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Journal of Chinese Pharmaceutical Sciences ›› 2019, Vol. 28 ›› Issue (5): 329-338.DOI: 10.5246/jcps.2019.05.032

• Original articles • Previous Articles     Next Articles

In vitro dissolution and oral bioavailability study of fenofibrate nanomatrix system prepared by hot-melt extrusion

Yajie Yin1, Xiaofei Zhang1, Zheng Cui1, Wei Qu1, Bing He1, Wenbing Dai1, Hua Zhang1, Xueqing Wang1, Qiang Zhang1,2*   

  1. 1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China    
    2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2019-01-15 Revised:2019-03-11 Online:2019-05-31 Published:2019-04-10
  • Contact: Tel.: +86-010-82802791, E-mail: zqdodo@bjmu.edu.cn
  • Supported by:

    National Basic Research Program of China (Grant No. 2015CB932100).

Abstract:

Solvent evaporation method for preparation of nanomatrix has the disadvantages, such as residual organic solvent, environmental pollution, explosion-proofing and so on. To overcome these shortcomings, a series of fenofibrate nanomatrix drug delivery system (NDDS) consisting of nano-porous silica Sylysia®350 (S350) and pH sensitive material Eudragit® L100-55 (EL100-55) were prepared using hot-melt extrusion (HME), and their in vitro dissolution and in vivo bioavailability were compared. Finally, the formulation with the highest in vivo bioavailability was selected as the optimized formulation for DSC and PXRD characterization. The results showed that the optimized NDDS showed a higher bioavailability than the reference formulation, although there was crystalline form drug remaining in NDDS. The relative bioavailability of the optimized formulation was 157.1% compared with the commercial product Lipanthyl®. In addition, the relative bioavailability of the optimized formulation was 124.8% in comparison with the formulation prepared by solvent evaporation method, showing that the NDDS prepared by the HME method was effective in improving the bioavailability of fenofibrate. In conclusion, HME was a promising method to prepare NDDS. 

Key words: Nanomatrix drug delivery system, Hot-melt extrusion, Fenofibrate, Dissolution, Bioavailability

CLC Number: 

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