Formulation and Evaluation of Sublingual tablet of Vonoprazan fumarate

Purpose Vonoprazan fumarate (VPF) is a novel potassium-competitive acid blocker with promising therapeutic potential for acid related disorders and as an adjunct to Helicobacter pylori eradication, yet its clinical utility is limited by poor solubility and low bioavailability. Here, we explore the development of amorphous solid dispersion (ASD)-loaded orodispersible films (ODFs) to overcome these barriers. Methods ASDs of VPF were prepared and characterized using hydroxypropyl methylcellulose (HPMC K4M), polyethylene glycol 4000, and Poloxamer 407. ODFs were fabricated by solvent-casting with sodium carboxymethyl cellulose, HPMC K4M, and polyvinyl alcohol (PVA) as film-forming polymers, incorporating glycerin as a plasticizer. Various parameters as weight and thickness variation, in-vitro drug release, disintegration time, moisture uptake, and in-vivo pharmacokinetic parameters were investigated. Results VPF ASDs were achieved the optimal dissolution at a 1:6 (w/w) drug-to-polymer (HPMC K4M) ratio with Higuchi-diffusion kinetics. Stability studies confirmed VPF integrity in the ASD form. Among the ODF formulations, ODF7 (contains 75 mg PVA) demonstrated superior performance with rapid disintegration, lowest moisture uptake, and maximum drug release within 10 min. In-vivo pharmacokinetic evaluation in rabbits revealed a 2.2-fold increase in relative bioavailability (221.98%) compared to the VPF marketed tablet, while palatability testing confirmed its acceptability. Conclusion These findings demonstrate the potential of VPF-ASD-loaded ODFs as a viable approach to enhance drug solubility, stability, and systemic exposure.

Background: Tapentadol hydrochloride is a potent analgesic commonly used to manage moderate to severe pain. Rapidly dissolving tablets of Tapentadol offer a significant advantage in enhancing patient compliance by providing quick pain relief. The development of fast-dissolving tablets (FDTs) requires careful consideration of formulation parameters to achieve optimal disintegration and dissolution profiles. In this study, the aim was to fabricate Tapentadol FDTs by selecting suitable super disintegrating agents such as croscarmellose sodium and crospovidone, which serve as two independent variables. The direct compression method was employed to formulate nine different Tapentadol hydrochloride formulations (TH1 to TH9). Materials and Methods: The study utilized Design-Expert® software version 13.0 and the Response Surface Methodology (RSM) for the optimization of Tapentadol FDTs. The formulations were prepared using the direct compression method with varying concentrations of the super disintegrants, croscarmellose sodium, and crospovidone. The primary response variables considered in this optimization study included disintegration time (Y1), percentage drug release at 15 minutes (Q15, Y2), and percentage drug release at 30 minutes (Q30, Y3). All pre-compressional and postcompressional parameters were evaluated for each formulation, along with in vitro dissolution studies. Furthermore, DD Solver, a statistical tool, was employed to determine the kinetics of drug release and the release order mechanism based on regression coefficient value (r²), Akaike Information Criterion (AIC), and Model Selection Criteria (MSC). Results: The evaluation studies indicated that the TH5 formulation exhibited the most rapid disintegration time and the highest drug release percentage within the specified time frame. The super disintegrants used demonstrated a significant impact on the response variables, notably enhancing the solubility and dissolution rate of Tapentadol hydrochloride. Based on the exponent release (n) value, the study concluded that the TH5 formulation followed a first-order release kinetics and Fickian diffusion mechanism for drug release. Stability studies were performed following the International Council for Harmonization (ICH) guidelines to assess the shelf-life of the optimized formulation. The ANOVA data revealed that the p-value was greater than 0.05, indicating no significant differences during the storage period. Additionally, a similarity factor (f2) analysis was conducted to compare the optimized formulation with the marketed formulation (Tydol 100 mg). Discussion: The findings highlight the crucial role of super disintegrants in fast-dissolving tablet formulation, significantly impacting disintegration time and dissolution profile. The TH5 formulation excelled in rapid disintegration and drug release, optimized using RSM and Design-Expert software, with statistical analysis confirming the Fickian diffusion mechanism for drug release. Conclusion: The study successfully developed and optimized Tapentadol fast-dissolving tablets using direct compression and response surface methodology. The TH5 formulation showed rapid disintegration and optimal drug release, with stability confirmed under ICH conditions. This highlights the importance of super disintegrants in FDT formulation for rapid action and patient compliance.

Objectives: To avoid swallowing problems of conventional tablets and improved patient compliance Plantago Ovata based Labetalol HCl Rapid disintegrating tablets have been prepared. Methods: Six different (F1 to F6) batches of Labetalol HCl Rapid disintegrating tablets were developed by ‘direct compression method’ using Plantago ovata as a natural super-disintegrating agent. The formulated RDT were tested for angle of repose’, densities like tapped and bulk density, Hausner’s ratio, Carr’s index like pre-compression parameters and for thickness, weight variation or weight uniformity, tablet hardness, % drug content or content uniformity, water absorption ratio’, time require for wetting of tablets’ means wetting time, in-vitro drug disintegration time and in-vitro drug dissolution studies under post-compression parameters of evaluation. Results: It was found that the all the results of these pre-compression and post-compression parameters comply with official standards. The drug release was determined using dissolution media of pH 6.8 phosphate buffer through in-vitro dissolution of drug. This study showed that a rapid drug release by prepared tablets. The optimized formulation F6 showed higher water absorption ratio`, lower wetting time, minimum in-vitro disintegration time’ and higher drug release amongst all the formulations. The F6 formulation was considered the best among all formulations. Conclusion: The prepared rapid disintegrating tablets shows rapid onset of action by quick drug release, minimize side effects and enhanced patient compliance. These prepared tablets containing selective alpha-1 and non-selective beta adrenergic antagonist’ drug candidate Labetalol HCl, will be very useful in the treatment of high blood pressure with enhanced bioavailability.
 Keywords: Rapid disintegrating tablets, Labetalol Hydrochloride, Bioavailability Enhancement, Natural Superdisintegrant, Plantago Ovata, High Blood Pressure, RDT, Patient Compliance

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.

Current research is focused on formulation and evaluation of natural gum based fast dissolving tablet of Cefixime trihydrate by applying 32 factorial designs for the improvement of the drug absorption. Direct compression method was used. Two factors as independent variable (x1) Fenugreek mucilage(x2) sodium saccharin glycolate were taken with three level (+1, 0,-1). The level two factors were selected on basis of preliminary experiments conducted and their effect on dependent variable (disintegration time) was estimated. Formulated tablets were evaluated for parameters in which the values were found to be in the range of hardness 2.1-2.6 kg/cm2, thickness 2.227-2.296 mm, weight variance 182-196 mg, wetting time 58-68 seconds, water absorption ratio 0.1628-0.2439, disintegration time 56 sec – 9 min, and friability 0.53-0.68 %. The software design expert (11.0) was used for getting experimental design, modeling the response surface and calculating the static evaluation. The tablet parameters tests of formulation (F1 to F10) were observed within prescribe limit. Disintegration time observed 56 seconds, % cumulative drug release 88.79 % to 98.90 %. Batch F6 was observed as promising batch.

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

Low bioavailability remains a challenge for poorly water-soluble drugs like flutamide, a key therapeutic agent for prostate cancer. To address this, Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) were formulated to enhance solubility, absorption, and therapeutic efficacy. SNEDDS improves drug delivery by forming nanosized emulsions, increasing surface area, and promoting bioavailability. The SNEDDS formulation of flutamide was developed using sesame oil as the oil phase, Tween 20 as the surfactant, and PEG 400 as the co-surfactant. A Design of Experiments (DoE) approach was used to optimize the formulations. The response variables, % CDR (% Cumulative Drug Release) and Self Emulsification Time were considered for systematic DoE optimization. After obtaining the responses, ANOVA was applied for both the responses i.e. self emulsification time studies and % CDR. Then 3 D plots and Contour plots were also plotted using Design Expert Software. Morphological studies were conducted using Transmission Electron Microscopy (TEM), and the particle size, zeta potential, and stability of the formulations were evaluated. Drug release and cytotoxicity were assessed via dialysis and MTT assay on PC-3 prostate cancer cells, respectively. The optimized formulation demonstrated rapid self-emulsification (7.9 s) and high %CDR (98.69%). TEM revealed nanoscale uniformity with particle sizes averaging 120.1 nm and a zeta potential of -0.0179 mV. FTIR analysis confirmed the stability of functional groups. The IC50 of the optimized formulation was 177.7 ± 0.05(µg/ml), significantly lower than the pure drug (644.8 ± 0.1405(µg/ml), highlighting its potent cytotoxicity against PC-3 cells. The optimized SNEDDS formulation improved the solubility, stability, and therapeutic efficacy of flutamide. The nanosized formulation facilitated better drug absorption and targeted delivery, enhancing its anticancer potential. The results of the in vitro drug release study were fitted with various kinetics equations like zero order (percent drug release vs. t) and first order (log % drug remaining vs. t) and Higuchi equation to understand the mechanism and kinetics of drug release. R2 values were calculated for the linear curves obtained by regression analysis of all the plots. Flutamide SNEDDS along with Flavonoid Rutin represent a promising strategy for enhancing bioavailability and therapeutic effectiveness in prostate cancer treatment. Future studies should focus on in vivo pharmacokinetics and safety profiles to confirm clinical applicability.

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis.
 Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 32 full factorial design was applied considering the concentration of HPMC E5 (X1) and concentration of PEG400 (X2) as independent variables and % cumulative drug release (Y1) (CDR), disintegration time (Y2) (DT) and tensile strength (Y3) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X1 and X2 were found to be having a positive effect on DT and TS and negative effects on CDR.
 Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm2 tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness.
 Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.

Background: This study aimed to develop and optimize an orodispersible herbal tablet incorporating Achyranthes aspera Linn extract. Sodium Starch Glycolate and Crospovidone were employed as superdisintegrants to promote rapid tablet disintegration, while β-cyclodextrin was utilized to enhance the solubility of specific constituents within the extract. The optimized formulation exhibited a rapid disintegration time of 1.805 seconds and achieved a cumulative drug release of 98.04%, indicating improved dissolution and potential enhancement in oral bioavailability. Methodology: Orodispersible tablets were formulated using Design of Experiments (DOE) software, with crospovidone and sodium starch glycolate as independent variables, and time of disintegration and cumulative drug release as dependent variables. The formulation was evaluated for weight variation, uniformity, hardness, wetting time, and in vitro dispersion time. Result & Discussion: The optimized F6 batch of orodispersible herbal tablets demonstrated the following characteristics: hardness of 2.98 kg/cm², friability of 0.58%, weight variation of 3.319%, disintegration time of 13.805 seconds, wetting time of 34.4 seconds, content uniformity of 99.5%, water absorption of 36%, and cumulative drug release of 98.04%, all within the permissible limits as per official pharmacopoeialstandards. Conclusion: The study concludes that crospovidone and sodium starch glycolate effectively reduce disintegration time and improve cumulative drug release. These findings validate the reliability of the model, with minor deviations attributed to experimental variability.

Objective: The objective of the present investigation is to develop a formulation of sublingual tablets of Nadolol. Materials and Method: For the preparation of sublingual tablets various super disintegrants were used like Kyron T-314, and SSG. A 3² factorial design was employed to optimize the formulation by systematically evaluating the effects of two independent variables. Kyron T-314 (X1) and sodium starch glycolate (SSG) (X2) were selected as the formulation factors. The study aimed to investigate their influence on key performance responses, namely in vitro disintegration time (Y1) and percentage cumulative drug release at 12 minutes (Y2). Results and Discussion: All precompression parameters like Carr’s Index, Hausner’s Ratio and Angle of Repose meets the standard values of powder indicating good flow properties. FTIR was performed to check compatibility between drug and excipients and no major changes were found. The average weight, friability and hardness were within compendial limits which showed that all formulations possessed good mechanical strength. The optimized formulation N9 showed minimum disintegration time of 17.41 ± 1.64 secs, and drug release of 99.48 % in 12 mins among all other batches of tablets. The result of stability study of the batch N9 showed that there was no significant change in hardness, in-vitro disintegration time, drug content, and in vitro dissolution profile for a period of one month when stored at 40° ± 2°C / 75 ± 5% RH for period of one month. From the study it was concluded that sublingual tablets of Nadolol is an acceptable dosage form which suggests that it is likely to become one of the choices of Nadolol preparations for the treatment of hypertension.

IntroductionThe first drug selected for treatment of gastro-oesophageal reflux disease (GERD) and prevention of the recurrence is a proton pump inhibitor (PPI), but recently, a potassium-competitive acid blocker (P-CAB) was...

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.

Varenicline tartrate is a smoking cessation aid that works by blocking nicotine receptors in the brain. It helps reduce cravings and withdrawal symptoms and helps you quit smoking. The study aimed to formulate and characterize varenicline tartrate orodispersible tablets using the synthetic disintegrants crospovidone and croscarmellose sodium in different ratios and directly compressible microcrystalline cellulose as diluent, and mannitol to improve mouthfeel using the direct compression method. A total of 13 varenicline orodispersible tablets are formulated and subsequently evaluated for pre-compression and post-compression physicochemical parameters such as angle of repose, Carr index, Hausner ratio, hardness, thickness, mass variation, drug content, friability, wetting time, disintegration time, dispersion time and water absorption ratio. Optimization was performed with percentage of crospovidone (X1 or A) and croscarmellose sodium (X2 or B) as independent variables, while disintegration time (Y1) and wetting time (Y2) were selected as dependent variables using the central composite design of Design-Expert® DX 12. Optimized formulations showed 99.68 % drug release in 60 min while the cumulative percentage drug release of pure drug was only 56.84 %. Finally, it was concluded that dissolution rate and bioavailability are improved with varenicline tartrate orodispersible tablets.

The present work involves the formulation of colon targeted matrix tablet of Ibuprofen by using direct compression method. Literatures regarding, Ibuprofen tablet dosage form preparation, excipients selection, manufacturing method etc., has been collected and reviewed. In this work, selection of excipients was done based on a literature review. Excipients include Eudragit S100, Ethyl cellulose, Lactose, Talc, Magnesium stearate. Quantities of the excipients were selected performing FT-IR method which is an HIS of Fourrts India Laboratory. Preformulation studies have also been performed to study the nature of API and compatibility of API with excipients by physical observation and FT-IR studies. The result showed that API was compatible with all the excipients selected. The tablets were formulated by direct compression method using the selected excipient quantities. The formulated tablets were tested for both pre-compression parameters and post compression parameters as per requirements of standards. Pre-compression parameters such asbulk density, tapped density, compressibility index, Hausner’s ratio and compressibility index. The results obtained indicate that it has good flow property for direct compression. The formulated Ibuprofen matrix tablets were coated with enteric polymer Eudragit FS30D by pan coating method. The prepared tablets were evaluated for weight variation, hardness, thickness, friability, drug content, and disintegration time and in-vitro dissolution studies. All these parameters were found to be within the standard limits. Comparative studies of coated Ibuprofen tablets and uncoated Ibuprofen tablets are evaluated for the hardness, thickness, in-vitro dissolution studies and disintegration time. Out of six formulations, the formulation F6 showed 98.51% drug release at 24 hrs. Since it provide greater protection to the core under acidic condition while at the same time show the fastest drug release under intestinal pH. So the formulation F6 was considered as the confirmatory trial and it was subjected for stability studies up to three months of accelerated stability 400C ± 2C0, 75 %± 5 % RH and found to be within limits.

This study demonstrates the potential of using orally disintegrating tablets (ODTs) as a delivery vehicle for Aprepitant to manage chemotherapy-induced vomiting effectively. Preformulation studies, including identification tests, solubility profiles, and drug-excipient interaction analyses, confirmed that Aprepitant has a melting point of 254-256°C and is hydrophobic, soluble in methanol, sparingly soluble in PBS pH 6.8, and insoluble in water. Solid dispersions with PEG 6000, PEG 4000, and β-cyclodextrin enhanced the solubility and dissolution rate of Aprepitant. The optimal solid dispersion (SD4, Drug: PEG6000, 1:2 ratio) exhibited excellent drug content (99.31%), solubility (3.91 mg/ml), and cumulative drug release (97.17% in 15 minutes). ODTs were prepared using different superdisintegrants and evaluated for hardness, friability, weight variation, disintegration time, wetting time, and in vitro drug release. Results indicated uniform tablet characteristics, with formulation F3 (containing crospovidone) showing the best disintegration time (21 seconds) and rapid dissolution within 15 minutes. Stability tests on F3 revealed no significant changes under varying temperature and humidity conditions. The dissolution efficiency of disintegrants followed the order: crospovidone > sodium starch glycolate > croscarmellose sodium, indicating that the formulation is ideal for fast release and absorption of Aprepitant while reducing swallowing difficulties associated with conventional tablets.