Excipient In Tablet Formulations Research Articles

Formulation and Evaluation of Paracetamol Tablet Using Konjac Glucomannan as Natural Halal Binder

Introduction: Discovery and development of novel halal excipients in tablet formulation have led to continuous interest in drug delivery research. In this study, Konjac Glucomannan, a polysaccharide derived from the tuber of Amorphophallus konjac, was used as a halal binder in the formulation of paracetamol tablets. Objective: This study aims to formulate and evaluate paracetamol tablets using konjac glucomannan as a halal binder. Methodology: Paracetamol tablets were formulated with different concentrations (5%, 10%, 15%, 20%) of KGM using the wet granulation method. The formulated paracetamol granules and tablets were subjected to different quality control tests. Results: All four formulation granules passed the pre-compression test, indicating good to passable powder flowability. The weight variation, hardness, thickness, and disintegration test results for all four formulations were within the USP limit except for the friability test. Only tablets with 20% KGM passed the test. Conclusion: 20% KGM shows good tablet binding properties compared to 5%, 10%, and 15% KGM. Hence, paracetamol tablets formulated with higher KGM as a binder produce paracetamol tablets with good physical and mechanical properties.

DEVELOPMENT OF MYCROCRYSTALLINE CELLULOSE ORIGINATE FROM SAGO (METROXYLON SAGU) STEM BARK BY HYDROLISIS METHODE USING NITRIC ACID

Objective: Microcrystalline cellulose (MCC) is an essential excipient in tablet formulation. Mostly MCC was obtained from wooden conifer stem fiber, therefore environment issues had been came up. Alternative sources for MCC which offer friendly conifer wood need to be explored. This study aimed to isolate and determine the characteristics of MCC originated from Sago (Metroxylon sago Rottb.) stem fibers as an promising alternative of MCC. Methods: MCC was prepared through pre-hydrolysis using an acetic acid solution, alkali heating using NaOH solution, and acid hydrolysis using nitric acid 0.3 N using three variations of heating temperature, namely 90, 95 and 100 °C. The characterization carried out were pharmaceutical grade, powder properties, FTIR analysis and powder morphology by SEM. Results: The yields obtained were 66.02; 65.53 and 65.08%, respectively. The characteristics of the MCC sample based on pharmaceutical grade quality were white to yellowish white powder, odorless, tasteless, insoluble in: ether, 96% alcohol, HCl 2N and NaOH 1N. The pH of the MCC suspension were 5.07-5.12, while moisture content were 3.67-4.17%, with loss on drying value as much as 0.37-0.4%, and ash content 1-2.17%. The value of permanganate number were 0.09-0.11, Hausner factor was between 1.05-1.25, and angle of repose were between 11.4-24.8°. Conclusion: Based on the results, it can be concluded that Sago is potent natural resource for MCC. The resulting MCC revealed physicochemical and characteristic of MCC, which almost similar to Avicel PH 102 as standard.

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.

Influences of different microcrystalline cellulose (MCC) grades on tablet quality and compression behavior of MCC-lactose binary mixtures

Microcrystalline cellulose (MCC) is one of the most commonly used excipients in tablet formulations. At present, numerous grades of MCC are available for pharmaceutical manufacturing and significantly differ in particulate and powder properties. The choice of MCC is important to the development of a tablet formulation with satisfactory quality. In this paper, five commercial grades of MCC from the same manufacturer were systematically evaluated by combination with lactose to investigate their influences on tablet quality. Furthermore, the key compression parameters obtained from empirical compression equations were used to analyze the compression behavior of the tablet formulations. When the proportion of MCC was up to ∼50%, PH 102, PH 102SCG, and PH 112 showed good and similar abilities in improving tablet tensile strength followed by PH 200, and PH 302 did the weakest. All the MCC successfully decreased the tablet friability and disintegration time values. The improvement effect of MCC on tablet disintegration followed the descending order: PH 200 > PH 102SCG > PH 302 > PH 102 > PH 112. Besides, the different effects of MCC grades on tablet quality could be weakened by lubricants when the mixtures mainly underwent plastic deformation during compression process. In conclusion, a clear understanding of the influences of commonly used grades of MCC on tablet quality is critical for future tablet formulation efforts.

Comparative Evaluation of the Disintegrant Properties of Starches from Three Cultivars of Dioscorea rotundata (Poir)

Poir starches from three cultivars (Lagos, Giwa, and Sule) were evaluated asexo-disintegrants (5 and 10%w/w) in paracetamol tablet formulations to determine whether the similarity in their physicochemical and material properties translates to performance in tablet formulation. The tablets were prepared by wet granulation and were evaluated for compressional properties (Heckel equation), mechanical strength (crushing strength and friability), and drug release (disintegration and dissolution times). Plastic deformation occurred in all tablets with rank order for the onset of plastic deformation Lagos>Giwa>Sule. An increase in the concentration of disintegrants in the tablets led to a decrease in mean yield pressure, total relative precompression density, and relative density at low pressure, but an increase in relative density at zero pressure. The crushing strength and disintegration times of the tablets were dependent on the disintegrants' concentration. All tablets passed the disintegration test (≤15min) with tablets containing the Sule cultivar producing the fastest disintegration (p<0.05). Tablets containing 10% of the Sule cultivar had the fastest release of paracetamol (t80=32.1min), though it failed the compendial standard for immediate release tablets (t80≤30min). Starches from the three cultivars despite their similar physicochemical and material properties exhibited different disintegrant properties and could find different applications as excipients in tablet formulations.

Tableting Performance of Maize and Potato Starches Used in Combination as Binder/Disintegrant in Metronidazole Tablet Formulation.

This study aimed to characterize the tableting performance of maize and potato starches, when used in combination either as a disintegrant or binder in solid dosage form development. Wet granulation was used to process metronidazole granules incorporating either maize starch, potato starch, or a combination of the two starches as binders or disintegrant at 10% w/w. Granule analysis was carried out on the various formulations and subsequently compressed into tablets weighing approximately 500 mg following the addition of extragranular excipients. Tablet properties were assessed after 24 h of storage. Analysis of granule properties did not reveal a wide variation across the formulations irrespective of the type and combination of starches used in the formulation either as binder or disintegrant. It was observed, however, that there were slight differences in particle size, bulk and tapped densities of granule formulations containing the combined starch as excipients compared to granule formulations containing individual starch as the excipient. Tablets prepared using the combined starches as binder had lower tensile strength and disintegration time compared to other formulations incorporating the individual starches as binders. However, when evaluated as disintegrant, the tablet formulation containing the combined starches produced tablets with relatively lower disintegration time compared to formulations containing the individual starches as disintegrant. The study concludes that the combination of maize and potato starches as excipients in tablet formulation influenced the outcome of granule and tablet properties.

STABILITY INDICATING HPTLC METHOD FOR ESTIMATION OF BUDESONIDE AND FORMOTEROL FUMARATE DIHYDRATE IN PHARMACEUTICAL FORMULATION

A sensitive, selective, precise and accurate stability-indicating high-performance thin layer chromatographic method for analysis of budesonide (BUD) and formoterol fumarate dihydrate (FFD) was developed along with forced degradation study and validated according to ICH guidelines. Densitometry analysis of BUD and FFD was carried out in the absorbance mode at 234 nm using toluene: methanol: ethyl acetate: ammonia (8:2:2.5:0.1,% V/V/V/V) as solvent system. This system was found to give compact spots for BUD at Rf value of 0.34 ± 0.06 and FFD at Rf value of 0.67± 0.05. It was found that besides oxidative, thermal and photo stability studies, acid and base induced degradation of drugs were more with resultant degradation product. 32 factorial design was used to predict base induced degradation. The drug undergoes degradation under mainly acidic and basic conditions. Also, the degraded products were well resolved from the pure drugs with significantly different Rf values. Linearity was found to be in the range of 1800-10600 and 1000-6000 ng band-1 for BUD and FFD, respectively. The LOQ for BUD and FFD were 392.48 ng band-1 and 1189.36 ng band-1 and LOD for BUD and FFD was115.79 ng band-1 and 350.88 ng band-1, respectively. ‘‘Bartlett’s test’’ applied on peak area for linearity, additionally proved validity of the developed method. Good accuracy and precision were obtained as revealed from percentage RSD value less than 2. Similarly, no interference was observed from common excipients in tablet formulation as well as degradation product, indicating specificity of the method. As the method could effectively separate the drug from its degradation product, it can be employed as a stability-indicating one.

Review Article: The Effectiveness of Avocado Seed Starch (Persea Americana Mill) As An Excipients in Tablets Formulation

Avocado consists of pericarp (husk), mesocarp (flesh), and endocarp (seed). In avocado seeds there is a fairly high starch content, which is around 80.1% with amylose content of 43.3% and amylopectin of 36.8%. Starch is defined as a natural polymer consisting of a structure composed of amylopectin and another structure called amylose. Amylose content has properties that are easy to absorb water and amylose content can have excellent swelling power in the tablet crushing process. This allows avocado seeds as an alternative source of starch which can be an excipient in tablets. The research explored the effectiveness of avocado seed starch (Persea americana Mill) as an excipient in tablet formulations based on research that has been done. The method of the research is using secondary data obtained from literature studies, which were analyzed by bibliographic annotation by searching and analyzing data related to the effectiveness of avocado seed starch as an excipient. The data collection technique in this research is in the form of a review of published scientific journals, national and international journals. Analysis of the physical and chemical properties of avocado seed starch showed that avocado seed was able to become an excipient. Several studies also showed that avocado seed starch used as a disintegrant and binder in tablet formulations had an optimum concentration of 10%. In addition, avocado seed starch can also be used as an active substance in tablets.

4‐in‐1 Multipurpose Excipient from Musa acuminata Fruit by Alkaline‐Steeping/Retrogradation (ASR) in Acetaminophen Tablet Formulation

AbstractThe conventional approach in the tablet formulation of acetaminophen (ACM) suggests the use of five or more different excipients in a wet granulation tableting process. The use of many excipients in tablet formulation may negatively create excipient–excipient interactions, excipient–drug interactions, exaggerated product side effects, and high drug load. Cutting‐edge technology would be the use of one excipient with a quadrupled functional purpose (4‐in‐1) by direct compression tableting. In this study, a novel two‐phase process called “alkaline‐steeping/retrogradation” (ASR) is employed to obtain the desired starch polymer excipient of quadrupled functional purpose. In phase I, the biopolymer is extracted from the unripe fruits of Musa acuminata by a modified alkaline solution steeping method, while in phase II, 50% w/w of the extracted polymer is retrograded. The retrograded product is re‐mixed with the non‐retrograded 50% w/w that is left from phase I. This gives a novel 50–50% w/w blend named Musa acuminata advanced starch polymer (MAP). To authenticate the efficiency of the ASR, the physicomechanical, analytical, and drug release properties of different concentrations of MAP/ACM solid systems are characterized to ascertain the compatibility. The ASR method produces a unique semi‐hygroscopic biopolymer excipient of quadruple‐function in ACM high‐dose tablet formulation by direct compression.

Potential and Comparative Tablet Disintegrant Properties of Pectin Obtained from Five Okra Genotypes in Ghana.

Okra pectin has been studied as a potential excipient in tablet formulations for pharmaceutical industries. Okra is widely grown and available in Ghana and other parts of the world. The prospective use of pectin from okra genotypes grown in Ghana as tablet disintegrants has not been reported. This study aims to determine the potential and comparative disintegrating properties of pectin from five okra genotypes (Abelmoschus esculentus L.) in Ghana using uncoated immediate release paracetamol tablet formulations. The yield of the pectin from the various genotypes ranged between 6.12 and 18.84% w/w. The extracted pectins had pH ranging from slightly acidic to almost neutral (6.39–6.92). Pectin from the various genotypes exhibited good swelling indexes (˃200%), varying solubility in different solvents, and low moisture content (˂20%). Elemental analysis of the extracted pectin from the various genotypes revealed very low levels of toxic metals and micronutrients. Pectin from the various genotypes was evaluated as disintegrants within concentrations of 5–10% w/w (F1–F18). Their disintegrating properties were compared to that of maize starch BP. All the formulated batches of uncoated immediate release paracetamol tablets (F1–F18) passed the following: uniformity of weight test, uniformity of dimensions, hardness, friability (˂1%), and drug content (95–105%). Significant differences (p ≤ 0.05) were observed between the hardness of the maize starch tablets and tablets formulated from pectin of the various genotypes. Pectin from all genotypes other than PC5 exhibited good disintegrating properties (DT ˂ 15 min) and subsequently passed the dissolution profile test (≥70% release in 45 minutes). Tablets formulated with PC5 as disintegrants at all concentrations (5% w/w (F5), 7.5% w/w (F11), and 10% w/w (F17)) failed the disintegration and dissolution tests. Ultimately, pectins extracted from PC1, PC2, PC3, and PC4 can be commercially exploited as disintegrants in immediate release tablets.

Evaluation of starch-clay composites as a pharmaceutical excipient in tramadol tablet formulations.

Co-processing starch with clay nanocomposite has been shown to yield a new class of materials, potentially with better properties than pristine starch, that could be used as directly compressible excipients in tablet formulations. In this study, starches from 3 botanical sources, i.e., millet starch from Pennistum glaucum (L) RBr grains, sorghum starch from Sorghum bicolor L. Moench grains and cocoyam starch from Colocasia esculenta L. Schott tubers, were co-processed with montmorillonite clay (MMT) and evaluated as a directly compressible excipient in tramadol tablet formulations. The effects of different starch-to-clay ratios on the material and drug release properties of the resulting tablets were evaluated. The starch-clay composites were prepared by heating a dispersion of the starch in distilled water, then precipitating the dispersion with an equal volume of 95% ethanol. The starch-clay composites were characterized and used as direct compression excipients for the preparation of tramadol tablets. The mechanical and drug release properties of the tablets were evaluated. Co-processing MMT with the starches yielded starch-clay composites with different material and tablet properties than the pristine starches. The co-processed starch-MMT biocomposites exhibited improved flowability and compressibility over the pristine starches. The mechanical and drug release properties of tramadol tablets containing starch-clay composites were significantly better than those containing only pristine starches. The properties of the starch-clay composites were not related to the botanical source of the starches. The study showed that starch-clay biocomposites could be used in the controlled release of tramadol.

Development of sweet potato (Ipomoea batatas Lamk.) as excipient in tablet formulation.

Background: Sweet potato has a potential to be used as a raw material for tablets. However, it needs chemical modifications to produce derivatives with excellent pharmaceutical characteristics. The primary purpose of this research was to use sweet potato starch (Ipomoea batatas Lamk.) as a tablet excipient modified through a chemical process.Design and Methods: This study is experimental and is divided into three stages. The first stage is the extraction process to obtain sweet potato starch. The second stage is the chemical modification of sweet potato starch using pentanol-1 and glacial acetic acid. The third step is the analysis of the pharmaceutical properties of the mutated lab model compared to the control sample and Amprotab.Results: The descriptive-comparative analysis showed sweet potato starch modified with panthenol-1 had a higher hardness value (=2.55±0.34) compared to native starch (1.00±0.08). The particle size distribution of the modified sample with acetate acid (=15.20±1.79) was higher than the others.Conclusions: In conclusion, modified sweet potato starch has better pharmaceutical properties than native starch. Further research needs to be conducted on the magnitude of the potential of sweet potato starch as an excipient, both as filler, a binder, and a crushing agent on tablet preparations.Significance for public healthSweet potatoes are Indonesia native plants that have potential for use as pharmaceutical raw materials. Starch from sweet potatoes needs a modification process to produce derivatives with better and specific pharmaceutical characteristics. We describes the development of sweet potato as excipient in tablet formulation can provide better level security for human than synthetic excipients, so it could avoid more serious side effects caused by the use of synthetic excipients.

Development of alginate esters as novel multifunctional excipients for direct compression

Methyl ester derivatives of alginic acid have been evaluated as potential multifunctional excipients for pharmaceutical direct compression. The use of alginic acid as an excipient in tablet formulation is limited because of certain drawbacks such as low tablet hardness and poor compressibility. The objective of this work is to improve these properties through esterification of alginic acid, chemical modification commonly used for enhancing the functionality of tableting excipients. It has been observed that the degree of methylation (DM) has a profitable impact in the physico-chemical and mechanical properties of the obtained materials. In general, an increase in the degree of methylation yielded tablets with higher tensile strength and better compressibility. Furthermore, modified alginates exhibited extended disintegration times compared to native alginic acid due to the introduced hydrophobicity. Finally, the functional versatility of the modified alginates as disintegrating and filling/binding agents was tested by formulating them with microcrystalline cellulose and lactose.

Evaluation of Acid-Modified Ethiopian Potato (Plectranthus edulis) Starch as Directly Compressible Tablet Excipient.

Ethiopian potato is one of the tuber-bearing members of the family Lamiaceae. It is an indigenous crop in Ethiopia and important source of starch. Unprocessed native starches are structurally weak and functionally restricted for application in pharmaceutical technologies. Consequently, starch is usually modified either chemically or physically to make it convenient for industrial use. The aim of the study was to prepare and characterize acid-modified Ethiopian potato starch (AMEPS) and evaluate its functionality as a direct compressible excipient in tablet formulations. The extracted starch from Ethiopian potato tuber was modified using 6% HCl concentration for 8 days, then dried using oven and spray drying techniques, and subsequently evaluated and compared with the native Ethiopian potato starch (NEPS) and S1500® as a direct compressible excipient. Acid modification of the NEPS decreased the moisture content and swelling power while increased the percent solubility. The X-ray diffraction revealed that both the NEPS and AMEPS have B-type crystal patterns. The AMEPS showed improved flowability compared to the NEPS. This improvement was further enhanced by the spray drying process. The compactability study revealed that the tensile strength of spray-dried AMEPS (16.76 kg/cm2) was significantly higher than that of the spray-dried NEPS (7.07 kg/cm2) and S1500® (11.66 kg/cm2). The AMEPS was less sensitive to lubricants compared to the NEPS and Starch 1500®. Similarly, the dilution potential of the AMEPS was superior to the NEPS and S1500®. The AMEPS accommodated up to 50% of paracetamol while the NEPS and S1500® were able to hold only up to 30%. Pharmacopoeial specifications for disintegration and dissolution were met by the paracetamol tablets prepared by AMEPS. Thus, considering all the results obtained, spray-dried AMEPS could be a potential alternative directly compressible tablet excipient.

Acetylation and Evaluation of Taro Boloso-I Starch as Directly Compressible Excipient in Tablet Formulation.

Taro Boloso-I (TB1), a newly improved Colocasia esculenta variety, is a potential source of starch with high yield. However, to improve some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch modifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the NS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic anhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072 (SA1) and 0.695 (SA2) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder flow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the swelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA1 (41.40) and SA2 (63.43 Kg/cm2), was significantly higher than tablets made of the NS (31.96) and Starch 1500® (15.12 Kg/cm2). The SAs also showed lower sensitivity towards lubrication than the NS and Starch 1500® as lower lubricant sensitivity ratios were recorded. In addition, tablets comprising the SAs satisfactorily accommodated at least up to 50 % w/w paracetamol—compared to 30 % w/w by Starch 1500®—upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications for disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in tablet formulations.

Structure-Properties Relationship in the Evaluation of Alginic Acid Functionality for Tableting.

The aim of this study is to investigate the relationship between the structural, molecular, and particulate properties of alginic acid and its functional characteristics in direct compression (tabletability, compressibility, elasticity, deformation mechanism, and disintegration ability). Therefore, accurate characterization of two different batches of alginic acid was executed (X-ray powder diffraction, Fourier-transform infrared spectroscopy, thermogravimetric analysis, scanning electronic microscopy, 1H nuclear magnetic resonance, size exclusion chromatography - multi angle light scattering, viscosimetry, carboxylic acid titration, powder flowability, true density, laser granulometry). Results showed that molecular weight seems to affect tablet properties and that the alginic acid with the lowest molecular weight provides the hardest tablets with the lowest elastic recovery. Furthermore, these results show the potential interest of exploiting alginic acid as filler excipient in tablet formulation. Finally, disintegration properties of tested materials were found to be close to that of commercial superdisintegrants (Glycolys® and Kollidon Cl®) but not correlated to their swelling force. It can be concluded, for the first time, that the determination of alginic acid molecular weight seems key for applications in direct compression and in particular for obtaining tablets with reproducible strength.

Performance Evaluation of Maize Starch as a Multifunctional Excipient in Metronidazole Tablet Formulation

Objective: The aim of this study was to evaluate the performance of maize starch as a multifunctional excipient in metronidazole tablet formulation. Methods: Metronidazole tablets were prepared by wet granulation containing maize starch as diluent (40 %), disintegrant (10 %), and binder (5 %) and compared with a reference formulation containing lactose as diluent (40 %), maize starch as disintegrant (10 %) and acacia as binder (5 %). The granules were analysed for particle size, flow properties, compressibility and moisture content. Tablets weighing 500 mg were compressed for both formulations on a Single Punch Tablet Press using a 12 mm flat-faced punches at 57.5 MPa. The tablets were kept for 24 h to allow for elastic recovery and evaluated for weight and content uniformity, thickness, crushing strength, friability, disintegration time and in vitro drug release. Results: The granule properties revealed differences in mean granule size, angle of repose, bulk and tapped densities for both formulations. Batch I tablets gave rise to better tableting properties compared to batch II tablets. Conclusion: This study confirms the suitability of maize starch as a multifunctional excipient in tablet formulation.

Optimization Combination of Suweg Starch (Amorphophallus campanulatus Decne) and Gembili Starch (Dioscorea esculenta (Lour.) Burk.) as Filler of Ibuprofen Tablet by Simplex Lattice Design Method

Tablet is pharmaceutical dosage form that simple and efficient in drug delivery system. Ibuprofen tablet is usually taken along with food or milk to reduce side effects on the gastrointestinal tract. Starch of Suweg and Gembili are not yet widely developed as excipients in tablet formulation. Based on Biopharmaceutics Classification Systems, ibuprofen includes in BCS class II with high permeability and low solubility. This study want to formulate ibuprofen tablets using combination of suweg and gembili starch with wet granulation method. However, the optimum proportion of starch composition is not yet known, so optimization is needed with the simplex lattice design method using Design Expert software. Obtained 8 formulas with physical response: granule flow time, tablet weight uniformity and disintegration time of tablets. The optimization shows that the optimum composition of suweg and gembili starch are 51.809%: 48.191%. The result of statistical analysis [t-test] physical parameters of granule and tablet of ibuprofen optimum formula were not significantly different (p-value > 0.05) with Design Expert prediction. Based on the requirements of Pharmacopeia Indonesia 4th Edition the results of optimum formula test provide good physical test with granule flow time 3.583±0.130 seconds; tablet weight uniformity 498.333±5.080 mg, hardness tablet 4.780±0.130 Kg, friability vvof tablets 0.904% and the disintegration time of tablets 6.833±0.750 minutes. The dissolution profile of the optimum formula showed %DE at 60 minutes is 76.975±0.037%. Consentration of ibuprofen in tablet is 191.755±5.847 mg and percentage of ibuprofen in tablet is 95.877±2.293%.

Tableting performance of various mannitol and lactose grades assessed by compaction simulation and chemometrical analysis

Mannitol and lactose are commonly used fillers in pharmaceutical tablets, available in several commercial grades that are produced using different manufacturing processes. These grades significantly differ in particulate and powder properties that impact tablet manufacturability. Choice of sub-optimum type or grade of excipient in tablet formulation can lead to manufacturing problems and difficulties, which are magnified during a continuous manufacturing process. Previous characterization of tableting performance of these materials was limited in scope and under conditions not always realistic to the commercial production of tablets. This work seeks to comprehensively characterize the compaction properties of 11 mannitol and 5 lactose grades using a compaction simulator at both slow and fast tableting speeds. These include tabletability, compressibility, tablet brittleness, die-wall stress transmission, and strain rate sensitivity. A chemometrical analysis of data, using the partial least square technique, was performed to construct a model to provide accurate prediction of tablet tensile strength for mannitol grades. Such knowledge facilitates the selection of suitable tablet filler to attain high quality tablet products.

Modified Starches as Direct Compression Excipients – Effect of Physical and Chemical Modifications on Tablet Properties: A Review

Starch is an abundant natural polymer with unique properties that make it amenable to various kinds of treatments. This deliberate attempt at altering the character of native starch results in modified starches. Starches are extensively used in the pharmaceutical industry, especially as excipients in tablet formulation. It is now widely acknowledged that starches in their native form have functional limitations. Modification is a means of enhancing the functionality of native starch for a wide variety of applications. The importance of modified starches as excipients for pharmaceutical direct compression has been identified. Although, there is a wealth of information on starch modification, characterization and applications in the literature, there does not appear to be as yet, any attempt at a methodological analysis of physical and chemical modification techniques as they apply to pharmaceutical direct compression. This review aims at addressing these gaps. It describes a range of physical and chemical techniques employed in producing modified starches and their potentials as excipients for direct compression. The effect of modification on the morphological and functional properties of starch in various direct compression formulations is also reviewed.