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In vitro and in vivo evaluation of fenofibrate solid dispersion prepared by hot-melt extrusion.

Author(s): He H, Yang R, Tang X

Affiliation(s): Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.

Publication date & source: 2010-06, Drug Dev Ind Pharm., 36(6):681-7.

Publication type: In Vitro; Randomized Controlled Trial

OBJECTIVE: This article aimed to develop fenofibrate solid dispersion with high bioavailability using hot-melt extrusion and compare the difference of Eudragit E100 and polyvinylpyrrolidone-vinyl acetate copolymer S630 (PVP-VA) in dissolution. METHODS: Solid dispersion with carrier of Eudragit E100 or PVP-VA was prepared by hot-melt extrusion and then characterized by differential scanning calorimetry (DSC), X-ray diffraction, in vitro dissolution test, and in vivo bioavailability study. RESULTS: Fenofibrate exited as noncrystal state in these two kinds of solid dispersions that can be proved by DSC and X-ray diffraction. Eudragit E100 1:2 solid dispersion has the dissolution of 84% and 65% at 60 minutes in 0.1M HCl and water, respectively. Eudragit E100 1:4 solid dispersion has lower dissolution in 0.1M HCl and higher dissolution in water; the values are 73.6% and 87.3%. PVP-VA 1:2 solid dispersion has the dissolution of 60% and 65% at 60 minutes in 0.1M HCl and water, respectively. PVP-VA 1:4 solid dispersion has higher dissolution in 0.1M HCl and lower dissolution in water; the values are 64% and 53%. The different dissolution of fenofibrate from the two polymers is because of their different solubility and gelling tendency. When Eudragit E100 1:4 solid dispersion was administrated to beagle dogs, its relative bioavailability to micronization Lipanthyl capsule was 177.1%. CONCLUSION: Hot-melt extrusion is an excellent method to improve the dissolution and therefore the bioavailability of fenofibrate.

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