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By using five different sieve sizes of ascorbic acid granules, affects of granule sizes on tablet properties, i.e. tablet weight and hardness have been studied with standard methods. Affects of lubricant types and concentrations on tablet properties, i.e. tablet hardness and disintegration time have also been studied by using magnesium stearate and...
Contexts in source publication
Context 1
... hardness (in SCU) for tablets produced with different sizes of granules, determined by using a hardness tester (Pharma Test, Germany; TIPT ID # TE0901), are presented in Table 3. ...
Context 2
... lot of mesh (x -bar . ) and lot 4 of mesh 1 (x -bar = 8.6) [ Table 3]. ot 5 (mesh ) and lot 1 (mesh 14) show the lowest (x -bar 5. ) and the second lowest (x -bar = 6.6) hardness (Table 3). ...
Context 3
... and lot 4 of mesh 1 (x -bar = 8.6) [ Table 3]. ot 5 (mesh ) and lot 1 (mesh 14) show the lowest (x -bar 5. ) and the second lowest (x -bar = 6.6) hardness (Table 3). Therefore, medium size granules, such as mesh 18, 30 and 40, are better to use for producing tablets within the specificity. ...
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Oral Disintegrating Tablets (ODTs) is a novel dosage form that can be dissolved on the tongue within 3min or less especially for geriatric and pediatric patients. Current ODT formulation studies usually rely on the personal experience of pharmaceutical experts and trial-and-error in the laboratory, which is inefficient and time-consuming. The aim o...
Citations
... A tablet may not disintegrate in the required amount of time if it is too hard, and if it is too soft, it may not resist handling. It has been observed that several factors may influence a tablet's hardness, including drug concentration, particle size and density, binder type, lubricant type and concentration, compression force, etc. [26][27][28] . The acceptable range of the hardness of an oral tablet is usually 4-8 kgf [25] . ...
Hydroxychloroquine is the most commonly prescribed antimalarial extensively used to treat rheumatoid arthritis. It is extensively utilized as a repurposing drug, as well, in many countries worldwide to treat COVID-19. The pharmaceutical sector of Bangladesh is much enriched, and different pharmaceutical companies in Bangladesh produce this drug. Since the drug quality might vary significantly among different brands, assuring the quality PMMB 2023, 6, 1; a0000336 2 of 11 of medicine is absolutely necessary considering the health issues, particularly therapeutic efficacy and safety. Therefore, this study examined the quality of hydroxychloroquine produced by Bangladeshi pharmaceutical companies, concentrating on quality control parameters: the assay, dissolution, disintegration, hardness, friability, and weight fluctuation. All the brands of hydroxychloroquine tablets contained the stated amount of API between the range of 96.41±0.62 and 100.61±0.71 that met USP specification (100±5%). All brands met the pharmacopeial limit for the percentage of weight fluctuation, hardness test, friability, and disintegration time. Weight variation was between 0.31±0.01% and 0.46±0.02%, hardness was between 4.31 ± 0.88 and 7.36 ± 0.74 kgf, friability was less than 1%, and disintegration time was 5.42± 0.11 and 5.42± 0.11 min. In the dissolution test, all the samples attained more than 70% dissolution after 30 minutes. The mean percentage of hydroxychloroquine released in phosphate buffer was between 95.44±0.55 (Brand B) and 98.19±0.39 (Brand C) after 60 min. No significant difference was among the tested drugs from different companies, and all quality assessment parameters were within USP specifications. Therefore, hydroxychloroquine from the Bangladesh market is safe and effective.
... It is indicated that the presence of lignin in the formulation enhances the dissolution of the API, by creating pores and facilitating swelling in the lower compression forces whereas at high compression forces through the effect of surface erosion [38]. The higher forces see a slower effect of the disintegrant due to high plastic deformation, intense reduction of the effective porosity and reduction in the equilibrium concentration of the API by reducing the surface area and surface energy for dissolution [35,36,38]. ...
... It is indicated that the presence of lignin in the formulation enhances the dissolution of the API, by creating pores and facilitating swelling in the lower compression forces whereas at high compression forces through the effect of surface erosion [38]. The higher forces see a slower effect of the disintegrant due to high plastic deformation, intense reduction of the effective porosity and reduction in the equilibrium concentration of the API by reducing the surface area and surface energy for dissolution [35,36,38]. Other authors have worked with the process of roll compaction and milling process and have reported that an increase of compression force has a significant decrease in the release of API [36,39] whereas using lignin as an excipient in the formulation enhances the release rates in the in vitro dissolution [35,40]. ...
AS (Aquasolv) Lignin produced via Liquid Hot Water Pretreatment and Enzymatic Hydrolysis has shown potential as an active pharmaceutical ingredient and/or excipient in solid dosage forms. Moreover, lignin is safe to consume and presents antioxidant and antidiabetic capacity, properties that can add to solid dosage forms in pharmaceuticals. This work aimed to evaluate the performance of tablets produced via direct compression and wet granulation when lignin is used in combination with commercial excipients. In order to find optimal tablet performance, different lignin formulations were assessed, and the concentrations were given by extreme vertices mixture design (13 formulations). The blends were composed of AS Lignin, Microcrystalline Cellulose, and Lactose monohydrate and the optimized blend was found to be 14.53 w/w% of disintegrant, 26.57 w/w% of binder and 58.9 w/w% of AS lignin. This proportion was further used to evaluate the performance of lignin-based tablets in drug release, using Ibuprofen as a drug model (50 w/w% and 70 w/w%) and for comparison of direct compression with wet granulation. Direct compressed tablets resulted in higher drug dissolution rates when compared with wet granulation, nevertheless; both tableting techniques showed promising results for lignin. More than 5 formulations tested in this work are compliant with International Pharmacopoeia regulations for solid dosage pharmaceutical forms, thus AS Lignin shows potential to be used as an excipient in pharmaceutical formulations.
Industrial relevance
Industrially, AS Lignin appears as promising excipient in the pharmaceutical technologies as well as boost in the biorefining technologies in the following years. Lignin produced is free of sulfur, can be labelled as clean and environmentally-friendly and in this study, was proven this non-cytotoxic AS lignin can be used for excipients and drug carriers. The findings in this paper showed the use of product formulation for life science purposes, thus stressing one of possibilities for lignin valorization in biorefineries.
... In addition, the intrinsic dissolution rate may have a greater correlation with the in vivo dissolution kinetics than the solubility test [22]. The size of the granules and the strength of the granules can affect fluidity, content uniformity, and solubility [32][33][34]. Granule fluidity parameters such as Carr's index and the angle of repose are related to the assay, content uniformity, and dissolution. The density of the granules can affect compressibility [35]. ...
... Based on the results of the contact angle, an ANOVA was conducted to identify the individual influence of control factors (CPPs) on response factors (IQAs and CQAs). The individual influence of control factors is described by the reduced 2FI (factor of interaction) mathematical model, which is presented in equation (34). ...
... The R 2 value of the response factors (q 27 ) was 0.9580 which indicates that the control factors had a significant effect on the response factors. According to Equation (34), the impeller speed and massing time decrease the contact angle. If the massing time and impeller speed increase, the granule size may increase because granule coalescence and growth may occur [24,41,42,49]. ...
In this study, we developed a control strategy for a drug product prepared by high-shear wet granulation and roller compaction using integrated quality by design (QbD). During the first and second stages, we optimized the process parameters through the design of experiments and identified the intermediate quality attributes (IQAs) and critical quality attributes (CQAs) relationship, respectively. In the first stage, we conducted an initial risk assessment by selecting critical process parameters with high impact on IQAs and CQAs and confirmed the correlation between control and response factors. Additionally, we performed Monte Carlo simulations by optimizing the process parameters to deriving and building a robust design space. In the second stage, we identified the IQAs and CQAs relationship for the control strategy, using multivariate analysis (MVA). Based on MVA, in the metformin layer, dissolution at 1 h was significantly correlated with intrinsic dissolution rate and granule size, and dissolution at 3 h was significantly correlated with bulk density and granule size. In dapagliflozin layer, dissolution at 10 min and 15 min was significantly correlated with granule size. Our results suggest that the desired drug quality may result through IQAs monitoring during the process and that the integrated QbD approach utilizing MVA can be used to develop a control strategy for producing high-quality drug products.
... When a tablet is too hard, it may not disintegrate in the required time, and when it is too soft, it will not withstand handling. Several factors have been found to affect the hardness of tablets; these include lubricant type and concentration, particle size and density, tableting speed, compression force, storage conditions, binder type, and drug concentration (29)(30)(31)(33)(34)(35)(36)(37)(38). An increase in binder concentration increases the mechanical strength of tablets. ...
... Hardness increases with the increase in compression force, while friability decreases. 13 In many cases, an exponential relationship exists between disintegration time and compression pressure. The disintegration time increases with the increase in pressure. ...
Tablets are a complex drug delivery system consisting of the active pharmaceutical ingredients and excipi-ents. Tablet production involves a series of unit operations in which drugs and excipients are subjected to mechanical stresses, such as compression pressure, thus imposing changes in the properties of these materials. Variations in the compression pressure and other processing parameters may affect the mechanical strength and release properties of the final tablet. It is generally expected that an increase in compression pressure should lead to an increase in mechanical strength and a decrease in release properties of tablets, but this may not be true in some practical situation, since tablet production is the result of complex interaction between many factors involving the drug, excipient, the formulation, and processing variables. The degree and extent of interaction of these variables are not absolutely dependent on one factor. The aim of this review is to study the interaction between compression pressure, mechanical strength and release properties of immediate and controlled release tablets. The effect of compression pressure on tablets is complemented by such factors as the material properties of the drug and excipient, the formulation and processing factors, which in turn affects mechanical strength and release properties.
... It is therefore explicable that when applied in carefully regulated amounts, they could develop the lubricating efficiency of lubricants in general use [9]. They have been studied for their effect on the characteristics of granules and tablets such as moisture content, tablet hardness, disintegration and dissolution, and the stability of active ingredients [10] showed that unlike magnesium stearate, which delays disintegration and dissolution of the active ingredient, the fatty acid esters promotes a reduction in disintegration time. Fatty acid esters have better-quality as lubricant than magnesium stearate because the tablets containing them have better stability. ...
Purpose
Optimal particle size distribution (PSD) is an important factor in wet granulation in order to achieve appropriate powder flow, compactibility, and content uniformity. Parameters like D50 and surface area (SA) are used to define PSD but both are only able to compare separate fractions of a granulate. In this work, we made an attempt to characterize PSD of a final dry granulate blend and suggest novel parameters (determination coefficient R² and trend line slope of a PSD model) to quantitatively describe PSD.
Method
The significance of these parameters was tested using machine learning. Laboratory-scale samples were used for training and commercial-scale samples for testing a model. Several machine learning techniques were used to further examine the importance of these input variables using a large data set from wet granulation scale-up study.
Results
The Gradient Boosted Regression Trees (GBRT) algorithm had the lowest root mean square error (RMSE) values for the several responses studied (tablet tensile strength, tablet diameter and thickness, compaction work, decompaction work, and net work). The GBRT model for tablet tensile strength had an R² model value of 0.87 and was not overfitted. The importance of input variables R² and a was proven by the stepwise regression model’s p value (0.0003) and GBRT importance score (0.37 and 0.44, respectively). The GBRT model was the most successful in predicting decompaction work (R² model = 0.97) with the least regularization effect.
Conclusion
The proposed parameters can be used in PSD characterization and applied in critical quality attributes (CQA) prediction and wet granulation scale-up.
Magnesium stearate is the salt of a complex mixture of fatty acids, with the majority being stearate and palmitate. It has multiple crystalline forms and, potentially, an amorphous form. Magnesium stearate is used in the pharmaceutical manufacturing industry as a powder lubricant, and typically is added at low levels (∼1%) during the manufacturing process and blended for a relatively short time (∼5 min). Proper levels and mixing times are needed, as too short a mixing time or too small a quantity will result in improper lubrication, and too much can negatively impact dissolution rates. The complex mixture of multiple fatty acids and crystalline forms in magnesium stearate leads to variability between commercial sources, and switching between sources can impact both the amount of lubricant and mixing time needed for proper lubrication. In order to better understand the complex nature of magnesium stearate, a variety of analytical techniques were used to characterize both synthesized and commercial magnesium stearate samples. The results show that correlation among differential scanning calorimetry, thermogravimetric analysis, solid-state NMR spectroscopy, and other techniques provides a unique insight into the forms of magnesium stearate. Finally, the ability to monitor form changes of magnesium stearate in an intact tablet using solid-state NMR spectroscopy is shown.
