engleski

Influence of Structuraly similar compounds on crystal of Entacaponr

Polymorphism in Active Pharmaceutical Ingredients (API) is a widespread phenomenon that has been observed in more than half of known pharmaceutical substances [1]. Different polymorphs typically have different physical and chemical properties, such as solubility, melting point, etc. These differences may affect the production process (filtration, miscibility), but also can change stability and bioavailability of the active substances in the final dosage form [2]. Therefore, the process of crystallization and obtaining desired polymorph of certain particle properties is one of the most important challenges in the selection and application of API. As described in literature, in several cases the addition of small amount of impurities (additives) had the influence on nucleation kinetics, crystal growth and morphology [3]. However, only a small number of articles describe the impact of impurities on crystallization of API. Entacapone (Figure 1) is a selective and reversible inhibitor of catechol‐O‐ methyltransferase enzyme and is used together with the active substances Levodopa and Carbidopa in the treatment of symptoms of Parkinson's disease. It is known that Entacapone shows polymorphism and 9 different polymorphic forms have been described. The influence of related compounds on crystallization outcome and variability of the Entacapone polymorphism will be presented.

Entacapone, polymorph, crystal growth, Impurity

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