scholarly journals A Comparative Evaluation of Fast Dissolving Tablets of Acetaminophen Using Super-disintegrant Blends and Sublimation Method

2020 ◽  
Vol 19 (1) ◽  
pp. 375-386
Author(s):  
S.O. Eraga ◽  
C.M. Okolo ◽  
B.U. Odionyenma ◽  
C.E. Mbadugha ◽  
M.A. Iwuagwu

Fast disintegrating tablets (FDTs) are gaining prominence as drug delivery systems and emerging as one of the popular and widely accepted dosage forms, especially for the peadiatric and geriatric patients. This study aims to evaluate and compare the tablet properties of fast disintegrating tablets of acetaminophen prepared by super-disintegrant blends and sublimation methods. Two groups of tablets comprising various batches were prepared by wet granulation. Granules batches of one group of tablets (A-G) were prepared with different concentrations of sodium starch glycolate and croscarmellose sodium while the other group of tablets (H-N) were incorporated with varying concentrations of menthol into the batches. The granules were subjected to analysis and compressed into tablets. The post-compression parameters of the tablets such as weight uniformity, crushing strength, friability, wetting and disintegration times, as well as dissolution studies were evaluated. Drug-excipient compatibility studies using Fourier transform infrared (FTIR) analysis was also carried out. Granules were fair to good in flow with Carr’s indices ≤ 20.14 and angles of repose ranging from 21.34 to 35.00°. Tablets crushing strength values were between 3.44 to 8.26 kp while their friability values were < 1.52%. They showed wetting and disintegration times that were ≥ 0.18 and ≥ 0.25 min. Dissolution studies showed that four batches of tablets (two from each method used in formulation) achieved 100% drug release within 30 min. FTIR analysis shows no interactions between acetaminophen and excipients used in formulation. Tablets from both methods were comparable in their tablet properties but the disintegrant blend tablets exhibited superior crushing strengths, hence formed harder tablets, while the sublimation method tablets were superior in their wetting and disintegration times. Keywords: acetaminophen, super-disintegrants, sublimation, tablet parameters

2015 ◽  
Vol 13 (2) ◽  
pp. 199-205
Author(s):  
Eraga Sylvester Okhuelegbe ◽  
Arhewoh Matthew Ikhuoria ◽  
Ajah Anthony Ike

Fast disintegrating tablets of nifedipine prepared by superdisintegrant addition and sublimation methods were evaluated. Twelve batches of tablets were formulated by direct compression using varying concentrations of crospovidone and croscarmellose sodium. Camphor was incorporated into six of the batches. Their granules were evaluated for pre-compression and post-compression parameters. FTIR analysis of the drug and excipients was also carried out. Results obtained showed that their granules were free flowing with angle of repose < 26° and Carr’s index < 19 %. The tablets gave hardness of 3.67-5.99 kgf, friability of < 1 %, wetting and disintegration times of < 101 and < 91 secs, respectively. Dissolution profiles showed all the tablets released over 92 % of their drug within 30 mins. FTIR analysis demonstrated no interactions between nifedipine and excipients. The sublimation method in combination with superdisintegrant addition method of formulation yielded fast disintegrating tablets of superior quality than the superdisintegrant addition method alone. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21901 Dhaka Univ. J. Pharm. Sci. 13(2): 199-205, 2014 (December)


Author(s):  
PRADIP KUMAR CHAUDHARY ◽  
ABDUL RAHEEM T. ◽  
MANJUNATH U MACHALE ◽  
VASIA ◽  
SHAIK SADIK

Objective: The aim of the present study was to prepare and optimize levamisole chewable tablets by using various super disintegrants, namely; sodium starch glycolate, DRC Indion 204, and DRC Indion 234. Methods: Drug excipient compatibility study was carried out by FTIR spectroscopy to verify the compatibility of levamisole with the excipients. Nine batches of levamisole chewable tablets were prepared according to 32 factorial designs using a direct compression method by optimizing the super disintegrant concentration. The powder blend was exposed to pre-compression studies of the powder blend followed by post-compression studies of the formulated tablets. Results: FTIR study revealed that the excipients used in the formulations were compatible with the drug. The pre-compression and post-compression parameters were found within the IP limits. Form the dissolution studies, it was evident that the formulation prepared with DRC Indion 234 (50 mg) showed maximum percentage drug release in 45 min (97.13%) hence it is considered as optimized formulation. When compared to all other formulation, the batches with DRC Indion 234 (F7-F9) showed a better release of the drug (90 % drug release within 45 min). Conclusion: Nine batches of levamisole chewable tablets were successfully formulated by optimizing the concentration of super disintegrants such as sodium starch glycolate, DRC Indion 204, and DRC Indion 234. It was concluded from the dissolution studies that the DRC Indion 234 is the best super disintegrant irrespective of their concentration for the formulation of levamisole chewable tablets when compared to sodium starch Glycolate and DRC Indion 204.


2019 ◽  
Vol 9 (3) ◽  
pp. 8-12
Author(s):  
B. Divya ◽  
J. Sreekanth ◽  
D. Satyavati

Extended release products are designed to release their medication in a controlled manner at a predetermined rate, duration, and location to achieve and maintain optimum therapeutic blood levels of a drug. The objective of the study is to formulate and evaluate Ilaprazole Controlled release tablets comparable to the innovator product. F1-F9 formulations were prepared using varying concentrations of super disintegrates like Crospovidone, Croscarmellose sodium and Sodium starch glycolate in different concentrations. Based on the hardness, friability, weight variation, drug content, F6 formulation was found to be optimised. The selected F6 formulation was sub coated with HPMC P 50 and followed by enteric coating with Acryl-EZE-80 (Eudragit L100-55). 3 formulations (F10-F12) were prepared by using coating. Among the three formulations, F11 formulation was found to be best. FTIR studies were carried out to find out drug and excipient compatibility studies, the studies revealed that there were no interactions. DSC studies also carried out to demonstrate any changes in physical forms of the drug molecule. Keywords: Ilaprazole, Extended release tablets, Crospovidone, Croscarmellose sodium, Sodium starch glycolate, HPMC P 50, Acryl-EZE-80.


2018 ◽  
Vol 10 (5) ◽  
pp. 270
Author(s):  
Asmaa A. Bayoumi

Objective: The scope of this work was to formulate sitagliptin and simvastatin rapidly dissolving tablets. However, simvastatin is practically insoluble in water. For improving its poor oral bioavailability and with the aim of facilitating administration to patients facing problems with swallowing rapidly dissolving tablets were preparedMethods: Tablets were prepared using superdisintegrant addition technique using croscarmellose sodium (Ac-di-sol), sodium starch glycolate (explotab) and crospovidone in different percentages. Evaluation tests such as weight variation, thickness, and content variation, and friability, disintegration, wetting time, in vitro dispersion and in vitro dissolution were carried out.Results: The results showed that the presence of crospovidone could enhance the dissolution rate of simvastatin greatly. The best-optimized formulae found were that F8, F9, and F10 which showed good disintegration and the dissolution rate of simvastatin and sitagliptin was more than 90% after 10 min while the dissolution rate for simvastatin and sitagliptin pure standards was 12% and 30%, respectively after 10 min.Conclusion: Some tablet formulae showed acceptable pharmacotechnical properties and complied with compendium requirements. Results of dissolution studies revealed that F8-F10 showed an increase in the dissolved sitagliptin and simvastatin to be more than 90% after 10 min. 


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.


2019 ◽  
Vol 9 (4-A) ◽  
pp. 442-449
Author(s):  
SM Shahidulla ◽  
Tayyaba Jeelani

Labetalol Hydrochloride is a β-blocker generally indicated for the treatment of hypertension, and it is extensively metabolized due to the hepatic metabolism. In the present work, an attempt was made to mask the taste by Solid Dispersion technique, with a formulation into Fast Disintegrating dosage form, using superdisintegrants such as Cross carmellose sodium (CCS), crospovidone (CP) and sodium starch glycolate (SSG). The complexes of Labetalol hydrochloride with HP-β-CD (1:3 ratio) were prepared by Co-precipitation method. Using the drug HP-β-CD complex, Fast Disintegrating tablets were prepared by Wet granulation Technique and evaluated for hardness, friability, weight variation, thickness, disintegrating time (DT), In-vitro dispersion time and  dissolution rate. The results of Direct compression optimized formulation WG9 (Sodium Starch Glycolate 15mg and Starch paste 18mg) has shown the % Drug release of  99.97%, In-vitro Dispersion time of 16 Secs respectively. Keywords: Solid dispersions, fast disintegrating tablets, Labetalol, Crospovidone, Croscarmellose sodium and Sodium starch glycolate.


Author(s):  
Suresh Kulkarni ◽  
Ranjit P. ◽  
Nikunj Patel ◽  
Someshwara B. ◽  
Ramesh B. ◽  
...  

The present investigation deals with the formulation of fast disintegrating tablets of Meloxicam that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Meloxicam is a newer selective COX-1 inhibitor. The tablets were prepared by wet granulation procedure. The influence of superdisintegrants, crosspovidone, croscaremellose sodium on disintegration time, wetting time and water absorption ratio were studied. Tablets were evaluated for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disintegrating tablets was found to be 18 sec. Tablets containing crospovidone exhibit quick disintegration time than tablets containing croscaremellose sodium. The fast disintegrating tablets of Meloxicam with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.


Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.


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.  


Author(s):  
Ashok Thulluru ◽  
Veeravalli Kumar Sai ◽  
Pavan Kumar M ◽  
Roshitha B

ABSTRACTObjective: The current research work is intended to formulate propranolol HCl (PLH) as orally disintegrating tablet (ODT). It is also intending to checkthe superiority in a combination of superdisintegrants and effervescent mixture than the use of superdisintegrants alone by a direct compressiontechnique. To fasten the onset of action and thereby enhancing the bioavailability of PLH in comparison to its conventional tablets.Methods: Standard calibration curve of PLH was obtained in pH 6.8 phosphate buffer by spectrophotometric method, drug-excipient compatibilitystudies were carried by Fourier transform infrared (FT-IR) studies. All the formulations were evaluated for pre and postcompression studies.Accelerated stability studies were carried out up to 6 months for the optimized formulation, EF3.Results and Discussion: Superdisintegrants used in the study are compatible with PLH. Pre- and post-compression parameters were within theacceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of PLH from ODT increases as the concentration ofsuperdisintegrants as well as the ratio of citric acid: NaHCO3 of effervescent mixture increases. Formulations with an effervescent mixture are havingrapid disintegration and dissolution rate when compared to the formulations with superdisintegrants alone. The order of superdisintegrants inenhancing the dissolution rate of PLH is crospovidone (CPV) > croscarmellose sodium (CCS) > sodium starch glycolate (SSG). Formulation, EF3 (10%CPV and 1:3, citric acid: NaHCO3 ratio, respectively) had the highest dissolution efficiency at 10 minutes (DE10=82.74%); the first order dissolutionrate constant (K1=0.141/minutes) with a regression coefficient (r2=0.974) and lesser time for 90% of drug release (t90=4 minutes), was considered asthe optimal ODT in this study. Formulation EF3, passed the test for stability.Conclusion: Hence, an effective PLH ODT was formulated by the direct compression technique with disintegration by combination of superdisintegrantsand effervescent mixture, will fasten the onset of action and enhances the bioavailability of PLH in comparison to its conventional tablets.Keywords: Propranolol HCl, Orally disintegrating tablet, Sodium starch glycolate, Croscarmellose sodium, Crospovidone, Direct compression, In vitrodissolution studies.


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