Enhanced Stability and Oral Bioavailability of Folic Acid-Dextran-Coenzyme Q 10 Nanopreparation by High-Pressure Homogenization.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY(2018)

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摘要
The preparation of folic acid dextran coenzyme Q(10) (FA-DEX-CoQ(10)) nanopreparation was optimized by high-pressure homogenization to improve the dissolution and oral bioavailability of CoQ(10). The preparation conditions of FA-DEX-CoQ(10) nanopreparation were optimized by single-factor and orthogonal experimental design. The properties of CoQ(10) raw materials, CoQ(10) physical mixtures, and FA-DEX-CoQ(10) nanopreparation were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The concentration of Cog, in rat plasma was determined by high-performance liquid chromatography, and the corresponding pharmacokinetic parameters were calculated. The optimal preparation method is as follows: mass ratio of CoQ(10)/FA-DEX of 1:18, mass ratio of stabilizer/CoQ(10) of 0.4:1, 6 homogenization cycles, and homogenization pressure of 800 bar. These conditions resulted in a mean particle size of 87.6 nm. SEM showed that the particles was spherical. DSC and XRD analyses showed that the crystallinity of FA-DEX-CoQ(10) nanopreparation decreased. FA-DEX-CoQ(10) possesses longterm stability. By single-factor and orthogonal experiments, the dissolution rate, C-max and area under the curve (AUC) of the optimized FA-DEX-CoQ(10) nanopreparation were 3.95, 2.7, and 2.4 times as much as those of the raw materials. The results showed that FA-DEX-CoQ(10) nanopreparation had better oral bioavailability.
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关键词
coenzyme Q(10) nanopreparation,high-pressure homogenization,dissolution,oral bioavailability
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