Avaliação da Goma Guar no desenvolvimento de comprimidos matriciais de liberação controlada de teofilina
Evaluation of Guar Gum in the development of theophylline controlled-release matrix tablets
Oliveira, Edilene Gadelha de; Campos, Rosana de Sousa; Machado, Anaiara Silva; Pereira, Juliana Fernandes; Araújo, Tamara Gonçalves de
http://dx.doi.org/10.1590/0104-1428.1756
Polímeros: Ciência e Tecnologia, vol.25, nSuppl, p.54-58, 2015
Resumo
O objetivo desse estudo foi formular e avaliar comprimidos de liberação controlada. Comprimidos de liberação controlada de teofilina foram preparadas pelo método de compressão direta usando dois polímeros como, o HPMC K 100M (polímero hidrofílico) e a Goma Guar (Polímero natural), isolado ou em mistura (GG:HPMC 3:1) e GG:HPMC 1:3). Os comprimidos foram caracterizados através do peso médio, diâmetro, altura, dureza, friabilidade. Todos os resultados estiveram em conformidade com os limites aceitáveis. O ensaio de intumescimento foi realizado em água destilada durante 4 horas, sendo determinado pela diferença de peso do comprimido seco e intumescido. O ensaio de dissolução foi realizado em água destilada (900 mL, 37 ± 0,5ºC, 50 rpm, aparato II) durante 8 horas. Os resultados demonstraram que a Goma guar isolada não possui capacidade de retardar a liberação da teofilina por 8 horas. Comprimidos matriciais contendo GG:HPMC (3:1) apresentaram um melhor controle de liberação da teofilina.
Palavras-chave
Goma Guar, teofilina, comprimidos, liberação controlada.
Abstract
Guar gum (GG) has been widely used in drug delivery systems due to its low cost and nontoxicity. Theophylline controlled release tablets were prepared by directly compressed method using two polymers such as HPMC K 100M (hydrophilic polymer) and Guar Gum (natural polymer), isolated or in mixture (GG:HPMC 3:1 and GG:HPMC 1:3). The formulated tablets were evaluated for: weight variation, diameter, height, hardness and friability. All the parameters were within the acceptable limits. The swelling test was performed in distilled water for 4 hours, it was determined by the difference in weight of the dry and swollen tablet. The dissolution test was performed in distilled water (900 mL, 37 ± 0.5ºC, 50 rpm, apparatus II) for 8 hours. The results showed that guar gum alone could not control the theophylline release effectively for 8 hours. Matrix tablet prepared from GG: HPMC (3:1) is a better formulation for the sustained released matrix tablets of theophylline.
Keywords
Guar Gum, theophylline, tablets, controlled release.
References
1. El-bagory, I., Barakat, N., Ibrahim, M. A., & El-enazi, F. (2012). Formulation and in vitro evaluation of theophylline matrix tablets prepared by direct compression: effect of polymer blends. Saudi Pharmaceutical Journal, 20(3), 229-238. http://dx.doi.org/10.1016/j.jsps.2011.11.007.
2. Freitas, A. B. R., & Cavalcanti, O. A. (2004). Goma Guar como excipiente em matrizes hidrofílicas: avaliação do índice de hidratação. Acta Farmaceutica Bonaerense, 23(3), 334-338. Recuperado em 30 de abril de 2014, de http://www.latamjpharm.org/trabajos/23/3/LAJOP_23_3_1_10_I8YB5IGLFQ.pdf
3. Cavalcanti, O. A. (2002). Excipientes farmacêuticos: perspectivas dos polissacarídeos na pesquisa e desenvolvimento de novos sistemas de liberação. Arquivos de Ciências da Saúde Unipar, 6(1), 53-56. Recuperado em 30 de abril de 2014, de http://revistas.unipar.br/saude/article/view/1151/1013
4. Pezzini, B. R., Silva, M. A. S., & Ferraz, H. G. (2007). Formas farmacêuticas sólidas orais de liberação prolongada: sistemas monolíticos e multiparticulados. Revista Brasileira de Ciências Farmacêuticas, 43(4), 491-502. http://dx.doi.org/10.1590/S1516-93322007000400002.
5. Lopes, C. M., Lobo, J. M. S., & Costa, P. (2005). Formas farmacêuticas de liberação modificada: polímeros hidrofílicos. Revista Brasileira de Ciências Farmacêuticas, 41(2), 143-154. http://dx.doi.org/10.1590/S1516-93322005000200003.
6. Vueba, M. L., Batista de Carvalho, L. A. E., Veiga, F., Sousa, J. J., & Pina, M. E. (2004). Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets. European Journal of Pharmaceutics and Biopharmaceutics, 58(1), 51-59. http://dx.doi.org/10.1016/j.ejpb.2004.03.006. PMid:15207537.
7. Gonçalves-Araújo, T., Rajabi-Siahboomi, A. R., & Caraballo, I. (2008). Application of percolation theory in the study of an extended release Verapamil hydrochloride formulation. International Journal of Pharmaceutics, 361(1-2), 112-117. http://dx.doi.org/10.1016/j.ijpharm.2008.05.022. PMid:18621491.
8. Novak, S. D., Šporar, E., Baumgartner, S., & Vrečer, F. (2012). Characterization of physicochemical properties of hydroxypropyl methylcellulose (HPMC) type 2208 and their influence on prolonged drug release from matrix tablets. Journal of Pharmaceutical and Biomedical Analysis, 66, 136-143. http://dx.doi.org/10.1016/j.jpba.2012.03.032. PMid:22510313.
9. Barakat, N. S., Elbagory, I. M., & Almurshedi, A. S. (2008). Controlled-release carbamazepine granules and tablets comprising lipophilic and hydrophilic matrix components. AAPS PharmSciTech, 9(4), 1054-1062. http://dx.doi.org/10.1208/s12249-008-9140-y. PMid:18843537.
10. Srivastava, P., Malviya, R., Gupta, S., & Sharma, P. K. (2010). Evaluation of various natural Gums as release modifiers in tablet formulations. Pharmacognosy Journal, 2(13), 525-529. http://dx.doi.org/10.1016/S0975-3575(10)80055-0.
11. Vendruscolo, C. W., Andreazza, I. F., Ganter, J. L. M. S., Ferrero, C., & Bresolin, T. M. B. (2005). Xanthan and galactomannan (from M. scabrella) matrix tablets for oral controlled delivery of theophylline. International Journal of Pharmaceutics, 296(1-2), 1-11. http://dx.doi.org/10.1016/j.ijpharm.2005.02.007. PMid:15885450.
12. Wu, B., Chen, Z., Wei, X., Sun, N., Lu, Y., & Wu, W. (2007). Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: I. Characterization and mechanistic study. European Journal of Pharmaceutics and Biopharmaceutics, 67(3), 707-714. http://dx.doi.org/10.1016/j.ejpb.2007.04.016. PMid:17540549.
13. Hodges, L. A., Connolly, S. M., Band, J., O’Mahony, B., Ugurlu, T., Turkoglu, M., Wilson, C. G., & Stevens, H. N. E. (2009). Scintigraphic evaluation of colon targeting pectin-HPMC tablets in healthy volunteers. International Journal of Pharmaceutics, 370(1-2), 144-150. http://dx.doi.org/10.1016/j.ijpharm.2008.12.002. PMid:19114096.
14. Jian, H., Zhu, L., Zhang, W., Sun, D., & Jiang, J. (2012). Galactomannan (from Gleditsia sinensis Lam.) and xanthan gum matrix tablets for controlled delivery of theophylline: In vitro drug release and swelling behavior. Carbohydrate Polymers, 87(3), 2176-2182. http://dx.doi.org/10.1016/j.carbpol.2011.10.043.
15. Serafin, W. E. (2005). Fármacos usados no tratamento da asma. In J. G. Hardman, L.E. Limbird, P. B. Molinoff, R. W. Ruddon, & A. G. Gilman (Ed.), Goodman & Gilman’s: as bases farmacológicas da terapêutica (13. ed., pp. 409-412). Rio de Janeiro: Guanabara Koogan.
16. Agência Nacional de Vigilância Sanitária. (2010). Farmacopeia Brasileira. Brasília: Editora Fiocruz.
17. Efentakis, M., Vlachou, M., & Choulis, N. H. (1997). Effects of excipients on swelling and drug release from compressed matrices. Drug Development and Industrial Pharmacy, 23(1), 107-112. http://dx.doi.org/10.3109/03639049709148487.
18. United States Pharmacopeial Convention .(2007). The United States Pharmacopeia (USP). Rockville: USP.
19. Gliko-Kabir, I., Yagen, B., Penhasi, A., & Rubinstein, A. (2000). Phosphated crosslinked guar for colon-specific drug delivery: I. Preparation and physicochemical characterization. Journal of Controlled Release, 63(1–2), 121-127. http://dx.doi.org/10.1016/S0168-3659(99)00179-0. PMid:10640585.
20. Krishnaiah, Y. S. R., Karthikeyan, R. S., & Satyanarayana, V. (2002). A three-layer guar gum matrix tablet for oral controlled delivery of highly soluble metoprolol tartrate. International Journal of Pharmaceutics, 241(2), 353-366. http://dx.doi.org/10.1016/S0378-5173(02)00273-9. PMid:12100863.
21. Singh, R., Maity, S., & Sa, B. (2014). Effect of ionic crosslink on the release of metronidazole from partially carboxymethylated guar gum tablet. Carbohydrate Polymers, 106, 414-421. http://dx.doi.org/10.1016/j.carbpol.2014.01.033. PMid:24721097.
22. Herder, J., Adolfsson, A., & Larsson, A. (2006). Initial studies of water granulation of eight grades of hypromellose (HPMC). International Journal of Pharmaceutics, 313(1-2), 57-65. http://dx.doi.org/10.1016/j.ijpharm.2006.01.024. PMid:16510256.
23. Ojoe, E., Miyauchi, E. M., Kaneko, T. M., Velasco, M. V. R., & Consiglieri, V. O. (2007). Influence of cellulose polymers type on in vitro controlled release tablets containing theophylline. Revista Brasileira de Ciências Farmacêuticas, 43(4), 571-579. http://dx.doi.org/10.1590/S1516-93322007000400010.
24. Viridén, A., Abrahmsén-Alami, S., Wittgren, B., & Larsson, A. (2011). Release of theophylline and carbamazepine from matrix tablets – consequences of HPMC chemical heterogeneity. European Journal of Pharmaceutics and Biopharmaceutics, 78(3), 470-471. http://dx.doi.org/10.1016/j.ejpb.2011.02.003. PMid:21316446.
2. Freitas, A. B. R., & Cavalcanti, O. A. (2004). Goma Guar como excipiente em matrizes hidrofílicas: avaliação do índice de hidratação. Acta Farmaceutica Bonaerense, 23(3), 334-338. Recuperado em 30 de abril de 2014, de http://www.latamjpharm.org/trabajos/23/3/LAJOP_23_3_1_10_I8YB5IGLFQ.pdf
3. Cavalcanti, O. A. (2002). Excipientes farmacêuticos: perspectivas dos polissacarídeos na pesquisa e desenvolvimento de novos sistemas de liberação. Arquivos de Ciências da Saúde Unipar, 6(1), 53-56. Recuperado em 30 de abril de 2014, de http://revistas.unipar.br/saude/article/view/1151/1013
4. Pezzini, B. R., Silva, M. A. S., & Ferraz, H. G. (2007). Formas farmacêuticas sólidas orais de liberação prolongada: sistemas monolíticos e multiparticulados. Revista Brasileira de Ciências Farmacêuticas, 43(4), 491-502. http://dx.doi.org/10.1590/S1516-93322007000400002.
5. Lopes, C. M., Lobo, J. M. S., & Costa, P. (2005). Formas farmacêuticas de liberação modificada: polímeros hidrofílicos. Revista Brasileira de Ciências Farmacêuticas, 41(2), 143-154. http://dx.doi.org/10.1590/S1516-93322005000200003.
6. Vueba, M. L., Batista de Carvalho, L. A. E., Veiga, F., Sousa, J. J., & Pina, M. E. (2004). Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets. European Journal of Pharmaceutics and Biopharmaceutics, 58(1), 51-59. http://dx.doi.org/10.1016/j.ejpb.2004.03.006. PMid:15207537.
7. Gonçalves-Araújo, T., Rajabi-Siahboomi, A. R., & Caraballo, I. (2008). Application of percolation theory in the study of an extended release Verapamil hydrochloride formulation. International Journal of Pharmaceutics, 361(1-2), 112-117. http://dx.doi.org/10.1016/j.ijpharm.2008.05.022. PMid:18621491.
8. Novak, S. D., Šporar, E., Baumgartner, S., & Vrečer, F. (2012). Characterization of physicochemical properties of hydroxypropyl methylcellulose (HPMC) type 2208 and their influence on prolonged drug release from matrix tablets. Journal of Pharmaceutical and Biomedical Analysis, 66, 136-143. http://dx.doi.org/10.1016/j.jpba.2012.03.032. PMid:22510313.
9. Barakat, N. S., Elbagory, I. M., & Almurshedi, A. S. (2008). Controlled-release carbamazepine granules and tablets comprising lipophilic and hydrophilic matrix components. AAPS PharmSciTech, 9(4), 1054-1062. http://dx.doi.org/10.1208/s12249-008-9140-y. PMid:18843537.
10. Srivastava, P., Malviya, R., Gupta, S., & Sharma, P. K. (2010). Evaluation of various natural Gums as release modifiers in tablet formulations. Pharmacognosy Journal, 2(13), 525-529. http://dx.doi.org/10.1016/S0975-3575(10)80055-0.
11. Vendruscolo, C. W., Andreazza, I. F., Ganter, J. L. M. S., Ferrero, C., & Bresolin, T. M. B. (2005). Xanthan and galactomannan (from M. scabrella) matrix tablets for oral controlled delivery of theophylline. International Journal of Pharmaceutics, 296(1-2), 1-11. http://dx.doi.org/10.1016/j.ijpharm.2005.02.007. PMid:15885450.
12. Wu, B., Chen, Z., Wei, X., Sun, N., Lu, Y., & Wu, W. (2007). Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: I. Characterization and mechanistic study. European Journal of Pharmaceutics and Biopharmaceutics, 67(3), 707-714. http://dx.doi.org/10.1016/j.ejpb.2007.04.016. PMid:17540549.
13. Hodges, L. A., Connolly, S. M., Band, J., O’Mahony, B., Ugurlu, T., Turkoglu, M., Wilson, C. G., & Stevens, H. N. E. (2009). Scintigraphic evaluation of colon targeting pectin-HPMC tablets in healthy volunteers. International Journal of Pharmaceutics, 370(1-2), 144-150. http://dx.doi.org/10.1016/j.ijpharm.2008.12.002. PMid:19114096.
14. Jian, H., Zhu, L., Zhang, W., Sun, D., & Jiang, J. (2012). Galactomannan (from Gleditsia sinensis Lam.) and xanthan gum matrix tablets for controlled delivery of theophylline: In vitro drug release and swelling behavior. Carbohydrate Polymers, 87(3), 2176-2182. http://dx.doi.org/10.1016/j.carbpol.2011.10.043.
15. Serafin, W. E. (2005). Fármacos usados no tratamento da asma. In J. G. Hardman, L.E. Limbird, P. B. Molinoff, R. W. Ruddon, & A. G. Gilman (Ed.), Goodman & Gilman’s: as bases farmacológicas da terapêutica (13. ed., pp. 409-412). Rio de Janeiro: Guanabara Koogan.
16. Agência Nacional de Vigilância Sanitária. (2010). Farmacopeia Brasileira. Brasília: Editora Fiocruz.
17. Efentakis, M., Vlachou, M., & Choulis, N. H. (1997). Effects of excipients on swelling and drug release from compressed matrices. Drug Development and Industrial Pharmacy, 23(1), 107-112. http://dx.doi.org/10.3109/03639049709148487.
18. United States Pharmacopeial Convention .(2007). The United States Pharmacopeia (USP). Rockville: USP.
19. Gliko-Kabir, I., Yagen, B., Penhasi, A., & Rubinstein, A. (2000). Phosphated crosslinked guar for colon-specific drug delivery: I. Preparation and physicochemical characterization. Journal of Controlled Release, 63(1–2), 121-127. http://dx.doi.org/10.1016/S0168-3659(99)00179-0. PMid:10640585.
20. Krishnaiah, Y. S. R., Karthikeyan, R. S., & Satyanarayana, V. (2002). A three-layer guar gum matrix tablet for oral controlled delivery of highly soluble metoprolol tartrate. International Journal of Pharmaceutics, 241(2), 353-366. http://dx.doi.org/10.1016/S0378-5173(02)00273-9. PMid:12100863.
21. Singh, R., Maity, S., & Sa, B. (2014). Effect of ionic crosslink on the release of metronidazole from partially carboxymethylated guar gum tablet. Carbohydrate Polymers, 106, 414-421. http://dx.doi.org/10.1016/j.carbpol.2014.01.033. PMid:24721097.
22. Herder, J., Adolfsson, A., & Larsson, A. (2006). Initial studies of water granulation of eight grades of hypromellose (HPMC). International Journal of Pharmaceutics, 313(1-2), 57-65. http://dx.doi.org/10.1016/j.ijpharm.2006.01.024. PMid:16510256.
23. Ojoe, E., Miyauchi, E. M., Kaneko, T. M., Velasco, M. V. R., & Consiglieri, V. O. (2007). Influence of cellulose polymers type on in vitro controlled release tablets containing theophylline. Revista Brasileira de Ciências Farmacêuticas, 43(4), 571-579. http://dx.doi.org/10.1590/S1516-93322007000400010.
24. Viridén, A., Abrahmsén-Alami, S., Wittgren, B., & Larsson, A. (2011). Release of theophylline and carbamazepine from matrix tablets – consequences of HPMC chemical heterogeneity. European Journal of Pharmaceutics and Biopharmaceutics, 78(3), 470-471. http://dx.doi.org/10.1016/j.ejpb.2011.02.003. PMid:21316446.
Facebook
Google+
Twitter
LinkedIn
Mendeley
StumbleUpon
CiteULike
Reddit
Email