Abstract
Sustained release mucoadhesive amoxicillin tablets with tolerance to acid degradation in the stomach were studied. The sustained-release tablets of amoxicillin were prepared from amoxicillin coated with ethyl cellulose (EC) and then formulated into tablets using chitosan (CS) or a mixture of CS and beta-cyclodextrin (CD) as the retard polymer. The effects of various (w/w) ratios of EC/amoxicillin, the particle sized of EC coated amoxicillin and the different (w/w) ratios of CS/CD for the retard polymer, on the amoxicillin release profile were investigated. The physicochemical properties of the EC coated amoxicillin particles and tablets were determined by scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry. The result showed that the release profiles of amoxicillin were greatly improved upon coating with EC, while the inclusion of CD to the CS retardant additionally prolonged the release of the drug slightly. Overall, a sustained release of amoxicillin was achieved using amoxicillin coated with EC at a (w/w) ratio of 1:1 and a particle size of 75–100 μm. Therefore, the tablet formulation of amoxicillin may be an advantageous alternative as an orally administered sustained-release formulation for the treatment of peptic ulcers.
Similar content being viewed by others
REFERENCES
Tokumura T, Machida Y. Preparation of amoxicillin intragastric buoyant sustained-release tablets and the dissolution characteristics. J Control Release. 2006;110:581–6. doi:10.1016/j.jconrel.2005.10.032.
Umamaheshwari RB, Ramteke S, Jain NK. Anti-helicobacter pylori effect of mucoadhesive nanoparticles bearing amoxicillin in experimental gerbils model. AAPS PharmSciTech. 2004;5(2): article 32. doi:10.1208/PT050232
Patel JK, Patel MM. Stomach specific anti-Helicobacter pylori therapy: preparation and evaluation of amoxicillin-loaded chitosan mucoadhesive microspheres. Currt Drug Deliv. 2007;4:41–50.
Sahasathian T, Kerdcholpetch T, Chanweroch A, Praphairaksit N, Suwonjandee N, Muangsin N. Sustained release of amoxicillin from chitosan tablets. Arch Pharm Res. 2007;30(4):526–31. doi:10.1007/BF02980229.
Aki H, Nakashima Y, Kawasaki Y, Niiya T. Thermodynamic evaluation of antibacterial activity for inclusion complexes of amoxicillin with cyclodextrins. J Therm Anal Calorim. 2006;85(3):685–8. doi:10.1007/s10973-006-7650-y.
Nagahara N, Akiyama Y, Masafumi N, Tada M, Kitano M, Ogawa Y. Mucoadhesive microspheres containing amoxicillin for clearance of Helicobacter pylori. Antimicrob Agents Chemother. 1998;42(10):2492–4.
Whitehead L, Collett JH, Fell JT. Amoxicillin release from a floating dosage form based on alginates. Int J Pharm. 2000;210:45–9. doi:10.1016/S0378-5173(00)00567-6.
Xu Y, Hanna MA. Electrosprayed bovine serum albumin-loaded tripolyphosphate cross-linked chitosan capsules: synthesis and characterization. J Microencapsul. 2007;24(2):143–51. doi:10.1080/02652040601058434.
Kofuji K, Ito T, Murata Y, Kawashima S. The controlled release of a drug from biodegradable chitosan gel beads. Chem Pharm Bull. 2000;48(4):579–81.
Arun R, Ashok KCK, Sravanthi VVNSS. Cyclodextrins as drug carrier molecule: a review. Sci Pharm. 2008;76:567–98. doi:10.3797/scipharm.0808-05.
Roux M, Perly B, Pilard FD. Self-assemblies of amphiphilic cyclodextrins. Eur Biophys J. 2007;36:861–7. doi:10.1007/s00249-007-0207-6.
Loftsson T, Duchene D. Cyclodextrins and their pharmaceutical applications. Int J Pharm. 2007;329:1–11. doi:10.1016/j.ijpharm.2006.10.044.
Agrawal AM, Neau SH, Bonate PL. Wet granulation fine particle ethylcellulose tablets: effect of production variables and mathematical modeling of drug release. AAPS PharmSciTech. 2003;13:5(2). doi:10.1208/ps050213
Desai J, Alexander K, Riga A. Characterization of polymeric dispersions of dimenhydrinate in ethyl cellulose for controlled release. Int J Pharm. 2006;308:115–23. doi:10.1016/j.ijpharm.2005.10.034.
Silverstein RM, Bassler GC, Morril TC. Spectrometric identification of organic compounds. New York: Wiley; 1991. p. 91–131.
ACKNOWLEDGMENTS
This work was supported by the Department of Chemistry and Research Funds from the Faculty of Science (A1B1), the Thai Government Stimulus Package 2 (TKK2555), under the Project for Establishment of Comprehensive Center for Innovative Food, Health Products and Agrigulture, Ratchadapisek Somphot Endowment Fund (AG001B) and Center for Petroleum Petrochemicals and Advanced Materials.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Songsurang, K., Pakdeebumrung, J., Praphairaksit, N. et al. Sustained Release of Amoxicillin from Ethyl Cellulose-Coated Amoxicillin/Chitosan–Cyclodextrin-Based Tablets. AAPS PharmSciTech 12, 35–45 (2011). https://doi.org/10.1208/s12249-010-9555-0
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1208/s12249-010-9555-0