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Merck

Design of fenofibrate microemulsion for improved bioavailability.

International journal of pharmaceutics (2011-09-13)
Liandong Hu, Hongyu Wu, Feng Niu, Cuihong Yan, Xun Yang, Yanhong Jia
ABSTRAKT

The objective of the present study was to formulate a microemulsion system for oral administration to improve the solubility and bioavailability of fenofibrate. Various formulations were prepared using different ratios of oils, surfactants and co-surfactants (S&CoS). Pseudo-ternary phase diagrams were constructed to evaluate the microemulsification existence area. The formulations were characterized by solubility of the drug in the vehicles, mean droplet size, and drug content. The stability was also investigated by store for 3 months under 4°C, 25°C and 40°C and diluted 100 times for 3 days. The optimal formulation consists of 25% Capryol 90, 27.75% Cremophore EL, 9.25% Transcutol P and 38% water (w/w), with a maximum solubility of fenofibrate up to ∼40.96 mg/mL. The microemulsion was physicochemical stable and mean droplet size was about 32.5-41.7 nm. The pharmacokinetic study was performed in dogs and compared with Lipanthy capsule. The result showed that microemulsion has significantly increased the C(max) and AUC compared to that of Lipanthy capsule (p<0.05). The oral bioavailability of fenofibrate microemulsions (FEN-MEs) in ME-3 and ME-4 were 1.63 and 1.30-fold higher than that of the capsule. Our results indicated that the microemulsions could be used as an effective formulation for enhancing the oral bioavailability of fenofibrate.

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Sigma-Aldrich
Di(ethylene glycol) ethyl ether, ≥99%
Sigma-Aldrich
Diethylene glycol monoethyl ether, ReagentPlus®, 99%