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目的研究葛根素固体分散体的制备及其在家兔体内药动学,以提高葛根素口服给药的生物利用度。方法采用溶出度法,确定葛根素固体分散体的最佳制备处方;采用HPLC法,测定家兔血浆中葛根素的含量,药动学参数经3P97药动学软件处理。结果葛根素固体分散体的最佳制备处方为葛根素:PEG6000:pluronicF-68=1:4:1(m/m/m);葛根素及葛根素固体分散体的血药浓度-时间过程均符合二室模型,主要药动学参数:α分别为(2.040±0.327)、(0.870±0.191)·h~(-1),β分别为(0.21 2±0.021)、(0.351±0.022)·h~(-1),AUC_(0-∞)分别为(11.966±1.370)、(91.419±3.531)mg·L~(-1)·h,t_(max)分别为(0.491±0.026)、(1.423±0.035)h,ρ_(max)分别为(3.917±0.066)、(20.416±1.870)mg·L~(-1)。葛根素固体分散体对葛根素的相对生物利用度为763.99%。结论葛根素固体分散体可提高葛根素口服给药在家兔体内的生物利用度。
Objective To study the preparation of puerarin solid dispersion and its pharmacokinetics in rabbits in order to improve the bioavailability of puerarin for oral administration. Methods The optimum preparation of puerarin solid dispersion was determined by dissolution method. The content of puerarin in rabbit plasma was determined by HPLC method. The pharmacokinetic parameters were determined by 3P97 pharmacokinetic software. Results The optimal preparation of puerarin solid dispersion was puerarin: PEG6000: pluronic F-68 = 1: 4: 1 (m / m / m); the plasma concentration-time course of puerarin and puerarin solid dispersion According to the two-compartment model, the main pharmacokinetic parameters were as follows: α (2.040 ± 0.327), (0.870 ± 0.191) · h -1, β (0.21 2 ± 0.021) and (0.351 ± 0.022) ~ (-1) and AUC_ (0-∞) were respectively (11.966 ± 1.370) and (91.419 ± 3.531) mg · L -1 · h -1 and t max were 0.491 ± 0.026 and 1.423 ± 0.035) h and ρ_ (max) were (3.917 ± 0.066) and (20.416 ± 1.870) mg · L -1, respectively. The relative bioavailability of puerarin solid dispersion to puerarin was 763.99%. Conclusion The puerarin solid dispersion can improve the bioavailability of puerarin in rabbits.