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    《亚洲药物制剂科学(英文版)》 2017-01
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    Application of hot melt extrusion to enhance the dissolution and oral bioavailability of oleanolic acid

    Nannan Gao;Mengran Guo;Qiang Fu;Zhonggui He;School of Traditional Chinese Medicine, Shenyang Pharmaceutical University;School of Pharmacy, Shenyang Pharmaceutical University;  
    The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA amorphous solid dispersions. The characterizations of the optimal formulation were performed by differential scanning calorimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy and in vitro dissolution test.The in vivo pharmacokinetic study was conducted in rats. As a result, OA solid dispersion based on PVP VA 64(OA-PVP) was successfully prepared. In the dissolution medium containing 0.3% SDS, OA-PVP dramatically increased the releasing rate of OA compared with the physical mixture(PM-PVP) and commercial tablet. Furthermore, OA-PVP exhibited higher AUC(P 0.05) and C_(max)(P 0.05) than PM-PVP and commercial tablet. The superior dissolution property and bioavailability of OA-PVP mainly attributed to the amorphous state of OA in PVP VA64 and the well dispersion caused by thermal melting and shearing. Overall, hot melt extrusion was an efficient strategy to enhance the dissolution rate and oral bioavailability of OA.
    【Fund】: financially supported by National Natural Science Foundation of China (No. 81502993);; Doctoral Research Funding of Liaoning Province (No. 20141066);; General Project in Department of Education of Liaoning Province (No. L2014379);; Career Development Program for Young Teachers in Shenyang Pharmaceutical University
    【CateGory Index】: R943;R965
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