Modelos “in silico” para la predicción de la absorción de fármacos administrados por vía oral (SIMCYP®)estatinas
- LÓPEZ, Adrián 1
- SANTOS, María Dolores 1
- GARCÍA, María José 1
- 1 Departamento de Ciencias farmacéuticas: Farmacia y Tecnología Farmacéutica. Facultad de Farmacia, Universidad de Salamanca
ISSN: 2445-1355
Argitalpen urtea: 2017
Alea: 2
Zenbakia: 2
Orrialdeak: 69-79
Mota: Artikulua
Beste argitalpen batzuk: Farmajournal
Laburpena
Using Simcyp® software, simulation studies were done in order to evaluate the capacity of this software to predict clinical evidence related to absorption profile of two statins: simvastatin and rosuvastatin. Specifically, we evaluate the influence of intestinal transit time, transporter abundance and enzymes responsible of metabolism in gastrointestinal tract. First of all we looked for bibliographic information about the absorption profile of these drugs. Then we carried out simulations in different population groups, mainly in normal populations, populations with accelerated intestinal transit and poor metabolizers. For rosuvastatin its efflux transporter (ABCG2) was also blocked and its permeability altered. The results are consistent with observations drawn from clinical experience. They show that the transit rate significantly affects the absorbed fraction of simvastatin, but not the rate of rosuvastatin; however the transporter abundance and permeability value are relevant in the absorption of rosuvastatin. CYP3A4 is shown as the most important isoenzyme responsible of the biotransformation of simvastatin, confirming that CYP3A4 does not participate in rosuvastatin intestinal metabolism.
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