scholarly journals Dissolution Behaviours of Acetaminophen and Ibuprofen Tablet Influenced By L–HPC 21, 22, and Sodium Starch Glycolate as Disintegrant

2019 ◽  
Vol 1 (3) ◽  
Author(s):  
Yoga Windhu Wardhana ◽  
Dradjad Priambodo

The dissolution of tablets is one of a drug absorption determinant. Disintegrant agent has play an important role on determining the dissolution of tablets. In this experiment, the dissolution behaviours of Acetaminophen and Ibuprofen Tablet was studied using various disintegrant agent such as Low substituted – Hydroxypropyl Cellulose (L–HPC) 21, L–HPC 22 and Sodium Starch Glycolate (SSG) as comparator. Those disintegrant agents were used at three concentration (6%, 7% and 8%) for every tablets formula. Tablets were made by wet granulation method and pressed using single punch 13 mm flat E. Korsch machine. Evaluation of each tablets quality were conducted include for uniformity of weight and size (diameter and thickness), hardness, friability, disintegration time and dissolution. Physically standards from tablets were in good condition, the standards of the weight and thickness uniformity, hardness and friability met the requirement. The dissolution profile on Acetaminophen Tablets showed that only tablet with 6 % L–HPC 21 did not meet the requirement of FI V (Q = 80%, 30 minutes), but on Ibuprofen Tablets where met the requirement of  FI V (Q = 80%, 60 minutes) only tablet with 8%  L– HPC 21,  7% and 8% SSG. The conclusion of the study was the L–HPC has more disintegrant character at hydrophilic active ingredients. Key words:  Acetaminophen Tablet, Ibuprofen Tablet, SSG, L-HPC 21 and 22, Dissolution Profile

2020 ◽  
Vol 21 (1) ◽  
pp. 35
Author(s):  
Dwi Setyawan ◽  
Widji Soeratri ◽  
Mahrus Naufal Nuruddin ◽  
Diajeng Putri Paramita ◽  
Bambang Widjaja

The aim of this study was to determine the effect of binder and disintegrant excipients toward tablet properties of levofloxacin as the latter tends to suffer brittle fracture upon compression. The excipients used were povidone K-30 as the binder and sodium starch glycolate (SSG) as the disintegrant which the tablets were formulated according to factorial design 22 with two factors and two levels on each factor. Four formulas were prepared by wet granulation method using 2 and 4% of each povidone K-30 and sodium starch glycolate in various compositions. Tablet properties were evaluated for its hardness, friability, and disintegration time as well as dissolution profile. The data obtained was statistically analyzed using Minitab® 17 software to optimize the formulation and resulted in different impacts caused by each excipient. Povidone K-30 exhibited an increment in hardness, friability, disintegration time but a decrease indissolution profile of levofloxacin tablet. SSG decreased hardnessand disintegration time, but increased friability and dissolution profile of levofloxacin tablet. Overlaid contour plot showed that the optimal formula regarding tablet properties of friability, disintegration time, and dissolution profile is in composition of 2.01% povidone K-30 and 2.01% sodium starch glycolate. Keywords: levofloxacin tablet, povidone K-30, sodium starch glycolate, factorial design.


Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  


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

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.


Author(s):  
Shohreh Alipour ◽  
MAHSA ASEF ◽  
FATEMEH AHMADI

Objective: Fast disintegrating tablets (FDTs) are found helpful in dysphagia (difficulty in swallowing) especially in Parkinson patients. Levodopa is still the first choice in Parkinson disease treatment and is co-administered by carbidopa for better efficacy. Methods: In the present study, a rapid and simple isocratic Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) method was developed and validated for simultaneous quantification of levodopa and carbidopa in optimized Fast Disintegrating Tablets (FDTs). The linearity, precision, accuracy, limit of detection (LOD) and limit of quantification (LOQ) of the method were determined. FDTs were prepared using direct compression, dry and wet granulation and were optimized for faster disintegration time. Tablets thickness, weight, hardness, friability, drug content and dissolution profile were also evaluated. Results: A RP-HPLC system with C18 column and mobile phase 90:10 (v/v) phosphate buffer: methanol was used. The method linearity was found to be within the concentration range of 3.125-50 μg/ml for levodopa, and 3.125-25 μg/ml for carbidopa. The intra and inter-day precision and accuracy were acceptable. LOD and LOQ of levodopa-carbidopa were 0.2-0.8 μg/ml and 0.5-2.4 μg/ml, respectively. The total chromatographic run time was 5 min. The optimized FDTs hardness was 3.81±0.4 and tablets were disintegrated within 30 sec. Levodopa and carbidopa were dissolved in dissolution media within 5 min. Conclusion: Results indicated that this method was suitable for simultaneous quantification of levodopa and carbidopa in the presence of different ingredients of a pharmaceutical solid dosage form. Therefore, this method could be applied in pharmaceutical quality control for rapid quantification of structurally similar substances with different physicochemical properties.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Y. Eshovo Apeji ◽  
IY. Muhammad ◽  
A. Kehinde Olowosulu ◽  
G. Owoicho Okpanachi ◽  
A. Rukayat Oyi

Abstract Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration time and dissolution profile evaluated subsequently. Results of granule properties showed that variations in parameters evaluated was as a result of differences in the type and composition of diluent used in formulation. Compactibility and tabletability profile of metronidazole granules revealed a better performance with granules processed with C-PE based diluents compared to SCE-based diluents. Tablets formulated with C-PEs as diluents were uniform in tablet weight, disintegrated faster and yielded a faster drug release compared to tablet formulations containing SCEs as diluent. This study reveals the performance advantage of C-PEs as diluents in tablets manufactured by wet granulation and highlights the importance of rational selection of excipients during tablet formulation.


Author(s):  
Sinodukoo Eziuzo Okafo ◽  
Avbunudiogba John Afokoghene ◽  
Christian Areruruoghene Alalor ◽  
Deborah Ufuoma Igbinake

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder. Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release. Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35% Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.


2014 ◽  
Vol 50 (1) ◽  
pp. 195-202 ◽  
Author(s):  
Haroon Rahim ◽  
Mir Azam Khan ◽  
Amin Badshah ◽  
Kamran Ahmad Chishti ◽  
Salimullah Khan ◽  
...  

To evaluate binding potential of Prunus domestica gum in tablets formulations. Six tablet batches (F-1B to F-6B) were prepared by wet granulation method, containing Avicel pH 101 as diluent, sodium diclofenac as model drug using 10, 15 and 20 mg of Prunus domestica gum as binder and PVP K30 was used as standard binder. Magnesium stearate was used as lubricant. Flow properties of granules like bulk density, tapped density, Carr index, Hausner’s ratio, angle of repose as well as physical parameters of the compressed tablets including hardness, friability, thickness and disintegration time were determined and found to be satisfactory. The FTIR spectroscopic analysis showed that the formulation containing plant gum is compatible with the drug and other excipients used in tablets formulation. Hence the plant gum has role as a potential binder in tablets formulations. The dissolution profile showed that tablets formulations containing Prunus domestica gum 15 mg/200 mg of total weight of tablet as binder showed better results as compared to PVP K30.


2015 ◽  
Vol 13 (2) ◽  
pp. 133-141 ◽  
Author(s):  
Alia Erum ◽  
Sajid Bashir ◽  
Shazia Saghir ◽  
Rai Muhammad Sarfraz

The aim of the present investigation was to evaluate the binding and disintegrating properties of arabinoxylan isolated from Ispaghula (Plantago ovata) husk. Atenolol and atorvastatin orodispersible tablet F1, F2 and F3 were prepared by direct compression method using arabinoxylan (12, 9, 6) mg as superdisintegrant, and F4 and F5 containing 12 mg Ispaghula husk and 12 mg sodium starch glycolate, respectively. Metformin tablets were prepared by wet granulation method F1 containing starch as binder, F2 containing arabinoxylan as binder and F3 containing arabinoxylan as binder and as superdisintegrant. Prepared tablets were evaluated for precompression parameters such as compatibility studies, bulk density, tapped density, angle of repose, Hausners ratio and Cars index and post compression parameters such as weight variation, hardness, thickness, diameter, wetting time, water absorption ratio disintegration time drug release and moisture uptake studies. Attempts were done to trace the possible disintegrant mechanism of arabinoxylan. FTIR spectra of physical blend of atenolol, atorvastatin, metformin with arabinoxylan confirmed the compatibility of excepient with formulation ingredients. All the formulations of atenolol, atorvastatin satisfied the limits of redispersion with a dispersion time of less than 60 sec. F1 showed minimum disintegration time 4 sec providing the evidence of arabinoxylan an excellent superdisintegrant when compared with F4 containing Ispaghula husk with disintegration time 30 sec and F5 contains sodium starch glycolate having disintegration time of 35 sec. Minimum wetting time of 17 sec and high water absorption ratio of F1 formulation confirmed the arabinoxylan as swelling disintegrant. The results of metformin tablet indicate that arabinoxylan could be useful to produce tablets with desired characteristics for specific purposes, and could be used as an alternative substitute binder and superdisintegrant in pharmaceutical industries. These studies provide a strong evidence for usefulness of arabinoxylan as binder and superdisintegrant and a good alternative to natural and synthetic superdisintegrant. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21891 Dhaka Univ. J. Pharm. Sci. 13(2): 133-141, 2014 (December)


Author(s):  
Y. Shravan Kumar ◽  
Prashanthi Patel ◽  
Sravanthi Ch ◽  
Rashmi B

Aripiprazole is an atypical antipsychotic agent used for treatment of schizophrenia, bipolar disorder and major depressive disorders. In the present work, oral  disintegrating tablets of aripiprazole were developed to  enhance the patient compliance and provide rapid onset of  action. The efficacy of aripiprazole is mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5HT-1A receptors and antagonist activity at 5HT-2A receptors. It has a bitter taste and poor-solubility in water. Thus, the main objective of the study is to formulate taste masked oral disintegrating tablets of aripiprazole by using inclusion complex beta-cyclodextrin to achieve a better dissolution rate and further improving the bioavailability of the drug. Oral disintegrating tablets were   prepared by direct compression method using  super disintegrant like crospovidone, croscarmellose sodium,  sodium starch glycolate and combinations of  cros-povidone with croscarmellose sodium, and crospovidone with sodium  starch glycolate in different concentrations. They were evaluated for the pre-compression parameters such as bulk density, compressibility, Hausner ratio and angle of repose. The prepared batches of tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time,    in vitro dispersion time, and in vitro dissolution profile. All these parameters were found to be satisfactory. Among all, the formulation F15 containing crospovidone 5% + cros-povidone with croscarmellose sodium 5% was considered to be the optimum formulation, which released nearly 99% of the drug in 20 minutes with a disintegration time of 10. 20 seconds. These studies indicate the viability and benefits of oral disintegrating tablets of aripiprazole. 


2020 ◽  
Vol 19 (3) ◽  
pp. 459-465
Author(s):  
Chukwuemeka P. Azubuike ◽  
Uloma N. Ubani-Ukoma ◽  
Abiola R. Afolabi ◽  
Ibilola M. Cardoso-Daodu

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


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