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目的:考察马钱子超微粉体与常规粉体中士的宁在大鼠体内的药代动力学特征。方法:采用HPLC法,3P97药代动力学软件拟合药动学模型。结果:大鼠灌胃马钱子超微粉体与常规粉体后士的宁的体内过程均符合二室模型,超微粉体的Cmaxμg/L(69.26±1.40)μg/L远远大于常规粉体的(51.13±0.48),说明药材超微粉碎后能大大提高其有效成分的吸收程度。参数K、Ka、B和β值显著增大(P<0.05),T1/2β显著减小(P<0.05),说明马钱子经超微化后士的宁在大鼠体内吸收相和消除相均增大,提示马钱子超微化以后能减少其蓄积中毒。结论:马钱子超微粉碎以后,血药浓度明显升高,生物利用度提高。
OBJECTIVE: To investigate the pharmacokinetics of strychnine in rats in superfine powder and conventional powder. Methods: The pharmacokinetic model was fitted by HPLC and 3P97 pharmacokinetic software. RESULTS: The in vivo processes of intragastric ultramicropowder and conventional powder of strychnine were consistent with the two-compartment model. The ultrafine powder Cmaxμg/L (69.26±1.40) μg/L was much greater than conventional The powder (51.13±0.48) indicates that the ultrafine pulverization of herbs can greatly increase the absorption of the active ingredients. The values of K, Ka, B, and β increased significantly (P<0.05), T1/2β decreased significantly (P<0.05), indicating that Strychon nucifera hypertensively absorbed and eliminated in rats. Both phases increase, suggesting that the ultra-micronization of Strychnine can reduce its accumulation of poisoning. Conclusion: After ultrafine pulverization, the concentration of blood drug is significantly increased and bioavailability is improved.