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

Author(s):  
J. A. Avbunudiogba ◽  
O. Oghenekevwe

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.

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.


2007 ◽  
Vol 76 (4) ◽  
pp. 547-552 ◽  
Author(s):  
T. Sýkora ◽  
M. Rabišková ◽  
J. Třináctý ◽  
D. Vetchý ◽  
A. Häring ◽  
...  

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.


Author(s):  
C Mallikarjuna Setty ◽  
Radhika Muthadi ◽  
V.R.M Gupta ◽  
M.V.R. Reddy ◽  
Jithan A.V.

 Aceclofenac, a non-steroidal anti-inflammatory drug, is used for posttraumatic pain and rheumatoid arthritis. The tablets were produced by simple wet granulation method. The post compressional parameters, hardness, friability, drug content of all the formulations were within the official limits. The disintegration time did not change with the type of diluents (mannitol, microcrystalline cellulose and dicalcium phosphate). However, it varied with the concentration of polyvinylpyrrolidone and microcrystalline cellulose. As the concentration of acacia was decreased, disintegration time decreased and hence, dissolution increased.  Incorporation of superdisintegrants improved the disintegration time as well as dissolution of the drug. As the granules size increased disintegration time decreased and increase in dissolution was noticed. It can be concluded that the selection of combination of variables and levels were important in the optimization of aceclofenac tablet formulation.


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


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 34-40
Author(s):  
V.L Narasaiah ◽  
◽  
Ch. Praneetha ◽  
P Mallika ◽  
K. Pullamma ◽  
...  

The aim of this project was to develop fast dissolving tablets (FDT) of aceclofenac by wet granulation using super disintegrating agents such as cross carmellose sodium (CCS), Crospovidone (CP) and sodium starch glycolate (SSG) were formulated and evaluated. The tablets evaluated for thickness, hardness, friability weight variation, drug content, water absorption ratio, wetting time, disintegration time and in vitro dissolution studies. The in vitro release studies were conducted in pH 7.4 phosphate buffer. Different release models like zero order, first order, Higuchi and Korsmeyer-Peppas were applied to in vitro drug release data in order to evaluate drug release mechanisms and kinetics. The formulation ‘F4’ showed satisfactory physico-chemical properties and drug content uniformity. The formulation ‘F4’ follows first order kinetics and the mechanism of drug release was governed by Higuchi. The ‘n’ value showed between <0.5, it was followed that Fickian transport. The FTIR studies were conducted and it shows that there is no interaction between drug and excipients.


Author(s):  
D. N. O. Kuevi ◽  
E. Ayertey ◽  
D. A. Bartels ◽  
F. W. A. Owusu

Background: Disintegrants are essential in the formulation of solid dosage forms such as tablets because they aid in the release of the active drug for therapeutic action. Disintegrating agents such as starch are currently posing challenges such as tablet softening and slow disintegration. In the quest for alternatives that are cheaper, readily available and possessing same or better disintegrating property, Khaya senegalensis gum was considered. Currently, there is no available literature pertaining to its disintegrating property. Objective: To investigate the disintegrating properties of Khaya senegalensis gum using paracetamol tablets. Methods: K. senegalensis gum was obtained by making an incision on the stem bark of the mahogany tree. The dried purified K. senegalensis gum was employed in the formulation of granule I whiles Tragacanth gum was used in formulating granule II using the wet granulation technique. The flow properties of both granules were subsequently determined and compared. Paracetamol tablets were then produced with the formulated granules I and II. Friability, hardness, weight uniformity and disintegration testing were performed on the paracetamol tablets formulated with both granules. Results: The results showed granule I had a better flowability with angle of repose 31.63°C, Hausner’s ratio 1.24 and Carr’s index 19.57 as compared to granule II with angle of repose 34.72°C, Hausner’s ratio 1.31 and Carr’s index 23.84. The study also revealed, paracetamol tablets formulated with granule I (K. senegalensis gum) passed the hardness test (6.57 Kg.f), disintegration time (2.44 min), weight uniformity test (2.2% standard deviation) and friability test (0.69%). Paracetamol tablets formulated with granule II (Tragacanth gum) also passed the hardness test (8.20 Kg.f), disintegration time (7.69 min), weight uniformity test (1.6% standard deviation) and friability test (0.86%). Conclusion: Khaya senegalensis gum can therefore be explored as an alternative disintegrant in the formulation of paracetamol tablets for improved bioavailability.


2019 ◽  
Vol 9 (2) ◽  
pp. 222-230
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh

The present study involves in the evaluation of starch xanthate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. By using gelatinization process starch xanthate was synthesized. Then the synthesized starch xanthate was evaluated under physical and micromeritic methods. To develop starch xanthate as a superdisintegrant, fast dissolving tablet of aceclofenac was prepared by direct compression method employing starch xanthate in different proportions in each case employing 23 factorial design. All the prepared fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like PD10, DE5 and K1. The prepared starch xanthate was found to be fine, free flowing slightly crystalline powder. Starch xanthate shown good swelling in water. The swelling index was 50% and all micrometric properties shown good flow and compressibility needed for solid dosage from manufacturing. All the formulated fast dissolving tablets employing starch xanthate were of good quality with regard to drug content, hardness and friability and fulfilled the official (IP/USP) requirements of compressed tablets with regard to the above mentioned physical properties. Starch xanthate was found to be a superdisintegrant which enhanced the dissolution efficiency when combined with croscarmellose sodium, with the aceclofenac and hence it could be utilized in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 10 minutes. Keywords: Fast Dissolving, Superdisintegrant, Starch xanthate, Dissolution efficiency


Author(s):  
Nausheen Tariq Siddiqui ◽  
Ramla Binte Baber ◽  
Rsfi Akhtar Sultan ◽  
Iqbal Azhar ◽  
Waseemuddin Ahmed ◽  
...  

Background: Pectin, a naturally occurring polysaccharide is more than a food additive and has got amazing properties as a gelling agent and as a binder. Objective: The current research entails the extraction and identification of pectin from peels of selected fruits mango (Magnifera indica) and banana (Musa paradisiaca) by direct heating and using alcohol as precipitating agent. The potential of pectin as a binding agent in tablet formulation was evaluated by screening its micromeritics and post compression properties. Method: quadruple formulations of ibuprofen with crude peel pectin extracted from mango and banana in concentration of 50, 75, 100 and 125 mg respectively were employed in the tablet manufacture process by wet granulation method. Results: Successful formulation of tablet was done with the extracted pectin from the two fruit peels. The micromeritics properties showed good binding and flowing properties. An increase in concentration of pectin increased the hardness and also the dissolution of tablets up to a certain extent. The disintegration time was suitable for all formulations. Conclusion: It was concluded that pectin extracted from mango and banana peels can be used as a super disintegrating agent in pharmaceutical formulations, where needed.


2020 ◽  
Vol 17 (4) ◽  
pp. 348-360
Author(s):  
Laiane J. Oliveira ◽  
Andressa Veiga ◽  
Nayana C. F. Stofella ◽  
Aline Carolina Cunha ◽  
Maria da Graça T. Toledo ◽  
...  

Background: Orodispersible Tablets (ODTs) are an option to facilitate the intake of pharmaceutical solid dosage forms, which dissolve in the mouth within 30 seconds releasing the drug immediately with no need for water intake or chewing. Objective: The main goal of our study is the technological development of lactose-free orodispersible tablets that contain ketoprofen. Methods: We assessed different variables during the pharmaceutical development of ODTs: compression techniques conducted after a wet granulation process, aiming to optimize the flow properties of the formulation, and a suspension freeze-drying molded in blisters. We developed three formulations for each method, each containing one of the superdisintegrants: croscarmellose, crospovidone, or starch glycolate. Result: During the production of ODTs, we performed quality control of the granulation process, since the production of pellets contributed to the enhancement of the disintegration time and content homogeneity. Quality control tests for ODTs produced by freeze-drying were also satisfactory, despite significant changes in the final physical aspect of these products when compared to that of ODTs produced by compression. In addition, the disintegration times of ODTs produced by freeze-drying were substantially higher. Furthermore, these tablets displayed greater friability and pose a challenge to the control of a standard individual weight. Conclusion: Among the superdisintegrants, croscarmellose contributed most significantly to reduce the disintegration time and to dissolve KTP effectively in 20 minutes.


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