Keywords
Dissolution Profile
Quality Control
Beta-lactams
How to Cite
Abstract
Amoxicillin is a broad-spectrum antimicrobial drug used in clinical practice for the treatment of infections, especially those of the respiratory tract. The physicochemical and pharmaceutical properties of amoxicillin make the development of a pharmaceutical preparation with this active principle a great challenge. In this sense, for this substance, it is necessary to consider as barriers in the process of developing a new product its restricted solubility in aqueous medium, as well as its susceptibility to the hydrolysis process. In view of these considerations, dry tablet production proves to be an interesting alternative for the preparation of tablets consisting of amoxicillin. In addition, this route of preparation presents numerous advantages over the industrial production process. Therefore, the objective of this study was to develop compressed dry tablets of amoxicillin and to promote quality control of these tablets. For this, a pharmaceutical formula was proposed using amoxicillin in a therapeutic dose of 500mg, having microcrystalline cellulose, magnesium stearate, anhydrous lactose and croscarmellose sodium as pharmacotechnical adjuvants. The preparation was subsequently subjected to quality control tests represented by: appearance evaluation, average weight, friability, desintegration time and dissolution profile. It was possible to obtain tablets containing amoxicillin with a dissolution profile compatible with immediate release preparations, as well as the suitability of this in the face of other quality control tests.
References
ANSEL, H. C.; POPOVICH, N. G.; ALLEN JR., L. V. Farmacotécnica: formas farmacêuticas e sistemas de liberação de fármacos. 7. ed. São Paulo: Editora Premier, 2000.
AULTON, M. E. Delineamento de formas farmacêuticas. Porto Alegre: Artmed, 2005.
BARICCATTI, R. A. et al. Degradação hidrolítica e fotoquímica da amoxicilina na presença de β-ciclodextrina. Eclética Química. v. 33, p. 79-83, 2008.
BELMAR-LIBERATO, R. et al. Amoxicillin and amoxicillin-clavulanic acid resistance in veterinary medicine – the situation in Europe: a review. Veterinarni Medicina, v. 56, p. 473-485, 2011.
BIRD, A. E. Analytical profiles of drug substances and excipients. v. 23, p. 1-52, 1994.
BOLHUIS, G. K. et al. Comparative evaluation of excipients for direct compression. Pharmaceutisch Weekblad Scientifi, v. 1, p. 203-215, 1979.
BRITISH PHARMACOPOEIA. Londres, 2011.v. 1 e 2.
CAIAFFA, M. C. et al. Estudo biofarmacotécnico de cápsulas de amoxicilina. Análise comparativa de produtos industrializados e magistrais. Cinética de dissolução. Revista Lecta, v. 20, n. 1, p. 77-90, 2002.
FARMACOPEIA Brasileira. 4. ed. São Paulo: Atheneu, 1988. v. 3 e 4.
FU, Y. et al. Orally fast disintegrating tablets: developments, technologies, taste-masking and Clinical Studies. Therapeutic Drug Carrier Systems, v. 21, p. 433-475, 2004.
GOMES, M. L. P. C; SOUZA, S. V. C. Validação de método para determinação de resíduos de amoxicilina aplicado à validação de limpeza em indústria farmacêutica de penicilânicos. Quim. Nova, v. 33, p. 972-977, 2010.
GORDON, M. S. et al. Effect of the mode of croscarmellose sodium incorporation on tablet dissolution and friability. J. Pharm. Sci., v. 79, p. 43-47, 1990.
GRESSER, U. Amoxicillin-clavulanic acid therapy may be associated with severe side effects – review of the literature. European Journal of Medical Research, v. 6, p. 139-149, 2001.
GUJRAL, R. S.; HAQUE, S. M. Simultaneous Determination of Potassium Clavulanate and Amoxicillin Trihydrate in Bulk, Pharmaceutical Formulations and in Human Urine Samples by UV Spectrophotometry. International Journal of Biomedical Science, v. 6, p. 335-343, 2010.
HANDBOOK OF PHARMACEUTICAL EXCIPIENTS. 6. ed. Pharmaceutical Press: London, 2009.
HARDMAN, J. G.; LIMBIRD, L. E. As bases farmacológicas da Terapêutica. 10. ed. Rio de Janeiro: Editora McGrow-Hill, 2004.
HASSAN, M. A. J.; NAJIB, N. M.; SULEIMAN, M. S. Characterization of glibenclamide glassy state. Int. J. Pharm. v. 67, p. 131-137, 1991.
HILTON, A. K.; DEASY, P. B. In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihidrate. Int. J. Pharm., v. 86, p. 79-88, 1993.
ISHIKAWA, T. et al. Preparation of Rapidly Disintegrating Tablet Using New Types of Microcrystalline Cellulose (PH-M Series) and Low Substituted- hydroxypropylcellulose or Spherical Sugar Granules by Direct Compression Method. Chem. Pharm. Bull., v. 49, p. 134-139, 2001.
KOROLKOVAS, A. Dicionário Terapêutico Guanabara. Rio de Janeiro: Guanabara Koogan, 1995.
LE HIR, A. Noções de Farmácia Galênica. 6. ed. São Paulo: Andrei, 1997.
MARTINDALE: The Extra Pharmacopoeia. London, The Royal Pharmaceutical Society, 1996.
ORTOFARMA: ESTUDO DE PERFIL DE DISSOLUÇÃO. Cápsulas de Amoxicilina (como tri-hidratada) 500mg. Disponível em: http://www.ortofarma.com.br/INTRANET/Web%20Forms/arquivos. Acesso em: 20 nov. 2011.
PALACIOS, A. Realidade em granulação e compresssão direta. A Fórmula, n. 1, p. 12-13, 2000.
PASQUALOTO, K. F. M. et al. Development and Evaluation of Amoxicillin Formulations by Direct Compression: Influence of the Adjuvants on Physicomechanical and Biopharmaceutical Properties of the Tablets. Acta Farm. Bonaerense, v. 24, p. 39-47, 2005.
PATIL, D. M.; PATHADE, B. A; BAIRAGI, V. A. Design and Evaluation of bilayer floating tablets of amoxicillin tryhydrate. Int. J. Res. Pharm. Sci., v. 2, p. 366-372, 2011.
PRISTA, L. N. et al. Tecnologia Farmacêutica. 5. ed. Lisboa: Fundação Calouste Gulbenkian, 1995.
RAVAL, J.; PATEL, J.; PATEL, M. Formulation and in vitro characterization of spray dried microspheres of amoxicillin. Acta Pharm., v. 60, p. 455-465, 2010.
REIER, G. E.; SHANGRA, W. Use of hydroxypropyl methylcellulose acetate succinate in an enteric polymer matrix to design controlled release tablets of amoxicillin trihydrate. Journal of Pharmaceutical Science, v. 55, p. 510-514, 2006.
REIS, A. M. M.; MOREIRA, L. M. M.; PIANETTI, G. A. Estudo da Biodisponibilidade de comprimidos de carbonato de cálcio. Rev. Bras. Farm., v. 84, p. 75-79, 2003.
SOUZA, T. P.; SPANIOL, B.; PETROVICK, P. R. Avaliação de comprimidos revestidos por película contendo alta concentração de produto seco por aspersão de Phyllanthus niruri. Acta Farm. Bonaerense, v. 24, p. 61-67, 2005.
UNITED STATES PHARMACOPEIA. 22. ed. Rockville: United States Pharmacopeial Convention, 1989.
UNITED STATES PHAMACOEIA. 23. ed. Rockville: United States Pharmacopoeial Convention, 1995.
WANCZINSKI, B. J. et al. Desenvolvimento de comprimidos de AAS 500 mg: influência do Amido 1500® na compressão direta. Acta Scientiarum, v. 24, p. 649-655, 2002.
WHITE, A. R. et al. Augmentin® (amoxicillin/clavulanate) in the treatment of community-acquired respiratory tract infection: a review of the continuing development of an innovative antimicrobial agent. Journal of Antimicrobial Chemotherapy., v. 53, p. 3-20, 2004.
WU, Y. et al. Properties of application of impinging streams. Chem. Indus. Eng. Progress., v. 20, n. 11, p. 8-13, 2001.
ZADE, P. S. et al. Formulation, Evaluation and Optimization of Fast dissolving tablet containing Tizanidine Hydrochloride. International Journal of PharmTech Research., v. 1, p. 34-42, 2009.
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