Disintegration Time Of Tablets Research Articles

Development of Oral Tablets of Nebivolol with Improved Dissolution Properties, Based on Its Combinations with Cyclodextrins.

New oral tablets of nebivolol have been developed aiming to improve, by cyclodextrin (CD) complexation, its low solubility/dissolution properties-the main reason behind its poor/variable oral bioavailability. Phase-solubility studies, performed using βCD and highly-soluble βCD-derivatives, indicated sulfobutylether-βCD (SBEβCD) as the best solubilizing/complexing agent. Solid drug-SBEβCD systems were prepared by different methods and characterized for solid-state and dissolution properties. The coevaporated product was chosen for tablet development since it provided the highest dissolution rate (100% increase in dissolved drug at 10 min) and almost complete drug amorphization/complexation. The developed tablets reached the goal, allowing us to achieve 100% dissolved drug at 60 min, compared to 66% and 64% obtained, respectively, with a reference tablet without CD and a commercial tablet. However, the percentage dissolved after 10 min from such tablets was only 10% higher than the reference. This was ascribed to the potential binding/compacting abilities of SBEβCD, reflected in the greater hardness and longer disintegration times of the new tablets than the reference (7.64 vs. 1.06 min). A capsule formulation with the same composition of nebivolol-SBEβCD tablets showed about a 90% increase in dissolved drug after 5 min compared to the reference tablet, and reached 100% dissolved drug after only 20 min.

The Formulation And Evaluation Of Metamizole Na Tablet With Porang Tubers(Amorphophallus Oncophyllus) Flour As A Binder

Many farmers are interested in planting porang tubers, and with many farmers planting porang tubers, the price of porang tubers has decreased at harvest time. Porang tubers contain several ingredients: starch, Glucomannan, fibre, fat, protein, minerals and vitamins. Glucomannan content can be used as a tablet binder, thickener, gelling agent, film former, coating material emulsifier, and stabilizer. This study used the wet granulation method to determine the concentration of porang tuber flour as a binder in Metamizole Na tablets. Tablets were made into three formulations with varying concentrations of porang tuber flour, namely FI 5%, FII 7.5% and FIII 10%. Tablets were tested for tablet uniformity, hardness, friability, disintegration time, and dissolution. The data obtained were analyzed using Kruskal Wallis. The analysis showed that variations in the concentration of porang tuber flour had a different effect, based on the Kruskal Wallis analysis, which showed a significant value of 0.10 (p>0.05). The formulation with a good physical quality test is formulation III, with a tablet hardness value of 6.84 kg and a disintegration time of 5.74 minutes, almost close to the control (+) 14.27 kg and 6.38 minutes. The higher the concentration of porang tuber flour, the higher the tablet hardness and the longer the disintegration and dissolution time.

Formulation and evaluation of nifedipine fast dissolving tablets

The current study aims to formulate and evaluate the fast-dissolving tablet. The optimal concentration of Guar gum super disintegrate was found to be 20 mg, with a disintegration time of 27 seconds. This study assessed the disintegration time of tablets containing natural super disintegrant for the Disintegration test at various weight concentrations (6,8,10,12,14,16,18, and 20 mg). As a result, the Nifedipine fast dissolving tablets with Guar gum super disintegrant provide a quick therapeutic effect, a high dissolve rate, and a shorter disintegration time. In this study, the use of a natural (guar gum) super disintegrating agent increases the rate of dissolution as well as length of disintegration of fast-dissolving tablets. In vitro drug release of 96% is demonstrated in 6 minutes with a disintegrating efficiency of 27 seconds for Nifedipine FDTs (guar gum). Consequently, our study has shown that formulations made with a natural super disintegrating agent exhibit shorter disintegration times as well as higher rates of dissolution along with drug release.

Effects of Beverage Solvents on Disintegration Time and Dissolution Rate of Metronidazole Tablets

Drug Disintegration time refers to the period within which a mechanical break-up of compressed tablet dissolve upon exposure to physiological fluids within a short period of time into tiny granules upon ingestion, while drug dissolution rate becomes a key tool in understanding the importance for its bioavailability and therapeutic effectiveness. Hence, the objective of this paper was to assess the impact of seven different solvents, which includes five non-alcoholic beverages (Exotic juice, soft drink, coffee, milk, and milo), one alcoholic beverage (beer), one dilute acid (0.1 M HCl) and a control distilled water (dil. H2O) on the disintegration time and dissolution rate of metronidazole tablets. The distilled water was used as control. The results obtained show that the mean disintegration times were 2.28 ± 0.04 (0.1 N HCl), 4.21 ± 0.12 (beer), 3.24 ± 0.05 (coffee), 3.23 ± 0.07 (distilled water), 5.21 ± 0.09 (Exotic juice), 3.17 ± 0.06 (Fanta), and 16.16 ± 0.11 (milk). The mean dissolution rates on the other hand were 98.87 ± 0.12, 78.09 ± 0.09, 84.27 ± 0.11, 86.52 ± 0.40, 67.98 ± 0.09, 92.70 ± 0.50, and 44.94 ± 0.22 respectively. Metronidazole tablets disintegrated and dissolved more in 0.1 N HCL than in other mediums and less in milk. From this study, although the disintegration time and dissolution rate of metronidazole were not greatly affected by the different beverages except for Exotic juice, and the mixture of milk and Milo, care should be taken when replacing water with any beverage in ingesting tablets.

A prediction model based on artificial intelligence techniques for disintegration time and hardness of fast disintegrating tablets in pre-formulation tests

BackgroundThe pharmaceutical industry is continually striving to innovate drug development and formulation processes. Orally disintegrating tablets (ODTs) have gained popularity due to their quick release and patient-friendly characteristics. The choice of excipients in tablet formulations plays a critical role in ensuring product quality, highlighting its importance in tablet creation. The traditional trial-and-error approach to this process is both expensive and time-intensive. To tackle these obstacles, we introduce a fresh approach leveraging machine learning and deep learning methods to automate and enhance pre-formulation drug design.MethodsWe collected a comprehensive dataset of 1983 formulations, including excipient names, quantities, active ingredient details, and various physicochemical attributes. Our study focused on predicting two critical control test parameters: tablet disintegration time and hardness. We compared a range of models like deep learning, artificial neural networks, support vector machines, decision trees, multiple linear regression, and random forests.ResultsA 12-layer deep neural network, as a form of deep learning, surpassed alternative techniques by achieving 73% accuracy for disintegration time and 99% for tablet hardness. This success underscores its efficacy in predicting complex pharmaceutical factors. Such an approach streamlines the drug formulation process, reducing iterations and material consumption.ConclusionsOur findings highlight the deep learning potential in pharmaceutical formulations, particularly for tablet hardness prediction. Future work should focus on enlarging the dataset to improve model effectiveness and extend its application in pharmaceutical product development and assessment.

Utilization and Evaluation of Rice Bran and Rice Bran Wax as a Tablet Lubricant.

The rice bran and rice bran wax of the KJ CMU107 rice strain were investigated as potential tablet lubricants in a directly compressed tablet formulation. Stabilized full-fatted rice bran (sFFRB), stabilized defatted rice bran (sDFRB), and rice bran wax (RBW) extracted and purified from crude rice bran oil (cRBO) were tested. Two commercial lubricants, including magnesium stearate (MGS) and hydrogenated cottonseed oil (HVO), were employed as the standards in the formulated mixtures, which contained spray-dried rice starch (SDRS) as a diluent. The tableting was carried out for each formulation, and the obtained tablets were physically and mechanically evaluated. Among the parameters investigated were the general appearance, ejection force, weight variation, hardness, friability, and disintegration time. The powder flow was also determined for each formulation. The results showed that the tablet ejection forces for all the lubricated formulations (58-259 N) were significantly lower than that of the non-lubricated control formulation (349 N). The use of sFFRB as a lubricant at 0.5-2.0% w/w could lower the ejection force up to 78%, but the hardness reduced so drastically that the formulations failed the friability test due to the chipping of the tablets' edges. Moreover, sDFRB performed significantly better as the use at 0.5-1.0% w/w in the formulation helped to lower the ejection forces by up to 80% while maintaining the changes in the tablet hardness within 10%. RBW functioned effectively as a tablet lubricant at a concentration of 0.5% w/w, yielding tablets with good strength comparable to standard HVO lubricant while helping to reduce the ejection force by 82%. In formulations with good lubrication, i.e., friability < 1%, the powder flow was improved, and the tablet disintegration times were within the same range as the control and HVO formulations. In conclusion, sDFRB displayed a lubricant property at concentrations between 0.5 and 1.0% w/w, with slightly negative effects on the tablet hardness. RBW from KJ CMU107 rice was an effective tablet lubricant at 0.5% w/w, with no effect on tablet hardness. Both materials can be further developed for use as commercial lubricants in direct compression.

Xanthan Gum-based Food Thickeners Reduce Disintegration Time of Medical and OTC Loxoprofen Sodium Tablets

Xanthan gum-based food thickeners have been reported to potentially interfere with tablet disintegration. Loxoprofen sodium (LOX) is widely used as an antipyretic analgesic and is expected to provide rapid pain relief. In this study, we aimed to investigate the impact of a xanthan gum-based food thickener on LOX tablet disintegration. We used four different brands each of medical and OTC-LOX tablets, each containing 60 mg of LOX as the sole active ingredient. Depending on the brand, tablet hardness varied between 50.1-96.6 N and was not associated with the disintegration time. Disintegration times for medical tablets not immersed in the food thickener were 536±215, 621±159, 348±22, 369±42 s and for OTC tablets, were 358±20, 336±13, 292±13, 172±27 s. Immersion in the food thickener for 15 min reduced medical tablet disintegration time to 177±46 and 233±150 s (the third and fourth brands were disintegrated during immersion), and that for OTC tablets to 77±40, 75±110, and 37±85 s (the fourth brand was disintegrated during immersion). Despite each tablet containing different pharmaceutical additives, no correlation was found between disintegration time and presence of superdisintegrants. The OTC tablet with a light anhydrous silicic acid coating exhibited the shortest disintegration time. Thus, the disintegration time of LOX tablets is accelerated when immersed in the xanthan gum-based food thickener, potentially leading to rapid pain relief for patients.

The Effect of PEG 4000 in Co-processed Excipient using Melt Granulation Method on the Physical Characteristics of Chitosan Tablets in Mangrove Crab Shells (Scylla serrata)

Mangrove Crab (Scylla serrata) is an animal that likes to be consumed but its shell waste is underutilized. The shell contains chitosan which has many benefits, one of which can lower cholesterol levels. The combination of 2 or more excipients is called co-processed excipients which are then continued into tablets by direct compression. The aim of the study was to find out whether chitosan could be formalized into coprocessed tablets (lactose, primogel, and PEG 4000 7.5% &amp; 15%) by direct compression method and the effect of differences in the characteristics of coprocessed and chitosan tablets with a ratio of PEG 4000 7.5% and 15 % as binder. The evaluation results showed that chitosan tablets fulfilled the requirements for the uniformity of weight, hardness, disintegration time (F1) tests, while they did not meet the requirements for the uniformity of tablet size, friability and disintegration times (F2) tests and the results of the coprocessing evaluation met specifications both F1 and F2, namely: particle size distribution, moisture content, flow rate, angle of repose (very good), compressibility index (adequate) and Hausner's ratio (very good). The evaluation results were then processed statistically using the SPSS application using the independent t-test method which showed that there was no significant difference in the effect of PEG 4000 7.5% and 15% as a binder on the characteristics of co-processed and chitosan tablets. Chitosan tablets from mangrove crab shells (Scylla serrata) cannot be formalized by direct compression with co-processing.

Curcumin- β-Cyclodextrin Molecular Inclusion Complex: A Water- Soluble Complex in Fast-dissolving Tablets for the Treatment of Neurodegenerative Disorders.

Orally disintegrating tablets (ODTs) have become an excellent choice for delivering drugs as their palatability is greatly improved. In this work, β-cyclodextrin has been used to improve the solubility of curcumin by encapsulating it into the hydrophobic cavity for the treatment of neurodegenerative disorders. The current study aimed to present the design, formulation, and optimisation of fastdissolving oral tablets of curcumin- β-cyclodextrin molecular inclusion complex using a 32-factorial design with sodium starch glycolate (SSG) and Neusilin® ULF2 as independent factors. The drug-excipient compatibility was studied by FTIR spectroscopy. The inclusion complex of curcumin-β-cyclodextrin was prepared using solvent casting and confirmed using XRD studies. Powder blends were evaluated for flow properties. Tablets prepared by direct compression were evaluated for post-compression parameters. Further, the effect of formulation variables, such as sodium starch glycolate (X1) and Neusilin® ULF2 (X2), on various responses, including disintegration time and dissolution at 2 hours, was studied using statistical models. Post-compression parameters, i.e., hardness (4.4-5 kg/cm2), thickness (3.82-3.93 mm), weight variation (±7.5%), friability (<1%), wetting time (51-85 seconds) and drug content (96.28- 99.32%) were all found to be within the permissible limits and the disintegration time of tablets with super-disintegrants ranged between 45-58 seconds. The in-vitro dissolution profile of tablets showed that higher SSG and Neuslin® ULF2 levels promoted drug release. For statistical analysis, the 2FI model was chosen. Optimised variables for formulation have been determined and validated with the experimental findings based on the significant desirability factor. The current study reveals the validated curcumin-β-cyclodextrin inclusion Complex fast-dissolving tablets with SSG and Neusilin® ULF2 to be an ideal choice for effectively treating neurodegenerative disorders.

Effect of Thickened Beverage and Swallowing Aid Jelly Used for Dysphagic Patients on the Disintegration of Orally Administered Tablets.

Thickened beverages or swallowing aid jelly (SAJ), commonly used as tablet-swallowing aids for dysphagic patients, may influence the disintegration of orally administered tablets. With this in mind, we evaluated the disintegration times of therapeutic tablets immersed in thickened beverages or SAJ compared to immersion in ones without them. Thickened beverages and SAJs were prepared with various beverages (water, orange juice, and milk) using food thickeners and SAJ powders marketed in Korea. The tablet disintegration times were the same in thickened beverages and SAJs, and there was no statistically significant difference associated with the thickness levels of the thickened beverages. The disintegration times of Tylenol immersed in orange juice or milk were slightly higher compared to those immersed in water. Moreover, there was no difference in disintegration time when using the thickened beverages and SAJs. The disintegration times of Aspirin were similar in all of the thickened beverages or SAJs, and there were no differences between non-immersed and immersed tablets. These results demonstrate that the disintegration of Tylenol and Aspirin is not greatly affected by immersion in any of the thickened beverages and SAJs.

Statistical Optimization of Fast Dissolving Tablet Contains Isosorbide Dinitrate for the Treatment of Angina Pectoris

ABSTRACT: The ultimate objective about this experiment was to create a fast-dissolving tablet Isosorbide dinitrate that released its medication quickly. The physical properties of tablets, such as hardness, angle of repose, weight variation, and friability were assessed. In-vitro release was investigated, and a 22-factorial design was created. The results show that the in-vitro release shows that the F2 formulation has the highest release at 20 min. Tablet disintegration time ranges from 31 to 48 s. The hardness ranges from 6-7 kg/cm3. The friability test shows the range from 0.49-0.68%. The weight variation test shows that all the formulation passes the tests. ANOVA statistical analysis revealed that the generated formulations are statistically significant. It is concluded that FDT formulations have optimum and reproducible disintegration time and increased dissolve characteristics, resulting in higher patient compliance.

Formulation and Drug Release Study of Rivaroxaban Oral Disintegrating Tablets Using Various Super-Disintegrants

This study aims to improve Rivaroxaban's solubility, dissolution, and bioavailability. Orally disintegrating tablets (ODTs) made with super-disintegrants like crospovidone, sodium starch glycolate, and cross-carmellose sodium will do this. Tablet preparation used direct compression and formulation optimization with design expert software. After a thorough factorial design and evaluation of pre- and post-compression parameters, the F3 batch, which contained Rivaroxaban (7.97%), Crospovidone (3.59%), Croscarmellose sodium (5.18%), Sodium Starch Glycolate (5.18%), Lactose Anhydrous (31.08%), Mannitol (15.94%), MCC (27.89%), SSF (1.59%), and Talc (1.59%), was the best. The enhanced tablet formulation (F3) showed positive qualities, including 3.3 kg/cm² hardness, 23 seconds disintegration time, and 99% drug release after 30 minutes. The innovative Rivaroxaban orally disintegrating tablet (ODT) method disintegrated and dissolved faster than market forms. Rivaroxaban's physical and chemical properties were assessed before formulation. The medication was colorless, scentless, crystalline, and melted at 227°C-229°C, as described in published research. The pharmaceutical was found to be a BCS Class II drug with low water solubility and high solubility in acetate buffer pH 4.5 and 0.1 N Hydrochloric acid. Fourier-transform infrared spectroscopy (FTIR) confirmed no drug-polymer-excipient interactions. Every batch of tablets exhibited uniform thickness (3.5 mm to 3.8 mm) and diameter (10.31 mm to 10.36 mm), indicating good compression without adhering to shaping tools. All samples had a 3-5 kg cm-² hardness, indicating strong mechanical properties. The Roche friability method showed that all batches had good abrasion resistance, ranging from 0.1% to 0.5%. Variations in croscarmellose sodium and crospovidone on tablet disintegration time and hardness were examined using design expert software. The ANOVA showed important factors affecting these attributes. Data-driven polynomial equations predict tablet disintegration time and hardness. These models reveal formulation parameters that affect tablet performance. Thus, the improved F3 batch of rivaroxaban orally disintegrating tablets (ODTs) improves solubility, dissolving, and bioavailability. This may improve treatment outcomes.

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 &lt;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 &lt; 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&gt; 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.

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 (&lt;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.

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 &amp; Söhne (JRS), Germany), Starch pregelatinized (Colorcon LTD., England), Kollidone SR (BASF, Germany), Croscarmellose sodium (J. Rettenmaier &amp; 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 &amp; Söhne (JRS), Germany), Calcium stearate (FACI, Italy), Film coating VIVACOAT® PA-1P-000 (J. Rettenmaier &amp; 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.

Differences In Destruction Time and Determination of Generic and Trademark Paracetamol Tablets Using UV Spectrophotometry Method

Paracetamol is one of the most widely used antipyretic analgesic drugs in the community. Paracetamol in circulation, both generic and trademarked, is generally given in the form of tablets containing 500 mg of the active ingredient. At this time people prefer to use trademarked paracetamol tablets with the assumption that trademarked drugs are more efficacious than generic drugs. This study aims to determine the difference in disintegration time and content of generic paracetamol tablets with trademarks. The study was conducted on 2 samples of generic paracetamol tablets with 2 samples of paracetamol tablets of different brands. The results of the disintegration time test showed that the average of generic A paracetamol tablets was 8.41 minutes, generic B 1.2 minutes, trademark A 2.14 minutes, trademark B 1.2 minutes. While the results of the average level test obtained paracetamol tablets generic A 109.87% generic B 105.95% trademark A 103.28% trademark B 92.49% with categories according to the standards set in the literature. The results of the Paired Sample T-test on disintegration time obtained a value of 0.006 and the results on the level test of 1.00 so that it can be concluded that between generic and trademarked paracetamol tablets only have differences in disintegration time with the same concentration.

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.

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.