Tablet Disintegration Research Articles

PENGEMBANGAN SEDIAAN TABLET ESTROGENIK DARI EKSTRAK RUMPUT KEBAR (Biophytum petersianum) MENGGUNAKAN VARIASI KONSENTRASI PENGIKAT PVP K-30

Kebar grass (Biophytum petersianum Klotzsch) contains steroid, saponins, flavonoids, alkaloids, and triterpenoids. The use of Kebar grass extract can increase the development of follicles because it contains saponins which are the basic ingredients for the synthesis of steroid hormones and can improve the performance of reproductive system. This study aims to determine the quality the tablets made from Kebar grass extract with varying concentrations of PVP K-30 binder. Tablets were made in 3 formulas with varying concentrations of PVP K-30 as a binder, namely 2% (F1), 3% (F2), and 4% (F3). Methods of making tablets by wet granulation. Tablet quality testing includes organoleptic, weight uniformity, thickness, diameter, hardness, friability, and disintegration time. The flavonoid quercetin was used as a marker for tablet analysis. The results showed that the tablets were round in shape, white-gray in color, had a slightly bitter taste and had a characteristic aromatic odor. The average value of tablet weight uniformity is 290.06 – 306.45 mg (KV <5%), tablet diameter is 0.91 -0.92 cm, thickness is 0.41 – 0.48 cm, hardness is 4.06 – 7.95 kp, friability 0.17 – 0.21% and tablet disintegration time < 15 minutes. The results of the statistical analysis showed that the differences in the concentration of PVP K-30 did not affect the hardness and friability of the tablets (p> 0.05). The level of the flavonoid quercetin in the tablet is 0.17 – 0.21%. The conclusion that Kebar grass extract tablets can be made using PVP K-30 at a concentration of 2-4% as a binder and the quality of the tablets is not significantly different.

Mechanistic modelling of drug dissolution for additively manufactured polymeric tablets: A novel layer-by-layer approach

Additive manufacturing has been consolidating its position in various fields over the last few decades. The development of drug delivery systems like oral tablets have been successfully accomplished using this ingenious technology. The effectiveness of an oral tablet can be analysed by its drug release behaviour and this study aims to predict this release by developing a model for a 3D printed tablet dissolution. A polymer-dissolution based mathematical model have been developed by considering a novel layer-by-layer approach that is found during additive manufacturing procedure. The shape and volume of the tablet have been found to be crucial in predicting the drug dissolution for a given time. Further, the model was verified against the drug dissolution trend obtained from a Fused Deposition Modeling (FDM)-printed polyvinyl alcohol (PVA) tablet having benidipine hydrochloride drug substance. Four different shapes have been considered to test the robustness of the model. Further, the sensitivity test have been conducted on the model and it revealed detachment rate and layer thickness as significant process parameters.

Formulation and Evaluation of Mouth Dissolving Tablet of Biperiden HCL for Treatments of Parkinson’s Disease

Seven formulations were developed using superdisintegrating substances like sodium starch glycolate, crospovidone, and cross-carmellose sodium at different concentrations. Three batches were created by employing varying concentrations of the super disintegration approach, utilizing sodium starch glycolate as the superdisintegrating agent. The batches underwent evaluation regarding sensory characteristics, firmness, breakability, weight consistency, disintegration time in a simulated environment, time is taken for wetting, laboratory tests on drug release within a controlled environment, and assessments of product stability. Fourier transform infrared spectroscopy (FTIR) studies confirmed the absence of drug-excipient interactions. In this examination, mouth-dissolve tablets of biperiden HCL were successfully ready with favorable parameters, including organoleptic properties, hardness (3.2 kg/cm3), friability (0.23%), weight variation (100 mg), disintegration time within a controlled laboratory environment (17 seconds), wetting time (11 seconds), and in-vitro drug release studies (99.80%). The study concluded that the biperiden hydrochloride mouth-dissolving tablet was effectively formulated using the direct compression method, demonstrating improved patient compliance.

Correlating mechanical and rheological filament properties to processability and quality of 3D printed tablets using multiple linear regression

Filament formulation for FDM is a challenging and time-consuming process. Several pharmaceutical polymers are not feedable on their own. Due to inadequate filament formulation, 3D printed tablets can also exhibit poor uniformity of tablet attributes. To better understand filament formulation process, 23 filaments were prepared with the polymer mixing approach. To yield processable filaments, brittle and pliable polymers were combined. A 20 % addition of a pliable polymer to a brittle one resulted in filament processability and vice versa. Predictive statistical models for filament processability and uniformity of tablet attributes were established based on the mechanical and rheological properties of filaments. 15 input variables were correlated to 9 responses, which represent filament processability and tablet properties, by using multiple linear regression approach. Filament stiffness, assessed by indentation, and its square term were the only variables that determined the filament’s feedability. However, the resulting model is equipment-specific since different feeding mechanism exert different forces on the filaments. Additional models with good predictive power (R2pred > 0.50) were established for tablet width uniformity, drug release uniformity, tablet disintegration time uniformity and occurrence of disintegration, which are equipment-independent outputs. Therefore, the obtained model outcomes could be used in other research endeavours.

Pengaruh Desain Punch Terhadap Mutu Fisik dan Disolusi Tablet MUPS Metformin HCl

The compaction of multi-unit pellet system (MUPS) into tablets is a potential alternative for sustained release drugs. Tableting tools (punch and die) affect the compaction process and quality of MUPS tablets. The punch design intends to preserve the desired drug release of compacted pellets. This study aims to investigate the effect of two punch shapes, the flat face radius edge (FFRE) and concave-faced punch (concave), each at two different cup depths, on the physical properties and release profile of metformin HCl MUPS tablets. Drug release parameters, t50 values, showed that the metformin HCl released from MUPS tablets was faster than the uncompacted sustained release pellets. The similarity of the dissolution profile (f2) between MUPS tablets and uncompacted metformin HCl pellets was lower than 50 as the minimum acceptance value. The tablet tensile strength obtained was below the requirements (<1.7 MPa). Tablet disintegration time was approximately less than 2 minutes. In conclusion, drug release profile of the MUPS tablets showed damage of the pellets due to compaction process. Nevertheless, pellets compacted at low compaction pressure using FFRE with a deeper cup depth (size 0.80 mm) showed a slightly better protection compared to other punch shapes and cup depth sizes applied.

Dissolution of pain-relief drugs: Does beverage choice matter?

Oral administration continues to be the most common route for drug delivery with the majority of approved medicines being tablets and capsule dosage forms. Standardised pharmacopeial media are typically used to test tablet dissolution in vitro, however patients use non-standard beverages to take with their medicines. Information about the dissolution of drugs in beverages consumed by patients has not been reported in the literature. Our aim was to investigate if the choice of beverage influences the dissolution of common pain relief tablets. The prevalence and type of alternative beverages used by patients to take their tablets was investigated in an online survey. The rate of dissolution of the common pain relief tablets, aspirin and acetaminophen, was measured in 15 different dissolution media including pharmacopeial dissolution media, simulated gastrointestinal fluids, and the common alternative beverages used by patients to take their tablets (including water, tea, coffee, soft drink and beer). The concentration of drug dissolved in each beverage over time was determined using either UV–vis spectroscopy or HPLC. The rate of dissolution of aspirin and acetaminophen tablets was in some cases significantly affected by the composition of the dissolution media. Factors such as mineral content, carbonation, and pH contributed to differences in the rate of dissolution for both aspirin and acetaminophen. The rate of dissolution of aspirin was significantly lower in some beverages compared to pharmacopeial media. When translated to the in vivo setting, these differences have the potential to alter the pharmacokinetics and bioavailability of orally administered medicines and so their efficacy.

Effect of Powdered Cellulose Nanofiber with Different Particle Sizes on the Physical Properties of Tablets Manufactured via Direct Compression.

Direct compression is a tableting technique that involves a few steps in non-demanding manufacturing conditions. High strength and rapid disintegration of tablet formulations were previously achieved through the addition of cellulose nanofibers (CNFs), which have recently attracted attention as a high-performance biomass material. However, CNF addition results in greater variation in tablet weight and drug content, potentially due to differences in particle size between CNF and other additives. Herein, we used pulverized CNF to evaluate the effect of CNF particle size on the variation in tablet weight and drug content. Tablet formulations consisted of CNF with different particle sizes (approximately 100 µm [CNF100] and 300 µm [CNF300], at 0, 10, 30, or 50%), lactose hydrate, acetaminophen, and magnesium stearate. Ten powder formulations with different particle sizes and CNF concentrations were prepared; thereafter, the tablets were produced using a rotary tableting press with a compression force of 10 kN. The variation in weight and drug content as well as the tensile strength, friability, disintegration time, and drug dissolution of tablets were evaluated. CNF100 addition to the tablets reduced the weight and drug content variation to a greater extent than CNF300 addition. Using CNF300, we produced tablets of sufficient strength and short disintegration time. These properties were also achieved with CNF100 addition. Our findings suggest that adding CNF of small particle size to the tablet formulation can reduce the variation in weight and drug content while maintaining high strength and short disintegration time.

Technology Criteria for the Manufacturing of Rebamipide Film-coated Tablets

Introduction. The current growth of the pharmaceutical market and stiff competition require from drug manufacturers make a more detailed and thorough fine-tuning of existing production lines. Direct compression technology is a modern and cost-effective technology for solid dosage form drug manufacturing. Roll-compaction tehnology (dry granulation) can be an alternative approach to optimize the manufacturing of formulations, for which the use of wet granulation or direct compression technologies is not possible due to their physical and chemical properties.Aim. The goal of this work is to investigate the possibility of manufacturing Rebamipide tablets by using direct compression technology and dry granulation technology (roll-compaction), avoiding such complicated and more ex-pensive technology as wet granulation. Also aim of this work is study the impact of production methods on such quality factors as disintegration and dis-solution time.Materials and methods. In this study were used such materials as Rebamipide substance (α-[(4-Chlorobenzoyl)amino]-1,2-dihydro-2-oxo-4-quinolinepropanoic acid) (experimental sample), MCC-102 (J. Rettenmaier & Söhne (JRS), Germany), Starch pregelatinized (Colorcon LTD., England), Kollidone SR (BASF, Germany), Croscarmellose sodium (J. Rettenmaier & Söhne (JRS), Germany), Anhydrous citric acid (Scharlau), Sodium lauryl sulfate (BASF, Germany), Aerosil 200 vv Pharma (Evonik Industries AG, Germany), Sodium stearyl fumarate (J. Rettenmaier & Söhne (JRS), Germany), Calcium stearate (FACI, Italy), Film coating VIVACOAT® PA-1P-000 (J. Rettenmaier & Söhne (JRS), Germany). Also were used such equipment as Y shape blender («AZT FARMA K.B.», Russia), roll compactor LGC100 (Beijing Gylongli Automation Tech. Co., Ltd, China), rotary tablet press PG16G (Beijing Gylongli Automation Tech. Co., Ltd, China), tablet coating system Labcoat™ M (O'Hara Technologies lnc, Canada), ionising air gun Simco Cobra (SimcoIon, Netherlands), flowability tester ERWEKA GT (ERWEKA GmbH, Germany), powder density tester ERWEKA SVM 122 (ERWEKA GmbH, Germany), vibrating sieve CISA RP 200N (CISA Cedaceria Industrial S.L., Spain), tablet hardness, thickness and height tester SOTAX HT 10 (SOTAX AG, Switzerland), dissolution tester DT 626/1000HH (ERWEKA GmbH, Germany) and disintegration tester ZT321 (ERWEKA GmbH, Germany).Results and discussion. In a series of experiments were obtained tablet’s cores and film coated tablets by direct compression and roll-compaction methods. Experimentally it was found, that in tablets with similar formulations roller compaction technology provides slower disintegration and dissolution time, compared to direct compression method. This fact should be taken into account during drug development when planning the rate of release of the active ingredient.Conclusion. As a result of the experiments it was shown a direct correlation between the use of a certain technology and its impact in such quality indicators as disintegration and dissolution time of tablets. It was also found that dry granulation technology provides a more technologically suitable tablet mass.

Effect of tableting temperature on tablet properties and dissolution behavior of heat sensitive formulations

The tableting process involves the conversion of mechanical to thermal energy. This study evaluated the influence of temperature on the tableting behavior of formulations with different compositions. The tableting machine was equipped with a thermally controlled die to mimic the heat evolution from tableting on an industrial scale. Six formulations containing binders with a comparably low glass transition temperature were examined. Besides the polymer type and concentration, the filler was varied. Paracetamol was chosen as the model active pharmaceutical ingredient. The investigation included alterations in tabletability, disintegration and dissolution. Elevated temperatures led to an enhanced tabletability. The polymer type and concentration were decisive for the extent of alterations. The variation of the filler composition played a minor role due to the high melting points of its components. The results were confirmed in disintegration and dissolution studies. A high binding capacity and a low glass transition temperature resulted in a stronger delay of disintegration. The dissolution was sustained. Increased concentrations of the binding polymer enhanced the effect. If the tableting behavior of a formulation is changed by elevated temperatures during formulation development and production, a change of the binder type or concentration should be considered to ensure a reproducible tablet quality.

The Development of Oral Solid Dosage Forms Using the Direct-Compression Tableting of Spray-Dried Bacteriophages Suitable for Targeted Delivery and Controlled Release

This study addresses the challenge of developing a cheap, patient-friendly alternative to antibiotics using bacteriophages for gastrointestinal applications. It explores the feasibility of manufacturing an enteric solid dosage form containing a salmonella-specific Myoviridae phage, Felix O1, encapsulated in spray-dried trehalose/Eudragit microparticles. The spray-dried powder was further formulated by combining the spray-dried microparticles with magnesium stearate to facilitate the fabrication of tablets using direct compression. The paper presents a comprehensive evaluation of the tablets with measurements of phage viability during tablet fabrication using a range of compression settings and, after tablet disintegration, dissolution and friability. Phage viability measurements were performed using storage stability testing of spray-dried powders and tablets in sealed vials at 4 °C, 20 °C and 30 °C and under different humidity conditions of 0%, 50% and 65% RH. The recommended compression force range was found to be 10–15 kN for a standard 10 mm diameter tablet. The storage of tablets at 4 °C/0% RH was found to be the most favourable condition resulting in a ~1 log loss in titre over a six-month storage period. Storage at higher temperatures and samples exposed to high levels of humidity resulted in a significant loss in phage viability. The paper highlights challenges in developing phage formulations suitable for direct-compression tableting, which afford the phages protection when exposed to temperatures and humidity levels that do not require a cold supply chain.

Formulation and optimization of Ambrisentan self-micro emulsifying drug delivery system (SMEDDS) tablet by wet granulation

Ambrisentan is an orally administered endothelin receptor antagonists used for the treatment of pulmonary hypertension. As it is fall under BCS class 2 medicine, its solubility, stability and oral bio availability are poor. Here, a self-micro-emulsifying drug delivery system (SMEDDS) was developed to improve its solubility and drug dissolution. The objective of our investigation was to formulate a self-micro-emulsifying drug delivery system (SMEDDS) of Ambrisentan using minimized quantity of oil, surfactant and co-surfactant that could improve its solubility, stability, and dissolution. The composition of optimized formulation consists of Maisine CC as oil, Acrysol EL 135 as surfactant and Capryol PGMC as cosurfactant, containing 200 mg of Ambrisentan showing mean droplet size (155.12 nm), rate of self-emulsification (56 sec) and Polydispersibility index (0.331). This optimized liquid SMEDDS is used as a liquid component in wet granulation and prepare tablet of Ambrisentan having 5 mg strength. A prepared tablet is evaluated further for tablet evaluation tests and dissolution. This research results in good dissolution and stability.

Microbiological Status and Pharmaceutical Evaluation of Commercially Available Herbal Medicinal Products in Lagos, Nigeria

Some herbal products were sourced from traditional medicine practitioners purposely to evaluate their microbial and pharmaceutical qualities. These products were 15 in number and were of different dosage forms. Phytochemical tests were carried out to determine their phyto-constituents. Also, the microbial qualities were determined and the pharmaceutical evaluation carried out through tablet disintegration of powders, crushing and friability. The powdered formulations were subjected to particle size determination and angle of repose. The density of the suspensions and solutions were taken. Results indicated presence of alkaloids, anthraquinones, tannins and cardenolides. The microbial load of the products varies. Seven (46.67%) of the products were contaminated with Salmonella, ten (66.67%) were contaminated with fungi, ten (66.67%) were contaminated by Staphylococcus aureus and nine (9) were contaminated with E.coli.(60%). The angle of repose for the powder dosage forms were high, this indicate that the powdered products were not free flowing and not highly cohesive. Also, acceptable crushing strength and friability was shown by the tablet formulation but it failed the disintegration time. Out of the fifteen products, two of the products were registered with NAFDAC (13.33%), all the products indicated their manufacturing and expiry dates while ten (66.67%) have their contents stated. All the products have their therapeutic claims indicated on their containers. In conclusion, there should be control of standards of herbal medicine in Nigerian markets as well as constant evaluation and monitoring of the various products.

Konjac gum and maltodextrin compound tablets as carriers of IgY for sustained release in stomach

Egg yolk immunoglobulin (IgY) is a biologically active ingredient with high immunogenicity; however, its instability in the acidic environment of the upper gastrointestinal tract limits its application in oral formulations. In the present work, an encapsulation system based on maltodextrin (MD) and konjac gum (KGM) was developed as a protective carrier for IgY for targeted release to retain stability. A simulated gastric model was used to compare the release characteristics of the different formulations, and to explore the optimal release mode. To better understand the controlled release mechanism of MD and KGM composite tablets, the release curve, macrostructure, microstructure, and water mobility were analysed. Results indicated that the sustained release of IgY from MD and KGM composite tablets was mainly driven by Fick diffusion and dissolution. As the concentration of KGM increased, the release rate of IgY from the tablets decreased, and the release mechanism gradually changed from diffusion to erosion. The dense cross-linkage between MD and KGM helped prevent tablet disintegration, and slowed down the release of IgY. In addition, the dissolved KGM formed a film on the tablet surface to control the erosion rate. It can be concluded that the optimal formulation of an IgY-loaded tablet was a mass fraction of 50% MD, 30% KGM, and 20% IgY. The present work provided a practical method to protect the biologically active ingredients from acidic destruction in the stomach during oral treatment.

Design of experiments approach on the compaction properties of co-amorphous tablets

Co-amorphous systems are an evolving strategy to stabilize the amorphous form of a drug molecule with the aim of overcoming its poor water-solubility. With research focussing on the molecular level of co-amorphous systems, little is known about their downstream processing. In this study, tablets of co-amorphous carvedilol and aspartic acid (CAR-ASP) with calcium hydrogen phosphate and croscarmellose sodium as excipients were produced using a compaction simulator. The amorphous form of spray dried CAR-ASP and the subsequently produced tablets was confirmed with XRPD. Over the storage time of 12 weeks, no recrystallization of the amorphous material was observed. A central composite face-centred design with three factors was set up to investigate the interplay of formulation and processing variables with the tablet characteristics elastic work, tensile strength and disintegration time. As a result, increasing the amount of co-amorphous material led to a decrease in elastic work and an increased tensile strength. These effects were beneficial for tablet properties, namely harder tablets and reduced elasticity. Disintegration time was prolonged by amounts of up to 25–30% co-amorphous material, while larger amounts induced faster tablet disintegration. While showing the feasibility of compacting co-amorphous material with calcium hydrogen phosphate, this study also gives insight into how tablet characteristics are affected by co-amorphous material and relevant process parameters.

Optimization of Fast Disintegrating Tablets Diphenhydramine HCl using Co-process of Cross-link Yellow Kepok Banana Starch, Crospovidone, and Microcrystalline Cellulose

Diphenhydramine HCl is an antihistamine drug that is available in conventional tablet form. This study aimed to produce the optimum formula for a diphenhydramine fast disintegrating tablet (FDT) using a modification of starch, crospovidone, and microcrystalline cellulose (MCC) to produce quality tablets that meet the tablet's physical requirements and tablet dissolution. Starch modification was made using a two-step method of starch cross-link, then continued with silica coprecipitation. FDT was prepared by the direct compression method. Optimisation with the simplex lattice design (SLD) model uses three components: co-process starch crosslink-silica, crospovidone, and MCC, which obtained 14 formula designs. The hardness, wetting time, disintegration time, and percent dissolution are optimisation parameters. Equations, contour plots, and desirability values were determined as the optimum formula. Based on the research results, an optimum formula was obtained with the proportion of co-process cross-link starch-silica was 56.185 mg, crospovidone at 6 mg, and MCC at 45.815 mg. The result of hardness was 5 kg, wetting time 51.061 seconds, disintegration time 63.129 seconds, and dissolution was 100.972%. The interaction of the three components reduces hardness and increases disintegration time, wetting time, and percent dissolution.

Eutectic phase transition during tablet manufacture: effect of melting point of eutectic forming drug

The aim was to investigate eutectic transition during tableting and storage. Mixtures of lidocaine and series of NSAIDs with increasing melting point were used as model systems to guide formulators to scaleup eutectic forming materials gaining enhanced dissolution while avoiding deleterious physical changes. Physical mixtures of NSAIDs with lidocaine were prepared at eutectic forming ratio. These were directly compressed, dry co-ground before compression, or compressed after wet granulation. Dissolution of tablets was compared to corresponding dry co-ground mixture. Thermograms of direct compressed tablet were compared to co-ground mixture and pure compound. Stability of direct compressed tablets was assessed. Tableting initiated eutexia which enhanced dissolution of NSAIDs. Eutexia was associated with tablet softening in case of low melting point ketoprofen and aceclofenac. Wet granulation hastened eutexia developing unacceptable tablet in case ketoprofen and aceclofenac. Tablets prepared by direct compression of physical mixtures underwent gradual eutectic transition upon storage with the magnitude of eutectic transition reducing with increased melting point of NSAIDs. Ketoprofen was physically unstable but aceclofenac degraded chemically as well. Tenoxicam and meloxicam tablets were physically and chemically stable. Direct compression after physical mixing is the best tableting technique, but low melting point drugs should consider different strategy before compression.

Dr DEVELOPMENT OF POSACONAZOLE DELAYED RELEASE FORMULATION FOR MUCORMYCOSIS BY HOT MELT EXTRUSION USING QBD APPROACH

Amorphous solid dispersion (ASD) by hot-melt extrusion (HME) is an industrially feasible approach to overcome the solubility and bioavailability limitations of poorly soluble active pharmaceutical actives. The creation of HME-based ASDs was significantly impacted by the implementation of Quality by Design (QbD). The objective of the study was to develop an ASD of posaconazole for the effective management of mucormycosis. The impact of change in levels of extra granular materials were identified as critical quality attributes (CQA's) for the development of delayed release tablet. A 23 full factorial design was employed to study the impact of independent variables HPMCAS (X1), HPC(X2) and CCS (X3) as CQA’s on the dependent variables such as hardness (Y1) and Disintegration Time (Y2) and % Drug release (Y3). The design was analyzed by using ANOVA by using MINITAB software. The influence of the extra granular components on the dissolution of tablet was closely evaluated while finalizing the optimized batch. The extrudes were also evaluated by FTIR, XRD and DSC analysis which confirmed the purity and in-situ conversion from crystalline to amorphous form ofthe drug. Systematic development of a bioavailable and stable ASD of posaconazole was achieved by studying the CQA’s at different levels by using the QbD and from the stability data, the optimized batch F4 was found to be stable up to 3 months at accelerated conditions40°C/75%Rh.

Development of an Image-based Method for Tablet Microstructure Description and Its Correlation with API Release Rate

The performance of a pharmaceutical formulation, such as the drug (API) release rate, is significantly influenced by the properties of the materials used, the composition of the final product and the tablet compression process parameters. However, in some cases, the knowledge of these input parameters does not necessarily provide a reliable description or prediction of tablet performance. Therefore, the knowledge of tablet microstructure is desirable to understand such formulations. Commonly used analytical techniques, such as X-ray tomography and intrusion mercury porosimetry, are not widely used in pharmaceutical companies due to their price and/or toxicity, and therefore, efforts are made to develop a tool for fast and easy microstructure description. In this work, we have developed an image-based method for microstructure description and applied it to a model system consisting of ibuprofen and CaHPO4∙2H2O (API and excipient with different deformability). The obtained parameter, the quadratic mean of the equivalent diameter of the non-deformable, brittle excipient CaHPO4∙2H2O, was correlated with tablet composition, compression pressure and API release rate. The obtained results demonstrate the possibility of describing the tablet dissolution performance in the presented model system based on the microstructural parameter, providing a possible model system for compressed solid dosage forms in which a plastic component is present and specific API release is required.Graphical

Effects of Citric Acid and Sodium Alginate on the Stability and Dissolution of Clarithromycin Extended-Release Tablet

The pharmacokinetics of clarithromycin (CLR) conventional tablets (T1/2: 5-7 h) demand 2 or 3 doses per day, which is inconvenient for patients. Therefore, a sustained-release CLR tablet is necessary. Based on Klacid MR tablets (AbbVie) composed of citric acid and sodium alginate (Na-ALG), we developed a 24-hour extended-release CLR tablet. Although citric acid had a significant effect on the CLR release profile, the incompatibility of citric acid and CLR was reported (via FT-IR and stability study). Based on the function of Na-ALG in controlling the release and reducing the incompatibility of citric acid and CLR, a process (CLR and citric acid were granulated separately) was proposed. The final tablet formulation showed 1-month stability and dissolution similarity to standard tablets in pH 6.8 medium (f2 > 50).

Towards simultaneous determination of tablet porosity and height by terahertz time-domain reflection spectroscopy

The quality control of pharmaceutical tablets is still based on testing small sample numbers using at- and off-line testing methods. Traditional in-process controls, such as tablet mass, height, mechanical strength, and disintegration time are time- and resource-consuming and poorly suited to support an effective transition towards continuous manufacturing. Another suitable parameter to monitor during production would be tablet porosity. Porosity can be linked to mechanical strength and disintegration but typically requires knowledge of tablet dimensions and mass. Tablet porosity measurements based on terahertz time-domain spectroscopy (THz-TDS) offer a fast and non-destructive approach to in-process control testing for physical tablet properties. This study presents THz-TDS reflection measurements as an alternative to the previously reported transmission setup. It is shown that the proposed method can determine porosity based on the reflected amplitude from the tablet surface, but also allows for precise determination of tablet height in the same measurement. The tablet mass can be estimated by combining the height and porosity measurements. This opens up for the opportunity to determine the tablet's mechanical strength by using the possible correlation to the determined porosity.