Immediate Release Tablet Formulation Research Articles

Formulation and Evaluation of Immediate-Release Tablet Containing Atorvastatin Phospholipid Solid Dispersion

Formulation and Evaluation of Immediate-Release Tablet Containing Atorvastatin Phospholipid Solid Dispersion

Initial development of web application to support excipient selection for immediate release tablets using message passing neural network

The formulation of immediate release tablets is a challenging task due to the need to balance multiple factors such as bioavailability and stability. The selection of appropriate excipients is critical in achieving these objectives. The recent successful application of Artificial Intelligence (AI) and Message Passing Neural Network (MPNN) in predicting physicochemical and biological properties of drug molecules suggests for the researchers on the ability to apply these models in selecting excipients. The aim of this study is to develop an innovative approach for selecting excipients using AI and MPNN and to create a user-friendly web application to support excipient selection for immediate release tablets. The study utilized a database of 13,278 immediate-release tablets to train, validate, and test the MPNN model on the basis of Simplified Molecular-Input Line-Entry system (SMILES) of drug substances. The performance of the model was validated based on its ability to predict the probability of selecting an excipient reasonably. A web application named FormAI was developed using the Streamlit web framework and integrated with the trained model. The MPNN model demonstrated good performance, with an average Area Under Curve > 0.98 and R2 > 0.99, indicating its ability to predict the probability of selecting an excipient reasonably. The FormAI application provides a user-friendly platform for excipient selection. The results of the study demonstrate the potential of using AI and MPNN in drug formulation design, specifically in excipient selection for immediate-release tablets. The FormAI application provides a practical solution for pharmaceutical scientists and formulators.

Formulation and Evaluation of Immediate Release Tablets of Zopiclone

The current study's objective is to directly compress a Zopiclone rapid release tablet and assess it. The superdisintegrants (crospovidone, croscarmellose sodium, fenugreek) were used to hasten drug release from tablets. The prepared tablets pre-compression, post-compression characteristics were scrutinised. The interactions between the medication excipients were investigated using FTIR. The research shows that direct compression F3 formulations had a faster drug release of 100.05% over a 45-minute period than other Zopiclone formulations, which had lower dissolving rates when utilising Crospovidone.

Technology Transfer and Process Validation of Metformin Hydrochloride Immediate Release Tablet

Metformin Hydrochloride, inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity (via effects on fat metabolism) and lowering cAMP, thus reducing the expression of gluconeogenic enzymes. Metformin improves blood sugar levels by lowering the amount of glucose (sugar) that we absorb from our diet. It also helps stop the production of new glucose and improves insulin sensitivity. Metformin Hydrochloride is videly used in the form of sustained release formulation of Tablets. The study aimed to formulate and validate novel process for the Metformin Hydrochloride in immediate release pharmaceutical solid dosage forms. The wet granulation method used for formulation of Metformin Hydrochloride Immediate Release Tablets. Metformin Hydrochloride 500 mg, 850 mg, 1000 mg film coated tablets was prepared using FBE granulation technology on lab scale size. This study was carried out through a systematic plan; critical parameters were optimized to engender a stable & robust manufacturing process. The result of all three batches & its critical steps clearly shows consistency & reproducibility of parameters and all results. Hence the manufacturing method of Metformin Hydrochloride 500 mg, 850 mg, 1000 mg Film Coated tablets are validated at above parameters & equipments. Three validation batches of commercial scale batch size were taken successfully and monitored the in-process critical parameters for commercial batches. Metformin Hydrochloride tablets were manufactured within specified Limits for meeting all quality attributes and loaded for stability study. The overall successful three consecutive validation batches of Metformin Hydrochloride film coated tablets (500, 850 & 1000 mg) verifies the international technology transfer success.

Formulation Development of Tolperisone Hydrochloride Film Coated Tablet

Among all the different routes of administration, oral route of administration continues to be the most preferred route due to various advantages including ease of ingestion, avoidance of pain, versatility and most importantly patient compliance. Likewise, among all dosage forms tablet is the most popular dosage form existing today because of its convenience of self-administration, compactness and easy manufacturing. Sometimes immediate onset of action is considered obligatory immediate release tablets are the final option. Recently immediate release tablets have started gaining popularity and acceptance as a drug delivery system, mainly because they are easy to administer and lead to better patient compliance. In the present work, we engage in discussion about formulation, development, and evaluation of immediate release tablets. An immediate release dosage form allows a manufacturer to extend market exclusivity. They are also a tool for expanding markets, extending product life cycles and generating opportunities. pharmaceutical products designed for oral delivery and currently available on the prescription and over-the-counter markets are mostly the immediate release type, which are designed for immediate release of drug for rapid absorption. Tolperisone Hydrochloride Film Coated Tablets 50 mg was prepared using various excipients listed as in formula. The tablets were prepared by wet granulation method using concave plane punch on multi-station compression machine. The formulations were evaluated for their physical characteristics like thickness, hardness and friability, weight variation, content uniformity study was carried out. Evaluated for chemical analysis like Assay, disintegration and dissolution. In-vitro comparative dissolution study was performed with the help of U.S.P dissolution test apparatus-II with 900 ml of 0.1 N HCL, Acetate buffer pH 4.5 & 0.1 M HCL Acid at the 75 rpm for 45min.

Formulation and evaluation of immediate release tablet of Cisapride

Formulation and evaluation of immediate release tablet of Cisapride

Formulation and evaluation of immediate release tablet of Cisapride

The term “immediate release” pharmaceutical formulation includes any formulation in which the rate of release of drug from the formulation or the absorption of drug, is neither appreciably, nor intentionally, retarded by galenic manipulations. These tablets which disintegrate rapidly and get dissolved to release the medicaments. It may be provided for by way of an appropriate pharmaceutically acceptable diluent or carrier, which diluent or carrier does not prolong, to an appreciable extent, the rate of drug release or absorption.

DEVELOPMENT AND CHARACTERIZATION OF TRANDOLAPRIL IMMEDIATE RELEASE TABLETS USING DIFFERENT SUPERDISINTEGRATING AGENTS

A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium

Formulation and Evaluation of Immediate Release Tablet of Metformin Hydrochloride

Formulation and Evaluation of Immediate Release Tablet of Metformin Hydrochloride

Design, Formulation and Evaluation of Fexofenadine HCl Immediate Release Tablets by Solid Dispersion Method using Solvent Evaporation Technique

Currently, this study focuses on developing immediate-release Fexofenadine hydrochloride tablets. The Fexofenadine HCl tablets have super disintegrants that help to accelerate dissolution and bioavailability. Sodium lauryl sulphate, microcrystalline cellulose as filler, crospovidone, and sodium starch glycolate were used to make the tablets using a direct compression method (2-8 percent). Pre and post compressional parameters were used in the preparation of the tablets. The In-vitro disintegration study shows that as concentration of sodium starch glycolate is increased, there is an increase in the amount of time it takes for the solution to disintegrate, but at the same time, there is a decrease in the amount of time it takes for the solution to disintegrate when the crospovidone level is increased. When combined with the crospovidone tablet formulation, the test found that the resulting tablets broke down in approximately 3 to 6 minutes, with enough force to release the fragments but not to harm the friability of the product. It was found that Fexofenadine hydrochloride tablet, a fast-acting form of treatment for allergic rhinitis, could be formulated in an immediate-release form.

Development of an Immediate-Release Prototype Tablet Formulation of Hydroxychloroquine Sulfate with an Interwoven Taste-Masking System

Hydroxychloroquine sulfate (HCQS) was granted US-FDA approval in 1955 for the prevention and treatment of malaria. Since then, its uses have expanded to treat systemic lupus erythematosus and rheumatoid arthritis. For each indication, HCQS is a crucial option for the treatment of pediatric, juvenile, adult, and elderly populations. Existing currently on the market are only 200-mg strength tablets exclusively for adult administration. To facilitate weight-based administration for pediatric and juvenile patients, an HCQS suspension is made by compounding a 200-mg HCQS tablet and suspending the crushed granules into water and Ora-Plus®. The Ora-Plus® suspension does not alter the extreme bitterness of HCQS such that it facilitates oral administration. Additional research has been executed to affirm that a slightly buffered, ion-pairing system, reduces the bitterness of HCQS. The buffered, ion-pairing system can be interwoven into an immediate-release tablet formulation likely without compromising tablet performance. With the taste-masking system embedded, the tablet could be more easily be compounded and suspended in water to generate a palatable oral suspension. Such a novel HCQS 200-mg tablet would be tailored for adult usages wherein the interwoven task-masking system could be utilized to facilitate weight-based administration for pediatric and juvenile patients. The dual quality target product profile of the tablet and the tablet compounded for suspension in water would make the tablet formulation applicable to a wide patient population ranging from pediatric to elder adults to facilitate in improving compliance and overall health outcomes.

Formulation and Evaluation of Immediate-Release Tablets of Edoxaban Tosylate

Formulation and Evaluation of Immediate-Release Tablets of Edoxaban Tosylate

The Effect of Humidity on the Dissolution Kinetics and Tablet Properties of Immediate-Release Tablet Formulation Containing Lamotrigine.

This study aims to find the effects of high (75%) and low (30%) humidity conditions and its correlation with formulation composition on dissolution kinetics of lamotrigine (LMT) from prepared immediate-release tablets during one- and four-week periods. Two types of fillers microcrystalline cellulose (MCC) or anhydrous lactose (LAC), disintegrant sodium starch glycolate (NaSG, 0.5% or 4%), and lubricant magnesium stearate (MgST, 0.25% or 5%) were used. A three-factor two-stage complete factorial design (23) was used to assess the influence of the composition of the tested formulations. The tablets were produced by direct compression and characterized using a disintegration test, a resistance to crushing test, and dissolution tests (pH 1.2 and pH 6.8). Using Design Expert software, it was concluded that in addition to the effect of fillers on pH 6.8, NaSG has a significant impact after exposure to high and low humidity, as well as its interaction with LAC and MCC. In the dissolution medium pH 1.2, under conditions of high humidity, the content of MgST and NaSG and their interaction show a significant influence. The release rate of LMT was affected by humidity as well as type of excipients and their interactions.

Design, Development and Characterization of Flash release wafers containing Levocetrizine hydrochloride and Montelukast sodium

The main objective of the current research investigation was to develop and characterize flash release wafers containing Levocetrizine hydrochloride and Montelukast sodium. The formulation of flash release wafers was done by the solvent casting method. HPMC E5 LV, HPMC E50 LV, HPMC Lab grade polymer and plasticizer like glycerol, di-butyl phthalate were screened for wafers formation. Amongst them, HPMC lab-grade as polymer basis and glycerol as plasticizer showed good smooth wafers, acceptable thickness, clear and easy to peel off from the Petri plate. There was no interaction found between drug-drug and drug-excipients by FT-IR spectral analysis and shown that the ingredients used for the formulation of wafers were highly compatible. Then the optimized flash release wafers were evaluated for main parameters like disintegration time, drug content, surface pH, thickness and percentage drug release. Batch ML-7 was found to be optimized formulation of wafers which showed the satisfactory acceptable results of drug content 99.56±1.03of Levocetrizine hydrochloride and 98.92±2.33 of Montelukast sodium, least disintegration time of about 15±0.68 seconds, surface pH was 6.78± 0.010 and percentage drug release of Levocetrizine hydrochloride and Montelukast sodium was 96% and 97.5% at 5th minute. Hence it was found that the optimized formulation ML-7 showed much faster drug release than the oral marketed immediate-release tablet formulation in a 5th minute. This depicted that the formulation containing a lower concentration of polymer and a higher concentration of superdisintegrates showed a positive effect on disintegration time and drug release.

In vivo Anticoagulant Activity of Immediate Release Tablets of Dabigatran Etexilate Mesylate Cocrystals

Dabigatran Etexilate Mesylate (DEM), a salt of prodrug dabigatran etexilate, is a potent, oral, reversible and direct thrombin inhibitor with low oral bioavailability. The present research investigation focused on the formulation of immediate release (IR) tablets of DEM cocrystals and evaluation of In vivo anticoagulant activity. The results of the study showed that the formulated IR tablets of DEM showed improved efficacy in comparison with the plain drug by enhancing the pre-compression parameters such as bulk density, tap density, Carr's index, angle of repose and Hausner's ratio and post-compression parameters like thickness and weight variation, hardness and friability, In vitro dissolution parameters. The improved efficacy was confirmed by improvement in the pharmacodynamic parameters such as cutaneous bleeding time and clotting time indicative of enhanced bioavailability of dabigatran. Thus, it can be concluded that the IR tablets of dabigatran cocrystals can be proven to be more effective in producing the anticoagulant effect in clinical practice as compared to the plain drug resulting in more patient compliance.

Formulation and Evaluation of Immediate Release Tablets of Etizolam

In the present investigation, immediate release tablet formulation of etizolam was developed for management of insomnia and anxiety using different Superdisintegrants (Sodium Starch Glycolate, Croscarmellose, Crospovidone), Povidone K-30 and Magnesium stearate by wet granulation method. The drug-excipients interaction was investigated by UV spectrophotometer. The granules and tablets of Etizolam were evaluated for various pre and post compression parameters like angle of repose, compressibility index, hausners ratio, tablet hardness, friability and in vitro disintegration and dissolution studies and their results were found to be satisfactory. These results suggest that maximum in vitro dissolution profile of formulation F6 were found to have equivalent percentage of drug release and concluded that F6 is better and similar to innovator product.

Formulation and Evaluation of Fixed-Dose Combination Immediate Release Tablets of Ibuprofen and Famotidine through Quality by Design Approach

Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed by the physicians for the management of pain due to their anti-inflammatory and analgesic properties. Long term use of NSAIDs causes gastrointestinal (GI) toxicity and the common GI disorders are indigestion, ulcers or bleeding. Therefore, the production of local oral tablets containing NSAIDs and gastro-protectant is inevitable. In this experiment, combination of ibuprofen 600 mg and famotidine 20 mg tablets were prepared by direct compression technique, which is unique in Bangladesh. To pursue the study Design of Experiments (DoE) approach was implemented to create fifteen trial formulations where Polyvinylpyrrolidone (PVPK30) 1%-3%, Microcrystalline Cellulose (Avicel PH-102) 1%-7% and Starch-1500 1%-13% were considered as independent variables and the responses were depicted in friability and disintegration time which were found 0.21–0.45% and 1.8–20.5 minutes respectively. Out of fifteen formulation trials (F-1 to F-15), seven formulations (F-3, F-6, F-8, F-9, F-10, F-13 and F-14) had met the acceptable criteria and one formulation (F-9) with independent variables PVP-K30 2.00%, Avicel PH-102 4.75% and Starch-1500 6.5% was selected because of its better disintegration, dissolution and friability profile. Data obtained from in-vitro dissolution tests were fitted to different kinetic models such as zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas models. Also, a compatibility study was conducted using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA) and X-Ray Diffraction (XRD). Furthermore, Scanning Electron Microscopy (SEM) was performed to analyze surface morphology. Finally, the selected formulation was compared to FDA regulated QC parameters and proved its superiority over conventional market products.
 Bangladesh Pharmaceutical Journal 24(2): 133-148, 2021

Formulation and Invitro evaluation of immediate release tablets containing febuxostat

In the present research work, Febuxostat Immediate Release Tablet was prepared by direct compression method using varying concentrations of Lycoat, Crospovidone& Croscarmellose sodium as disintegrants. The formulations prepared were evaluated for precompression& post-compression parameters. From the drug excipient compatibility studies, we observe that there are no interactions between the pure drug (Febuxostat) and optimized formulation (Febuxostat+ excipients) which indicates there are no physical changes. Post compression parameters were found to be within the limits. Among the formulation prepared the tablet containing 12mg of CCS shows 98.13% of the drug release within 45 min & follows first-order kinetics.

Small-scale dissolution test screening tool to select potentially substandard and falsified (SF) medicines requiring full pharmacopoeial analysis

The purpose of this study was to design a convenient, small-scale dissolution test for extracting potential substandard and falsified (SF) medicines that require full pharmacopoeial analysis. The probability of metronidazole samples complying with the US Pharmacopoeia (USP) dissolution test for immediate-release tablet formulations was predicted from small-scale dissolution test results using the following criteria: (1) 95% confidence interval lower limit (95% CIlow) of the average dissolution rate of any n = 3 of n = 24 units of each sample, and (2) average and minimum dissolution rates for any n = 3 of n = 24 units. Criteria values were optimized via bootstrap sampling with Thinkeye data-mining software. Compliant metronidazole samples in the USP first-stage and second-stage dissolution test showed complying probabilities of 99.7% and 81.0%, respectively, if the average dissolution rate of n = 3 units is equal to or greater than the monograph-specified amount of dissolved drug (Q; 85% of labeled content for metronidazole). The complying probabilities were 100.0% and 79.0%, respectively, if the average dissolution rate of n = 3 units is 91% or higher and the minimum dissolution rate is 87% or higher. Suitable compliance criteria for the small-scale dissolution test are: average dissolution rate of n = 3 units is Q + 6% or more and minimum dissolution rate is Q + 2% or more.

Development and evaluation of physical and release properties of a tablet formulation containing dry hydroethanolic extract from Lippia alba leaves

The development of an immediate-release solid formulation which contains natural products is a challenge considering several variables. These include the physical properties of the drug, the complex composition of the herbal extracts, and its ability to be released in the body. The present study describes the development and characterization of an immediate-release tablet formulation of a hydroethanolic extract of Lippia alba (Mill.) N. E. Br. dried leaves which possess potential gastroprotective properties and sedative effects. L. alba is a Brazilian herb known as “cidreira,” and the ethnopharmacological use of the leaf infusion has been reported in many South and Central America countries. However, no study has considered phytotherapeutics containing extracts of this herb. To achieve this goal, 14 solid formulations were produced using direct compression, wet granulation, or dry granulation. These were characterized by physical tests, such as average weight, friability, hardness, and disintegration tests. The tablet formulation produced by the dry granulation of 100 mg of the L. alba extract exhibited better physical properties, and it was characterized using acteoside (verbascoside) as a chemical marker, presenting 6.9 % w/w of acteoside content per tablet, corresponding to 41.3 mg of this constituent per unit. This formulation dissolves rapidly in simulated gastric fluid without enzymes, achieving amounts >80 % after 20 min. Thus, an immediate-release tablet formulation with L. alba extract was successfully prepared.