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Desarrollo de suspensiones de pamoato de vortioxetina intramuscular de acción prolongada: optimización de la
Yanhui Li1, Ting Wang1, Menghan Liu2
1CSPC Pharmaceutical Group Co., Ltd., 896 East Zhongshan Road, Shijiazhuang 050035, PR China; State Key Laboratory of New Pharmaceutical Preparations and Excipients, Shijiazhuang 050035, PR China.
Resumen
Este estudio desarrolló suspensiones de pamoato de vortioxetina (VTXP) intramuscular de acción prolongada. La suspensión optimizada de VTXP de 2,5 µm demostró una liberación prolongada del fármaco y una baja liberación inicial en modelos animales, confirmando su potencial para la administración sostenida.
Área de la Ciencia:
- Ciencias Farmacéuticas
- Sistemas de administración de fármacos
- Farmacocinética
Sus antecedentes:
- La vortioxetina es un antidepresivo que requiere formulaciones mejoradas de acción prolongada para mejorar la adherencia del paciente.
- La administración de fármacos intramuscular (IM) ofrece potencial para la liberación sostenida, pero los desafíos incluyen la estabilidad de la formulación y las propiedades de inyección.
Objetivo del estudio:
- Desarrollar y caracterizar suspensiones de pamoato de vortioxetina (VTXP) intramuscular de acción prolongada.
- Evaluar los perfiles farmacocinéticos y el rendimiento in vivo de las suspensiones optimizadas de VTXP.
Principales métodos:
- Se prepararon suspensiones de VTXP utilizando un molino de bolas planetario y se estabilizaron con poloxamer 338.
- La caracterización incluyó análisis del tamaño de partícula (difracción láser), viscosidad, fuerza de inyección, análisis de estado sólido (XRPD) y estudios de liberación in vitro.
- Se realizaron estudios farmacocinéticos (PK) en ratas y perros comparando la administración IM e intragástrica (IG).
Principales resultados:
- Las suspensiones optimizadas de VTXP al 15% con poloxamer 338 al 3% mostraron una viscosidad y una fuerza de inyección adecuadas.
- Una suspensión de VTXP de 2,5 µm exhibió una semivida (t1/2) significativamente prolongada mediante administración IM en comparación con la administración IG en ratas y perros.
- Se observaron porcentajes bajos de liberación inicial (rata 10,2%, perro 3,8%) para la suspensión administrada por IM.
Conclusiones:
- La formulación de suspensión de VTXP desarrollada es adecuada para la administración intramuscular de acción prolongada.
- La suspensión con un tamaño de partícula de 2,5 µm demuestra una liberación sostenida del fármaco y una reducción de la liberación inicial, ofreciendo una opción prometedora de administración de acción prolongada.
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