摘要
目的 研究复方甘草酸苷胶囊在健康男性体内的药代动力学和生物等效性.方法 用自身前后对照方法,24例健康男性受试者按随机号分为受试组和参比组,交替服用75 mg复方甘草酸苷胶囊和复方甘草酸苷片两种制剂,72 h内间断采血;采用液-质联用法测定甘草酸苷代谢物甘草次酸的血药浓度,计算药代动力学参数,判定两制剂是否人体生物等效.结果 复方甘草酸苷胶囊和片剂在人体内药时曲线符合二室模型,主要药代动力学参数AUC0~t分别为（4 284±1 149） ng·h/ml和（4 513±1 639） ng·h/ml,AUC0~∞分别为（4 369±1 179） ng·h/ml和（4 691±1 839） ng·h/ml,Cmax分别为（290.0±69.6） ng/ml和（293.4±80.9） ng/ml,Tmax分别为（12.08±1.38） h和（11.92±2.32） h;两种制剂的主要药代动力学参数Cmax,AUC0~t经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂人体生物等效,受试制剂复方甘草酸苷胶囊的人体相对生物利用度为（112.7±51.6）%.结论 两制剂具有生物等效.
Objective To study the bioequivalence and pharmacokinetics of compound glycyrrhizin capsules in human plasma. Methods 75 mg compound glycyrrhizin preparations were given to 24 healthy male volunteers in randomized two-way crossover design for the pharmacokinetic and relative bioavailability study. The volunteers were equally and randomly divided into test preparation group and reference preparation group, which were given com-pound glycyrrhizin capsules followed by compound glycyrrhizin tablets, compound glycyrrhizin tablets followed by compound glycyrrhizin capsules, respectively, with an interval of 14 d. The blood samples were collected within 72 h after taking medicine. Plasma concentration of glycyrrhetic acid were determined by high performance liquid chroma-tography-mass spectrometry （HPLC-MS）. Results The concentration-time curves of compound glycyrrhizin cap-sules and compound glycyrrhizin tablets in vivo were in accordance with two compartment model. The main pharmaco-kinetic parameters of the two preparations were： AUC0~t （4 284±1 149） ng·h/ml and （4 513±1 639） ng·h/ml, AUC0~∞（4 369±1 179） ng·h/ml and （4 691±1 839） ng·h/ml, respectively, Cmax （290.0±69.6） ng/ml and （293.4±80.9） ng/ml, Tmax （12.08 ± 1.38） h and （11.92 ± 2.32） h. The mean relative bioavailability of test preparation to reference preparation were （112.7±51.6）%. Conclusion The reference preparation and the test preparation are bioequivalent.
出处
《海南医学》
CAS
2015年第19期2931-2934,共4页
Hainan Medical Journal
