Polymer blends used to develop felodipine-loaded hollow microspheres for improved oral bioavailability.

Pi C, Feng T, Liang J, Liu H, Huang D, Zhan C, Yuan J, Lee RJ, Zhao L, Wei Y
Int J Biol Macromol 112 1038-1047 06/01/2018

Abstract

Felodipine (FD) has been widely used in anti-hypertensive treatment. However, it has extremely low aqueous solubility and poor bioavailability. To address these problems, FD hollow microspheres as multiple-unit dosage forms were synthesized by a solvent diffusion evaporation method. Particle size of the hollow microspheres, types of ethylcellulose (EC), amounts of EC, polyvinyl pyrrolidone (PVP) and FD were investigated based on an orthogonal experiment of three factors and three levels. In addition, the release kinetics in vitro and pharmacokinetics in beagle dogs of the optimized FD hollow microspheres was investigated and compared with Plendil (commercial FD sustained-release tablets) as a single-unit dosage form. Results showed that the optimal formulation was composed of EC

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