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3-aminopyridine release study from polymeric supports in homogeneous and heterogeneous media

Hafida Sehil, Zohra Bengharez, Zineb El Bahri, Houaria Merine, Kaddour Guemra


In order to control and modify the drug release, in one hand 3-aminopyridine as active agent was grafted via chemical azomethine bond on monomer then copolymerized with N-vinylpyrrolidone. The obtained supports were characterized and the drug release from these formulations was followed using UV-Vis spectrophotometer in homogeneous media at four different pH (pH=1.2, 4.0, 6.0 and 8.0) simulating the human digestive rout. The results showed that the hydrolysis of monomer and copolymer obeyed to the first order and the apparent kinetic constants were calculated. In the other hand, spherical dosage forms composed from Eudragit RL100 and the active agent or the copolymer support were prepared and tested to control the drug release. The heterogeneous kinetics were established successively in the four cited media. The drug release seemed that be governed by diffusion model according to the Fick’s laws. So, the diffusivities were calculated and the results demonstrated that the drug release can be modified using these formulations.

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- M. Popa , C. L. Dumitriu, Scientific Study& Research., ISSN 1582-540X. 2003, Vol. IV (1 -2).

- A. Zaffaroni, Annals of New York Academy of Sciences, 1991, 618, 405-421.

- D. L. Bernik , D. Zubiri, M. E. Monge, R. M Negri, Physicochem. Eng. Aspects, 2006, 273,165.

- H. Merine, Z. Bengharez, L. Belarbi, A. Mesli , Journal de la Société Chimique de Tunisie, 2006, 8, 259.

- N. Chafi, A. Benghalem, A. Mesli, European polym. J., 2003, 1063

- S. Davaran, J. Hanaee, A. Klosravi, J. of controlled release, 1999, 58, 279.

- A. Bichara, J-P. Monthéard, J-L.Taverdet, Die Angewandte Makromolekulare chimie, 1998, 254, 47.

- A. Bichara, J-P. Monthéard, J-L. Taverdet, Eur. polym. J., 1998, 34, 1283.

- B. Z. Weiner, M. Tahan, A. Zilkha, J. Med. Chem., 1972, 15, 410.

- B. Rihova, K. Ulbrich, J. Kopecek, P. Mancal, Folia Microbiol, 1983, 28, 217.

- I. Katime, R. Novoa, E. Diaz de Apodaca, E. Mendizàbal, J. Puig, Polymer Testing, 1999, 18, 559.

- J. Kopecek , K. Ulibrich, Prog. Polym. Sci., 1983, 9, 2.

- J. Kopecek , Recent Advances in Drug Delivery Systems, Ed. Anderson et al., Plenum Press, New York, 1984, 41.

- R. Duncan, J. B. Lioyd, P. Rejmanova, J. Kopecek, Makromol. Chem Suppl., 1985, 9, 3.

- J. Kopecek, P. Rejmanova, V. Chytry, Makromol. Chem., 1981,182, 799.

- H. O. Ammar, R. M. Khalil, Drug Development and Industrial pharmacy, 1997, 23(11), 1043-1054.

- M. Miyajima, A. Koshika, J. Okada, A. Kusai, M. Ikeda, J. Controlled Release, 1998, 56, 85-94.

- J. Huang, H. Kao, X.Y. Wu, J. Controlled Release, 2000, 67, 45-54.

- Z. Elbahri, N. Chafi, A. Mesli, J. de la Société Chimique de Tunisie, 2004, 6, 77-84.

- D. Bidah, J. M. Vergnaud, Int. J. Pharm., 1990, 58, 215-220.

- A. R. Mollo, O.I. Corrigan, International J. pharmaceutics, 2003, 268, 71-79.

- I. Katime, R. Novoa, E.D. de Apodaca, E. Mendizábal, J. Puig, Polymer Testing, 1999,18, 559-566.

- A. R. C. Duarte , M. S. Costa, A. Lu´ısa Simpl´ıcio, M. M. Cardoso , C. M.M. Duarte, Inter. J. Pharm., 2006, 308, 168–174

- S.H. Wang , L.C. Zhang , F. Linb, X.Y. Sa, J.B. Zuo, Q.X. Shao, G.S. Chen, S. Zeng,Int. J. Pharm. 2005, 301, 217–225.

- J-T. He, H-B. Su, G-P. Li, X-M. Tao, W. Mo, H-Y. Song, Int. J. Pharm. 2006, 309,101–108.

- A. Rick Finch, Mao Chin Liu, Susan P. Grill, William C. Rose, Regina Loomis, Karen M. Vasquez, Yung-Chi-Cheng et Alan C. Sartorelli, Biochemical Pharmacology, 2000, 59, 983-991.

- J. Li, S. H. Chen, X. Li, C. Niu and T.W.Doyle, Tetrahedron., 1998, 54, 393-400.

- M. A. Khan and I.K.Reddy, S.T.P Pharmasciences, 1997, 6, 483

- P. B. O’Donnell and J.W. McGinity, Advanced Drug Delivery Reviews, 1997, 28, 25-42.

- P. Ahlin, J. Kristl, A. Kristl, F. Vrečer, Int. J. Pharm., 2002, 239, 113-120.

- J. Cranck, The mathematics of diffusion, 2nd ed, Clarendon, Oxford, 1975

- H. Kamogawa, T. Sakai et H. Sohma, J. Polym. Sci. Polym. Chem. Ed., 1988, 26,1335-1341.

- J. P. Monthéard, J. M. Vergnaud, M. Kolli, Polymer. Bull., 1990, 23, 331.

- Polymer Handbook, 4th Ed., 1999,vol.2, wiley-interscience .

- L. Michaelis et M.Mizutani, J.Phys.Chem., 1925, 116,146 .



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