펠로디핀이 함유된 미립구의 생체이용률

Bioavailability of Microspheres Containing Felodipine

Microspheres of felodipine, which is one of the calcium channel blocker, using a mixture of Eudragit(R) RL, L, E, and cellulose on the base of Eudragit(R) RS were investigated. Cremophor(R) was added to each preparation of polymers in order to increase the release of felodipine from microspheres. Felodipine-loaded microspheres were prepared by a solvent evaporation method, which is based on dispersion of methylene chloride containing felodipine and polymers in 0.5 w/v% polyvinyl alcohol solution. The average diameter based on the size distribution of the felodipine-loaded microspheres was observed to be ca. 40-55mcm. A good and smooth surface were showed in all types of the microspheres. The amount of felodipine loaded was over 90 w/w% in all types of microspheres. The dissolution profiles of felodipine from microspheres were similar with each type of polymer, and about a 60 w/w% of the total amount of felodipine loaded to microsphere was released within 7 hours. Dissolution rate of felodipine from the microsphere was increased by addition of Cremophor(R). After oral administration of the felodipine-loaded microspheres in PVA solution and felodipine alone in PEG solution to rats, respectively, the pharmacokinetic study revealed that (R)the Tmax values of the microspheres were observed in the range of 0.67-1.0hr while that of the felodipine solution was obtained 0.33hr. In addition, the AUC of the microspheres at 0 to 7hr was remarkably increased in comparison to that of felodipine solution. These results revealed that the microspheres based on Eudragit(R) RS could be a good candidate for the controlled release drug delivery system for felodipine.