Formulation, characterization and physicochemical evaluation of amoxicillin effervescent tablets

Authors

Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran

Abstract

Background: Amoxicillin is a semisynthetic antibiotic, which is used as an antimicrobial drug. This study was designed to formulate amoxicillin effervescent tablets, aimed at improved patient compliance and increased drug stability.
Materials and Methods: In this study, nine effervescent tablet formulations were prepared from amoxicillin trihydrate. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Powders and granules were evaluated for their particle size, bulk density, tapped density, compressibility index, Hausner's ratio and angle of repose. The effervescent tablets were then prepared from powders and granules of acceptable quality by direct compression and fusion methods. The tablets were evaluated for weight variation, friability, pH of solution, carbon dioxide (CO 2 ) content, hardness, effervescence time, thickness, assay, content uniformity, water content and equilibrium moisture content.
Results: The results indicated better flowability of granules prepared by fusion method as compared with the direct compression. The percent weight variations of tablets were within the acceptable limit of 0.5%. The friability was less than 1% in all formulations. The solution pH of tablets prepared by direct compression and fusion methods ranged from 4.55 to 5.74 and 4.74-5.84, respectively. The CO 2 amounts generated by of fusion method tablets were smaller as compared to the direct compression method. The hardness of tablets was 40.66-56 for direct compression method and 60.6-74.6 for fusion method. The tablets produced by the fusion method had a larger thickness and lower water content than tablets produced by direct compression method.
Conclusion: Tablets prepared by the fusion method exhibited superior pre- and post-compression characteristics as compared to tablets prepared by direct compression method.

Keywords

1.
Palanisamy P, Abhishehn R, Yoganand KD. Formulation and evaluation of effervescent tablets of aceclofenac. Inter Res J Pharmacol 2011;2:185-90.  Back to cited text no. 1
    
2.
European Pharmacopeia. 5 th ed. Strasbourg Cedex, France: Council of Europe; 2007. p. 749, 1193.  Back to cited text no. 2
    
3.
Altomare E, Vendemiale G, Benvenuti C, Andreatta P. Bioavailability of a new effervescent tablet of ibuprofen in healthy volunteers. Eur J Clin Pharmacol 1997;52:505-6.  Back to cited text no. 3
    
4.
Hedges A, Kaye CM, Maclay WP, Turner P. A comparison of the absorption of effervescent preparations of paracetamol and penicillin V (phenoxymethylpenicillin) with solid dose forms of these drugs. J Clin Pharmacol 1974;14:363-8.  Back to cited text no. 4
    
5.
Lee RE. Effervescent tablets. Available from: http://www.amerilabtech.com/wp-content/uploads/EffervescentTabletsKeyFacts.pdf. [Last accessed on 2011 Dec 20].  Back to cited text no. 5
    
6.
Lachman L, Liberman HA, Kaning JL. The theory and practice of industrial pharmacy. 3 rd ed. Philadelphia: Lea and Febiger; 1987. p. 334-410.  Back to cited text no. 6
    
7.
Srinath KR, Pooja Chowdary C, Palaniamy P, Krishna V, Aparna S. Formulation and evaluation of effervescent tablets of paracetamol. Inter J Pharmacol Res Dev 2011;3:76-104.  Back to cited text no. 7
    
8.
Strickley RG, Iwata Q, Wu S, Dahl TC. Pediatric drugs - A review of commercially available oral formulations. J Pharm Sci 2008;97:1731-74.  Back to cited text no. 8
    
9.
Hespe W, Verschoor JS, Olthoff M. Bioavailability of new formulations of amoxicillin in relation to its absorption kinetics. Arzneimittelforschung 1987;37:372-5.  Back to cited text no. 9
    
10.
Amela J, Salazar R, Cemeli J. Effervescent tablets of ascorbic acid I. Physical study of the possible components to be used. Drug Dev Ind Pharm 1996;22:407-16.  Back to cited text no. 10
    
11.
Eichman JD, Robinson JR. Mechanistic studies on effervescent-induced permeability enhancement. Pharm Res 1998;15:925-30.  Back to cited text no. 11
    
12.
Kaye CM, Allen A, Perry S, McDonagh M, Davy M, Storm K, et al. The clinical pharmacokinetics of a new pharmacokinetically enhanced formulation of amoxicillin/clavulanate. Clin Ther 2001;23:578-84.  Back to cited text no. 12
    
13.
Cooreman MP, Krausgrill P, Hengels KJ. Local gastric and serum amoxicillin concentrations after different oral application forms. Antimicrob Agents Chemother 1993;37:1506-9.  Back to cited text no. 13
    
14.
File TM Jr. The development of pharmacokinetically enhanced amoxicillin/clavulanate for the management of respiratory tract infections in adults. Int J Antimicrob Agents 2007;30 Suppl 2:S131-4.  Back to cited text no. 14
    
15.
Hoizey G, Lamiable D, Frances C, Trenque C, Kaltenbach M. Simultaneous determination of amoxicillin and clavulanic acid in human plasma by HPLC with UV detection. J Pharm Bio Anal 2002;30:661-6.  Back to cited text no. 15
    
16.
Kraus G, Shimidt PC. Optimization of an effervescent formulation using a central composite design optimization of an effervescent tablet formulation containing spray dried L-lucine and polyethylene glycol 6000 as lubricants using a central composite design. Eur J Pharm Biopharm 1998;46:85-94.  Back to cited text no. 16
    
17.
Murray RB. New approach to the fusion method for preparing granular effervescent products. J Pharm Sci 1968;57:1776-9.  Back to cited text no. 17
    
18.
Yanze FM, Duru C, Jacob M. A process to produce effervescent tablets: Fluidized bed dryer melt granulation. Drug Dev Ind Pharm 2000;26:1167-76.  Back to cited text no. 18
    
19.
Moghimipour E, Akhgari A, Ghassemian Z. Formulation of glucosamine effervescent granules. Sci Med J 2010;9:21-34.  Back to cited text no. 19
    
20.
Remington's Pharmaceutical Sciences, the science and practice of pharmacy 21 st ed. Eastrol, Pennsylvania: Mack Publishing Company; 2006. p. 895-6, 900, 916-7.  Back to cited text no. 20
    
21.
The United State Pharmacopeia and National Formulary. 29 th ed. Washington: The United State Pharmacopeia and Convention; 2006. p. 9, 209, 640-1, 675, 3157-8.  Back to cited text no. 21
    
22.
Kschmit M, Heinz-Dieter I. Fischer titration a method for determination the true water content of cereals. Fresenius J Anal Chem 1998;360:465-9.  Back to cited text no. 22
    
23.
Aslani A, Fattahi F. Formulation, characterization and physicochemical evaluation of potassium citrate effervescent tablets. APB 2013;3:217-25.  Back to cited text no. 23
    
24.
Aslani A, Jahangiri H. Formulation, characterization and physicochemical evaluation of effervescent ranitidine hydrochloride tablets. APB 2013;3:315-22.  Back to cited text no. 24