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Desarrollo de fórmulas de clorhidrato de trazodona amorfa palatables a través del intercambio iónico

Zhaohua Li¹, Junjie Wang¹, Huijian Wang¹

¹Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.

|August 28, 2025

Resumen

El desarrollo de una formulación de clorhidrato de trazodona amorfa palatable utilizando el intercambio iónico enmascaró efectivamente su sabor amargo. Esta técnica de amorfización mejora la aceptación del fármaco para su administración oral.

Área de la Ciencia:

Ciencias farmacéuticas
Sistemas de administración de fármacos
Ciencias de los materiales

Sus antecedentes:

Se prefiere la administración oral del medicamento, pero a menudo se ve obstaculizada por el sabor amargo del medicamento, lo que reduce el cumplimiento del paciente.
El clorhidrato de trazodona (TRA) es un medicamento eficaz cuyo sabor amargo presenta un desafío significativo para las formulaciones orales.
El desarrollo de formulaciones de fármacos apetecibles es crucial para mejorar los resultados terapéuticos y la adherencia del paciente.

Objetivo del estudio:

Desarrollar una formulación amorfa aceptable de clorhidrato de trazodona (TRA) utilizando el intercambio iónico con Amberlite IRP88.
Caracterizar las propiedades físicas de los complejos TRA-Amberlite IRP88 (TRC).
Evaluar la eficacia de enmascaramiento del sabor y los perfiles de disolución de los TRC desarrollados.

Principales métodos:

Preparación de complejos TRA-Amberlite IRP88 (TRC) mediante el método de intercambio estático.
Caracterización física de los TRC, incluida la confirmación de la dispersión amorfa.
Acoplamiento molecular para investigar las interacciones fármaco-resina.
Estudios de disolución in vitro y evaluación del enmascaramiento del sabor in vivo.

Principales resultados:

La caracterización física confirmó la dispersión amorfa de TRA dentro de Amberlite IRP88.
Los estudios in vivo demostraron un enmascaramiento eficaz del sabor amargo del TRA.
El mecanismo implicó la supresión de la disociación de TRC en la saliva, reduciendo la disolución oral.

Conclusiones:

La amorfización del clorhidrato de trazodona utilizando Amberlite IRP88 es una estrategia exitosa para el enmascaramiento del sabor.
Este enfoque mejora significativamente la palatabilidad de las formulaciones de medicamentos orales.
Los hallazgos proporcionan información valiosa para el desarrollo de medicamentos orales amigables para el paciente.

Palabras clave:

En el caso de la amberlita IRP88 amorfo amargura Intercambio iónico Enmascaramiento del sabor

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