Design Of Tablets Research Articles

Design and Optimization of Ibuprofen and Ranitidine Hydrochloride TriLayer Tablets in Immediate Release Formulation by Quality by Design.

The current trend in pharmaceutical process development and optimization is known as quality by design (QbD). This methodical approach is founded on the concept that quality should be integrated into the product from the start, rather than assessed after manufacture. In this study, we demonstrate methods to improve the process parameters for making tri-layer tablets by applying QbD principles in a methodical way. Dependent elements with high to medium impact on the process. According to the study’s results, all systems showed signs of instant release. It appears that the structure of each formulation and the properties of the polymer utilized have a significant impact on the rate and mechanism of drug release. Substantial medication release is observed in the three-layer formulations. Both the pace and mechanism of drug release are significantly affected by the tablet’s geometrical features and structure, as well as the weight and thickness of the barrier layers. While data suggested that Fickian diffusion was primarily responsible for drug release in two-layer tablets, three-layer tablets showed signs of either anomalous diffusion or erosion/relaxation. Therefore, the drug was stabilized as immediate-release directly compressible triple layered Average core weight of tri-layered tablets (mg) was 1000 for ibuprofen, 100 for placebo and 200 for ranitidine, thickness (mm) was 9.00 ± 0.3, hardness (N) was 110 ± 25, core tablet weight was 1300.000 ± 2% mg and coated tablet weight was 1325 mg. Using other moisture-sensitive medications. This study provides the foundation for future research into optimizing the properties of tablets made by direct compression.

HYDROPHILIC MATRIX TABLETS AS ORAL CONTROLLED DRUG DELIVERY SYSTEMS IN 20TH CENTURY: A REVIEW

Matrix systems are easy to formulate compared to other controlled release dosage forms. The manufacture of matrix tablets involves the direct compression of blend of drug, retardant material and additives to form a tablet in which drug is embedded in a matrix core of the retardant. Alternatively, retardant-drug blends may be granulated prior to compression. Of the three classes of retardant material used to formulate matrix tablets, polymers that form hydrophilic matrices are attracting the attention of pharmaceutical technologists. These polymers include Methyl cellulose (MC), Hydroxy ethyl cellulose (HEC), Hydroxy popyl methyl cellulose (HPMC), Sodium carboxy methyl cellulose (NaCMC), carbomers, chitosan, plant gums etc. The hydrophilic matrix-formers alone or in combination with other excipients form gels in situ on coming in contact with biological fluids which control the drug release. The present review gives a detailed account on the factors to be considered in the design of hydrophilic matrix systems, formulation of hydrophilic matrix tablets, in vitro and in vivo evaluation methods and advances in the design of hydrophilic matrix tablets. This review further focuses on the development of oral controlled drug delivery systems using hydrophilic matrix carriers in 20th century.

Design and Optimization of 3D-Printed Tablets Containing Mucuna Extracts for Erectile Dysfunction Management: A DoE-Guided Study.

Erectile dysfunction (ED) refers to the inability of the penis to maintain a firm erection during sexual activity. Mucuna, or M. pruriens, contains levodopa, a compound showing promise in ED treatment. However, formulating Mucuna extract into tablet dosage forms is challenging due to its semisolid nature. This study aimed to develop sustained-release tablets containing Mucuna extract via semisolid extrusion 3D printing. Eudragit RS PO (Eudragit) served as a sustained-release polymer, with poly (vinyl alcohol) (PVA) as a co-polymer for forming the tablet matrices. This study had the following two main phases: screening, which identified the factors affecting the printability, and optimization, which focused on the factors influencing the levodopa release and its consistency. The results showed that both the polymeric solid percentage content (PSPC) in the semisolid slurry and the Eudragit-PVA ratio significantly affected the printability. All of the formulations were printable, and the PSPC and Eudragit-PVA ratios were incorporated into the optimized model. The desired formulation, achieving targeted levodopa release and consistency, had a PSPC of 58.8% and a Eudragit-PVA ratio of 2.87:1. In conclusion, semisolid extrusion 3D printing guided by the design of experiments (DoE) proved feasible for producing reliable 3D-printed tablets with consistent active ingredients and desired release rates.

Design and evaluation of cost-effective oro-dispersible tablets of venlafaxine hydrochloride by effervescent method

Design and evaluation of cost-effective oro-dispersible tablets of venlafaxine hydrochloride by effervescent method

Design and evaluation of oseltamivir phosphate dual-phase extended-release tablets for the treatment of influenza

In this study, once-daily extended-release tablets with dual-phase release of oseltamivir phosphate were developed for the treatment of influenza. The goal was to improve patient adherence and offer more therapeutic choices. The tablets were manufactured using wet granulation, bilayer tablet compression, and enteric membrane-controlled coating processes. Various polymers, such as hydroxypropyl methylcellulose (HPMC K100MCR, K15MCR, K4MCR, K100LV), enteric polymers (HPMC AS-LF, Eudragit L100-55) and membrane-controlled polymers (OPADRY® CA), were used either individually or in combination with other common excipients. The formulations include enteric-coated extended-release tablet (F1), hydrophilic matrix extended-release tablet (F2), semipermeable membrane-controlled release tablet (F3) and a combination extended-release tablet containing both enteric and hydrophilic matrix (F4). The in vitro drug release profile of each formulation was fitted to the first-order model, and the Ritger-Peppas model suggested that Fickian diffusion was the primary mechanism for drug release. Comparative bioequivalence studies with Tamiflu® (oseltamivir phosphate) capsules revealed that formulations F1, F2, and F3 did not achieve bioequivalence. However, under fed conditions, formulation F4 achieved bioequivalence with a relative bioavailability of 95.30% (90% CI, 88.83%-102.15%). This suggests that the formulation F4 tablet could potentially be a new treatment option for patients with influenza.

Amorphous solid dispersion of a binary formulation with felodipine and HPMC for 3D printed floating tablets

This study focuses on the combination of three-dimensional printing (3DP) and amorphous solid dispersion (ASD) technologies for the manufacturing of gastroretentive floating tablets. Employing hot melt extrusion (HME) and fused deposition modeling (FDM), the study investigates the development of drug-loaded filaments and 3D printed (3DP) tablets containing felodipine as model drug and hydroxypropyl methylcellulose (HPMC) as the polymeric carrier. Prior to fabrication, solubility parameter estimation and molecular dynamics simulations were applied to predict drug-polymer interactions, which are crucial for ASD formation. Physical bulk and surface characterization complemented the quality control of both drug-loaded filaments and 3DP tablets. The analysis confirmed a successful amorphous dispersion of felodipine within the polymeric matrix. Furthermore, the low infill percentage and enclosed design of the 3DP tablet allowed for obtaining low-density systems. This structure resulted in buoyancy during the entire drug release process until a complete dissolution of the 3DP tablets (more than 8 h) was attained. The particular design made it possible for a single polymer to achieve a zero-order controlled release of the drug, which is considered the ideal kinetics for a gastroretentive system. Accordingly, this study can be seen as an advancement in ASD formulation for 3DP technology within pharmaceutics.

Design and Development of Fast-dissolving Tablets of Apixaban using Single Coprocessed Excipient

Background: Apixaban is administered orally as an anticoagulant action and minimizes the chances of strokes and systemic embolism. The conventional film-coated tablet showed less bioavailability due to its minimal solubility in the gastrointestinal tract. Rationale: The goal of designing the current analysis is to prepare a prompt release tablet using a single Coprocessed excipient which minimizes multistep processing, time, and cost effectiveness. Methods: The prompt release tablets of Apixaban were developed by direct compression technique using multifunctional material like Prosolve ODT G2 and Prosolve Easytab. Drug excipients inertness was confirmed with FTIR and DSC. Flowing characteristics of Apixaban and co-processed excipients were evaluated in terms of Carr’s index, Angle of repose, and Hausner’s ratio. These co-processed excipients indicated exceptional flowing and compression characteristics. The ready tablets were assessed for weight variation, hardness, friability, dispersion time, disintegration, and dissolution studies. Results: Among 12 batches, the least disintegration time was shown with C6 with a cumulative drug release of 99.06 % within 25 min. The optimized batch C6 was highly stable when tested under stability guidelines at 40 0 C and at 75 % relative humidity. Conclusion: Among these co-processed excipients, Prosolve Easytab SP was found the best one for direct compression intended for the immediate or fast dissolving tablets.

Bilayer tablet overview: A revolutionary approach in sustained drug release & combination drug therapy

A fresh method of administering drug, the bilayer tablet is a single dosage form containing 2 or more Active Pharmaceutical Ingredients (API).By incorporating two distinct layers, bilayer tablets provide improved drug release profiles and enhanced therapeutic efficacy. This review's objective is to pinpoint the challengesthat arise when making bilayer tablets and to suggest solutions for these difficulties. To help you better grasp bilayer tablets, types like double side presses, single side presses, and bilayer tablet displacement presses are discussed along with their uses, advantages, and disadvantages.In this thorough guide, we will look into the design, manufacturing, and applications of bilayer tablets

Design of an Oral Tablet Containing Furosemide Nanoparticles with Elevated Bioavailability.

The solubility and permeability of the Biopharmaceutics Classification System (BCS) class IV drugs, such as furosemide (FUR), are low. Thus, the oral bioavailability of these drugs needs to be augmented. Here, we aimed to design orally disintegrating tablets containing FUR nanoparticles to improve bioavailability after oral administration. The FUR nanoparticles were generated by bead-milling in water containing 0.5% methylcellulose and 0.5% 2-hydroxypropyl-β-cyclodextrin (w/w%). Particle size was approximately 47-350 nm (mean particle size, 188 nm). An orally disintegrating tablet (FUR-NP tablet) comprising FUR nanoparticles (1%) was successfully produced by employing suspensions outlined above that incorporated additives (4% D-mannitol, 0.4% polyvinylpyrrolidone, and 16% gum Arabic, w/w%), followed by freeze-drying. The FUR-NP tablet disaggregated after only 5 s in water, liberating nano-sized FUR particles (172 nm). Experiments using rats showed the absorption of the FUR-NP tablet was significantly improved by comparison with a FUR tablet containing microparticles. In summary, the orally disintegrating tablet containing FUR nanoparticles markedly enhanced the bioavailability of FUR. We anticipate this formulation will also improve the bioavailability of other BCS class IV drugs.

Design, Development and Physicochemical Evaluation of Effervescent Tablets of Antihistamine Drug

Purpose: Effervescent bilastine tablets were the focus of this investigation because of their ease of administration and the fact that some patients, especially younger ones or those with impaired swallowing abilities, have trouble ingesting oral dosage forms. Methods: Using the wet granulation process, 20 mg of effervescent bilastine tablets were produced. Pre-compression properties assessed for powder blend and granule combination. Here are some post-compression properties of the tablets that were examined: friability, hardness, drug content, pH, dissolution time, content uniformity, water content, X-ray, and Differential scanning calorimetry (DSC). We also measured carbon dioxide content and effervescence duration. To get the greatest results, we looked for effervescent systems that dissolved quickly in water and had the right properties before and after compression. Results: Based on their physicochemical properties, F2 formulations were determined to be best formulations, and the results demonstrated that the wet granulation process had greater flowability. Conclusion: Sweeteners such as mannitol, sodium saccharine, methylparaben, and citric acid were chosen for this investigation, along with sodium bicarbonate. If you want to hide the bitter flavor of bilastine, sodium saccharine is your best bet. From a physicochemical and physical property standpoint, the wet granulation process outshines the alternatives.

Design and Characterization of Mangiferin Sustained-Release Tablets

Background: Mangiferin is a natural bioactive compound used for various pharmacological activities like antidiabetic, anticancer, and anti-inflammatory. Objective: The development of unique sustained-release matrix tablets of mangiferin is the purpose of the work that is being presented here. Method: In this study, an effort is made to formulate mangiferin sustained-release matrix tablets by combining the sustained-release polymers HPMC K100M, Kollidone@SR, Keltone LVCR. Mangiferin matrix tablets have been synthesized by wet granulation utilizing the lactose works as the diluent. Systems were developed with different polymer percentages. Results: Refine the design based on observed differences in weight, hardness, thickness, percent friability, percent drug content, and in-vitro drug release. In-vitro release trials conducted by utilizing a USP type II device utilizing a 6.8 pH phosphate buffer as the separation medium revealed that the most successful F2 formulation, which included 20% polymer, was capable of supporting the mangiferin release for a time of 12 hours period. This sample showed the greatest coefficient (R) value in the Hixson-Crowell model, and release kinetics studies showed that this sample exhibited an erosion process and followed zero-order kinetics. Conclusion: We can conclude that Kollidone@Sr can be used to prepare sustained-release mangiferin.

Strategic design and clinical evaluation of a fixed-dose combination tablet comprising valsartan, amlodipine, rosuvastatin and ezetimibe for patients with hypertension and dyslipidemia

Strategic design and clinical evaluation of a fixed-dose combination tablet comprising valsartan, amlodipine, rosuvastatin and ezetimibe for patients with hypertension and dyslipidemia

Successful Formulation Window for the design of pharmaceutical tablets with required mechanical properties

Pharmaceutical tablet formulations combine the active ingredient with processing aids and functional components. This paper evaluates compressibility based predictive models for binary and ternary formulations to establish an acceptable range of tablet compression parameters that satisfy prescribed quality target criteria for tablets including minimum tablet strength and processing constraints such as maximum ejection stress and maximum compaction pressure. The concept of Successful Formulation Window (SFW) is introduced. A methodology is proposed to determine the SFW for a given formulation based on compaction simulator data collected for individual formulation components. The methodology is validated for binary and ternary mixtures and lubricated formulations. The SFW analysis was developed to support tablet formulation design to meet mechanical requirements.

Potentials of Sterculia tragacantha Lindl seed husk gum as a release modifier in matrix tablet formulation

Natural gums have been utilized severally in the design of matrix tablets, either in their native or modified forms. The primary objective of this work was the extraction, characterization and utilization of the seed husk gum from Sterculia tragacantha Lindl as a release modifier in theophylline matrix tablets. Gum was extracted from the fresh seed husk of Sterculia tragacantha and tablet formulated via wet granulation. Drug-polymer compatibility was determined by FTIR and DSC while formulated tablets were evaluated for their in vitro dissolution release profile in two media, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) and compared with a commercial brand. Extracted gum powder presented a poor flow which improved on granulation, had a better swelling index and water holding capacity than tragacanth gum. Formulated tablets passed standard tablets test and sustained theophylline release up to 90.97 % and 88.09 % in SGF and SIF respectively at the twelfth hour. Drug release kinetics was by zero order in SGF via non-fickian diffusion. S. tragacantha seed husk gum presented a promising potential as a release retarding agent.

Design, Development and Optimization of Buccal Tablet Containing Extract of Terminalia chebula Retz. for the Treatment of Asthma

Design, Development and Optimization of Buccal Tablet Containing Extract of Terminalia chebula Retz. for the Treatment of Asthma

Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin

The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. Based on the early testing, a 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The FTIR, DSC, and XRD investigations validated the Quercetin interaction with nanosponges. The medicine released from the nanosponges buccal tablets in-vitro at a rate of 99.75%, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27 ± 0.06 ng/mL was significantly higher (p

Optimization and Advantages of Molded Tablets Using Trehalose as a Binder.

Molded tablets are manufactured by molding wet powder at low pressure and drying. Typically, water-soluble polymers are used as a binder; however, the ratio to achieve both tablet strength and rapid disintegration is limited, and designing an optimal formulation according to the active ingredients can be challenging. In addition, production may be temporarily interrupted owing to the adherence of wet powder to the inside of the mortar, which can hamper stable production. Therefore, optimization was performed by design of experiments to utilize the disaccharide trehalose as a binder for molded tablets. We formulated placebo tablets with high tablet strength and rapid disintegration. On examining the tablet interior, we confirmed the formation of solid bridges between particles and high porosity, suggesting that trehalose can be used as a binder for molded tablets. The viscosity of the trehalose saturated solution was lower than that of the polyvinyl alcohol (PVA) solution (3.8 wt%). Moreover, the trehalose formulation exhibited a significantly lower wet powder adhesion rate to the upper punch than the PVA formulation. This study provided valuable results for the future formulation design of molded tablets.

P‐19: A Design and application of MIP special driving system for low power Glass‐based products

In this paper, a design and application of low power handwritten tablet is proposed. Based on glass‐based MIP low power LCD technology for a 8‐inch product , the multi‐lane SPI series parallel decoding circuit is used to improve the decoding speed of image data transmission, At the same time, it can be refreshed in units of 1 line for partial refresh by means of address decoding. Because the communication and decoding interface of MIP LCD technology is a non‐general interface, an adaptive dedicated driving system is proposed simultaneously, including SOC, MCU, MIP LCD screen, stylus and touch sensor processing. In this driving system, SOC is transmitted to MCU through USB HS, and MCU drives MIP display by customized SPI interface. It can realize the global refresh, partial refresh and stylus touch through data processing which matching the unique data requirements of MIP and adopting multi‐buffer and thread separation. The low‐ power handwritten tablet solution proposed in this paper can significantly reduce power consumption with static power consumption of 25uW and full‐screen refresh rate reach 25Hz while partial refresh rate (100 lines) can be up to 300Hz. Combined with 8color display and stylus partial refresh application, the display content is richer and the response speed is increased by 42.8%, user experience is greatly improved.

Potent Lipophilic Melatoninergic x-fluoro-y-methoxy Substituted Phenylalkylamides: Molecular Dynamics Calculations and in vitro Modified Release in Aqueous Media from Tablet Formulations.

We report herein on the design and development of matrix tablets containing potent synthetic melatonin (MLT) receptor analogues, the x-fluoro-y-methoxy substitiuted phenylalkylamides (compounds I-IV), the preparation and melatoninergic potency of which was recently communicated. > Methods: The presence of the fluorine atom in compounds I-IV, besides not affecting their binding affinity, compared to the pineal hormone melatonin, it also slows down their metabolism, which is a major drawback of MLT. However, as fluorine increases the lipophilicity, solid pharmaceutical formulations of I-IV, involving the appropriate biopolymers for their modified release in aqueous media, were developed in the context of the present work. > Results: The release profile of analogues I-IV was found to be similar to that of MLT and also of the commercially available drug, Circadin®. Some of these systems are suitable for dealing with sleep onset problems, whilst others for dealing with combined sleep onset/sleep maintenance problems. > Conclusion: Apart from the nature and relevant content of the formulants used, this bimodal release profile of the new analogues depends, to a large extent, on the diverse structural arrangement of their side chains in space, as nicely demonstrated by the molecular dynamics calculations, conducted in the context of this study. >.

Design and Development of Multiparticulate Mini Tablets of Verapamil Hydrochloride for Pulsatile Drug Delivery

Abstract: Objectives: The objective of the research was to develop and evaluate the multiparticulate pulsatile release minitablets of verapamil hydrochloride for the treatment of hypertension at a desired time to mimic the circadian rhythms and improve the patient compliance. Materials and Methods: Formulation was prepared by CODAS technology. It was designed to initiate the release of verapamil after 4h lag time and reached the therapeutic levels at in the early morning hours, when the blood pressure is at its highest. The core minitablets were prepared by wet granulation process and coated with water insoluble polymer like ethylcellulose along with hydrophilic plasticizer. The formulation attributes were optimized and evaluated the in vitro performance. Results: The in vitro dissolution studies revealed that the coating build-up of ethylcellulose controls the initial lag time and release rate of drug product. Among the formulations (F1a) 10% w/w ethylcellulose coated minitablets showed lag time for 4 hr and controlled the release up to 24 hr. The formulation optimization studies illumined the critical attributes like fumaric acid (F2), which modified the microenvironment and improved the dissolution profile of drug product in phosphate buffer. The optimized formulation (F1a) was compared against the marketed product (CALAPTIN 120 mg SR tablets) and observed that the dissolution behaviour of the drug product followed first-order kinetics. Conclusion: The outcomes were presumed that the pulsatile release has been accomplished from coated minitablets with a lag time of 4hr, which is reliable with the demands of the chronotherapeutic drug delivery by efficiently control the blood pressure at early morning. Keywords: Multiparticulates, Pulsatile release minitablets, Verapamil hydrochloride, Chronotherapeutic drug delivery, Fumaric acid, ethylcellulose.