scholarly journals Evaluation of super-disintegrant potential of acid-modified starch derived from Borassus aethiopum (Aracaceae) shoot in paracetamol tablet formulations

2020 ◽  
Vol 19 (3) ◽  
pp. 459-465
Author(s):  
Chukwuemeka P. Azubuike ◽  
Uloma N. Ubani-Ukoma ◽  
Abiola R. Afolabi ◽  
Ibilola M. Cardoso-Daodu
Keyword(s):  
Low Cost ◽  
Wet Granulation ◽  
Modified Starch ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations ◽  
Ftir Spectrophotometry ◽  
Borassus Aethiopum ◽  
Expected Increase ◽  
Paracetamol Tablet

Purpose: To evaluate the super-disintegrant potentials of acid modified Borassus aethiopum starch (AMS) in comparison with native starch (NS) and commercial disintegrant sodium starch glycolate (SSG). Methods: Compatibility of AMS with paracetamol powder was evaluated using Fourier transform infrared (FTIR) spectrophotometry. Seven batches of paracetamol granules and tablets were prepared by wet granulation. AMS and NS were employed as disintegrants at concentrations of 2.43, 4.86 and 9.72 %w/w, respectively while 4.86 %w/w SSG was used as standard disintegrant. All the batches of the granules were compressed under the same compression settings. The properties of the granules as well as those of the tablets were assessed. Results: AMS was compatible with paracetamol powder as no noticeable interaction was observed in FTIR study. The paracetamol tablets formulated using AMS as disintegrant demonstrated satisfactory friability, weight uniformity, hardness, and superior disintegration characteristics to the formulations containing NS and SSG as disintegrant. Even at a lower concentration (2.43 %w/w), AMS possessed better disintegrant property than NS and SSG. AMS and NS had dimensionless disintegrant quantity of 1.447 and 0.005, respectively. As expected, increase in AMS concentration showed a decrease in disintegration time. Conclusion: AMS could be a potential low-cost super-disintegrant in formulation of paracetamol tablets. Keywords: Acid modified starch, Borassus aethiopum, Disintegrant, Compatibility

scholarly journals Influence of process variables on release properties of paracetamol tablets

2007 ◽  
Vol 57 (1) ◽  
pp. 73-86 ◽  
Author(s):  
Gbenga Alebiowu ◽  
Oludele Itiola
Keyword(s):  
Interaction Effects ◽  
Process Variables ◽  
Factorial Experimental Design ◽  
Disintegration Time ◽  
Individual Effects ◽  
Pregelatinized Starch ◽  
Tablet Formulations ◽  
Binder Concentration ◽  
The Individual ◽  
Paracetamol Tablet

Influence of process variables on release properties of paracetamol tablets A 23 factorial experimental design has been used to quantitatively study individual and interaction effects of the nature of binder (N), binder concentration (c) and relative density of tablet (d) on the disintegration time (DT) and dissolution times, t1, t50 and t90, of paracetamol tablet formulations. The factorial design was also used to study the quantitative effects of pregelatinization of starch binders on these parameters, i.e., N, c and d. In general, the most common ranking of the individual effects on DT, t1, t50 and t90 for native/native, pregelatinized/pregelatinized and native/pregelatinized starch binder formulations was c > d > N. For interaction effects, the most common ranking was N-c > c-d > N-d for all formulations. The results generally showed that c can considerably affect DT, t1, t50 and t90 of the tablets.

scholarly journals Evaluating the Flow and Release Profiles of Ibuprofen Formulations by Increasing the Binder Concentration

2021 ◽  
Vol 16 (2) ◽  
pp. 111-117
Author(s):  
B.B. Mohammed ◽  
E.J. John ◽  
G.T. Abdulsalam ◽  
K.P. Bahago
Keyword(s):  
Release Rate ◽  
Active Drug ◽  
Release Profile ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Dissolution ◽  
Tablet Formulations ◽  
Release Profiles

Background: Tablets must be able to release the active drug in the gastrointestinal tract for absorption. The release profile of solid pharmaceutical dosage formulations can be quantified by assessing the disintegration and dissolution times tests. Binders are adhesives either from sugar or polymeric material that are added to tablet formulations to provide the cohesiveness required for the bonding together of the granules under compaction to form tablets.Objective: The objective of the study was to formulate and assess ibuprofen tablets using different concentrations of binders (Acacia and Gelatin).Methods: The granules were prepared using wet granulation method and analysed for flow properties based on USP/NF protocols. After granule compression, the tablets release profiles were thereafter assessed via the tablet dissolution and disintegration tests.Results: Weight variation, thickness and diameter were within the acceptable values for all batches indicative of a uniform flow. Batches with binder concentrations of 10 % and 20 % failed disintegration test due to a disintegration time above 15 min while the release rate for batches 1 and 4 was about 88 % in 60 min as against the other batches whose release rate was less than 50 % in 60 min as a result of increasing their binder concentrations.Conclusion: The study concluded that increasing the concentration of acacia and gelatin above 5% led to a decrease in percentage of drug released and an increase in disintegration time above 30 mins because 5% batches gave the best release profiles.

scholarly journals Formulation and Optimization of Immediate Release Cajanus Cajan Starch-Based Tablets Containing Metronidazole

2020 ◽  
Vol 5 (1-2) ◽  
pp. 16-19
Author(s):  
Ahmed Abdalla Bakheit Abdelgader ◽  
Daud Baraka Abdallah ◽  
Elnazeer I. Hamedelniel ◽  
Hiba Atif Mutwakil Gafar ◽  
Mohammed Abdelrahman Mohammed
Keyword(s):  
Cajanus Cajan ◽  
Immediate Release ◽  
Wet Granulation ◽  
Maize Starch ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Upper Level ◽  
High Level ◽  
Starch Paste ◽  
Tablet Dosage

Starch is found almost in all organs of plants as a carbohydrate reserve. It is considered one of the most commonly used pharmaceutical additives, mainly in tablet dosage forms; it used as a tablet binder when incorporated through the wet granulation process or as a disintegrant. Cajanus cajan has a high level of carbohydrate, which makes it another potential choice as a source for starch. This study aims to investigate and optimize the effect of Cajanus cajan starch concentrations as well as wet massing granulation time on physicochemical properties of metronidazole tablets. The hardness, friability percentage, and disintegration time of prepared tablets were determined, and the central composite design was employed in the optimization process. Then the tablets of optimized batch were compared against those tablets in which maize starch and sodium starch glycolate were used instead of Cajanus cajan starch. The results indicated that metronidazole tablets containing the upper level of starch paste (Cajanus cajan and/or maize starch paste) exhibited better percentage friability, hardness, and disintegration time than those formulated with lower levels and those without starch paste. The study showed that experimental design is a useful technique for optimizing Cajanus cajan starch-based tablets, which enabled a better understanding of how different variables could affect the responses. In addition, the study demonstrated that incorporation of Cajanus cajan starch in tablets formulation led to improvement of its physical properties compared to the formulations of maize starch and sodium starch glycolate respectively.

scholarly journals Formulation and Evaluation of Conventional Metronidazole Tablets using Natural Gum Extracted from Grewia species

2021 ◽  
pp. 128-137
Author(s):  
J. A. Avbunudiogba ◽  
O. Oghenekevwe
Keyword(s):  
Low Cost ◽  
Wet Granulation ◽  
State University ◽  
Disintegration Time ◽  
Solid Dosage ◽  
Drug Content ◽  
Compression Properties ◽  
Acacia Gum ◽  
Grewia Gum ◽  
Delta State University

Aims: The pharmaceutical world has been paying increasing attention to the extraction, development and use of natural gums as binders in the formulation of solid dosage forms. The use of natural gums as binders is more advantageous than the use of synthetic ones due to availability, low cost, biodegradability and biocompatibility. In this study, gum extracted from Grewia species was compared with that fromAcacia in metronidazole tablets. Study Design: Ten batches of metronidazole tablets were formulated with varied concentration of Grewiaspp gum and Acacia gum. Place and Duration of Study: The study was carried out in Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Delta State University, Abraka, Nigeria; between January and December 2019. Methodology: Five batches of metronidazole tablets containing 0.5, 0.75, 1.0, 1.25 and 1.5% w/w of Grewia gum were preparedby wet granulation. Resulting granules were characterised by measuring flow and packing properties. In other experiments, five batches of tablets were formulated using same concentration of gum, with Acacia gum substituted for Grewia gum. Both sets of granules were compressed into tablets using tableting machine at a load of 27 arbitrary units. Tablets so formed were evaluated for hardness, friability, disintegration time, drug content and drug release profiles. Drug – excipient interaction was investigated with FTIR. Results: The resulting metronidazole tablets showed hardness of 5.46 kgF to 7.87 kgF (Grewiagum) and 6.06 kgF-8.20 kgF (Acacia gum). Friability percentages of all the batches were above 1% except for A3-A5 and B5 which are less than 1%. All formulations released more than 75 % of the drug content within 60 min. The FTIR analysis revealed no interaction between the metronidazole and Grewia species gum. Conclusion: Metronidazole granules and tablets were successfully prepared using Grewiagum and showed comparable pre-compression and post-compression properties with those formulated with Acacia.

Preparation and Characterization of Carboxymethylated and Cross-Linked Enset Starch as a Disintegrant in Tablets

2020 ◽  
Vol 35 (2) ◽  
pp. 119-134
Author(s):  
Yohannes Mengesha ◽  
Anteneh Belete ◽  
Tsige Gebre-Mariam
Keyword(s):  
Reaction Medium ◽  
Moisture Sorption ◽  
Modified Starch ◽  
Disintegration Time ◽  
Native Starch ◽  
Swelling Power ◽  
Sodium Starch Glycolate ◽  
Modified Starches ◽  
The Fourier Transform

Starch and modified starches have been commonly employed as excipient in pharmaceutical industry. The use of non-modified or “native” starch,  However, is mostly confined due to limitation in several physicochemical properties. Cross-linked sodium carboxymethyl starch which is also known as sodium starch glycolate is extensively used in fast dissolving tablets to disperse the drugs within short span of time. In this study, enset starch was carboxymethylated and subsequently cross-linked. Carboxymethyl enset starch (CMES) was obtained by reacting enset starch and monochloroacetic acid (MCA) in the presence of sodium hydroxide. CMESs having different degree of substitution (DS) were cross-linked at variousconcentrations (2.5, 5 and 10% w/w) of sodium hexametaphosphate (SHMP) to provide sodium starch glycolate of enset starch (SSG-E). The fourier transform infrared (FTIR) spectra confirmed the presence of carboxymethylated group in the modified starch granules with new band at 1608.52 cm-1. This dually modified enset starch (SSG-E) was evaluated as a potential disintegrant in paracetamol tablets in comparison with commercially available sodium starch glycolate, Disegel. Carboxymethylation was significantly influenced by reaction medium, reaction temperature and reaction time (p < 0.05). CMES with higher DS (0.437 ± 0.03) exhibited higher peak viscosity than CMES with lower DS (0.224 ± 0.01). Despite exhibiting greater swelling power, CMES showed significantly lower pasting viscosity compared to the native starch (p < 0.05). At 2.5% SHMP, the dually modified starch (SSG-E) exhibited significant increase in swelling but its rate of water-uptake was lower than that of Disegel. As the SHMP concentration wasincreased from 2.5 to 5%, the swelling power decreased significantly (p < 0.05). When the concentration was increased to 10% the swelling power increased significantly (p < 0.05). At 2.5% SHMP concentration SSG-E showed a viscosity comparable to that of CMES. As the concentration of SHMP increased to 5 and to 10% w/w, significant decrease in viscosity (p < 0.05) was observed. Compared to the native enset starch (NES), the solubility of SSG-E was more than 4-fold, but its viscosity was much lower than that of CMESs. The SSG-E exhibited lower moisture sorption than CMES but higher sorption than NES. SSG-E showed good flowability, superior swelling power and solubility than NES. The disintegration time (DT) of paracetamol tablets containing SSG-E as a disintegrant was comparable to those tablets with similar concentration of Disegel. At 4% SSG-E, paracetamol tablets exhibited DT less than 1 min. Keywords: carboxymethylation, degree of cross-linking, enset starch, paracetamol tablets, sodium starch glycolate 

scholarly journals Formulation and Evaluation of Tablets Containing Fenugreek Extract Using Sodium Starch Glycolate as Super Disintegrant

2021 ◽  
pp. 47-53
Author(s):  
Divya Jyothi
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Antidiabetic Activity ◽  
Wet Granulation ◽  
Onset Of Action ◽  
Plant Materials ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations

The present work is aimed to formulate the tablets containing fenugreek extract as drug by wet granulation method. Further the effect of Sodium Starch Glycolate as super disintegrant on disintegration and drug release was studied. Fenugreek extract contains mucilage which retards the disintegration of tablets and hence shows slower drug release. Hence in order to improve disintegration and thereby in vitro drug release, Sodium Starch Glycolate was used as super disintegrant. Tablet formulations were prepared without the SSG (Conventional-F1) and also with sodium starch glycolate (F2-F4) by wet granulation method. Assessment of flow properties of granules, physicochemical characterization of tablet formulations was carried out. Fenugreek is widely used for its antidiabetic activity which is attributed to mainly to the presence of an alkaloid Trigonelline. Hence in vitro release study of trigonelline was carried out which showed that the percentage release from F1 and F2 was found to be 58.12±4.49 and 99.08±0.01 respectively after 6 hrs. This study concludes that tablet formulation of fenugreek seed extracts with super disintegrants will be more desirable, advantageous and therapeutically more beneficial than incorporating the direct plant materials for the treatment of diabetes for faster onset of action.

scholarly journals Physicochemical Characterization and Evaluation of the Binding Effect of Acacia etbaica Schweinf Gum in Granule and Tablet Formulations

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla
Keyword(s):  
Water Solubility ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hot Water ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Binding Effect ◽  
Tablet Formulations

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.

scholarly journals Evaluation of xerogels of cassava and cocoyam starches as dry granulation binders and disintegrants in directly compressed paracetamol tablet formulations

2019 ◽  
Author(s):  
Sylvester Okhuelegbe Eraga ◽  
Ogochukwu Augustina Meko ◽  
Magnus Amara Iwuagwu
Keyword(s):  
Flow Properties ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Dry Granulation ◽  
Standard Procedures ◽  
Wetting Time ◽  
Tablet Formulations ◽  
Tablet Manufacture ◽  
Paracetamol Tablet ◽  
Excipient Compatibility

The physicochemical properties of excipients play vital roles in the process of tablet manufacture. A comparative evaluation of the binding and disintegrant properties of xerogels of cassava and cocoyam starches with microcrystalline cellulose (MCC) in paracetamol tablet formulations was investigated. Cassava and cocoyam starches were extracted from their tubers following standard procedures. Xerogels of both starches were prepared and used to prepare batches of paracetamol granules for direct compression into tablets at concentrations of 3.8, 7.6 and 11.4 %w/w and with 7.6 %w/w MCC for comparison. Granules were analysed for their flow properties and drug-excipient compatibility and the tablets were evaluated for their tablets properties. The paracetamol granules prepared with the xerogel powders were comparable in flow properties with those made with MCC. Differential Scanning Calorimetry and Fourier Transform Infrared analyses revealed no interaction between the xerogel powders and paracetamol. Increase in concentrations of the xerogel powders led to an increase in hardness, wetting time, water sorption, disintegration time, drug release and a decrease in friability of the tablets. Tablets formulated with the starch xerogel powders met compendial requirements at 7.6 %w/w concentration. The study confirms the potentials of xerogels of cassava and cocoyam starches as dry granulation binders/disintegrants. Tablets made with the xerogel powders are superior to those made with MCC in terms of disintegration time but MCC produces harder and less friable tablets, as a superior binder.

scholarly journals Postruminal Delivery System for Amino Acids and Proteins in Cattle

2007 ◽  
Vol 76 (4) ◽  
pp. 547-552 ◽  
Author(s):  
T. Sýkora ◽  
M. Rabišková ◽  
J. Třináctý ◽  
D. Vetchý ◽  
A. Häring ◽  
...  
Keyword(s):  
Amino Acids ◽  
Small Intestine ◽  
Low Cost ◽  
Ph Sensitive ◽  
Wet Granulation ◽  
Average Weight ◽  
Disintegration Time ◽  
The Core ◽  
Ph Sensitive Polymer

The purpose of this experiment was to develop an effective postruminal transport system (PTS) with a high content of suitable vegetable proteins and amino acids. PTS serves for nutrient delivery to the abomasum and small intestine of dairy cows in order to increase the milk yield. Direct addition of proteins and amino acids to the diet is not useful as the ruminal microbes will utilize active substances before they reach absorption sites in the small intestine. PTS has several advantages, e.g. a possibility of the direct application in a food, low cost, and nutritional and therapeutical improvement. PTS consists of a core (pellets, small tablets) and a coating, which protects the core against the environment of rumen and enables to release the core content in the environment of abomasum and small intestine. Lenticular tablets - cores of PTS were prepared by wet granulation method and compression. Qualitative indicators of tablets (average weight, weight uniformity, hardness, friability, disintegration time) were determined according to valid Czech and European Pharmacopoeias. Cores were subsequently coated with several types of coating - ethylcellulose, stearic acid and pH sensitive polymer poly-(2-vinylpyridine-co-styren), alone or in combination of various rates. Nine samples of coated protein tablets exhibiting appropriate characteristics in vitro were prepared. The presence of the pH sensitive polymer at least in 10% concentration of the coating and the coating amount of 9.0 to 12.6% per tablet were necessary to ensure the requested PTS properties.

An Evaluation of Dictyophora indusiata Mucilage as a Binder in Tablet Formulations

2021 ◽  
Vol 901 ◽  
pp. 22-27
Author(s):  
Kanokporn Burapapadh ◽  
Narumon Changsan ◽  
Chutima Sinsuebpol ◽  
Phennapha Saokham
Keyword(s):  
Research Work ◽  
Edible Mushroom ◽  
High Viscosity ◽  
Commercial Product ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Pharmaceutical Excipients ◽  
Tablet Formulations ◽  
Paracetamol Tablet

Dictyophora indusiata known as bamboo mushroom is an edible mushroom in Genus Dictyophora, Family Phallaceae that could produce highly viscous mucilage encased in the peridium. The viscous mucilage is clear-colorless hydrocolloid with high viscosity and high adhesive nature which made it possible to be developed into pharmaceutical excipients. This research work aimed at the application of the mucilage as a tablet binder. The mucilage was prepared as redispersible powder by lyphilization before used. The dried mucilage could be effectively used as a binder in paracetamol tablet formulations both as dry and wet binder. Increasing of the dried mucilage amount caused the stronger tablet with higher disintegration time. The optimum concentrations of the dried mucilage in tablet formulations were 2.0% w/w as dry binder and 1.0% w/w as wet binder. The obtained tablets revealed low friability and fast disintegration time. The drug dissolution was conformable to USP37 standard and comparable to that of commercial product. Accordingly, the Dictyophora indusiata mucilage could be functionally used as a tablet binder

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