of saliva. This formulation is helpful for paediatric and geriatric patients who are unable to swallow the conventional tablet. Sublimation of camphor makes the tablet more porous and improve disintegration time as well. The direct compression method is used with different ratio of Croscarmellose Sodium (CS) and Sodium Starch Glycolate (SSG) as super disintegrants to formulate Nifedipine loaded Sublingual tablets. All formulations contain various ratio between super disintegrants and camphor, followed by the sublimation method. FTIR and DSC studies were conducted to investigate compatibility between drugs and disintegrants. Formulated tablets were subjected for precompression parameters, e.g., bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose and for post-compression parameters, e.g. weight variation, thickness, hardness, friability, drug content, wetting time, disintegration time followed by dissolution study and found satisfactory as per IP.

The present study aims at the formulation, characterization, and evaluation of oral dispersible tablets (ODTs) of Tenoxicam to improve patient compliance and ensure faster onset of action, particularly in patients with swallowing difficulties. Tenoxicam, a non-steroidal anti-inflammatory drug (NSAID) with poor aqueous solubility and delayed onset when administered in conventional tablet form, was selected for this study. Oro dispersible tablets were prepared by direct compression method using various super disintegrants such as sodium starch glycolate, Starch and Spray dried lactose in different concentrations. The pre-compression parameters including bulk density, tapped density, angle of repose, and compressibility index were evaluated and found within acceptable limits. The formulated tablets were assessed for post-compression parameters such as hardness, friability, weight variation, drug content, wetting time, disintegration time, and in vitro drug release. Among the various formulations, the F2 optimized batch exhibited rapid disintegration within seconds and showed more than 95% drug release within 60 minutes, indicating improved dissolution characteristics.