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目的研究苦参碱在健康志愿者近端小肠内定点释放后的药代动力学特征。方法用自主研制的遥控释药胶囊系统,将200mg苦参碱定位释放于志愿者的近端小肠内。用高效液相色谱法,以槐果碱为内标,甲醇-水-乙二胺(70∶30∶0.02)为流动相,测定志愿者血浆中苦参碱的含量。采用3p87程序计算药代动力学参数。结果近端小肠定点释放苦参碱的药代动力学符合二室开放模型,Cmax为10.52μg/ml,Tmax为2.08h,T1/2α和T1/2β分别为0.90h和9.02h,AUC(0-t)为91.90μg·h/ml。结论苦参碱在健康人近端小肠段定位释放后,小肠对苦参碱有明显的吸收且吸收过程呈二室模型分布。
Objective To study the pharmacokinetics of matrine after it was released from the proximal intestine of healthy volunteers. Methods Using self-developed remote controlled release capsule system, 200mg matrine was released into the proximal intestine of volunteers. The content of matrine in plasma of volunteers was determined by HPLC with the use of sophocarpine as internal standard and methanol-water-ethylenediamine (70:30:0.02) as the mobile phase. Pharmacokinetic parameters were calculated using the 3p87 program. Results The pharmacokinetics of matrine released by the proximal intestine were consistent with the two-compartment open model. The Cmax was 10.52μg / ml, the Tmax was 2.08h, the T1 / 2α and T1 / 2β were 0.90h and 9.02h, -t) was 91.90 μg · h / ml. Conclusion Matrine in the proximal part of healthy people after the release of the small intestine, the intestine obvious absorption of matrine and the absorption process was two-compartment model distribution.