氢溴酸加兰他敏控释胶囊在健康人体的生物等效性  

Bioequivalence of galanthamine hydrobromide released capsule in healthy volunteers

作　　者：刘薏[1] 邱健文[1] 司天梅[1] 舒良[1] 孙丽丽[1] 张鸿燕[1] 

机构地区：[1]北京大学精神卫生研究所,卫生部精神卫生学重点实验室,北京100191

出　　处：《中国临床药理学杂志》2008年第5期418-421,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的用HPLC-荧光检测法测定氢溴酸加兰他敏(中枢兴奋药)的血药浓度,评价其在健康人体内的药代动力学和生物等效性。方法24名健康男性志愿者单剂量随机交叉口服加兰他敏控释胶囊(8 mg)和片剂(2次口服,每次4 mg),血浆样品经碱化后用乙醚提取,用HPLC-荧光检测法测定血浆中加兰他敏浓度;用3P97软件计算药代动力学参数和相对生物利用度,并对参数进行方差分析和双单侧t检验。结果加兰他敏控释胶囊和片剂的主要药代动力学参数:C_(max)分别为(28.11±4.34)和(32.71±8.18)μg·L^(-1);t_(max)分别为(6.43±1.97)和(1.17±0.54)h;t_(1/2)分别为(10.41±3.34)和(8.65±2.06)h;AUC_(0→∞)分别为(670.96±116.46)和(699.70±133.55)μg·h·L^(-1)。结论本方法灵敏、准确、简便,统计学结果表明,这2种制剂生物等效。Objective To determine the concentration of galanthamine in plasma with HPLC - fluorescence method and study its pharmaeokinetics profiles and bioequivalenee in healthy voluteers. Methods Eight mg oral dose of galanthamine hydrobromide released capsule and tablets was given to 24 healthy male volunteers in a randomized cross - over study. Galanthamine was obtained from alkalinized plasma by liquid -liquid extraction with ether. Concentrations of galanthamine in plasma were determined by HPLC fluorescence. The pharmacokinetie parameters and relative bioavailability were calculated by 3P97 pharmaeokinetie software. Variance analysis and two - one sided test statistical analysis were performed for pharmaeokinetic parameters. Results The main pharmacokinetic parameters of galanthamine hydrobromide released capsule and tablets were as follows： Cmax were （28.11 ±4.34） and （32.71 ±8.18） μg · L^-1 ; tmax were （6.43 ± 1.97 ） and （ 1.17 ± 0.54） h ; t1/2 were （ 10.41 ±3.34） and （8.65 ±2.06） h;AUC（0→∞） were （670.96 ±116.46） and （699.70 ± 133.55 ） μg · h · L^-1. Conclusion The result of statistical analysis showed the two formulations were bioequivalent.

关 键 词：氢溴酸加兰他敏控释胶囊 生物等效性 药代动力学 高效液相色谱-荧光检测法 

分 类 号：R969.1[医药卫生—药理学] R971.7[医药卫生—药学]