Estudios de estabilidad física y química de una preparación extemporánea de enalapril maleato para uso hospitalario
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Ariza Paba, Javier Enrique
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Resumen El enalapril es un derivado de dos aminoácidos, L-alanina y L-prolina, que inhibe la hipertensión actuando sobre la enzima convertidora de angiotensina, bloqueando la producción de la angiotensina II, como resultado de la unión directa de su grupo funcional carboxilo en el sitio del ión zinc de la enzima. El enalapril es un profármaco de amplio uso, altamente selectivo y no interactúa directamente con otros componentes del sistema renina angiotensina (SRA). La elaboración de una preparación extemporánea de maleato de enalapril a partir de tabletas, es una alternativa en la práctica hospitalaria, por presentar ventajas como permitir la individualización de la dosis para los pacientes que lo requieran y poder cumplir los tratamientos establecidos, evitando así los errores de dosificación cuando se administran dosis por fractura de tabletas. En la presente investigación se validó una metodología analítica que demostró ser selectiva, lineal, precisa y exacta. Posteriormente, se llevó a cabo el estudio de estabilidad física y química de la preparación extemporánea durante 15 días, de muestras almacenadas a 5 y 25 ± 2°C y utilizando dos vehículos de uso hospitalario: el primero, una solución de agua – dextrosa al 5% 1:1 y el segundo, una solución agua - dextrosa al 5% 1:1 ajustado a pH 3.0 con ácido ascórbico. La preparación extemporánea fue envasada en recipientes plásticos transparentes y de color ámbar con tapa rosca plástica y expuesta a las condiciones de estudio. La cuantificación del fármaco se realizó utilizando la metodología analítica por HPLC. Los resultados del estudio de estabilidad, indican que el vehículo dextrosa al 5% - agua en proporción 1:1, mostró una mayor estabilidad respecto al segundo vehículo que fue ajustado a un pH de 3.0. El pH ácido de la preparación extemporánea es el factor de mayor incidencia sobre la estabilidad.
Abstract: Enalapril is derived from two amino acids, L-alanine and L-proline, which inhibits hypertension converting enzyme acting on the angiotensin, blocking the production of angiotensin II, as a result of its direct binding to the carboxyl functional group site zinc ion of the enzyme. This drug is widely used and highly selective and do not interact directly with other components of the renin angiotensin system (RAS). The extemporaneous preparation of enalapril maleate from tablets has been a great alternative in hospital practice, for the countless benefits it brings, such as: allow individualization of dosage for patients in need and meet established treatments. Not like the fractures that are administered to the tablet dosage dose. In this research the analytical methodology was validated this being selective linear, accurate and precise. Subsequently, a study was conducted for the stablishement of physical and chemical stability of the extemporaneous preparation for 15 days when stored at 5 ± 2 °C and 25 ± 2 °C prepared in solutions of water - 5% dextrose dextrose water 1:1 to 5 % 1:1 adjusted to pH 3.0 with ascorbic acid. Extemporaneous preparations were packaged in plastic containers and transparent amber plastic screw cap exposed to the experimental conditions. The quantification of the drug was performed using the validated analitycal methodology. The results of stability studies show that the vehicle 5% dextrose water 1:1 showed better stability. They also indicated that the time and pH are the most critical factors which affect the lifetime of extemporaneous liquid preparations developed.
Abstract: Enalapril is derived from two amino acids, L-alanine and L-proline, which inhibits hypertension converting enzyme acting on the angiotensin, blocking the production of angiotensin II, as a result of its direct binding to the carboxyl functional group site zinc ion of the enzyme. This drug is widely used and highly selective and do not interact directly with other components of the renin angiotensin system (RAS). The extemporaneous preparation of enalapril maleate from tablets has been a great alternative in hospital practice, for the countless benefits it brings, such as: allow individualization of dosage for patients in need and meet established treatments. Not like the fractures that are administered to the tablet dosage dose. In this research the analytical methodology was validated this being selective linear, accurate and precise. Subsequently, a study was conducted for the stablishement of physical and chemical stability of the extemporaneous preparation for 15 days when stored at 5 ± 2 °C and 25 ± 2 °C prepared in solutions of water - 5% dextrose dextrose water 1:1 to 5 % 1:1 adjusted to pH 3.0 with ascorbic acid. Extemporaneous preparations were packaged in plastic containers and transparent amber plastic screw cap exposed to the experimental conditions. The quantification of the drug was performed using the validated analitycal methodology. The results of stability studies show that the vehicle 5% dextrose water 1:1 showed better stability. They also indicated that the time and pH are the most critical factors which affect the lifetime of extemporaneous liquid preparations developed.