Controle de qualidade e avaliação das propriedades tecnológicas das formas polimórficas de talidomida / Quality control and evaluation of technological properties of polymorphic forms of thalidomide

AUTOR(ES)
FONTE

IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia

DATA DE PUBLICAÇÃO

2011

RESUMO

Thalidomide was widely prescribed between 1950 and 1960, in nearly 50 countries, as sedative and antiemetic for morning sickness during pregnancy. After the occurrence of serious problems of teratogenicity it was heavily controlled. Growing interest has been observed in recent years to identify and elucidate the anti-inflammatory, immunomodulatory and anti-angiogenic properties of thalidomide. In the same direction, clinical investigations have been conducted in patients with various diseases such as myeloma, renal carcinoma, and prostate cancer, among others. Thalidomide possesses a chiral center and two amide rings in its structure and is synthesized as racemate, consisting of two active enantiomers: (+)-(R)- and (+)-(S)-thalidomide. It is known that the racemic thalidomide has two polymorphic forms, alpha ( ) and beta ( ). Thus, the observed variability in relation to the polymorphism represents a critical point considering the potential of changes in biopharmaceutical properties due to the predominance of one of them. In Brazil thalidomide tablets are manufactured exclusively by FUNED ¿ Fundação Ezequiel Dias, the public laboratory of the State of Minas Gerais, which integrates the Country s Official System of drug production. In this context, the objectives of this work are the assessment of physical characteristics, physicalchemical and technological properties of polymorphic forms of thalidomide, with emphasis on crystallization, dissolution, degradation and compression. The results of this work contributed to a better understanding of the relationship between characteristic crystallographic properties and pharmaceutical properties, aggregating a scientific basis to assess the differences of these polymorphs and ensure the appropriate quality control of the final product produced in an official laboratory. These studies contributed to compliance with regulatory requirements.

ASSUNTO(S)

thalidomide talidomida polimorfismo polymorphism quality control controle de qualidade de medicamentos dissolution degradacao validation degradation pharmaceutical industry physics of compression

ACESSO AO ARTIGO

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