Keywords
dissolution
similar
polymorphism
How to Cite
Abstract
Some active pharmaceutical ingredients (API) might present polymorphism at any stage of the industry production process. In caseit is not characterized and specified, a different polymorph might be erroneously used during the manufacturing procedure. Polymorphisms cause some variations in the physicochemical properties of APIs, especially in solubility. Therapeutic inefficacy was detected in some glyburide drug products, and the occurrence of polymorphs might be one of the possible reasons. This study analyzed five drug products and five APIs., The characteristic pharmaceutical equivalence tests were used for analyzing the drug products. The techniques employed to evaluate the APIs showed no differences in polymorphism, no significant changes in the physicochemical properties or in the intrinsic dissolution rate. However, the dissolution profiles of the drug products, mainly between two similar products A and B, showed significant differences in the f2 factor values, being 20 and 42, respectively, indicating that these values were related to the occurrence of different excipients, such as mannitol.
References
1. Rang HP, Dale MM, Ritter JM. Farmacologia. 4.ed. Rio de Janeiro: Guanabara Koogan; 2001. p.323-329.
2. Merck index: an encyclopedia of chemicals, drugs and biologicals. 14.ed. Whitehouse Station: Merck Research Laboratories, 2006. p.773.
3. Moffat AC, Osselton MD, Widdop B. Clarke’s analysis of drugs and poisons. 3.ed. London: Pharmaceutical Press. 2004, v.2. p.1078.
4. Farmacopéia Brasileira. 5.ed. Brasília: ANVISA, 2010. v.2, p.442-5.
5. Suleiman MS, Najib NM. Isolation and Physicochemical characterization of solids forms of glibenclamide. Int J Pharm.1989;50:103-9.
6. Hassan MA, AL-hindawi MK, Sallam E, Sheikh Salem M. Preparation and characterization of a new polymorphic form and a solvate of glibenclamide. Acta Pharm Hung. 1997; 67:81-8.
7. Panagopoulou-KaplanI A, Malamataris S. Preparation and characterization of a new insoluble polymorphic form of glibenclamide. Int. J. Pharm. 2000 ; 19:239-46.
8. Rodríguez MS, Luna J, Carlucci A, Bregni C. Relación de estabilidad termodinámica relativa entre polimorfos de glibenclamida. Acta Farm Bonaer. 2004 ; 23(2):169-75.
9. Cuffini SL, Pitaluga AJR, Tombari DG. Polimorfismo em Fármacos. In: Storpirtis S, Gonçalves JE, Chiann C, Gai MN. Biofarmacotécnica. Rio de Janeiro: Guanabara Koogan, 2009. p.21-29.
10. Neugebauer G, Betzien G, Hrstka V, Kaufman B, Vonmöllendorff E, Abshagen U. Absolute bioavailability and bioequivalence of glibenclamide (Semi-Euglucon N). Int J Clin Pharmacol Ther Toxicol. 1985;23(9):453-60.
11. Blume H, Ali SL, Siewert M. Pharmaceutical quality of glibenclamide products: Multinational post market comparative study. Drug Dev Ind Pharm. 1993; 19(20):2713-41.
12. United States Pharmacopeia. 32. ed. Rockville: United StatesPharmacopeial Convention, v.1, p.549–552, 2009.
13. Aulton ME. Delineamento de Formas Farmacêuticas: 2.ed. Rio Grande do Sul: Artmed, 2005. p. 25.
14. Brasil. Agência Nacional de Vigilância Sanitária. Resolução RDC No 31, de 11 de agosto de 2010. Dispõe sobre a realização dos Estudos de Equivalência Farmacêutica e de Perfil de Dissolução Comparativo. Diário Oficial [da] República Federativa do Brasil. Brasília, DF, 12. Ago. 2010. Nº 154, p. 36-8
15. O’hara T, Dunne A, Butler J, Devane J. A review of methods used to compare dissolution profile data. Pharm Sci Technol Today. 1998; 1:214-23.
16. Zhang G, Law D, Schmitt E, Qiu Y. Phase transformation considerations during process development and manufacture of solid oral dos age forms. Adv Drug Deliv Rev. 2004; 56:371-90.
17. Brasil. Agência Nacional de Vigilância Sanitária. Resolução RDC No 134, de 29 de maio de 2003. Dispõe sobre a adequação dos medicamentos já registrados. Diário Oficial [da] República Federativa do Brasil. Brasília, DF, Jun. 2003. p.47-8.
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