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This paper discusses the multi-level capacitated lot-sizing problem with linked lot sizes and backorders (MLCLSP-L-B) considering deterministic product shelf-life applied to pharmaceutical tablets manufacturing processes. This paper's motivation, essential concepts, and conclusions for the pharmaceutical industry were already presented and discussed in the International Workshop on Lot-Sizing (IWLS), see Simonis and Nickel (2023a. International Workshop on Lot-Sizing-IWLS'2023, Vol. 13, 30–33). Material's shelf-life depends on the remaining shelf-life of issued ingredients in tablets manufacturing processes. This particular shelf-life behaviour is named integrated shelf-life rules. The MLCLSP-L-B is extended by integrated shelf-life rules (MLCLSP-L-B-SL). Moreover, an exact mathematical problem formulation is provided. First In-First Out (FIFO) and First Expire-First Out (FEFO) heuristics are developed for the MLCLSP-L-B. The MLCLSP-L-B-SL, FIFO, and FEFO heuristics are evaluated based on anonymised real-world data of five multi-level tablets manufacturing problem instances. Additionally, proposed solutions regarding manufacturing costs and shelf-life conflicts are compared. Finally, planning rules and managerial insights are derived for tablets manufacturing processes. [ABSTRACT FROM AUTHOR]

Solid forms transformations and new crystal structures of an active pharmaceutical ingredient (API) can occur due to various manufacturing process conditions, especially if the drug substance is formulated as a hydrate. The conversion between hydrate and anhydrate forms caused by changes in temperature and humidity must be evaluated because of the risk of dehydration and phase transitions during the manufacturing process. Differences in physicochemical, mechanical, and rheological properties have been observed between solid forms of the same API that can cause manufacturing and product-related issues. Atorvastatin calcium trihydrate (ACT) is a synthetic lipid-lowering agent that was discovered during Lipitor® (its anhydrous form) Phase 3 clinical trials after passing Phase I and II. This case highlights the importance of routinely performing solid form screenings because of the probability of finding new solid forms during the development and scale-up process. Therefore, in this contribution, ACT tablet formulation was performed and evaluated starting from the compatibility of 1:1 proportions of drug and the excipients microcrystalline cellulose 101 (MCC 101), calcium carbonate, lactose monohydrate, croscarmellose sodium, hydroxypropyl cellulose, magnesium stearate, and polysorbate 80. Then, 40 mg ACT tablets were prepared on a small pilot scale, and manufacturing process assessment was conducted by sampling process stages selected as critically prone to solid forms formation or phase transition. Final product quality was evaluated regarding weight variation, hardness, disintegration, dissolution, and assay tests. Powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA) were applied to solid state evaluation. The starting raw material was confirmed to be ACT Form I. From the preformulation studies, PXRD, FT-IR and TGA analyses showed no interactions between ACT and excipients, while DSC results revealed a physical interaction with MCC 101, not considered an incompatibility. The effect of the tablet manufacturing process was achieved by amorphization, while some ACT long-range crystalline structure remained, as confirmed by PXRD, FT-IR and DSC. However, the tablets' quality parameters were found to be within the acceptable range of both the pharmacopeia guidelines and manufacturer parameters regarding weight variation, hardness, disintegration, dissolution, and assay tests. [ABSTRACT FROM AUTHOR]

Copyright of Science & Technology of Food Industry is the property of Science & Technology of Food Industry Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Numerical simulation is a technique that utilizes electronic computers to combine concepts of the discrete element method (DEM), finite element method (FEM), computational fluid dynamics (CFD), etc., and express simulated behaviors utilizing numerical computations and images. Compaction is the main process of tablet manufacturing; most of the current studies have focused on macroscopic compaction and tablet characterization, while the internal stress state and microstructure changes as a result of the compaction process are not well understood. Therefore, an in-depth understanding of the flow and compaction behavior of pharmaceutical powders is essential for the analysis and control of the compaction process. Methods: Current research shows that compaction is shifting from macroscopic behavior toward internal microscopic behavior using numerical simulation technology. Results: This review focuses on the application of various numerical simulation technologies during compaction and the contact model, or the constitutive equation commonly used in numerical simulation. In addition, the difficulties of numerical simulation technology in calibrating powder parameters and the limitations of the current research are also discussed. Conclusions: Numerical simulation research in medicine and other fields will continue to flourish as numerical simulation technology advances, attracting more and more researchers using it effectively. [ABSTRACT FROM AUTHOR]

Background/Objectives: Only a few studies performed at industrial scale in non-simulated conditions have investigated the effect of input variability from the product's lifecycle on product quality. The purpose of this work was to identify the root causes for the low and variable hardness of core tablets prepared using high-shear wet granulation through batch statistical modeling and to verify the short- and long-term effectiveness of the improvement actions. Methods: The novelty of this study is the use of multivariate methods for the complex assessment of a wide data set belonging to two proportional composition strengths, manufactured at an industrial scale, with different tablet shapes and sizes, with the aim of identifying inter-related active ingredient and process variables with the highest impact on hardness value and for defining optimal processing conditions leading to a robust product. Results: Four main variables affecting the output variable were identified: API particle size, nozzle type used for granulation, wet discharge, and drying intensity. These were included in an updated control strategy (3 out of 4 variables having to be within the desired ranges: API d0.5 < 45 microns; granulation nozzle that ensures liquid dispersion into droplets; gentle wet discharge and drying processes). In the case of the product studied, the newly defined process conditions could even accommodate d0.5 up to 70 microns and still ensure adequate core tablet hardness (at least 30% above the lower specification limit) for the successive film-coating step. Conclusions: Besides the beneficial impact of reducing the risk for out-of-specification hardness results, this study also offered the benefit of cost avoidance and yield improvement. The improvement was confirmed through the significant average hardness increase (15–20%) and between-batch variability decrease, leading to decent sigma quality levels (2.5) for the control phase batches. [ABSTRACT FROM AUTHOR]

The study aimed to apply the quality by design (QbD) methodology to optimize the fluidized-bed granulation process to produce high-quality pharmaceutical granules intended for tablet manufacturing. Research focused on defining the quality target product profile (QTPP) and identifying critical quality attributes (CQAs), critical material attributes (CMAs), and critical process parameters (CPPs) crucial to ensuring product quality. The experimental design employed a three-level fractional factorial design to investigate the effects of key process parameters, including the mass flow rate of the binder, the temperature of the inlet air, and the drying time, on the granulation results. Measurements such as particle size distribution, moisture content, and flowability were used to assess the granules. The results indicated that parameters such as the inlet air temperature and drying time significantly impact the quality of the granules, confirming their status as CPPs. Further analysis of tablet mass and hardness revealed that these granule properties directly influenced tablet uniformity and mechanical strength. The application of the failure mode and effect analysis (FMEA) matrix helped to identify and prioritize these critical parameters based on their risk priority number (RPN). The study concluded that a systematic QbD approach, combined with a robust experimental design and risk management, is crucial for optimizing the fluidized-bed granulation process. This ensures consistent production of granules with the desired quality attributes and enhances the safety and efficacy of the final pharmaceutical product. [ABSTRACT FROM AUTHOR]

Background/Objectives: This study aimed to establish a predictive model for critical quality attributes (CQAs) related to tablet integrity, including tablet breaking force (TBF), friability, and capping occurrence, using machine learning-based models and nondestructive experimental data. Methods: The machine learning-based models were trained on data to predict the CQAs of metformin HCl (MF)-containing tablets using a commercial-scale wet granulation process, and five models were each compared for regression and classification. We identified eight input variables associated with the process and material parameters that control the tableting outcome using feature importance analysis. Results: Among the models, the Gaussian Process regression model provided the most successful results, with R2 values of 0.959 and 0.949 for TBF and friability, respectively. Capping occurrence was accurately predicted by all models, with the Boosted Trees model achieving a 97.80% accuracy. Feature importance analysis revealed that the compression force and magnesium stearate fraction were the most influential parameters in CQA prediction and are input variables that could be used in CQA prediction. Conclusions: These findings indicate that TBF, friability, and capping occurrence were successfully modeled using machine learning with a large dataset by constructing regression and classification models. Applying these models before tablet manufacturing can enhance product quality during wet granulation scale-up, particularly by preventing capping during the manufacturing process without damaging the tablets. [ABSTRACT FROM AUTHOR]

Amorphous solid dispersion (ASD) tablets based on hydrophilic polymer carriers may encounter disintegration challenges. In this work, the effect of different formulation composition variables on the ASD tablet disintegration performance was systematically studied. GDC-0334: copovidone (PVPVA) 60: 40 ASD prepared by spray drying was selected as the model ASD system. The effects of ASD loading, filler type and ratio, disintegrant type and level were then investigated using tablets made by direct compression process. Tablet disintegration time increased with the increase of ASD loading, especially when ASD loading exceeded 50 %. At the same tablet solid fraction, when lactose was used as the soluble filler, faster tablet disintegration was observed compared to the tablets with mannitol as the soluble filler. Among the three tested disintegrants, croscarmellose sodium performed the best in facilitating the ASD tablet disintegration, followed by sodium starch glycolate, and crospovidone was the poorest. When croscarmellose sodium was used as the disintegrant, 5 % level was sufficient to enable ASD tablet disintegration at 60 % ASD loading and further increase of croscarmellose sodium level to 8 % did not provide additional benefit. Water uptake experiments were performed on selected tablets and the results demonstrated a positive correlation with tablet disintegration time, indicating water penetration is a major contributing step for the disintegration of our ASD tablets. Overall, this work provides a rationale for excipient selection and insights into building a platform formulation approach for developing immediate-release ASD tablets. [Display omitted] [ABSTRACT FROM AUTHOR]

Additive manufacturing (AM) processes, such as fused deposition modelling (FDM), have emerged as transformative technologies in pharmaceutical manufacturing, enabling the production of drug delivery systems with complex and customised geometries. These advancements provide precise control over drug release profiles and facilitate the development of patient-specific medicines. This study investigates the dissolution behaviour of AM-fabricated tablets made from polyvinyl alcohol (PVA), a hydrophilic and biocompatible polymer widely used in drug delivery systems. The influence of the initial mass, surface area, and surface-area-to-volume ratio (S/V) on dissolution kinetics is evaluated for tablets with intricate geometries. Our findings demonstrate that these parameters, while critical for conventional tablet shapes, are insufficient to fully predict the dissolution behaviour of complex geometries. Furthermore, this study highlights how geometric modifications can enable the administration of the same drug dosage through sustained or immediate release profiles, offering enhanced versatility in drug delivery. By leveraging the geometric design freedom provided by AM technologies, this research underscores the potential for optimising drug delivery systems to improve therapeutic outcomes and patient compliance. [ABSTRACT FROM AUTHOR]

Multilayer and Bilayer tablets are winning popularity over single-layer tablets because of their controlled release advantages. Since each layer of API must be compatible with the others and with excipients to extend the effects of the medication or drugs and improve patient compliance, technology for creating multilayers and bilayers is less widespread than that for single-layer tablets. Hydrophilic polymers are more frequently employed in the formulation of biliary and multilayer tablets as both medication carriers and release barriers. But the ratio of using polymer is different from each other in the drug barrier layer and carrier layer that can make alteration by a researcher to develop a difference in the release rate of different APIs in a single unit of the tablet. With a larger surface area and a faster rate of drug release over time, multilayer and biliary tablets can help mitigate the non-linearity and drug interactions that arise with diffusioncontrolled matrix devices. This review article covers the different techniques used to create biliary and multilayered tablets as well as the challenges associated with their formulation. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Education, Theory & Practical Research (JETPR) / Eğitim Kuram ve Uygulama Araştırmaları Dergisi (EKUAD) is the property of Journal of Education, Theory & Practical Research (JETPR) / Egitim Kuram ve Uygulama Arastirmalari ) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Component regulation in perovskite single crystals (SCs) sets the precondition for designing energy band and carrier dynamics, which is essential for exploring functional optoelectronic devices. However, entropy‐driven ion diffusion in SCs leads to component homogenization in a few hours, while the gradient films exhibit long‐term gradient stability. Therefore, tableting engineering is proposed to introduce appropriate boundaries, ensuring good short‐range alignment within the grains and suppressed ion diffusion in the long range. With 6–10 MPa pressure, transverse/longitudinal gradient MAPbX3 (X = Cl, Br, I) tablets are constructed. Due to the alignment of the valence band maximum from MAPbCl3 to MAPbBr3 to MAPbI3, the hole extraction is significantly promoted. As well, different metal electrodes are utilized to regulate the main carrier types. Hole‐type Au/gradient tablet/Au devices show an obvious rectification effect, while electron‐type Ag/gradient tablet/Ag devices have near‐Ohmic contact. Compared to the electron‐type devices, Au/gradient tablet/Au devices show a 3.9‐fold improvement in terahertz responsivity to 3.51 µA W−1, a 2.6‐fold reduction in noise‐equivalent power to 2.22 × 10−8 W Hz−1/ 2; and a 2.6‐fold increase in specific detectivity to 1.89 × 107 Jones. This work demonstrates the tableting engineering to realize stable compositional gradients for energy band regulation in weak‐signal THz detection. [ABSTRACT FROM AUTHOR]

This research aims to develop ranitidine HCl tablets that can be expanded with a matrix from Balinese salak seeds (Salacca zalacca) as a natural matrix material. This formulation is expected to prolong the release time of the drug in the body, thereby increasing the effectiveness of ranitidine therapy in the treatment of gastric diseases. The research method included the extraction of the active components from Balinese salak seeds and the process of making tablets using the wet granulation method, followed by physical tests of the tablets which included the hardness, crushing time, and ability of the tablets to expand. The results showed that ranitidine HCl tablets with Balinese salak seed matrix had physical characteristics that met the requirements of pharmacopooeia, with a slower drug release time than tablets without a developer matrix. Analysis of development capabilities shows that Balinese salak seeds are effective as natural matrix agents to prolong the release time of ranitidine HCl. In conclusion, Balinese salak seed matrix can be used as an alternative in the development of expandable ranitidine HCl tablets, potentially increasing the therapeutic effect of the drug. [ABSTRACT FROM AUTHOR]

Background/Objectives: Improving the production rates of modern tablet presses places ever greater demands on the performance of excipients. Although co-processing has emerged as a promising solution, there is still a lack of directly compressible excipients for modified-release formulations. The aim of the present study was to address this issue by investigating the potential of novel co-processed excipients for the manufacture of modified-release tablets containing ibuprofen. Methods: The excipients were prepared by melt granulation of lactose monohydrate with glyceryl palmitostearate as a binder. The influence of glyceryl palmitostearate particle size, ibuprofen content, compression pressure, and compression speed on the compaction behavior of the tablet blends was analyzed. Results: Novel co-processed excipients ensured good flowability and acceptable mechanical properties of the tablets containing up to 70% ibuprofen. Furthermore, lipid-based co-processed excipients proved to be very promising for directly compressible formulations with high-dose, highly adhesive active pharmaceutical ingredients such as ibuprofen, as they do not require additional lubricants. The influence of compression speed on the tensile strength of the tablets prepared was not pronounced, indicating the robustness of these directly compressible excipients. The investigated lipid-based excipients enabled a prolonged release of ibuprofen over 10 h. Conclusions: The novel lipid-based co-processed excipients have shown great potential for directly compressible formulations with modified release of high-dose, challenging active pharmaceutical ingredients. [ABSTRACT FROM AUTHOR]

The most important component of the concept Quality-by-Design (QbD) is the provision of a scientific approach to substantiation and optimization of each critical process parameter (CPP) and identification of the link between CPPs and critical quality indicators. Wet granulation is one of the most critical stages of the technological process in GSB-106 tablet production technology. The process of optimizing the wet-granulation stage using regression analysis was considered in the present study in relation to determination of the granulation process time for a low shear force mixer. Samples of tablet masses taken at various time points from 10 to 60 min were analyzed for several indicators such as the particle-size distribution, flowability, bulk density before and after compaction, and Carr and Hausner indices. Tablets were produced from the selected model samples at various pressing forces and assessed for hardness and disintegration. The results were analyzed using regression analysis to obtain linear regression equations describing the dependence of pharmaceutical and technological characteristics on the duration of wet granulation. Critical indicators were identified. The optimum time for a given technological process was determined. Dynamic equilibrium in the granule agglomeration process was shown to occur between 30 and 40 min of mixing. The optimal duration of the technological process was set from 40 to 50 min. [ABSTRACT FROM AUTHOR]

In the United States, illicit fentanyl is often trafficked as blue tablets mimicking the legitimate M‐30 oxycodone tablet produced by Mallinckrodt. The analysis of dyes extracted from seized fentanyl tablets could provide a useful tool for law enforcement to establish linkages between cases and could prove useful for attributing a seizure to a given trafficking organization. Fentanyl tablet seizures associated with a particular drug trafficking organization (DTO), either through investigative or intelligence information, were used as the sample set for this study. The blue dye from the tablets was isolated by solid phase extraction and then qualitatively and quantitatively analyzed via ultraviolet‐visible spectroscopy. This research revealed that the illicit tableting facilities use a different dye than several known pharmaceutical companies. The concentration of dye in individual tablets within a seizure proved to be very minimal, and the small sample size made it difficult to draw linkages from case to case. Analysis of the dyes could not effectively differentiate between the drug trafficking organizations in the tested population due to each DTO using the same dye; however, it is important to note that the dye found was consistent between illicit tablets. [ABSTRACT FROM AUTHOR]

In recent years, researchers have been exploring alternative sources of starch for drug delivery. Traditional options like corn, potato, and rice starches have been widely used, but sustainability concerns have prompted the investigation of nonconventional starches. Elephant foot yam starch, derived from an agricultural polymer, has gained popularity due to its wide availability. Starches are fundamentally unsuited for the majority of applications; they must be physically and/or chemically altered to maximize their advantages and/or minimize their drawbacks. Due to the chemical toxicity, starch modification is often done using physical techniques that are inexpensive. This study aims to evaluate the impact of elephant foot yam starch on the physicochemical properties and drug delivery of potato starch. Pregelatinization, a crucial process, is found to increase amylose content and improves starch flow properties, as confirmed by Fourier‐transform infrared spectroscopy analysis showing gelatinization in the mixture. Field emission scanning electron microscopy images reveal complete disruption of the starch granular structure after modification. Tablets made with a mixture of pregelatinized starches exhibit a slower drug release compared to those with pregelatinized starch alone. Notably, inclusion of potato starch in the mixture results in a more sustained drug release. Hence, modified starches have diverse applications for enhancing solubility of poorly soluble drugs. [ABSTRACT FROM AUTHOR]

This study investigated the impact and non-impact of tuned energy density (ED) on sinterability and other physicochemical characteristics of a sintered 3D-printed material tableting structure. The selected SLS 3D printer enables the alteration of direct ED values, which aids in analyzing the impact and non-impact of the overall process parameters, including hatch spacing (HS), laser scanning speed (LSS), layer thickness (LT), and laser power (LP). The progressively enhanced ED from 200 J/cm3 to 350 J/cm3 and 500 J/cm3 was impacted by the increased weight, hardness, and amorphization of the rifampicin (RIF) in the sintered 3D-printed material tableting structure. In the case of the surface morphology of sintered 3D-printed material tableting structure, inter-particle spaces were reduced, which increased neck formation and ultimately, increased consolidation. An increase in the ED decreased the average surface roughness of the sintered 3D-printed material tableting structure. The in vitro release of RIF diminished over 12 h as the ED progressively increased from 200 J/cm3 to 350 J/cm3 and 500 J/cm3. In addition, tuning the progressively enhanced ED had no impact on the printing yield, average thickness of the sintered layers, or thermal analysis of the 3D printed material tablet structures. The ultimate finding of this study is that it is necessary to optimize the ED and other sintering parameters according to the desired features of the sintered 3D printed material tableting structure. In addition, the utilization of SLS and incorporation of the co-processed polymer Eudragit L 100–55 in the printing process resulted in the release of RIF above physiological pH-5.5. This strategy effectively reduces the degradation of RIF under acidic conditions. Subsequently, the sintered 3D printed material tableting structures can be subjected to an in vivo pharmacokinetic study to confirm the obtained results. [ABSTRACT FROM AUTHOR]

In this study, SeDeM–ODT parametric tests were performed to determine the use of ludipress as a directly compressible tableting excipient for the development of a flurbiprofen orally disintegrating tablet. The preformulation features of different formulations (F1 –F9) were analyzed by the SeDeM–ODT tool which showed that all the powder blends were appropriate for direct compression since all the blends had index of good compressibility and bucodispersibility (IGCB) values above 5, signifying direct compression is the most appropriate method. The powder blend of the optimized formulation was assessed by the DSC–TGA technique. The optimization of nine different formulations blends of orally disintegrating tablets (ODTs) was prepared in various ratios by the implementation of design of experiments (DoE), using the central composite design by selecting ludipress (X1) (49–55%) and croscarmellose sodium (X2) (1–5%) while hardness, friability, and disintegration tests were selected as responses. The optimized formulations were evaluated by various tests and the results indicated that all the formulations were found to be in adequate range. Formulations were subjected to stability studies at accelerated states following ICH guidelines. Shelf life was found to be 51.144–56.186 months. Results of multiple-point dissolution studies revealed that formulations followed the Higuchi kinetic model. This study revealed that the SeDeM—ODT tool has been successfully used to determine the compression behavior of active compounds and their powder blends for the direct compression (DC) method in formulating flurbiprofen–ODT tablets. [ABSTRACT FROM AUTHOR]

This study aimed to optimize modified starch from Mangifera indica (mango) fruit using acid hydrolysis and pre-gelatinization via computer-assisted techniques as a substituent for pharmaceutical tableting excipients. The hydrolysis and microwave-assisted pre-gelatinization time and temperature were optimized using a three-level factorial design. The modified starches were characterized for flowability, compressibility, and swelling properties. It was found that all parameters fit a quadratic model, which can be used to predict the properties of the modified starch. The optimized hydrolysis reaction was 3.8 h at 56.4 °C, while the pre-gelatinization reaction was 3 min at 150 °C. Structural changes were found, ascertaining that starch modification was successful. The optimized hydrolyzed starch showed superior properties in relative to unmodified M. indica fruit starch and comparable characteristics to conventional excipients. The optimized pre-gelatinized starch presented an excellent enhancement in the flow and compression properties, with %swelling greatly augmented 3.95-fold and 1.24-fold compared to unmodified starch and SSG, respectively. Additionally, the pre-gelatinized starch presented comparable binding effect, while the hydrolyzed powder had reduced binding capacity due to shorter chains. The findings revealed that the use of software-assisted design of experiment facilitated a data-driven approach to optimize the modifications. The optimized modified mango starch demonstrated potential as a multifunctional excipient, capable of functioning as binder, disintegrant, and diluent. [ABSTRACT FROM AUTHOR]

We present a systematic and automatic approach for integrating tableting reduced-order models with upstream unit operations. The approach not only identifies the upstream critical material attributes and process parameters that describe the coupling to the first order and, possibly, the second order, but it also selects the mathematical form of such coupling and estimates its parameters. Specifically, we propose that the coupling can be generally described by normalized bivariate rational functions. We demonstrate this approach for dry granulation, a unit operation commonly used to enhance the flowability of pharmaceutical powders by increasing granule size distribution, which, inevitably, negatively impacts tabletability by reducing the particle porosity and imparting plastic work. Granules of different densities and size distributions are made with a 10% w/w acetaminophen and 90% w/w microcrystalline cellulose formulation, and tablets with a wide range of relative densities are fabricated. This approach is based on product and process understanding, and, in turn, it is not only essential to enabling the end-to-end integration, control, and optimization of dry granulation and tableting processes, but it also offers insight into the granule properties that have a dominant effect on each of the four stages of powder compaction, namely die filling, compaction, unloading, and ejection. [ABSTRACT FROM AUTHOR]

Umifenovir, an antiviral drug that is used to treat influenza, has recently been used in regards to COVID-19 infection. According to a literature survey, no UV technique for the estimation of umifenovir has yet been established; hence, there is an imperative need for a simple analytical method. Additionally, we developed an alternative reverse-phase high-performance liquid chromatography (RP-HPLC) method for the estimation of umifenovir. UV spectrophotometry was carried out at 223 nm absorption maxima using the solvent methanol. A concentration range of 2–12 μg/mL was found to obey Beer's law, with a correlation coefficient (r2) of 0.9995. A C-18 column (250 mm, 4.6 μm, 5 μm) was used for chromatographic separation using the isocratic mode. The mixture consisted of acetonitrile: 0.1% trimethylamine (pH adjusted to 2.7 by the addition of orthophosphoric acid) 60:40 as the mobile phase with a flow rate of 1 mL/min. The temperature was kept at 25°C, and detection at 223 nm was performed using a PDA detector. The estimated percentage of the drug was close to 100%, corresponding to the label claim of the tablet made in the laboratory. The results and statistical study demonstrated the utility of the current methods in the routine evaluation of umifenovir bulk and formulation. [ABSTRACT FROM AUTHOR]

Dwell time is an important parameter responsible for the material deformation and the mechanical and biopharmaceutical properties of the tablet. Thus, it is widely used for scale-up purposes. The geometric dwell time (GDT) can be assumed based on the shape of the punch head and the diameter and speed of the turret. This research is aimed to compare compaction simulator-recorded dwell time according to force (DTF) and the GDT calculated for the simulated rotary tablet press using the microcrystalline cellulose and calcium phosphate mixtures (CEOLUS™ UF-711 and DI-CAFOS® A60) in different proportions. Tablets were prepared, and DTF was analyzed with a compaction simulator (STYL'One Nano and Alix software) upon simulating a small rotary press at 70 rpm and a compression pressure of 10–50 kN (100–500 MPa). While GDT comprised of 14.4 ms, DTF was compression force and formulation dependent. The differences between the DTF values of the formulations decreased as the compression force increased, which was most pronounced at compression forces of 10 and 15 kN. [ABSTRACT FROM AUTHOR]

Background: The percentage of pregnant women experiencing anemia in Indonesia has increased 37.1% compared to 2018 Riskesdas. The incidence of stunting is also influenced by the anemia and nutritional status of the mother during pregnancy. The implementation of 1000HPK has been widely implemented in all districts and cities throughout Indonesia but there are still obstacles in policy integration and cross-sector coordination caused by a lack of understanding of the program so that priority placement is not determined. Aim: to obtain policy recommendations for improving programs to prevent and alleviate anemia and Chronic Energy Deficiency (CED) for pregnant women through the process of prospective bride's preparation. Research method: The method used Action research with 3 stages. The sample are key persons of 1000 HPK program which are Public Health Office, BKKBN, Midwifery and Nursing Health Providers, and Regional Ministry of Religion (Kemenag and KUA). 24 people participate in FGD and 5 people for the In-depth Interview which was carried out at a place agreed upon by the respondents. Results: of the research provide recommendations for the need for collaboration between schools and universities for health education, schools and community health centers in providing blood supplement tablets, the need for an SOP for administration flow and procurement flow for Fe tablets as well as evaluation and monitoring. Modifying Fe tablets to make them popular with teenagers, creating health check formats for use, utilizing research and community service results and utilizing digital-based communications. Conclusion: achieving the goals of the anemia policy program requires cooperation and collaboration between various stakeholders. [ABSTRACT FROM AUTHOR]

MoV‐based composites stand out as the most promising potential catalysts targeted for direct production of acrylic acid from alkane/alkene substances. Herein, MoVTeNbO powder was synthesized and successfully fabricated by adding graphite as an appropriate tableting agent. Without employing graphite as lubricant, the fabrication of tablets was not practicable. The physicochemical effects of graphite on the catalyst properties were investigated via characterization by X‐ray diffraction (XRD), Brunauer–Emmett–Teller (BET), scanning electron microscopy (SEM), ammonia temperature‐programmed desorption (NH3‐TPD), and thermal gravimetric analysis (TGA) methods. In addition to the easy and operative formation of tablets by consisting graphite, TGA results indicated better thermal stability compared to the bare powder. No harmful impact of graphite on the catalyst crystalline phases and morphology was detected by XRD and SEM analysis. The SEM images proved the graphite incorporation as a binder in the physical combination of the catalyst particles along the compression process, resulting in the desired physical resistance. Graphite caused a slight decrease in the BET surface area and final catalyst acidity. Despite the effect of reducing propene conversion, interestingly, a substantial improvement in the yield of acrylic acid was found by tableting. The graphite as an inert agent suppressed hot spots on the catalyst surface, leading to superior consistency in activity over time as well as lower selectivity to undesirable COx. [ABSTRACT FROM AUTHOR]

There are some notable drawbacks of ordinary magnetic effervescent tablets including their quick disintegration, hygroscopicity, and impracticability for field use. In order to solve the above problems for further extraction and preconcentration of three phenolic pesticides from crop flour samples, an effervescent tablet-assisted acidic ionic liquid-based in situ solvent formation magnetic solid-phase extraction (ETA-AIL-MSPE) technique was developed. In contrast to conventional imidazole ionic liquids, acidic ionic liquids can be employed as an acid source for effervescent processes in addition to being used as extractants. Not only does this reduce the need for organic solvents, but the production of CO2 by the effervescent tablet also provides a rapid dispersion effect, removing the requirement for further dispersion stages and streamlining the experiment. The magnetic effervescent tablet is made of Na2CO3 as an alkaline source, [BMIM][HSO4] as extractant and acidic sources, NaCl as a viscosity modifier, and Fe3O4 as magnetic nanoparticles. The Plackett–Burman design and the central composite design were used to screen and optimize three key variables (93 mg of Na2CO3, 451 mg of AIL, and 37 mg of Fe3O4), respectively. Through the integration of high-performance liquid chromatography-diode array detection (HPLC-DAD), the ETA-AIL-MSPE technique provided enhanced recoveries of 85.0–107.2% and limits of detection of 0.14–0.17 μg kg−1 for three representative species (ioxynil, bromoxynil, and dinoseb) in four different types of crop flour samples. For both intra-day and inter-day precision, the relative standard deviations were below 7.7%. Generally, the recently developed technique is convenient, efficient and environmental-friendly, and it has great potential for on-site sample preparation for the detection of phenolic pesticides in crop flour samples. [ABSTRACT FROM AUTHOR]

Objectives The quality of amoxicillin capsules, ceftriaxone for injection, and ciprofloxacin tablets was evaluated to determine whether there is any difference in quality when comparing the country of origin. This was undertaken because it has been claimed that antibiotics manufactured in Europe are of superior quality to those originating from Africa or Asia. Methods Samples of amoxicillin capsules, ceftriaxone for injection, and ciprofloxacin tablets were collected from three randomly selected wholesale pharmacies in each city, namely Arusha, Dar es Salaam and Mwanza, Tanzania. The collected samples of collected brands were subjected to quality control testing as per their respective pharmacopoeial monographs. Amoxil 250 mg capsules (Glaxo Wellcome, Mayenne, France), Rocephin (Roche, Switzerland) and Cipro-Denk 500 (Allphamed Pharbil Arzneimittel GmbH, Gottingen, Germany) were used as reference brands for the other generic brands of amoxicillin, ceftriaxone and ciprofloxacin, respectively. Results A total of 31 brands (10 different brands of amoxicillin capsules, 9 of ceftriaxone sodium injections, and 12 of ciprofloxacin tablets) were collected from the targeted regions and subjected to quality control testing. All samples of collected brands complied with the requirements of their respective pharmacopoeial monographs. Conclusions There was no significant difference in quality between brands of amoxicillin capsules, ceftriaxone for injection, and ciprofloxacin tablets manufactured in Africa and Asia against those manufactured in Europe in terms of compliance with the respective pharmacopoeial monographs. [ABSTRACT FROM AUTHOR]

New co-processed excipients comprising lactose (filler and sweetener), microcrystalline cellulose (MCC, filler), and low-substituted hydroxypropyl cellulose (L-HPC, disintegrant and binder) were developed via solvent evaporation for the preparation of metoclopramide orally disintegrating tablets (MCP ODTs). Single-factor and Box–Behnken experimental designs were employed to optimize the formulation. The optimized formulation ratios were water: MCC: lactose (g/g) = 17.26:2.79:4.54:1. The results demonstrated that particles formed by solvent evaporation had superior flowability and compressibility compared to the physical mixture. Tablets compressed with these co-processed excipients exhibited a significantly reduced disintegration time of less than 25 s and achieved complete dissolution within 5 min. Pharmacokinetic studies revealed that MCP ODTs significantly improved Cmax, which was 1.60-fold higher compared to conventional tablets. In summary, the lactose/L-HPC/MCC triple-based co-processed excipients developed in this study are promising and could be successfully utilized in orally disintegrating and fast-release tablets. [ABSTRACT FROM AUTHOR]

The Heckel and Kawakita equations are the most common mathematical models used in modern studies of the pressing process to evaluate the mechanical properties of tablets. However, these classical models do not take into account the whole spectrum of processes occurring during interparticle interaction, which necessitates the development of new approaches to modeling the tableting process. For this reason, a rather large number of direct- pressing models have now been developed. The choice of the optimal equation for each specific case has become a nontrivial problem. Currently used mathematical descriptions of the direct-pressing process were analyzed in the present study. [ABSTRACT FROM AUTHOR]

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Aim: This study aimed to qualitatively identify the ranges of the factors involved in the tablet compression process for ivabradine Sustained Release (SR) tablets. Materials and Methods: A full factorial design of experiments study was used to identify three factors (pre- and main-compression force and paddle rotation time) involved in the compression process of ivabradine SR tablets. For robust tableting, three responses (content uniformity, friability, and dissolution) were evaluated as critical quality attributes via analysis of variance using Design Expert software. Results: The main compression force significantly influenced dissolution (1 hr, p<0.0001; 3 hr, p<0.0001; and 8 hr, p=0.0002). Precompression and paddle rotation time slightly influenced friability (p=0.0510) and content uniformity (p=0.0968). These results showed that paddle rotation time (0.27-1.37 sec), pre-compression (1.5 kN), and main compression (7.7-9.2 kN) influenced the tablet compression process of the optimal ivabradine SR tablet. Conclusion: In summary, robust ranges of three factors for tableting were successfully evaluated. It can be concluded that the ranges of tablet compression leading to high quality (low friability and content uniformity, and optimal dissolution) for tableting were successfully observed by the DoE approach. [ABSTRACT FROM AUTHOR]

Analytical and real‐time technology in pharmaceutical manufacturing process is an important need to ensure that manufactured drugs are safe and effective. Raman spectroscopy is an emerging technique that is able to perform quantitative analysis nondestructively due to the molecular structure of many drugs. Monitoring the content uniformity and quantification of active pharmaceutical ingredient (API) in the tablet preparation process, without the assistance of solvent, is one of the key concerns in the formulation design in order to provide stable, pure, and homogenous finished products. In this study, we investigated the possibility of using Raman data as an analytical method to quantify API, the intra‐ and inter‐sample uniformity of content in the tableting process of Metformin hydrochloride tablets (C4H11N5.HCl). Analysis of all standard samples for prediction of API uniformity represents an acceptable accuracy and precision with a relative standard deviation of 2.55%. Further investigation of tablets regarding to relative Raman intensity of some characteristic peaks demonstrates the amount of API content with an accuracy of ≥96%. These values have a good adaption with pharmacopeia monograph. Findings reveal that the Raman method can be routinely utilized for quantifying API, controlling the content uniformity and the stability of drugs in different stages of manufacturing. [ABSTRACT FROM AUTHOR]

The present study compared vacuum drum drying (VDD) and conventional spray drying (SD) for solidifying crystalline ABT-199 nanosuspensions into redispersible oral drug products. The aim was to optimize formulation compositions and process conditions to maintain nanoparticle size after tablet redispersion. The impact of drug load (22%, 33%, 44%) and type of drying protectant (mannitol, mannitol/trehalose mix (1:1), trehalose) on redispersibility and material powder properties were investigated. Moreover, compression analysis was performed assessing the influence of compaction pressure on primary nanocrystal redispersibility and tablet disintegration. Higher drug loads and lower drying protectant levels resulted in particle growth, confirming a drug load dependence on redispersibility behavior. Notably, all drying protectants showed similar protection properties at properly chosen drying process parameters (Tg-dependent), except when VDD was used for mannitol formulations. Differences between the applied drying processes were observed in terms of downstream processing and tabletability: mannitol-containing formulations solidified via VDD showed an improved processability compared to formulations with trehalose. In conclusion, VDD is a promising drying technique that offers advantageous downstream processability compared to SD and represents an attractive novel processing technology for the pharmaceutical industry. As demonstrated in the present study, VDD combines higher yields with a leaner manufacturing process flow. The improved bulk properties provide enhanced tabletability and enable direct compression. [ABSTRACT FROM AUTHOR]

Background and Objective: Ornidazole, the third generation of nitroimidazole derivatives after metronidazole and tinidazole, it exerts both bactericidal and antiprotozoal effects. The purpose of this study was to evaluate the pharmacokinetic and bioequivalence of two ornidazole tablets manufactured by two different manufacturers based on their pharmacokinetic parameters. Patients and Methods: Fasted and fed healthy Chinese volunteers participated in a randomized sequence, single-dose, open-label, two-period crossover trial. There were 24 participants in both the fed study and the fasted study. Following a 7-day washout period before receiving the alternative formulation, eligible research participants were randomly assigned (1:1) to receive a single dosage of either the reference formulation or the test formulation. Following tablet administration, plasma samples were obtained over 72 h and analyzed using liquid chromatography tandem mass spectrometry (LC–MS/MS) to evaluate ornidazole contents. maximum plasma concentration (Cmax), time to Cmax (Tmax), the area under the curve (AUC) from t = 0 to infinity (AUC0–∞), AUC from t = 0 to the last quantifiable concentration (AUC0–t), half-life (t1/2), and terminal elimination rate constant (z) were evaluated as pharmacokinetic (PK) parameters. The safety evaluation involved adverse events (AEs) incidence and alterations in laboratory tests (hepatic function, blood biochemistry, hematology, and urinalysis) or vital signs (temperature, pulse, and blood pressure). Results: For the bioequivalence assessment in the fast trial, the prime PK parameters comparison between the reference and test formulation revealed that the GMR (90% CI) values for AUC0–t, Cmax, and AUC0–∞ were 100.97% (99.12–102.85%), 99.88% (90.63–110.08%), and 101.12% (99.17–103.11%), respectively. For the bioequivalence assessment in the fed trial, the key PK parameters comparison between the reference and test formulations revealed that the GMR (90% CI) values for AUC0–t, Cmax, and AUC0–∞ were 103.00% (100.94–105.11%), 101.90% (99.63–104.22%), and 102.99% (100.87–105.16%), respectively. The geometric mean ratios (GMRs) for the primary pharmacokinetic parameters (Cmax, AUC0–72, and AUC0–∞) between the two formulations and the corresponding 90% confidence intervals (CIs) were all within the range of 80.00–125.00% for both the fasting and fed states. Both treatments have comparable safety profiles. Conclusion: The bioequivalence and tolerability of ornidazole tablet reference and test formulations were evaluated among healthy Chinese participants under both fasting and fed conditions. The results indicated that both formulations were bioequivalent and generally well tolerated; besides, the interaction between food and drug may affect drug pharmacokinetics. Trial Registration: CTR20212873, registered on 15 November 2021; ChiCTR2300069098, registered on 7 March 2023. [ABSTRACT FROM AUTHOR]

The grinding of medical tablets is generally discouraged due to stability issues and various other issues. However, in specific scenarios directed by doctors, pharmacists may engage in grinding medical tablets, particularly to cater to pediatric or dysphagia patient populations as extra-label use. In the case of ground film-coated tablets, many film fragments arise in ground powder. Hence, the determination of the grinding endpoint for film-coated tablets is more challenging compared to uncoated tablets. The reports about grinding efficiency are limited because of the assumption that film-coated tablets are taken as tablets. The purpose of this report is to clarify how pharmaceutical excipients, particularly cellulose derivatives, utilized in film coating influence the grinding efficiency of film-coated tablets. Preliminary findings from the grinding of ten medical commercial tablets suggest that a higher concentration of hydroxypropyl methylcellulose (HPMC) correlated with increased difficulty in grinding film-coated tablets. Four film coating solutions with different HPMC-based components were used to coat model tablets prepared by the authors and their grindability was evaluated. The grinding of these film-coated tablets investigated those higher concentrations of HPMC resulted in increased tablet strength and larger residual film fragments. Moreover, the introduction of small quantities of additional plasticizer to the HPMC solution was found to decrease film strength, making the tablets more amenable to grind. It was shown that the components in the film coating solution affected the mechanical properties of the film and also the grinding characteristics of FC tablets. [ABSTRACT FROM AUTHOR]

Reducing the dimensions, when other additives are present, shows potential as a method to improve the dissolution and solubility of biopharmaceutical classification system class II drugs that have poor solubility. In this investigation, the process involved grinding naproxen with nicotinamide with the aim of improving solubility and the rate of dissolution. Naproxen was subjected to co-milling with urea, dimethylurea, and nicotinamide using a planetary ball mill for a duration of 90 min, maintaining a 1:1 molar ratio for the excipients (screening studies). The co-milled combinations, naproxen in its pure milled form, and a physical mixture were subjected to analysis using X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), and solubility assessment. The mixture displaying the highest solubility (naproxen-nicotinamide) was chosen for further investigation, involving testing for intrinsic dissolution rate (IDR) and Fourier-transform infrared spectroscopy (FTIR) after co-milling for both 90 and 480 min. The co-milled combination, denoted as S-3b and consisting of the most substantial ratio of nicotinamide to naproxen at 1:3, subjected to 480 min of milling, exhibited a remarkable 45-fold increase in solubility and a 9-fold increase in IDR. XRPD analysis of the co-milled samples demonstrated no amorphization, while SEM images portrayed the aggregates of naproxen with nicotinamide. FTIR outcomes negate the presence of any chemical interactions between the components. The co-milled sample exhibiting the highest solubility and IDR was used to create a tablet, which was then subjected to comprehensive evaluation for standard attributes. The results revealed improved compressibility and dissolution properties. [ABSTRACT FROM AUTHOR]

The misuse and abuse of opioid analgesics continue to pose a serious public health concern, but for some patients, opioids remain an important analgesic option. Extended-release (ER) opioid formulations are effective for treating chronic pain and are supported by multiple 12-week efficacy studies. ER opioids often contain a high opioid content, and similar to immediate-release (IR) formulations, are subject to abuse, misuse, and diversion. Unintentional misuse may also occur when ER formulations are manipulated for medicinal administration, such as crushing a dose for easier oral intake. As part of a multipronged strategy designed to fight the opioid epidemic, abuse-deterrent formulations (ADFs) were developed to deter misuse, abuse, and diversion of opioids by making manipulation more difficult and nonoral routes of administration less rewarding. Although ADF opioids have been shown to decrease rates of abuse and diversion, they are not equally effective in terms of deterring manipulation for abuse or misuse. Xtampza ER utilizes DETERx technology, which allows it to retain ER characteristics when chewed or crushed, making it the only ER opioid without a boxed warning against these types of manipulation. OxyContin was also developed as an ADF but uses RESISTEC technology, making the tablet hard to crush and viscous in aqueous solutions. ADF utilization has been hampered by patient access issues, including high prices due to lack of insurance coverage. Postmarket real-world studies demonstrate lower rates of abuse, misuse, and diversion for ADF ER opioids compared with non-ADF formulations. However, similar studies comparing abuse-related effectiveness and health care costs for ADF opioids are warranted if clinicians are expected to utilize these potentially safer opioid formulations. These studies would support further education surrounding the benefits and utilization of ADFs and manipulation potential of different ADFs. [ABSTRACT FROM AUTHOR]

Corn, wheat, rice, potato, and cassava starches have been widely used as pharmaceutical excipients. However, the search for cost‐effective local starch alternatives is necessary due to the availability and usage constraints. In Ethiopia, various plant species, including Taro Boloso‐I, have been explored as potential sources of pharmaceutical starch. It is a variety of Colocasia esculenta with a high tuber yield and high starch content. However, the native starch requires modifications to enhance its functionality. Therefore, this study aimed to improve the native starch through acid modification and evaluate its performance as a direct compressible tablet excipient. The native starch was treated with a 6% w/v HCl solution for 192 hours, resulting in acid‐modified Taro Boloso‐I starch, which was then evaluated for suitability for direct compression. XRD patterns of both the native and modified starch showed characteristic A‐type crystals, with significantly higher relative crystallinity observed in the latter. Additionally, the acid‐modified starch exhibited a lower moisture content and improved flow properties. The compaction study also demonstrated its improved compactibility (tensile strength: 16.82 kg/cm2), surpassing both the native starch (13.17) and Starch 1500® (11.2). The modified starch also showed a lower lubricant sensitivity compared to the native starch and Starch 1500®. Furthermore, paracetamol tablets made with the modified starch exhibited higher mechanical strength and lower friability in all paracetamol concentrations. It incorporated up to 40% paracetamol while maintaining acceptable tablet characteristics, whereas the native starch and Starch 1500® were limited to 30% (w/w). Based on these findings, the modified starch showed promise as an alternative direct compressible excipient in tablet manufacturing. [ABSTRACT FROM AUTHOR]

This study aims to improve the biopharmaceutical, mechanical, and tableting properties of a poorly soluble drug, ibuprofen (IBP), by preparing amorphous solid dispersion (ASD) followed by a sustained-release tablet formulation. A suitable polymer to develop an ASD system was chosen by utilizing the apparent solubility of IBP in various polymer solutions. ASDs containing various ratios of IBP and selected polymer were prepared by the melt fusion (MF) method. ASD containing optimized drug-polymer ratio prepared by freeze-drying (FD) method was characterized and compared physicochemically. The solubility of IBP in water increased 28-fold and 35-fold when formulated as ASD by MF and FD, respectively. Precise formulations showed amorphization of IBP and increased surface area, improving solubility. The dissolution pattern of optimized ASD-IBP in pH 6.8 phosphate buffer after 60 min in MF and FD was enhanced 3-fold. In addition, direct compression tablets comprising optimized ASD granules from MF and FD were made and assessed using compendial and noncompendial methods. ASD-IBP/MF and ASD-IBP/FD formulations showed a similar drug release profile. In addition, 12 h of sustained IBP release from the ASD-IBP-containing tablets was obtained in a phosphate buffer with a pH of 6.8. From the dissolution kinetics analysis, the Weibull model fitted well. The drug release pattern indicated minimal variations between tablets formed using ASD-IBP prepared by both procedures; however, pre- and postcompression assessment parameters differed. From these findings, the application of ASD and sustained-release polymers in matrix formation might be beneficial in improving the solubility and absorption of poorly soluble drugs such as IBP. [ABSTRACT FROM AUTHOR]

There has recently been growing interest in exploring the potential of direct compression (DC) method of tableting as an alternative to the conventional granulation technique. This approach involves straightforward powder mixing and compression, resulting in time and cost savings, and has successfully been applied to various drugs. However, drugs require good micromeritic qualities, such as flowability, good reproducible compression behaviour to be directly compressed because it affects its in-vitro and in-vivo performance. Since many active pharmaceutical ingredients lack these qualities, the crystallo co-agglomeration technique hasemergedas a potential area of research for particle design, utilised in the development of active ingredients best suited for direct compression of tablet dosage forms. Pure metronidazole exhibited significantly higher Carr's index, Hausner's ratio, and angle of repose of 41.93°±1.05, indicating cohesiveness and irregular shape of the crystals. Whereas the crystallo-co-agglomerates were found to have an angle of repose of 29.33°±0.96, denoting an improvement in the flowability of the agglomerated crystals. Improvements in mechanical handling parameters was revealed in metronidazole co-agglomerate tablets produced with DC excipients (F1, F2). These tablets were found to be more robust and of higher quality compared to those formulated using pure metronidazole (F4, F5, F6), which were of no significant difference with metronidazole formulated via wet granulation method (F7, F8, F10, F11). In-vitro dissolution studies of metronidazole co-agglomerates tablets showed no significant difference in the percentage drug release profilebetween tablets produced via direct compression and wet granulation method. Thus, the crystallo co-agglomeration technique can be effectively used in the formulation of metronidazole tablets by direct compression using Avicel® and Prosolv®, presenting an efficient and streamlined approach to tablet manufacturing. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the usage of solid dispersion (SD) to enhance the dissolution rate of the poorly soluble drug piroxicam for sublingual formulation. Poloxamer grade 407 (Kolliphor® P-407), a commercially available polymer, was chosen, and various solid dispersions with different weight ratios of piroxicam and Poloxamer were prepared using the hot melt method. Compatibility tests using FTIR spectroscopy, DSC, and XRD were conducted to assess any chemical or physical interactions between the drug and polymer. In vitro dissolution tests were performed on the solid dispersions. The results of the FTIR spectroscopy study indicated no chemical interaction between the drug and the polymer. Similarly, the DSC and XRD analyses showed no physical interaction between the drug and the polymer. The maximum cumulative percentage release of the pure drug and the solid dispersion at 15 minutes were 40.90±1.83% and 99.56±3.25%, respectively. Based on these findings, it was concluded that the solid dispersion with a ratio of 2:1 (Drug: Poloxamer-407) showed a noteworthy upsurge in the dissolution rate in comparison to the pure drug. [ABSTRACT FROM AUTHOR]

The aim. To investigate the polymorphic structure of the API-dapagliflozin propanediol monohydrate and to reveal the absence of an effect of the tabletting process on the polymorphic structure of the API in model compositions of tablets. Materials and methods. Model mixtures of API-dapagliflozin propanediol monohydrate and excipients were studied. The research used the method of designing pharmaco-technological parameters of solid dosage forms, the method of quantum-chemical modelling of the mechanical properties of polymorphic modifications of APIs, the modelling of shear deformation, the nanoindentation method, the Rietveld method for calculating X-ray patterns, X-ray structural analysis of API and selected model compositions of tablets. Results. The polymorphic structure of API-dapagliflozin propanediol monohydrate and its polymorphic structure in selected model compositions of tablets produced by the pressing method were studied and analyzed. An X-ray structural study was carried out, and the qualitative and phase composition of samples and polymorphic modifications of API and model series of tablets were determined. According to the results of the X-ray structural analysis, it was established that there is no polymorphic transition and that the polymorphic structure of API is invariant under the influence of pressing pressure, which ensures the quality of the tablet form. Conclusions. The design of an experimental study was determined based on the application of the QbD concept, design of experiments -- DoE, for designing and ensuring a high-quality technological process -- tabletting of API-dapagliflozin propanediol monohydrate and excipients. To manage a critical technological parameter -- the stability of the polymorphic structure of the API, which guarantees the quality of the tablet form, its bioavailability and bioequivalence, it is necessary to use a set of methods for studying structural changes and polymorphic modifications of the API during the tableting process. According to the results of the X-ray structural study of API and selected model compositions of tablets, it was established that during the process of tabletting under pressure, the structure of the polymorphic modification of dapagliflozin propanediol monohydrate does not change, and no polymorphic transition is observed [ABSTRACT FROM AUTHOR]