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La heparina no fraccionada administrada por vía oral con agente portador es terapéutica para la trombosis venosa
M D Gonze1, K Salartash, W C Sternbergh
1Department of Surgery, The Ochsner Medical Institutions, New Orleans, LA, USA.
Circulation
|June 7, 2000
Resumen
La heparina administrada por vía oral en combinación con SNAC trató eficazmente la trombosis venosa profunda (TVP) en ratas, mostrando resultados comparables a la heparina de bajo peso molecular. Esta nueva formulación oral ofrece una alternativa prometedora para el tratamiento de la TVP.
Área de la Ciencia:
- Farmacología Farmacología.
- Investigación de la trombosis.
- Sistemas de suministro de drogas Sistemas de suministro de drogas.
Sus antecedentes:
- La heparina administrada por vía oral (OHEP) presenta una pobre biodisponibilidad, lo que limita su eficacia terapéutica.
- El caprilato de N-(8[2-hidroxibenzoil]amino) de sodio (SNAC) es un potenciador de la absorción para la administración gastrointestinal de medicamentos.
- Se investigó la combinación de OHEP y SNAC (OHEP/SNAC) para el tratamiento de la trombosis venosa profunda (TVP).
Objetivo del estudio:
- Para evaluar la eficacia de OHEP / SNAC en un modelo de rata de TVP.
- Para comparar la efectividad de OHEP/SNAC con las formulaciones y controles de heparina existentes.
Principales métodos:
- La trombosis venosa profunda fue inducida en ratas Sprague-Dawley.
- Los animales fueron tratados durante 7 días con varios agentes: control no tratado, heparina subcutánea (SC HEP), solo SNAC, solo OHEP, heparina de bajo peso molecular (LMWH) y OHEP / SNAC.
- Se midieron el tiempo de tromboplastina parcial activado (aPTT) y los niveles de antifactor X (anti-Xa).
Principales resultados:
- OHEP/SNAC y LMWH redujeron significativamente la incidencia de TVP residual (10% frente al 100% para el control, P<0,001).
- Tanto OHEP/SNAC como LMWH demostraron reducciones significativas en los pesos de coágulos en comparación con los controles.
- OHEP/SNAC mostró niveles significativamente más altos de aPTT y niveles elevados de anti-Xa después de la administración en comparación con otros grupos.
Conclusiones:
- OHEP/SNAC demostró una eficacia significativa en el tratamiento de la TVP en un modelo de rata.
- La combinación de OHEP con el portador SNAC logró efectos terapéuticos comparables a los de LMWH.
- Este estudio pone de relieve el potencial de SNAC como portador para la administración de heparina oral en el manejo de la TVP.
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